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Patchouli
Pogostemon cablin, known in the West as patchouli or guang huo-xiang in China, is a long-time staple in traditional Chinese medicine for various indications, particularly gastrointestinal and skin disorders1.
Patchouli oil, which contains several mono- and sesquiterpenoids, alkaloids, and flavonoids, is thought to possess significant anti-inflammatory and antioxidant qualities2.In fact, it is reputed to impart antiviral, antioxidant, anti-inflammatory, and analgesic effects, and is also known to protect intestinal barrier function3. Peng et al. have found that patchouli oil exerts significant antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)4.
After a comprehensive 2013 review, Chen et al. deemed P. cablin to have potential clinical benefits as an effective adaptogenic herbal treatment3. It is thought to have some antiacne properties as well1. Further, P. cablin is among the Top 10 most-often-used traditional Chinese medicine prescriptions for skin care and appearance1.
In Brazil, China, Indonesia, and Malaysia, P. cablin is cultivated for its essential oil, which plays an important role in the perfume industry. Patchouli essential oil, featured in perfumes, soaps, cosmetics, and as incense, is used by aromatherapists for its calming and reviving effects. The essential oil has also been shown to impart antioxidant activity5.
In 2014, Lin et al. studied the protective effects of P. cablin essential oil against ultraviolet (UV)-induced skin photoaging in mice. The researchers applied patchouli oil for 2 hours before UV exposure to the dorsal depilated skin of mice. They found that patchouli oil doses of 6 mg/mouse and 9 mg/mouse significantly suppressed skin wrinkle formation, mitigated skin elasticity impairment, and augmented collagen content (21.9% and 26.3%, respectively). The same doses also yielded significant reductions in epidermal thickness and malondialdehyde content, and blocked the disruption of collagen and elastic fibers. Patchouli oil treatment also resulted in the up-regulation of the antioxidant enzymes superoxide dismutase, glutathione peroxidase, and catalase. The investigators concluded that patchouli oil, perhaps due to its antioxidant characteristics, and sesquiterpene constituents in particular, was effective in preventing photoaging in mice, and warrants attention as a potential agent to hinder photoaging in humans1.
Feng et al. also investigated the effects of topically applied patchouli alcohol on UV-induced photoaging in mice that year. For 9 weeks, investigators applied patchouli oil solution or a vehicle to the depilated dorsal skin of 6-week-old mice. They found that patchouli oil significantly hastened the recovery of UV-induced skin lesions, which they ascribed to the antioxidant and anti-inflammatory activity of the agent and its down-regulation of the expression of matrix metalloproteinase (MMP)-1 and MMP-32.
Antimicrobial and mosquito repellent activity
In a 2005 study by Trongtokit et al. of the mosquito-repellent activity of 38 essential oils at three concentrations (10%, 50%, or undiluted) against the mosquito Aedes aegypti under laboratory conditions using human volunteers, undiluted P. cablin oil was one of four [along with Cymbopogon nardus (citronella), Syzygium aromaticum (clove), and Zanthoxylum limonella (Thai name: makaen)] undiluted oils to yield an effect, 2 hours of full repellency. The investigators then tested the same concentrations of these oils for repellency against Culex quinquefasciatus (the Southern house mosquito) and Anopheles dirus (the mosquito considered to be a vector of malaria in Asian forested zones. The undiluted oils provided the greatest protection, with clove oil rendering the most durable repellency6.
Photoaging
Wu et al. determined the acaricidal activity of compounds extracted from patchouli oil against the house dust mite (Dermatophagoides farinae) in 2012. They isolated 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), the hydrolysate of pogostone, and 15 other constituents in patchouli oil, ultimately ascertaining that DHEMH and patchouli oil itself were the most toxic substances to D. farinae. The investigators concluded that patchouli oil and DHEMH warrant consideration and more study for their acaricidal potential as environmentally friendly, effective, and simple fumigant alternatives to chemical agents7.
In 2013, Yang et al. used molecular docking technology to evaluate the antibacterial activity of patchouli oil in vitro. They identified 26 compounds in patchouli oil displaying antibacterial activity, with pogostone and (-)-patchouli alcohol exhibiting the strongest activity8. Later that year, Yang et al. used the same technology to establish that Herba pogostemonis oil exhibited potent antibacterial effects, especially the constituents pogostone and (-)-Herba pogostemonis alcohol9. Raharjo and Fatchiyah also used molecular docking tools and Chimera 1.7s viewer software in a virtual screening of compounds from patchouli oil, concluding that alpha-patchouli alcohol is a potential inhibitor of the cyclo-oxygenase (COX)-1 enzyme. This is notable given the pivotal role of COX-1 in the inflammatory response10.
The next year, Peng et al. isolated one of the primary constituents of patchouli oil, pogostone, and assessed its antibacterial activity in vitro and in vivo. They found that pogostone suppressed both gram-negative and gram-positive bacteria in vitro. The researchers noted that pogostone was active against some drug-resistant bacteria (such as MRSA). Via intraperitoneal injection, pogostone displayed antibacterial activity in male and female Kunming mice against Escherichia coli and MRSA. At concentrations of 50 and 100 mg/kg, 90% of the mice infected with E. coli were protected; 60% of the mice at 25 mg/kg were protected. For mice with MRSA, 60% were protected at a dose of 100 mg/kg and 50% at a dose of 50 mg/kg. The investigators concluded that pogostone is a viable antibacterial agent for clinical use4.
Transdermal delivery
A 2008 study by Luo et al. showed that patchouli oil was among three volatile oils that improved the skin penetration of the flavonoids baicalin11. It was less effective than several compounds, including clove oil, camphor, menthol, and oleic acid, as a transdermal enhancer in a subsequent study by Zheng et al.12.
Conclusion
Patchouli oil continues to be used today in traditional Chinese medicine. In the West, the established literature on Pogostemon cablin is thin, but what has emerged recently, particularly studies on the protection against photoaging in mice, supports the continued investigation of this ancient herb to determine its potential role in dermatologic practice. As it is, much more research is necessary.
References
1. J Ethnopharmacol. 2014;154(2):408-18.
2. Eur J Pharm Sci. 2014;63:113-23.
3. Expert Opin Investig Drugs. 2013;22(2):245-57.
4. Chin Med J. (Engl) 2014;127(23):4001-5.
5. J Agric Food Chem. 2007;55(5):1737-42
6. Phytother Res. 2005;19(4):303-9.
7. Chem Pharm Bull (Tokyo). 2012;60(2):178-82.
8. Iran J Pharm Res. 2013 Summer;12(3):307-16.
9. Pak J Pharm Sci. 2013;26(6):1173-9.
10. Bioinformation 2013;9(6):321-4.
11. Zhong Yao Cai. 2008;31(11):1721-4
12. Zhongguo Zhong Yao Za Zhi. 2009;34(20):2599-603.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Pogostemon cablin, known in the West as patchouli or guang huo-xiang in China, is a long-time staple in traditional Chinese medicine for various indications, particularly gastrointestinal and skin disorders1.
Patchouli oil, which contains several mono- and sesquiterpenoids, alkaloids, and flavonoids, is thought to possess significant anti-inflammatory and antioxidant qualities2.In fact, it is reputed to impart antiviral, antioxidant, anti-inflammatory, and analgesic effects, and is also known to protect intestinal barrier function3. Peng et al. have found that patchouli oil exerts significant antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)4.
After a comprehensive 2013 review, Chen et al. deemed P. cablin to have potential clinical benefits as an effective adaptogenic herbal treatment3. It is thought to have some antiacne properties as well1. Further, P. cablin is among the Top 10 most-often-used traditional Chinese medicine prescriptions for skin care and appearance1.
In Brazil, China, Indonesia, and Malaysia, P. cablin is cultivated for its essential oil, which plays an important role in the perfume industry. Patchouli essential oil, featured in perfumes, soaps, cosmetics, and as incense, is used by aromatherapists for its calming and reviving effects. The essential oil has also been shown to impart antioxidant activity5.
In 2014, Lin et al. studied the protective effects of P. cablin essential oil against ultraviolet (UV)-induced skin photoaging in mice. The researchers applied patchouli oil for 2 hours before UV exposure to the dorsal depilated skin of mice. They found that patchouli oil doses of 6 mg/mouse and 9 mg/mouse significantly suppressed skin wrinkle formation, mitigated skin elasticity impairment, and augmented collagen content (21.9% and 26.3%, respectively). The same doses also yielded significant reductions in epidermal thickness and malondialdehyde content, and blocked the disruption of collagen and elastic fibers. Patchouli oil treatment also resulted in the up-regulation of the antioxidant enzymes superoxide dismutase, glutathione peroxidase, and catalase. The investigators concluded that patchouli oil, perhaps due to its antioxidant characteristics, and sesquiterpene constituents in particular, was effective in preventing photoaging in mice, and warrants attention as a potential agent to hinder photoaging in humans1.
Feng et al. also investigated the effects of topically applied patchouli alcohol on UV-induced photoaging in mice that year. For 9 weeks, investigators applied patchouli oil solution or a vehicle to the depilated dorsal skin of 6-week-old mice. They found that patchouli oil significantly hastened the recovery of UV-induced skin lesions, which they ascribed to the antioxidant and anti-inflammatory activity of the agent and its down-regulation of the expression of matrix metalloproteinase (MMP)-1 and MMP-32.
Antimicrobial and mosquito repellent activity
In a 2005 study by Trongtokit et al. of the mosquito-repellent activity of 38 essential oils at three concentrations (10%, 50%, or undiluted) against the mosquito Aedes aegypti under laboratory conditions using human volunteers, undiluted P. cablin oil was one of four [along with Cymbopogon nardus (citronella), Syzygium aromaticum (clove), and Zanthoxylum limonella (Thai name: makaen)] undiluted oils to yield an effect, 2 hours of full repellency. The investigators then tested the same concentrations of these oils for repellency against Culex quinquefasciatus (the Southern house mosquito) and Anopheles dirus (the mosquito considered to be a vector of malaria in Asian forested zones. The undiluted oils provided the greatest protection, with clove oil rendering the most durable repellency6.
Photoaging
Wu et al. determined the acaricidal activity of compounds extracted from patchouli oil against the house dust mite (Dermatophagoides farinae) in 2012. They isolated 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), the hydrolysate of pogostone, and 15 other constituents in patchouli oil, ultimately ascertaining that DHEMH and patchouli oil itself were the most toxic substances to D. farinae. The investigators concluded that patchouli oil and DHEMH warrant consideration and more study for their acaricidal potential as environmentally friendly, effective, and simple fumigant alternatives to chemical agents7.
In 2013, Yang et al. used molecular docking technology to evaluate the antibacterial activity of patchouli oil in vitro. They identified 26 compounds in patchouli oil displaying antibacterial activity, with pogostone and (-)-patchouli alcohol exhibiting the strongest activity8. Later that year, Yang et al. used the same technology to establish that Herba pogostemonis oil exhibited potent antibacterial effects, especially the constituents pogostone and (-)-Herba pogostemonis alcohol9. Raharjo and Fatchiyah also used molecular docking tools and Chimera 1.7s viewer software in a virtual screening of compounds from patchouli oil, concluding that alpha-patchouli alcohol is a potential inhibitor of the cyclo-oxygenase (COX)-1 enzyme. This is notable given the pivotal role of COX-1 in the inflammatory response10.
The next year, Peng et al. isolated one of the primary constituents of patchouli oil, pogostone, and assessed its antibacterial activity in vitro and in vivo. They found that pogostone suppressed both gram-negative and gram-positive bacteria in vitro. The researchers noted that pogostone was active against some drug-resistant bacteria (such as MRSA). Via intraperitoneal injection, pogostone displayed antibacterial activity in male and female Kunming mice against Escherichia coli and MRSA. At concentrations of 50 and 100 mg/kg, 90% of the mice infected with E. coli were protected; 60% of the mice at 25 mg/kg were protected. For mice with MRSA, 60% were protected at a dose of 100 mg/kg and 50% at a dose of 50 mg/kg. The investigators concluded that pogostone is a viable antibacterial agent for clinical use4.
Transdermal delivery
A 2008 study by Luo et al. showed that patchouli oil was among three volatile oils that improved the skin penetration of the flavonoids baicalin11. It was less effective than several compounds, including clove oil, camphor, menthol, and oleic acid, as a transdermal enhancer in a subsequent study by Zheng et al.12.
Conclusion
Patchouli oil continues to be used today in traditional Chinese medicine. In the West, the established literature on Pogostemon cablin is thin, but what has emerged recently, particularly studies on the protection against photoaging in mice, supports the continued investigation of this ancient herb to determine its potential role in dermatologic practice. As it is, much more research is necessary.
References
1. J Ethnopharmacol. 2014;154(2):408-18.
2. Eur J Pharm Sci. 2014;63:113-23.
3. Expert Opin Investig Drugs. 2013;22(2):245-57.
4. Chin Med J. (Engl) 2014;127(23):4001-5.
5. J Agric Food Chem. 2007;55(5):1737-42
6. Phytother Res. 2005;19(4):303-9.
7. Chem Pharm Bull (Tokyo). 2012;60(2):178-82.
8. Iran J Pharm Res. 2013 Summer;12(3):307-16.
9. Pak J Pharm Sci. 2013;26(6):1173-9.
10. Bioinformation 2013;9(6):321-4.
11. Zhong Yao Cai. 2008;31(11):1721-4
12. Zhongguo Zhong Yao Za Zhi. 2009;34(20):2599-603.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Pogostemon cablin, known in the West as patchouli or guang huo-xiang in China, is a long-time staple in traditional Chinese medicine for various indications, particularly gastrointestinal and skin disorders1.
Patchouli oil, which contains several mono- and sesquiterpenoids, alkaloids, and flavonoids, is thought to possess significant anti-inflammatory and antioxidant qualities2.In fact, it is reputed to impart antiviral, antioxidant, anti-inflammatory, and analgesic effects, and is also known to protect intestinal barrier function3. Peng et al. have found that patchouli oil exerts significant antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)4.
After a comprehensive 2013 review, Chen et al. deemed P. cablin to have potential clinical benefits as an effective adaptogenic herbal treatment3. It is thought to have some antiacne properties as well1. Further, P. cablin is among the Top 10 most-often-used traditional Chinese medicine prescriptions for skin care and appearance1.
In Brazil, China, Indonesia, and Malaysia, P. cablin is cultivated for its essential oil, which plays an important role in the perfume industry. Patchouli essential oil, featured in perfumes, soaps, cosmetics, and as incense, is used by aromatherapists for its calming and reviving effects. The essential oil has also been shown to impart antioxidant activity5.
In 2014, Lin et al. studied the protective effects of P. cablin essential oil against ultraviolet (UV)-induced skin photoaging in mice. The researchers applied patchouli oil for 2 hours before UV exposure to the dorsal depilated skin of mice. They found that patchouli oil doses of 6 mg/mouse and 9 mg/mouse significantly suppressed skin wrinkle formation, mitigated skin elasticity impairment, and augmented collagen content (21.9% and 26.3%, respectively). The same doses also yielded significant reductions in epidermal thickness and malondialdehyde content, and blocked the disruption of collagen and elastic fibers. Patchouli oil treatment also resulted in the up-regulation of the antioxidant enzymes superoxide dismutase, glutathione peroxidase, and catalase. The investigators concluded that patchouli oil, perhaps due to its antioxidant characteristics, and sesquiterpene constituents in particular, was effective in preventing photoaging in mice, and warrants attention as a potential agent to hinder photoaging in humans1.
Feng et al. also investigated the effects of topically applied patchouli alcohol on UV-induced photoaging in mice that year. For 9 weeks, investigators applied patchouli oil solution or a vehicle to the depilated dorsal skin of 6-week-old mice. They found that patchouli oil significantly hastened the recovery of UV-induced skin lesions, which they ascribed to the antioxidant and anti-inflammatory activity of the agent and its down-regulation of the expression of matrix metalloproteinase (MMP)-1 and MMP-32.
Antimicrobial and mosquito repellent activity
In a 2005 study by Trongtokit et al. of the mosquito-repellent activity of 38 essential oils at three concentrations (10%, 50%, or undiluted) against the mosquito Aedes aegypti under laboratory conditions using human volunteers, undiluted P. cablin oil was one of four [along with Cymbopogon nardus (citronella), Syzygium aromaticum (clove), and Zanthoxylum limonella (Thai name: makaen)] undiluted oils to yield an effect, 2 hours of full repellency. The investigators then tested the same concentrations of these oils for repellency against Culex quinquefasciatus (the Southern house mosquito) and Anopheles dirus (the mosquito considered to be a vector of malaria in Asian forested zones. The undiluted oils provided the greatest protection, with clove oil rendering the most durable repellency6.
Photoaging
Wu et al. determined the acaricidal activity of compounds extracted from patchouli oil against the house dust mite (Dermatophagoides farinae) in 2012. They isolated 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), the hydrolysate of pogostone, and 15 other constituents in patchouli oil, ultimately ascertaining that DHEMH and patchouli oil itself were the most toxic substances to D. farinae. The investigators concluded that patchouli oil and DHEMH warrant consideration and more study for their acaricidal potential as environmentally friendly, effective, and simple fumigant alternatives to chemical agents7.
In 2013, Yang et al. used molecular docking technology to evaluate the antibacterial activity of patchouli oil in vitro. They identified 26 compounds in patchouli oil displaying antibacterial activity, with pogostone and (-)-patchouli alcohol exhibiting the strongest activity8. Later that year, Yang et al. used the same technology to establish that Herba pogostemonis oil exhibited potent antibacterial effects, especially the constituents pogostone and (-)-Herba pogostemonis alcohol9. Raharjo and Fatchiyah also used molecular docking tools and Chimera 1.7s viewer software in a virtual screening of compounds from patchouli oil, concluding that alpha-patchouli alcohol is a potential inhibitor of the cyclo-oxygenase (COX)-1 enzyme. This is notable given the pivotal role of COX-1 in the inflammatory response10.
The next year, Peng et al. isolated one of the primary constituents of patchouli oil, pogostone, and assessed its antibacterial activity in vitro and in vivo. They found that pogostone suppressed both gram-negative and gram-positive bacteria in vitro. The researchers noted that pogostone was active against some drug-resistant bacteria (such as MRSA). Via intraperitoneal injection, pogostone displayed antibacterial activity in male and female Kunming mice against Escherichia coli and MRSA. At concentrations of 50 and 100 mg/kg, 90% of the mice infected with E. coli were protected; 60% of the mice at 25 mg/kg were protected. For mice with MRSA, 60% were protected at a dose of 100 mg/kg and 50% at a dose of 50 mg/kg. The investigators concluded that pogostone is a viable antibacterial agent for clinical use4.
Transdermal delivery
A 2008 study by Luo et al. showed that patchouli oil was among three volatile oils that improved the skin penetration of the flavonoids baicalin11. It was less effective than several compounds, including clove oil, camphor, menthol, and oleic acid, as a transdermal enhancer in a subsequent study by Zheng et al.12.
Conclusion
Patchouli oil continues to be used today in traditional Chinese medicine. In the West, the established literature on Pogostemon cablin is thin, but what has emerged recently, particularly studies on the protection against photoaging in mice, supports the continued investigation of this ancient herb to determine its potential role in dermatologic practice. As it is, much more research is necessary.
References
1. J Ethnopharmacol. 2014;154(2):408-18.
2. Eur J Pharm Sci. 2014;63:113-23.
3. Expert Opin Investig Drugs. 2013;22(2):245-57.
4. Chin Med J. (Engl) 2014;127(23):4001-5.
5. J Agric Food Chem. 2007;55(5):1737-42
6. Phytother Res. 2005;19(4):303-9.
7. Chem Pharm Bull (Tokyo). 2012;60(2):178-82.
8. Iran J Pharm Res. 2013 Summer;12(3):307-16.
9. Pak J Pharm Sci. 2013;26(6):1173-9.
10. Bioinformation 2013;9(6):321-4.
11. Zhong Yao Cai. 2008;31(11):1721-4
12. Zhongguo Zhong Yao Za Zhi. 2009;34(20):2599-603.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Black tea
Camellia sinensis, an evergreen tree belonging to the Theaceae family and used by human beings for approximately 4,000 years, is the source of the beverage tea, which is popular throughout the world, especially in Asia.1 Of the four main true teas (that is, derived from the tea plant C. sinensis), green and white are unfermented, black tea is fermented, and oolong tea is semifermented.2,3
Polyphenols, many of which act as strong antioxidants, are a diverse family of thousands of chemical substances found in plants. Theaflavins are black tea polyphenols with well-documented tumor-suppressing activity.4 In fact, they are thought to be the primary constituents of black tea responsible for conferring chemoprotection against cancer.5 Black tea, through oral administration and topical application, has been shown in the laboratory setting to protect skin from UV-induced erythema, premature aging, and cancer.6
Halder et al. have found that theaflavins and thearubigins, another key class of black tea polyphenols, can suppress A431 (human epidermoid carcinoma) and A375 (human malignant melanoma) cell proliferation without adversely impacting normal human epidermal keratinocytes. The researchers concluded that theaflavins and thearubigins appear to impart chemopreventive activity via cell cycle arrest and promotion of apoptosis in human skin cancer cells through a mitochondrial death cascade.7
In a 2005 English-language literature review, Thornfeldt cited green and black tea, as well as pomegranate, as the only ingredients supported by clinical trial evidence for effectiveness in treating extrinsic aging.2
Oral administration findings in animals and humans
More than 2 decades ago, Wang et al. found that the effects of orally administered black tea were comparable to those of green tea in suppressing UVB-induced skin carcinogenesis in 7,12-dimethylbenz[a]anthracene (DMBA)-initiated SKH-1 mice.8
In 1997, Lu et al. found that orally administered black tea inhibited the proliferation of skin tumors and enhanced apoptosis in nonmalignant and malignant skin tumors in female CD-1 mice with tumors initiated by the application of DMBA and promoted with 12-O-tetradecanoylphorbol-13-acetate (TPA).9 Record et al. reported in 1998 that black tea may confer greater protection than green tea against simulated solar irradiation.10
Hakim and Harris conducted a population-based case-control study in 2001 to assess the effects of the consumption of citrus peel and black tea on squamous cell skin cancer. They found that participants who reported intake of hot black tea and citrus peel had a significant reduction in the risk of squamous cell carcinoma. Further, they concluded that hot black tea and citrus peel displayed independent potential protection against SCC.11
Two years earlier, Zhao et al. used cultured keratinocytes and mouse and human skin to evaluate the effect of both orally and topically administered standardized black tea extract and its two major polyphenolic subfractions against UVB-induced photodamage. Topical pretreatment with the extract on SKH-1 hairless mice significantly lowered the incidence and severity of erythema and diminished skinfold thickness, compared with UVB-exposed nontreated mice. The black tea extract was similarly effective in human subjects. UVB-induced inflammation in murine as well as human skin also was reduced when the standardized extract was administered 5 minutes after UVB exposure. The investigators suggested that their findings indicated that black tea extracts have the capacity to mitigate UVB-generated erythema in human and murine skin.12
In 2011, George et al. assessed the chemopreventive effects of topical resveratrol and oral black tea polyphenols in blocking skin carcinogenesis in a two-stage mouse model initiated and promoted by DMBA and TPA, respectively. The combined treatment was found to reduce tumor incidence by approximately 89% (resveratrol alone, approximately 67%; black tea polyphenols alone, approximately 75%). Tumor volume and number also were significantly diminished by the synergistic combination, which, histologically, was noted for suppressing cellular proliferation and inducing apoptosis. The investigators concluded that oral black tea polyphenols combined with topical resveratrol exert greater chemopreventive activity than either compound alone and warrant study in trials for treating skin and other cancers.13
Animal studies on topical application
In 1997, Katiyar et al. investigated the anti-inflammatory effects of topically applied black tea polyphenols, primarily theaflavin gallates and (-)-epigallocatechin-3-gallate (EGCG), against TPA-induced inflammatory responses in murine skin. Significant inhibition against TPA-promoted induction of epidermal edema, hyperplasia, leukocyte infiltration, and proinflammatory cytokine expression was rendered by the preapplication of black tea polyphenols prior to TPA exposure. The investigators concluded that black tea polyphenols may be effective against human cutaneous inflammatory responses.14
Just over a decade later, Patel et al. investigated the in vivo antitumor-promoting effects of the most plentiful polymeric black tea polyphenols (thearubigins) in mice exposed to tumor-initiating DMBA and tumor-promoting TPA over a 40-week period. Pretreatment with topical thearubigins resulted in antipromoting effects in terms of latency, multiplicity, and incidence of skin papillomas. The black tea polyphenols also were found to reduce TPA-induced cell proliferation and epidermal cell apoptosis. The researchers attributed the protective effects of these compounds to their inhibitory impact on TPA-induced cellular proliferation.15
In 2011, Choi and Kim assessed the whitening effect of black tea water extract topically applied twice daily (6 days a week for 4 weeks) to UVB-induced hyperpigmented spots on the backs of brown guinea pigs. Treatment was divided into control (UVB and saline), vehicle control (UVB, propylene glycol, ethanol, and water), positive control (UVB and 2% hydroquinone), and two experimental groups (UVB and 1% black tea; UVB and 2% black tea). The investigators observed that the hyperpigmented spots treated with hydroquinone and black tea were clearly lighter than those treated by the control or vehicle-control groups. Histologic examination revealed that melanin pigmentation, melanocyte proliferation, and melanin production were significantly diminished in the groups treated with hydroquinone and both concentrations of black tea. The authors concluded that black tea suppresses melanocyte proliferation and melanosome synthesis in vivo, thus displaying the capacity to whiten skin in brown guinea pigs.16
In 2013, Yeh et al. found in nude mouse skin in vitro that niosomes appear to be feasible as a delivery vehicle for the dermal administration of black tea extracts as a sunscreen agent.1
Topical studies in humans
Building on findings 3 years earlier18, Türkoglu et al., in 2010, assessed the photoprotective effects of dermal gels produced from green and black tea aqueous extracts tested in vivo in the forearms of six volunteers exposed to artificial UV light (200-400 nm). In addition to the green tea and black tea gels, a 0.3% caffeine gel, a carbomer gel base, and a control were tested. The investigators reported no eruptions of UV-induced erythema in any of the black and green tea gel sites, but erythema was present to varying degrees at the areas treated with caffeine gel, carbomer gel, and control. The investigators concluded that the black and green tea extracts exhibited potent UV absorbance and that the formulated gels were effective in protecting the skin against UV-induced erythema. Further, the investigators suggested that these agents have the potential to protect against other harm caused by UV radiation, including photoaging.19
Conclusion
Though not as widely investigated as green tea, the therapeutic potential of black tea is of great interest. Although an abundance of laboratory evidence has emerged, clinical evidence is sparse. Nevertheless, laboratory data suggest the potential uses of black tea in the dermatologic realm and justify more human trials.
References
1. Cancer Lett. 1997 Mar 19;114(1-2):315-7.
2. Dermatol. Surg. 2005;31(7 Pt 2):873-80.
3. Oxid Med Cell Longev. 2012:2012:560682.
4. J Environ Pathol Toxicol Oncol. 2010;29(1):55-68.
5. Mol Carcinog. 2000 Jul;28(3):148-55.
6. Am J Clin Dermatol. 2010;11(4):247-67.
7. Carcinogenesis. 2008 Jan;29(1):129-38.
8. Cancer Res. 1994 Jul 1;54(13):3428-35.
9. Carcinogenesis. 1997 Nov;18(11):2163-9.
10. Mutat Res. 1998 Nov 9;422(1):191-9.
12. Photochem Photobiol. 1999 Oct;70(4):637-44.
13. PLoS One. 2011;6(8):e23395.
14. Carcinogenesis. 1997 Oct;18(10):1911-6.
15. Cell Prolif. 2008 Jun;41(3):532-53.
16. Toxicol Res. 2011 Sep;27(3):153-60.
17. Int J Dermatol. 2013 Feb;52(2):239-45.
18. Int J Cosmet Sci. 2007 Dec;29(6):437-42.
19. Drug Discov Ther. 2010 Oct;4(5):362-7.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Camellia sinensis, an evergreen tree belonging to the Theaceae family and used by human beings for approximately 4,000 years, is the source of the beverage tea, which is popular throughout the world, especially in Asia.1 Of the four main true teas (that is, derived from the tea plant C. sinensis), green and white are unfermented, black tea is fermented, and oolong tea is semifermented.2,3
Polyphenols, many of which act as strong antioxidants, are a diverse family of thousands of chemical substances found in plants. Theaflavins are black tea polyphenols with well-documented tumor-suppressing activity.4 In fact, they are thought to be the primary constituents of black tea responsible for conferring chemoprotection against cancer.5 Black tea, through oral administration and topical application, has been shown in the laboratory setting to protect skin from UV-induced erythema, premature aging, and cancer.6
Halder et al. have found that theaflavins and thearubigins, another key class of black tea polyphenols, can suppress A431 (human epidermoid carcinoma) and A375 (human malignant melanoma) cell proliferation without adversely impacting normal human epidermal keratinocytes. The researchers concluded that theaflavins and thearubigins appear to impart chemopreventive activity via cell cycle arrest and promotion of apoptosis in human skin cancer cells through a mitochondrial death cascade.7
In a 2005 English-language literature review, Thornfeldt cited green and black tea, as well as pomegranate, as the only ingredients supported by clinical trial evidence for effectiveness in treating extrinsic aging.2
Oral administration findings in animals and humans
More than 2 decades ago, Wang et al. found that the effects of orally administered black tea were comparable to those of green tea in suppressing UVB-induced skin carcinogenesis in 7,12-dimethylbenz[a]anthracene (DMBA)-initiated SKH-1 mice.8
In 1997, Lu et al. found that orally administered black tea inhibited the proliferation of skin tumors and enhanced apoptosis in nonmalignant and malignant skin tumors in female CD-1 mice with tumors initiated by the application of DMBA and promoted with 12-O-tetradecanoylphorbol-13-acetate (TPA).9 Record et al. reported in 1998 that black tea may confer greater protection than green tea against simulated solar irradiation.10
Hakim and Harris conducted a population-based case-control study in 2001 to assess the effects of the consumption of citrus peel and black tea on squamous cell skin cancer. They found that participants who reported intake of hot black tea and citrus peel had a significant reduction in the risk of squamous cell carcinoma. Further, they concluded that hot black tea and citrus peel displayed independent potential protection against SCC.11
Two years earlier, Zhao et al. used cultured keratinocytes and mouse and human skin to evaluate the effect of both orally and topically administered standardized black tea extract and its two major polyphenolic subfractions against UVB-induced photodamage. Topical pretreatment with the extract on SKH-1 hairless mice significantly lowered the incidence and severity of erythema and diminished skinfold thickness, compared with UVB-exposed nontreated mice. The black tea extract was similarly effective in human subjects. UVB-induced inflammation in murine as well as human skin also was reduced when the standardized extract was administered 5 minutes after UVB exposure. The investigators suggested that their findings indicated that black tea extracts have the capacity to mitigate UVB-generated erythema in human and murine skin.12
In 2011, George et al. assessed the chemopreventive effects of topical resveratrol and oral black tea polyphenols in blocking skin carcinogenesis in a two-stage mouse model initiated and promoted by DMBA and TPA, respectively. The combined treatment was found to reduce tumor incidence by approximately 89% (resveratrol alone, approximately 67%; black tea polyphenols alone, approximately 75%). Tumor volume and number also were significantly diminished by the synergistic combination, which, histologically, was noted for suppressing cellular proliferation and inducing apoptosis. The investigators concluded that oral black tea polyphenols combined with topical resveratrol exert greater chemopreventive activity than either compound alone and warrant study in trials for treating skin and other cancers.13
Animal studies on topical application
In 1997, Katiyar et al. investigated the anti-inflammatory effects of topically applied black tea polyphenols, primarily theaflavin gallates and (-)-epigallocatechin-3-gallate (EGCG), against TPA-induced inflammatory responses in murine skin. Significant inhibition against TPA-promoted induction of epidermal edema, hyperplasia, leukocyte infiltration, and proinflammatory cytokine expression was rendered by the preapplication of black tea polyphenols prior to TPA exposure. The investigators concluded that black tea polyphenols may be effective against human cutaneous inflammatory responses.14
Just over a decade later, Patel et al. investigated the in vivo antitumor-promoting effects of the most plentiful polymeric black tea polyphenols (thearubigins) in mice exposed to tumor-initiating DMBA and tumor-promoting TPA over a 40-week period. Pretreatment with topical thearubigins resulted in antipromoting effects in terms of latency, multiplicity, and incidence of skin papillomas. The black tea polyphenols also were found to reduce TPA-induced cell proliferation and epidermal cell apoptosis. The researchers attributed the protective effects of these compounds to their inhibitory impact on TPA-induced cellular proliferation.15
In 2011, Choi and Kim assessed the whitening effect of black tea water extract topically applied twice daily (6 days a week for 4 weeks) to UVB-induced hyperpigmented spots on the backs of brown guinea pigs. Treatment was divided into control (UVB and saline), vehicle control (UVB, propylene glycol, ethanol, and water), positive control (UVB and 2% hydroquinone), and two experimental groups (UVB and 1% black tea; UVB and 2% black tea). The investigators observed that the hyperpigmented spots treated with hydroquinone and black tea were clearly lighter than those treated by the control or vehicle-control groups. Histologic examination revealed that melanin pigmentation, melanocyte proliferation, and melanin production were significantly diminished in the groups treated with hydroquinone and both concentrations of black tea. The authors concluded that black tea suppresses melanocyte proliferation and melanosome synthesis in vivo, thus displaying the capacity to whiten skin in brown guinea pigs.16
In 2013, Yeh et al. found in nude mouse skin in vitro that niosomes appear to be feasible as a delivery vehicle for the dermal administration of black tea extracts as a sunscreen agent.1
Topical studies in humans
Building on findings 3 years earlier18, Türkoglu et al., in 2010, assessed the photoprotective effects of dermal gels produced from green and black tea aqueous extracts tested in vivo in the forearms of six volunteers exposed to artificial UV light (200-400 nm). In addition to the green tea and black tea gels, a 0.3% caffeine gel, a carbomer gel base, and a control were tested. The investigators reported no eruptions of UV-induced erythema in any of the black and green tea gel sites, but erythema was present to varying degrees at the areas treated with caffeine gel, carbomer gel, and control. The investigators concluded that the black and green tea extracts exhibited potent UV absorbance and that the formulated gels were effective in protecting the skin against UV-induced erythema. Further, the investigators suggested that these agents have the potential to protect against other harm caused by UV radiation, including photoaging.19
Conclusion
Though not as widely investigated as green tea, the therapeutic potential of black tea is of great interest. Although an abundance of laboratory evidence has emerged, clinical evidence is sparse. Nevertheless, laboratory data suggest the potential uses of black tea in the dermatologic realm and justify more human trials.
References
1. Cancer Lett. 1997 Mar 19;114(1-2):315-7.
2. Dermatol. Surg. 2005;31(7 Pt 2):873-80.
3. Oxid Med Cell Longev. 2012:2012:560682.
4. J Environ Pathol Toxicol Oncol. 2010;29(1):55-68.
5. Mol Carcinog. 2000 Jul;28(3):148-55.
6. Am J Clin Dermatol. 2010;11(4):247-67.
7. Carcinogenesis. 2008 Jan;29(1):129-38.
8. Cancer Res. 1994 Jul 1;54(13):3428-35.
9. Carcinogenesis. 1997 Nov;18(11):2163-9.
10. Mutat Res. 1998 Nov 9;422(1):191-9.
12. Photochem Photobiol. 1999 Oct;70(4):637-44.
13. PLoS One. 2011;6(8):e23395.
14. Carcinogenesis. 1997 Oct;18(10):1911-6.
15. Cell Prolif. 2008 Jun;41(3):532-53.
16. Toxicol Res. 2011 Sep;27(3):153-60.
17. Int J Dermatol. 2013 Feb;52(2):239-45.
18. Int J Cosmet Sci. 2007 Dec;29(6):437-42.
19. Drug Discov Ther. 2010 Oct;4(5):362-7.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Camellia sinensis, an evergreen tree belonging to the Theaceae family and used by human beings for approximately 4,000 years, is the source of the beverage tea, which is popular throughout the world, especially in Asia.1 Of the four main true teas (that is, derived from the tea plant C. sinensis), green and white are unfermented, black tea is fermented, and oolong tea is semifermented.2,3
Polyphenols, many of which act as strong antioxidants, are a diverse family of thousands of chemical substances found in plants. Theaflavins are black tea polyphenols with well-documented tumor-suppressing activity.4 In fact, they are thought to be the primary constituents of black tea responsible for conferring chemoprotection against cancer.5 Black tea, through oral administration and topical application, has been shown in the laboratory setting to protect skin from UV-induced erythema, premature aging, and cancer.6
Halder et al. have found that theaflavins and thearubigins, another key class of black tea polyphenols, can suppress A431 (human epidermoid carcinoma) and A375 (human malignant melanoma) cell proliferation without adversely impacting normal human epidermal keratinocytes. The researchers concluded that theaflavins and thearubigins appear to impart chemopreventive activity via cell cycle arrest and promotion of apoptosis in human skin cancer cells through a mitochondrial death cascade.7
In a 2005 English-language literature review, Thornfeldt cited green and black tea, as well as pomegranate, as the only ingredients supported by clinical trial evidence for effectiveness in treating extrinsic aging.2
Oral administration findings in animals and humans
More than 2 decades ago, Wang et al. found that the effects of orally administered black tea were comparable to those of green tea in suppressing UVB-induced skin carcinogenesis in 7,12-dimethylbenz[a]anthracene (DMBA)-initiated SKH-1 mice.8
In 1997, Lu et al. found that orally administered black tea inhibited the proliferation of skin tumors and enhanced apoptosis in nonmalignant and malignant skin tumors in female CD-1 mice with tumors initiated by the application of DMBA and promoted with 12-O-tetradecanoylphorbol-13-acetate (TPA).9 Record et al. reported in 1998 that black tea may confer greater protection than green tea against simulated solar irradiation.10
Hakim and Harris conducted a population-based case-control study in 2001 to assess the effects of the consumption of citrus peel and black tea on squamous cell skin cancer. They found that participants who reported intake of hot black tea and citrus peel had a significant reduction in the risk of squamous cell carcinoma. Further, they concluded that hot black tea and citrus peel displayed independent potential protection against SCC.11
Two years earlier, Zhao et al. used cultured keratinocytes and mouse and human skin to evaluate the effect of both orally and topically administered standardized black tea extract and its two major polyphenolic subfractions against UVB-induced photodamage. Topical pretreatment with the extract on SKH-1 hairless mice significantly lowered the incidence and severity of erythema and diminished skinfold thickness, compared with UVB-exposed nontreated mice. The black tea extract was similarly effective in human subjects. UVB-induced inflammation in murine as well as human skin also was reduced when the standardized extract was administered 5 minutes after UVB exposure. The investigators suggested that their findings indicated that black tea extracts have the capacity to mitigate UVB-generated erythema in human and murine skin.12
In 2011, George et al. assessed the chemopreventive effects of topical resveratrol and oral black tea polyphenols in blocking skin carcinogenesis in a two-stage mouse model initiated and promoted by DMBA and TPA, respectively. The combined treatment was found to reduce tumor incidence by approximately 89% (resveratrol alone, approximately 67%; black tea polyphenols alone, approximately 75%). Tumor volume and number also were significantly diminished by the synergistic combination, which, histologically, was noted for suppressing cellular proliferation and inducing apoptosis. The investigators concluded that oral black tea polyphenols combined with topical resveratrol exert greater chemopreventive activity than either compound alone and warrant study in trials for treating skin and other cancers.13
Animal studies on topical application
In 1997, Katiyar et al. investigated the anti-inflammatory effects of topically applied black tea polyphenols, primarily theaflavin gallates and (-)-epigallocatechin-3-gallate (EGCG), against TPA-induced inflammatory responses in murine skin. Significant inhibition against TPA-promoted induction of epidermal edema, hyperplasia, leukocyte infiltration, and proinflammatory cytokine expression was rendered by the preapplication of black tea polyphenols prior to TPA exposure. The investigators concluded that black tea polyphenols may be effective against human cutaneous inflammatory responses.14
Just over a decade later, Patel et al. investigated the in vivo antitumor-promoting effects of the most plentiful polymeric black tea polyphenols (thearubigins) in mice exposed to tumor-initiating DMBA and tumor-promoting TPA over a 40-week period. Pretreatment with topical thearubigins resulted in antipromoting effects in terms of latency, multiplicity, and incidence of skin papillomas. The black tea polyphenols also were found to reduce TPA-induced cell proliferation and epidermal cell apoptosis. The researchers attributed the protective effects of these compounds to their inhibitory impact on TPA-induced cellular proliferation.15
In 2011, Choi and Kim assessed the whitening effect of black tea water extract topically applied twice daily (6 days a week for 4 weeks) to UVB-induced hyperpigmented spots on the backs of brown guinea pigs. Treatment was divided into control (UVB and saline), vehicle control (UVB, propylene glycol, ethanol, and water), positive control (UVB and 2% hydroquinone), and two experimental groups (UVB and 1% black tea; UVB and 2% black tea). The investigators observed that the hyperpigmented spots treated with hydroquinone and black tea were clearly lighter than those treated by the control or vehicle-control groups. Histologic examination revealed that melanin pigmentation, melanocyte proliferation, and melanin production were significantly diminished in the groups treated with hydroquinone and both concentrations of black tea. The authors concluded that black tea suppresses melanocyte proliferation and melanosome synthesis in vivo, thus displaying the capacity to whiten skin in brown guinea pigs.16
In 2013, Yeh et al. found in nude mouse skin in vitro that niosomes appear to be feasible as a delivery vehicle for the dermal administration of black tea extracts as a sunscreen agent.1
Topical studies in humans
Building on findings 3 years earlier18, Türkoglu et al., in 2010, assessed the photoprotective effects of dermal gels produced from green and black tea aqueous extracts tested in vivo in the forearms of six volunteers exposed to artificial UV light (200-400 nm). In addition to the green tea and black tea gels, a 0.3% caffeine gel, a carbomer gel base, and a control were tested. The investigators reported no eruptions of UV-induced erythema in any of the black and green tea gel sites, but erythema was present to varying degrees at the areas treated with caffeine gel, carbomer gel, and control. The investigators concluded that the black and green tea extracts exhibited potent UV absorbance and that the formulated gels were effective in protecting the skin against UV-induced erythema. Further, the investigators suggested that these agents have the potential to protect against other harm caused by UV radiation, including photoaging.19
Conclusion
Though not as widely investigated as green tea, the therapeutic potential of black tea is of great interest. Although an abundance of laboratory evidence has emerged, clinical evidence is sparse. Nevertheless, laboratory data suggest the potential uses of black tea in the dermatologic realm and justify more human trials.
References
1. Cancer Lett. 1997 Mar 19;114(1-2):315-7.
2. Dermatol. Surg. 2005;31(7 Pt 2):873-80.
3. Oxid Med Cell Longev. 2012:2012:560682.
4. J Environ Pathol Toxicol Oncol. 2010;29(1):55-68.
5. Mol Carcinog. 2000 Jul;28(3):148-55.
6. Am J Clin Dermatol. 2010;11(4):247-67.
7. Carcinogenesis. 2008 Jan;29(1):129-38.
8. Cancer Res. 1994 Jul 1;54(13):3428-35.
9. Carcinogenesis. 1997 Nov;18(11):2163-9.
10. Mutat Res. 1998 Nov 9;422(1):191-9.
12. Photochem Photobiol. 1999 Oct;70(4):637-44.
13. PLoS One. 2011;6(8):e23395.
14. Carcinogenesis. 1997 Oct;18(10):1911-6.
15. Cell Prolif. 2008 Jun;41(3):532-53.
16. Toxicol Res. 2011 Sep;27(3):153-60.
17. Int J Dermatol. 2013 Feb;52(2):239-45.
18. Int J Cosmet Sci. 2007 Dec;29(6):437-42.
19. Drug Discov Ther. 2010 Oct;4(5):362-7.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Naringenin
The flavanone naringenin (5,7,4-trihydroxyflavanone) is known to exhibit anticarcinogenic, antioxidative, antiatherogenic, estrogenic, and immunomodulatory activity (Nutr. Cancer. 2012;64:714-24; J. Nutr. 2001;131:235-41; Life Sci. 2013;93:516-24). Naringenin can be found in high concentrations in grapefruits, oranges, and other citrus fruits as well as tomatoes (skin), with grapefruit juice found to yield much higher levels in plasma than orange juice (J. Nutr. 2001;131:235-41; Am. J. Physiol. Gastrointest. Liver Physiol. 2000;279:G1148-54; Nutr. Cancer 2012;64:714-24). Naringenin has been shown, along with other flavanones such as hesperetin and ponciretin, to strongly inhibit IgE-induced beta-hexosaminidase release from RBL-2H3 cells. Sung-Hwan Park and associates have suggested that the glycosides of these substances have potential as agents for treating IgE-induced atopic allergies (Planta Med. 2005;71:24-7).
In 2012, Kushi Anand and associates also showed that the combination of curcumin and naringenin exerted antiangiogenic and antitumor effects in Swiss albino mice, adding that neither compound has been associated with reports of toxicity in animals or humans (Nutr. Cancer 2012;64:714-24).
Potential cutaneous benefits
Tae-Ho Kim and colleagues studied the effects of naringenin on 2,4-dinitrofluorobenzene (DNFB)-induced atomic dermatitis in NC/Nga mice in 2013. After repetitive skin contact with DNFB, mice received intraperitoneal injections of naringenin for 1 week, with the treatment with the fruit flavonoid significantly diminishing ear swelling and back skin lesions. The flavonoid also significantly inhibited interferon (IFN)-alpha production by activated CD4+ T cells and lowered serum IgE levels as well as DNFB-induced infiltration of eosinophils, mast cells, CD4+ T cells, and CD8+ T cells in skin lesions (Life Sci. 2013;93:516-24).
Also that year, a naringenin glucoside (naringenin-7-O-glucoside) was found in an industrial blanch water extract, a byproduct of almond processing, and believed to play a role in exerting or contributing to a photoprotective effect in a small in vivo study with 12 volunteers (Molecules 2013;18:12426-40).
In 2014, K. Murata and associates screened several Prunus species in a search for skin-whitening compounds. Using an antityrosinase assay, the investigators determined that P. persica exhibited the greatest inhibitory activity and, in additional evaluation, it was found to hinder melanogenesis in B16 rat melanoma cells. Further, they identified afzelin (3-O-alpha-L-rhamnosylkaempferol) and the flavanone naringenin as the active ingredients responsible for inhibition of tyrosinase and melanogenesis and concluded that these substances warrant attention as potential skin-whitening agents (Nat. Prod. Commun. 2014;9:185-8).
A 2014 study in the ophthalmologic literature may also shed light on the photoprotective properties of naringenin. Jun-Li Lin and colleagues, studying the effects of the flavanone in eye drops used to treat N-methyl-N-nitrosourea (MNU)-induced photoreceptor cell death in rats, found that topical naringenin dose-dependently shielded the outer nuclear layer, outer retina, and whole retina, and prevented structural and functional damages to retinal neurons (Int. J. Ophthalmol. 2014;7:391-6).
Conclusion
The antioxidative, antiatherogenic, anticarcinogenic, antiproliferative, antimutagenic, estrogenic, and immunomodulatory properties of naringenin have been established in the laboratory. It remains to be seen whether such activity can be harnessed for medical applications, particularly in the dermatologic arena. Nevertheless, this flavanone warrants watching as research into its potential cutaneous applications proceeds. Currently, there is a dearth of research, though, regarding the use of naringenin in topical products.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
The flavanone naringenin (5,7,4-trihydroxyflavanone) is known to exhibit anticarcinogenic, antioxidative, antiatherogenic, estrogenic, and immunomodulatory activity (Nutr. Cancer. 2012;64:714-24; J. Nutr. 2001;131:235-41; Life Sci. 2013;93:516-24). Naringenin can be found in high concentrations in grapefruits, oranges, and other citrus fruits as well as tomatoes (skin), with grapefruit juice found to yield much higher levels in plasma than orange juice (J. Nutr. 2001;131:235-41; Am. J. Physiol. Gastrointest. Liver Physiol. 2000;279:G1148-54; Nutr. Cancer 2012;64:714-24). Naringenin has been shown, along with other flavanones such as hesperetin and ponciretin, to strongly inhibit IgE-induced beta-hexosaminidase release from RBL-2H3 cells. Sung-Hwan Park and associates have suggested that the glycosides of these substances have potential as agents for treating IgE-induced atopic allergies (Planta Med. 2005;71:24-7).
In 2012, Kushi Anand and associates also showed that the combination of curcumin and naringenin exerted antiangiogenic and antitumor effects in Swiss albino mice, adding that neither compound has been associated with reports of toxicity in animals or humans (Nutr. Cancer 2012;64:714-24).
Potential cutaneous benefits
Tae-Ho Kim and colleagues studied the effects of naringenin on 2,4-dinitrofluorobenzene (DNFB)-induced atomic dermatitis in NC/Nga mice in 2013. After repetitive skin contact with DNFB, mice received intraperitoneal injections of naringenin for 1 week, with the treatment with the fruit flavonoid significantly diminishing ear swelling and back skin lesions. The flavonoid also significantly inhibited interferon (IFN)-alpha production by activated CD4+ T cells and lowered serum IgE levels as well as DNFB-induced infiltration of eosinophils, mast cells, CD4+ T cells, and CD8+ T cells in skin lesions (Life Sci. 2013;93:516-24).
Also that year, a naringenin glucoside (naringenin-7-O-glucoside) was found in an industrial blanch water extract, a byproduct of almond processing, and believed to play a role in exerting or contributing to a photoprotective effect in a small in vivo study with 12 volunteers (Molecules 2013;18:12426-40).
In 2014, K. Murata and associates screened several Prunus species in a search for skin-whitening compounds. Using an antityrosinase assay, the investigators determined that P. persica exhibited the greatest inhibitory activity and, in additional evaluation, it was found to hinder melanogenesis in B16 rat melanoma cells. Further, they identified afzelin (3-O-alpha-L-rhamnosylkaempferol) and the flavanone naringenin as the active ingredients responsible for inhibition of tyrosinase and melanogenesis and concluded that these substances warrant attention as potential skin-whitening agents (Nat. Prod. Commun. 2014;9:185-8).
A 2014 study in the ophthalmologic literature may also shed light on the photoprotective properties of naringenin. Jun-Li Lin and colleagues, studying the effects of the flavanone in eye drops used to treat N-methyl-N-nitrosourea (MNU)-induced photoreceptor cell death in rats, found that topical naringenin dose-dependently shielded the outer nuclear layer, outer retina, and whole retina, and prevented structural and functional damages to retinal neurons (Int. J. Ophthalmol. 2014;7:391-6).
Conclusion
The antioxidative, antiatherogenic, anticarcinogenic, antiproliferative, antimutagenic, estrogenic, and immunomodulatory properties of naringenin have been established in the laboratory. It remains to be seen whether such activity can be harnessed for medical applications, particularly in the dermatologic arena. Nevertheless, this flavanone warrants watching as research into its potential cutaneous applications proceeds. Currently, there is a dearth of research, though, regarding the use of naringenin in topical products.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
The flavanone naringenin (5,7,4-trihydroxyflavanone) is known to exhibit anticarcinogenic, antioxidative, antiatherogenic, estrogenic, and immunomodulatory activity (Nutr. Cancer. 2012;64:714-24; J. Nutr. 2001;131:235-41; Life Sci. 2013;93:516-24). Naringenin can be found in high concentrations in grapefruits, oranges, and other citrus fruits as well as tomatoes (skin), with grapefruit juice found to yield much higher levels in plasma than orange juice (J. Nutr. 2001;131:235-41; Am. J. Physiol. Gastrointest. Liver Physiol. 2000;279:G1148-54; Nutr. Cancer 2012;64:714-24). Naringenin has been shown, along with other flavanones such as hesperetin and ponciretin, to strongly inhibit IgE-induced beta-hexosaminidase release from RBL-2H3 cells. Sung-Hwan Park and associates have suggested that the glycosides of these substances have potential as agents for treating IgE-induced atopic allergies (Planta Med. 2005;71:24-7).
In 2012, Kushi Anand and associates also showed that the combination of curcumin and naringenin exerted antiangiogenic and antitumor effects in Swiss albino mice, adding that neither compound has been associated with reports of toxicity in animals or humans (Nutr. Cancer 2012;64:714-24).
Potential cutaneous benefits
Tae-Ho Kim and colleagues studied the effects of naringenin on 2,4-dinitrofluorobenzene (DNFB)-induced atomic dermatitis in NC/Nga mice in 2013. After repetitive skin contact with DNFB, mice received intraperitoneal injections of naringenin for 1 week, with the treatment with the fruit flavonoid significantly diminishing ear swelling and back skin lesions. The flavonoid also significantly inhibited interferon (IFN)-alpha production by activated CD4+ T cells and lowered serum IgE levels as well as DNFB-induced infiltration of eosinophils, mast cells, CD4+ T cells, and CD8+ T cells in skin lesions (Life Sci. 2013;93:516-24).
Also that year, a naringenin glucoside (naringenin-7-O-glucoside) was found in an industrial blanch water extract, a byproduct of almond processing, and believed to play a role in exerting or contributing to a photoprotective effect in a small in vivo study with 12 volunteers (Molecules 2013;18:12426-40).
In 2014, K. Murata and associates screened several Prunus species in a search for skin-whitening compounds. Using an antityrosinase assay, the investigators determined that P. persica exhibited the greatest inhibitory activity and, in additional evaluation, it was found to hinder melanogenesis in B16 rat melanoma cells. Further, they identified afzelin (3-O-alpha-L-rhamnosylkaempferol) and the flavanone naringenin as the active ingredients responsible for inhibition of tyrosinase and melanogenesis and concluded that these substances warrant attention as potential skin-whitening agents (Nat. Prod. Commun. 2014;9:185-8).
A 2014 study in the ophthalmologic literature may also shed light on the photoprotective properties of naringenin. Jun-Li Lin and colleagues, studying the effects of the flavanone in eye drops used to treat N-methyl-N-nitrosourea (MNU)-induced photoreceptor cell death in rats, found that topical naringenin dose-dependently shielded the outer nuclear layer, outer retina, and whole retina, and prevented structural and functional damages to retinal neurons (Int. J. Ophthalmol. 2014;7:391-6).
Conclusion
The antioxidative, antiatherogenic, anticarcinogenic, antiproliferative, antimutagenic, estrogenic, and immunomodulatory properties of naringenin have been established in the laboratory. It remains to be seen whether such activity can be harnessed for medical applications, particularly in the dermatologic arena. Nevertheless, this flavanone warrants watching as research into its potential cutaneous applications proceeds. Currently, there is a dearth of research, though, regarding the use of naringenin in topical products.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Why your patients should buy skincare products from you
The Internet has changed many facets of modern life, and the practice of medicine has not gone untouched. Consider, for better or worse, the reliance of many patients on WebMD and various other sites for self-diagnosis before consulting with a physician. Even before the Internet, patients would self-diagnose their skin type (more than 80% of them get it wrong). The Internet allows them access to most cosmeceutical brands, the misuse of which leads to unintended consequences that can affect skin health. Clearly, patients who receive advice from a trained medical professional have better outcomes. One reason for this is that the doctor (or aesthetician) spends time with the patient, explaining what products to use and in which order to use them, and follows up with the patient to assess the outcome and adjust the regimen as needed. The problem arises when these patients decide to purchase the products from a source other than their treating physician. Only about 30% of patients buy refills from their doctor for second purchases, and just 15% purchase products from their doctor the third time around. Why is this? It is likely the convenience and the low cost that drive patients to purchase from sources other than their physician or aesthetician. This desire to save money carries significant risks. Many the products online are expired or counterfeit, or are old containers refilled with a different formulation. Patients should be cautioned to only buy products from a source they trust.
I have had dozens of patients bringing in counterfeit products in the last few months. It seems that the problem is becoming more common. I interviewed several companies about this to see whether others were experiencing the same trend. This is what I found:
Some companies report that they have seen their samples and trade size containers being sold on eBay. Joe Ragosta of Topix Pharmaceuticals reports that when his company has asked such sellers if they are obtaining these products – marked as samples – from the company, they hear a range of defensive responses, including: “I got it at a show” or “My doctor gave me samples, and I decided to sell them” and “I work at a doctor’s office, and they let me take products as needed.” Make sure that no one on your staff is taking samples and selling them online.
One example: NeoStrata is concerned about the fraudulent use of their products. They recommend that patients purchase their products only from a known physician, ideally from the physician’s office rather than the website. The company understands that customers may want to save money wherever they can and might prefer to buy products online. NeoStrata urges customers who opt to buy online to make such purchases through physician-affiliated websites, where the doctor is clearly identified. At the very least, the company urges patients to choose only sites where they can contact someone and obtain the name of a physician. Further, they strongly discourage using eBay or other auction sites, which do not vouch for the safety and authenticity of products sold through their services.
Other potential problems with skin care products sold online include the following.
Counterfeit products
Several reports have indicated that counterfeit skin products originating in other countries have made their way into the United States and, according to the article published on the website Fact Based Skin Care, pharmaceuticals and personal care products, including cosmetics, are among the top five types of products seized by U.S. Customs and Border Patrol agents (Coy, C. Dangers of Counterfeit Cosmetics, Aug. 4, 2014). Such products include old bottles refilled with inexpensive imitation creams or bottles made to look like legitimate products that in fact contain imitation creams. I once had a patient present with an adverse reaction to a retinol product, which she brought with her to the visit. I sent the bottle to the company, which confirmed my suspicion that the product was counterfeit – a different bottle with a similar label.
In February 2014, CBS New York ran a segment on the potential inclusion of carcinogenic and other harmful ingredients found in online personal care products touted for their low prices (CBS New York. Counterfeit Cosmetics May Be Harmful To Your Health. Feb. 27, 2014). Not even 2 weeks later, CNN reported on the arrest of two brothers in New York alleged to have masterminded a multimillion-dollar counterfeit health and beauty product ring (CNN. Zulueta A. Massive Fake Health and Beauty Supplies Ring Busted. March 9, 2014). ABC’s Good Morning America followed suit with a segment in April 2014 that exposed aspects of the use of knock-off cosmetic products (ABC News, Good Morning America. Online Beauty Bargains: Is It the Real Deal? April 3, 2014).
The Federal Bureau of Investigation has posted memos concerning counterfeit and potentially compromised and hazardous cosmetics and fragrances, offering tips aimed at readily identifying or avoiding unauthorized products.
Torie Hardee of EltaMD summarized that counterfeit products can sometimes be identified by lack of an expiration date on the bottle, discoloration or slightly different fonts on bottles and packaging, and the manufacturer’s address on the bottle.
Jan Marini Company representative Stuart Mohr noted that their company has received returns of products that they had not manufactured, as well as their own current or discontinued products returned years after the expiration date. The Jan Marini Co., and most other companies, will not guarantee any product purchased via nonauthorized resellers, because the authenticity and safety of such products cannot be verified.
“These unauthorized resellers are sophisticated, often even working in rings, and find it easy to hide their real identity,” said Mr. Mohr. “Addresses are often hidden or vague; emails are not linked to any specific person; and it’s easy to use false names. If a person is caught in an unauthorized online transaction, it’s easy to change the email address or name and start again,” he added.
FBI’s tips for spotting counterfeit cosmetics and fragrances
• The product is a sample size.
• The packaging differs slightly from the authentic brand (different color or font).
• The product’s wrapping appears haphazard.
• The product is being advertised as a “limited edition” even though the authentic manufacturer doesn’t offer it as a limited edition.
• The product is not listed on the manufacturer’s website.
• The price is drastically lower than the MSRP.
• The product’s consistency or texture doesn’t feel or look like the authentic brand.
• For fragrances, something seems off about the scent, and the color of the fluid in the bottle might be different than the original.
• They are being sold at nonauthorized retailers, including flea markets and discount stores.
• The label does not contain lot number, bar code, manufacturer’s address, or expiration date.
Expired products
Unscrupulous online retailers may slash prices on expired products and remove the expiration date from the package. In my practice, a patient experiencing an erythematous reaction brought in the “SkinMedica” product bottle, which looked suspicious to me. The packaging that the product was in had been discontinued 8 years earlier. It is important to remember that ingredients, particularly retinol, degrade with exposure to air, sun, and heat, and over time. This is most likely what caused my patient’s adverse reaction, and her initial savings from the product caused her several weeks of irritated skin.
Diverted products
SkinMedica reports that diverted products are a trickier issue than counterfeit products, because their packaging and formulas are sufficiently complex to make counterfeiting too difficult to be profitable. Instead, their products have been sold on the so-called gray market below the manufacturer suggested retail price (MSRP), typically online. In these cases, the company cannot help patients with returns or complaints because they cannot verify the chain of custody of the purchased product. They are addressing this problem, though, with an awareness campaign called “Authentic and Authorized.” Its goal is to alert patients and the physicians who dispense their products of the benefits of a physician-dispensed model of skin care, with best outcomes achieved when doctors are prescribing a skin care regimen. SkinMedica emphasizes that no website can guarantee outcomes comparable to a skin care professional and product quality and safety can only be enforced when dispensed through authorized channels.
Potentially illegal or toxic ingredients
Several products that have entered the United States marketed as skin lighteners, antiaging agents, and acne treatment products have been found to contain mercury, according to a consumer update from the FDA. Arsenic, lead, beryllium, and other harmful toxins as well as allergy-inducing fragrances or preservatives not approved as safe in the U.S. may also be found in such products of dubious origin.
Improper storage
Products purveyed online are often stored in hot warehouses. As mentioned above, heat degrades and alters ingredients, rendering compounds such as retinol, benzoyl peroxide, peptides, and ascorbic acid worthless. Extreme cold can also damage the chemical integrity of products. Notably, organic products are more vulnerable because they lack preservatives to gird them against temperature variations and microbes that grow in hot, damp environments.
Lookalike imposters
Generic formulations are packaged to piggyback onto the success of well-known products. Such products found in drugstores may be packaged to look like Cetaphil or Aveeno items, but cost less, and deliver less. While the ingredients on the copycats are identical to those found in the branded preparations, the order in which ingredients are added, the temperature, pH, and even when and how fast ingredients are stirred are part of the proprietary recipe of the company and play a significant role in the potential of the end product and the actions the product exerts on the skin.
Conclusion
Whether or not you sell skin care products in your office, there is much you can do to educate your patients about skin care product safety. Namely, the farther a consumer gets from the source of the product or from reliable endorsers of products, the greater the opportunity for encountering fraudulent or counterfeit products. Patients are best served by sources they can trust, such as their dermatologist. If you sell products in your office, encourage your patients to buy refills from you so they can be assured of the proper formulations. Finally, encourage your patients not to skimp when it comes to the health of their skin, reminding them that it may cost them much more in terms of time, skin irritation, improper treatment, and all related expenses to buy products cheaply from unreliable sources.
Give your patients a copy of this article so that they will understand the enormity of the problem.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
The Internet has changed many facets of modern life, and the practice of medicine has not gone untouched. Consider, for better or worse, the reliance of many patients on WebMD and various other sites for self-diagnosis before consulting with a physician. Even before the Internet, patients would self-diagnose their skin type (more than 80% of them get it wrong). The Internet allows them access to most cosmeceutical brands, the misuse of which leads to unintended consequences that can affect skin health. Clearly, patients who receive advice from a trained medical professional have better outcomes. One reason for this is that the doctor (or aesthetician) spends time with the patient, explaining what products to use and in which order to use them, and follows up with the patient to assess the outcome and adjust the regimen as needed. The problem arises when these patients decide to purchase the products from a source other than their treating physician. Only about 30% of patients buy refills from their doctor for second purchases, and just 15% purchase products from their doctor the third time around. Why is this? It is likely the convenience and the low cost that drive patients to purchase from sources other than their physician or aesthetician. This desire to save money carries significant risks. Many the products online are expired or counterfeit, or are old containers refilled with a different formulation. Patients should be cautioned to only buy products from a source they trust.
I have had dozens of patients bringing in counterfeit products in the last few months. It seems that the problem is becoming more common. I interviewed several companies about this to see whether others were experiencing the same trend. This is what I found:
Some companies report that they have seen their samples and trade size containers being sold on eBay. Joe Ragosta of Topix Pharmaceuticals reports that when his company has asked such sellers if they are obtaining these products – marked as samples – from the company, they hear a range of defensive responses, including: “I got it at a show” or “My doctor gave me samples, and I decided to sell them” and “I work at a doctor’s office, and they let me take products as needed.” Make sure that no one on your staff is taking samples and selling them online.
One example: NeoStrata is concerned about the fraudulent use of their products. They recommend that patients purchase their products only from a known physician, ideally from the physician’s office rather than the website. The company understands that customers may want to save money wherever they can and might prefer to buy products online. NeoStrata urges customers who opt to buy online to make such purchases through physician-affiliated websites, where the doctor is clearly identified. At the very least, the company urges patients to choose only sites where they can contact someone and obtain the name of a physician. Further, they strongly discourage using eBay or other auction sites, which do not vouch for the safety and authenticity of products sold through their services.
Other potential problems with skin care products sold online include the following.
Counterfeit products
Several reports have indicated that counterfeit skin products originating in other countries have made their way into the United States and, according to the article published on the website Fact Based Skin Care, pharmaceuticals and personal care products, including cosmetics, are among the top five types of products seized by U.S. Customs and Border Patrol agents (Coy, C. Dangers of Counterfeit Cosmetics, Aug. 4, 2014). Such products include old bottles refilled with inexpensive imitation creams or bottles made to look like legitimate products that in fact contain imitation creams. I once had a patient present with an adverse reaction to a retinol product, which she brought with her to the visit. I sent the bottle to the company, which confirmed my suspicion that the product was counterfeit – a different bottle with a similar label.
In February 2014, CBS New York ran a segment on the potential inclusion of carcinogenic and other harmful ingredients found in online personal care products touted for their low prices (CBS New York. Counterfeit Cosmetics May Be Harmful To Your Health. Feb. 27, 2014). Not even 2 weeks later, CNN reported on the arrest of two brothers in New York alleged to have masterminded a multimillion-dollar counterfeit health and beauty product ring (CNN. Zulueta A. Massive Fake Health and Beauty Supplies Ring Busted. March 9, 2014). ABC’s Good Morning America followed suit with a segment in April 2014 that exposed aspects of the use of knock-off cosmetic products (ABC News, Good Morning America. Online Beauty Bargains: Is It the Real Deal? April 3, 2014).
The Federal Bureau of Investigation has posted memos concerning counterfeit and potentially compromised and hazardous cosmetics and fragrances, offering tips aimed at readily identifying or avoiding unauthorized products.
Torie Hardee of EltaMD summarized that counterfeit products can sometimes be identified by lack of an expiration date on the bottle, discoloration or slightly different fonts on bottles and packaging, and the manufacturer’s address on the bottle.
Jan Marini Company representative Stuart Mohr noted that their company has received returns of products that they had not manufactured, as well as their own current or discontinued products returned years after the expiration date. The Jan Marini Co., and most other companies, will not guarantee any product purchased via nonauthorized resellers, because the authenticity and safety of such products cannot be verified.
“These unauthorized resellers are sophisticated, often even working in rings, and find it easy to hide their real identity,” said Mr. Mohr. “Addresses are often hidden or vague; emails are not linked to any specific person; and it’s easy to use false names. If a person is caught in an unauthorized online transaction, it’s easy to change the email address or name and start again,” he added.
FBI’s tips for spotting counterfeit cosmetics and fragrances
• The product is a sample size.
• The packaging differs slightly from the authentic brand (different color or font).
• The product’s wrapping appears haphazard.
• The product is being advertised as a “limited edition” even though the authentic manufacturer doesn’t offer it as a limited edition.
• The product is not listed on the manufacturer’s website.
• The price is drastically lower than the MSRP.
• The product’s consistency or texture doesn’t feel or look like the authentic brand.
• For fragrances, something seems off about the scent, and the color of the fluid in the bottle might be different than the original.
• They are being sold at nonauthorized retailers, including flea markets and discount stores.
• The label does not contain lot number, bar code, manufacturer’s address, or expiration date.
Expired products
Unscrupulous online retailers may slash prices on expired products and remove the expiration date from the package. In my practice, a patient experiencing an erythematous reaction brought in the “SkinMedica” product bottle, which looked suspicious to me. The packaging that the product was in had been discontinued 8 years earlier. It is important to remember that ingredients, particularly retinol, degrade with exposure to air, sun, and heat, and over time. This is most likely what caused my patient’s adverse reaction, and her initial savings from the product caused her several weeks of irritated skin.
Diverted products
SkinMedica reports that diverted products are a trickier issue than counterfeit products, because their packaging and formulas are sufficiently complex to make counterfeiting too difficult to be profitable. Instead, their products have been sold on the so-called gray market below the manufacturer suggested retail price (MSRP), typically online. In these cases, the company cannot help patients with returns or complaints because they cannot verify the chain of custody of the purchased product. They are addressing this problem, though, with an awareness campaign called “Authentic and Authorized.” Its goal is to alert patients and the physicians who dispense their products of the benefits of a physician-dispensed model of skin care, with best outcomes achieved when doctors are prescribing a skin care regimen. SkinMedica emphasizes that no website can guarantee outcomes comparable to a skin care professional and product quality and safety can only be enforced when dispensed through authorized channels.
Potentially illegal or toxic ingredients
Several products that have entered the United States marketed as skin lighteners, antiaging agents, and acne treatment products have been found to contain mercury, according to a consumer update from the FDA. Arsenic, lead, beryllium, and other harmful toxins as well as allergy-inducing fragrances or preservatives not approved as safe in the U.S. may also be found in such products of dubious origin.
Improper storage
Products purveyed online are often stored in hot warehouses. As mentioned above, heat degrades and alters ingredients, rendering compounds such as retinol, benzoyl peroxide, peptides, and ascorbic acid worthless. Extreme cold can also damage the chemical integrity of products. Notably, organic products are more vulnerable because they lack preservatives to gird them against temperature variations and microbes that grow in hot, damp environments.
Lookalike imposters
Generic formulations are packaged to piggyback onto the success of well-known products. Such products found in drugstores may be packaged to look like Cetaphil or Aveeno items, but cost less, and deliver less. While the ingredients on the copycats are identical to those found in the branded preparations, the order in which ingredients are added, the temperature, pH, and even when and how fast ingredients are stirred are part of the proprietary recipe of the company and play a significant role in the potential of the end product and the actions the product exerts on the skin.
Conclusion
Whether or not you sell skin care products in your office, there is much you can do to educate your patients about skin care product safety. Namely, the farther a consumer gets from the source of the product or from reliable endorsers of products, the greater the opportunity for encountering fraudulent or counterfeit products. Patients are best served by sources they can trust, such as their dermatologist. If you sell products in your office, encourage your patients to buy refills from you so they can be assured of the proper formulations. Finally, encourage your patients not to skimp when it comes to the health of their skin, reminding them that it may cost them much more in terms of time, skin irritation, improper treatment, and all related expenses to buy products cheaply from unreliable sources.
Give your patients a copy of this article so that they will understand the enormity of the problem.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
The Internet has changed many facets of modern life, and the practice of medicine has not gone untouched. Consider, for better or worse, the reliance of many patients on WebMD and various other sites for self-diagnosis before consulting with a physician. Even before the Internet, patients would self-diagnose their skin type (more than 80% of them get it wrong). The Internet allows them access to most cosmeceutical brands, the misuse of which leads to unintended consequences that can affect skin health. Clearly, patients who receive advice from a trained medical professional have better outcomes. One reason for this is that the doctor (or aesthetician) spends time with the patient, explaining what products to use and in which order to use them, and follows up with the patient to assess the outcome and adjust the regimen as needed. The problem arises when these patients decide to purchase the products from a source other than their treating physician. Only about 30% of patients buy refills from their doctor for second purchases, and just 15% purchase products from their doctor the third time around. Why is this? It is likely the convenience and the low cost that drive patients to purchase from sources other than their physician or aesthetician. This desire to save money carries significant risks. Many the products online are expired or counterfeit, or are old containers refilled with a different formulation. Patients should be cautioned to only buy products from a source they trust.
I have had dozens of patients bringing in counterfeit products in the last few months. It seems that the problem is becoming more common. I interviewed several companies about this to see whether others were experiencing the same trend. This is what I found:
Some companies report that they have seen their samples and trade size containers being sold on eBay. Joe Ragosta of Topix Pharmaceuticals reports that when his company has asked such sellers if they are obtaining these products – marked as samples – from the company, they hear a range of defensive responses, including: “I got it at a show” or “My doctor gave me samples, and I decided to sell them” and “I work at a doctor’s office, and they let me take products as needed.” Make sure that no one on your staff is taking samples and selling them online.
One example: NeoStrata is concerned about the fraudulent use of their products. They recommend that patients purchase their products only from a known physician, ideally from the physician’s office rather than the website. The company understands that customers may want to save money wherever they can and might prefer to buy products online. NeoStrata urges customers who opt to buy online to make such purchases through physician-affiliated websites, where the doctor is clearly identified. At the very least, the company urges patients to choose only sites where they can contact someone and obtain the name of a physician. Further, they strongly discourage using eBay or other auction sites, which do not vouch for the safety and authenticity of products sold through their services.
Other potential problems with skin care products sold online include the following.
Counterfeit products
Several reports have indicated that counterfeit skin products originating in other countries have made their way into the United States and, according to the article published on the website Fact Based Skin Care, pharmaceuticals and personal care products, including cosmetics, are among the top five types of products seized by U.S. Customs and Border Patrol agents (Coy, C. Dangers of Counterfeit Cosmetics, Aug. 4, 2014). Such products include old bottles refilled with inexpensive imitation creams or bottles made to look like legitimate products that in fact contain imitation creams. I once had a patient present with an adverse reaction to a retinol product, which she brought with her to the visit. I sent the bottle to the company, which confirmed my suspicion that the product was counterfeit – a different bottle with a similar label.
In February 2014, CBS New York ran a segment on the potential inclusion of carcinogenic and other harmful ingredients found in online personal care products touted for their low prices (CBS New York. Counterfeit Cosmetics May Be Harmful To Your Health. Feb. 27, 2014). Not even 2 weeks later, CNN reported on the arrest of two brothers in New York alleged to have masterminded a multimillion-dollar counterfeit health and beauty product ring (CNN. Zulueta A. Massive Fake Health and Beauty Supplies Ring Busted. March 9, 2014). ABC’s Good Morning America followed suit with a segment in April 2014 that exposed aspects of the use of knock-off cosmetic products (ABC News, Good Morning America. Online Beauty Bargains: Is It the Real Deal? April 3, 2014).
The Federal Bureau of Investigation has posted memos concerning counterfeit and potentially compromised and hazardous cosmetics and fragrances, offering tips aimed at readily identifying or avoiding unauthorized products.
Torie Hardee of EltaMD summarized that counterfeit products can sometimes be identified by lack of an expiration date on the bottle, discoloration or slightly different fonts on bottles and packaging, and the manufacturer’s address on the bottle.
Jan Marini Company representative Stuart Mohr noted that their company has received returns of products that they had not manufactured, as well as their own current or discontinued products returned years after the expiration date. The Jan Marini Co., and most other companies, will not guarantee any product purchased via nonauthorized resellers, because the authenticity and safety of such products cannot be verified.
“These unauthorized resellers are sophisticated, often even working in rings, and find it easy to hide their real identity,” said Mr. Mohr. “Addresses are often hidden or vague; emails are not linked to any specific person; and it’s easy to use false names. If a person is caught in an unauthorized online transaction, it’s easy to change the email address or name and start again,” he added.
FBI’s tips for spotting counterfeit cosmetics and fragrances
• The product is a sample size.
• The packaging differs slightly from the authentic brand (different color or font).
• The product’s wrapping appears haphazard.
• The product is being advertised as a “limited edition” even though the authentic manufacturer doesn’t offer it as a limited edition.
• The product is not listed on the manufacturer’s website.
• The price is drastically lower than the MSRP.
• The product’s consistency or texture doesn’t feel or look like the authentic brand.
• For fragrances, something seems off about the scent, and the color of the fluid in the bottle might be different than the original.
• They are being sold at nonauthorized retailers, including flea markets and discount stores.
• The label does not contain lot number, bar code, manufacturer’s address, or expiration date.
Expired products
Unscrupulous online retailers may slash prices on expired products and remove the expiration date from the package. In my practice, a patient experiencing an erythematous reaction brought in the “SkinMedica” product bottle, which looked suspicious to me. The packaging that the product was in had been discontinued 8 years earlier. It is important to remember that ingredients, particularly retinol, degrade with exposure to air, sun, and heat, and over time. This is most likely what caused my patient’s adverse reaction, and her initial savings from the product caused her several weeks of irritated skin.
Diverted products
SkinMedica reports that diverted products are a trickier issue than counterfeit products, because their packaging and formulas are sufficiently complex to make counterfeiting too difficult to be profitable. Instead, their products have been sold on the so-called gray market below the manufacturer suggested retail price (MSRP), typically online. In these cases, the company cannot help patients with returns or complaints because they cannot verify the chain of custody of the purchased product. They are addressing this problem, though, with an awareness campaign called “Authentic and Authorized.” Its goal is to alert patients and the physicians who dispense their products of the benefits of a physician-dispensed model of skin care, with best outcomes achieved when doctors are prescribing a skin care regimen. SkinMedica emphasizes that no website can guarantee outcomes comparable to a skin care professional and product quality and safety can only be enforced when dispensed through authorized channels.
Potentially illegal or toxic ingredients
Several products that have entered the United States marketed as skin lighteners, antiaging agents, and acne treatment products have been found to contain mercury, according to a consumer update from the FDA. Arsenic, lead, beryllium, and other harmful toxins as well as allergy-inducing fragrances or preservatives not approved as safe in the U.S. may also be found in such products of dubious origin.
Improper storage
Products purveyed online are often stored in hot warehouses. As mentioned above, heat degrades and alters ingredients, rendering compounds such as retinol, benzoyl peroxide, peptides, and ascorbic acid worthless. Extreme cold can also damage the chemical integrity of products. Notably, organic products are more vulnerable because they lack preservatives to gird them against temperature variations and microbes that grow in hot, damp environments.
Lookalike imposters
Generic formulations are packaged to piggyback onto the success of well-known products. Such products found in drugstores may be packaged to look like Cetaphil or Aveeno items, but cost less, and deliver less. While the ingredients on the copycats are identical to those found in the branded preparations, the order in which ingredients are added, the temperature, pH, and even when and how fast ingredients are stirred are part of the proprietary recipe of the company and play a significant role in the potential of the end product and the actions the product exerts on the skin.
Conclusion
Whether or not you sell skin care products in your office, there is much you can do to educate your patients about skin care product safety. Namely, the farther a consumer gets from the source of the product or from reliable endorsers of products, the greater the opportunity for encountering fraudulent or counterfeit products. Patients are best served by sources they can trust, such as their dermatologist. If you sell products in your office, encourage your patients to buy refills from you so they can be assured of the proper formulations. Finally, encourage your patients not to skimp when it comes to the health of their skin, reminding them that it may cost them much more in terms of time, skin irritation, improper treatment, and all related expenses to buy products cheaply from unreliable sources.
Give your patients a copy of this article so that they will understand the enormity of the problem.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Portulaca oleracea (purslane)
Portulaca oleracea, also known as purslane, has long been used in various traditional medicine systems to relieve pain and edema.1Portulaca oleracea is a warm-climate annual plant originally found in the Middle East, North Africa, and the Indian subcontinent and now cultivated in the Arabian peninsula; Japan, where it is an abundant garden plant from spring to fall;2,3 and throughout the world.
The use of P. oleracea, a member of the Portulacaceae family, as a vegetable as well as herbal medicine dates back several centuries.4 In modern times, purslane has been found to be rich in antioxidants, particularly omega-3 fatty acids, vitamins C and E, beta-carotene, melatonin, and glutathione, as well as several minerals.5,6,7 Currently, it is considered one of the top ten most common plants in the world, and one of the most-used medical plants according to the World Health Organization.6 It is considered a weed in the United States, but is eaten in many parts of the world.
Antioxidant activity
Using two different assays, Uddin et al. determined in 2012 that P. oleracea cultivars exhibited significant antioxidant activity through various growth stages. In addition, the researchers suggested that purslane could provide multiple minerals as well as antioxidants in the context of nutraceutical products and functional food.7 Early this year, Silva et al. studied the antioxidant activity of P. oleracea leaves, flowers, and stems from two different locations in Portugal, with assays revealing significantly greater antioxidant activity in the stems of both samples compared to the leaves and flowers. However, the phenolic extracts of all three plant sections from both samples were found to protect DNA against hydroxyl radicals. The investigators concluded that their findings, particularly related to high antioxidant activity, support the potential benefits of purslane consumption to human health.8
A 2014 analysis of 13 collected purslane accessions revealed significant mineral content (particularly potassium, followed by nitrogen, sodium, calcium, magnesium, phosphorus, iron, zinc, and manganese) and showed that antioxidant activity was more strongly associated with ornamental as opposed to common purslane, the latter of which was richer in mineral content.6
Anti-inflammatory activity
In 2000, Chan et al. found that a 10% ethanolic extract of the dried leaves and stem of a P. oleracea cultivar displayed significant anti-inflammatory and analgesic properties after topical and intraperitoneal, but not oral, administration in comparison to diclofenac sodium, a synthetic drug used as active control. They added that these activities corresponded to the reputed effects of the traditional uses of the wild species.9
Wound healing activity
Rashed et al. reported in 2003 that a crude extract of P. oleracea accelerates wound healing. They used Mus musculus JVI-1 to show that fresh homogenized crude aerial parts of the plant topically applied on excision wound surfaces reduced wound surface areas and increased tensile strength. The best documented contraction was associated with a single dose of 50 mg, followed by two doses of 25 mg each.10
Oral lichen planus treatment
In 2010, Agha-Hosseini et al. conducted a randomized double-blind placebo-controlled 3-month study to assess the effectiveness of purslane in the treatment of oral lichen planus. Thirty-seven symptomatic patients (confirmed by biopsy) were divided into a purslane treatment group (n = 20) and a placebo group (n = 17). The investigators reported that partial to complete clinical improvement was observed in 83% of the treatment group, with no response in the remaining 17%, whereas partial improvement was seen in 17% of the placebo group, 73% had no response, and the condition was aggravated in 10% of the placebo group. No adverse side effects were reported in either group, and the researchers concluded that purslane was clinically effective in treating oral lichen planus and warrants consideration as a treatment option for the disorder.5
Other activities
In 2001, Radhakrishnan et al. identified several neuropharmacological actions, particularly anti-nociceptive and muscle-relaxing activity, with a range of effects on the central and peripheral nervous system observed in animal studies.1 The betacyanins found in P. oleracea have subsequently been found to confer a protective effect against neurotoxicity, specifically, ameliorating the D-galactose-induced cognitive deficits in senescent mice.11P. oleracea also has been shown to efficiently eliminate the endocrine-disrupting chemical bisphenol A from a hydroponic solution.12
In 2012, Yan et al. showed that three newly isolated homoisoflavonoids, known as portulacanones, and the compound 2,2’-dihydroxy-4’,6’-dimethoxychalcone selectively exhibited in vitro cytotoxic activities against four human cancer cell lines.2
Conclusions
This antioxidant-rich plant is found throughout the world and has long been associated with traditional health care. Modern research into its potential dermatologic uses is ongoing, but the evidence is relatively scarce. There are indications that the antioxidant, anti-inflammatory, and wound healing activity reportedly exhibited by purslane may be harnessed for various cutaneous applications. However, much more research is necessary to determine how extensive a role purslane may play in skin care.
References
1.J. Ethnopharmacol. 2001;76:171-6
2.Phytochemistry 2012;80:37-41
3.J. Biosci. Bioeng. 2007;103:420-6
4.J. Ethnopharmacol. 2000;73:445-51
5.Phytother. Res. 2010;24:240-4
6.Biomed. Res. Int. 2014;2014:296063
7.Int. J. Mol. Sci. 2012;13:10257-67
8.Nat Prod. Commun. 2014;9:45-50
9. J. Ethnopharmacol. 2000;73:445-51
10. J. Ethnopharmacol. 2003;88:131-6
11. Phytomedicine. 2010 Jun;17:527-32
12. Biosci. Biotechnol. Biochem. 2012;76:1015-7
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Portulaca oleracea, also known as purslane, has long been used in various traditional medicine systems to relieve pain and edema.1Portulaca oleracea is a warm-climate annual plant originally found in the Middle East, North Africa, and the Indian subcontinent and now cultivated in the Arabian peninsula; Japan, where it is an abundant garden plant from spring to fall;2,3 and throughout the world.
The use of P. oleracea, a member of the Portulacaceae family, as a vegetable as well as herbal medicine dates back several centuries.4 In modern times, purslane has been found to be rich in antioxidants, particularly omega-3 fatty acids, vitamins C and E, beta-carotene, melatonin, and glutathione, as well as several minerals.5,6,7 Currently, it is considered one of the top ten most common plants in the world, and one of the most-used medical plants according to the World Health Organization.6 It is considered a weed in the United States, but is eaten in many parts of the world.
Antioxidant activity
Using two different assays, Uddin et al. determined in 2012 that P. oleracea cultivars exhibited significant antioxidant activity through various growth stages. In addition, the researchers suggested that purslane could provide multiple minerals as well as antioxidants in the context of nutraceutical products and functional food.7 Early this year, Silva et al. studied the antioxidant activity of P. oleracea leaves, flowers, and stems from two different locations in Portugal, with assays revealing significantly greater antioxidant activity in the stems of both samples compared to the leaves and flowers. However, the phenolic extracts of all three plant sections from both samples were found to protect DNA against hydroxyl radicals. The investigators concluded that their findings, particularly related to high antioxidant activity, support the potential benefits of purslane consumption to human health.8
A 2014 analysis of 13 collected purslane accessions revealed significant mineral content (particularly potassium, followed by nitrogen, sodium, calcium, magnesium, phosphorus, iron, zinc, and manganese) and showed that antioxidant activity was more strongly associated with ornamental as opposed to common purslane, the latter of which was richer in mineral content.6
Anti-inflammatory activity
In 2000, Chan et al. found that a 10% ethanolic extract of the dried leaves and stem of a P. oleracea cultivar displayed significant anti-inflammatory and analgesic properties after topical and intraperitoneal, but not oral, administration in comparison to diclofenac sodium, a synthetic drug used as active control. They added that these activities corresponded to the reputed effects of the traditional uses of the wild species.9
Wound healing activity
Rashed et al. reported in 2003 that a crude extract of P. oleracea accelerates wound healing. They used Mus musculus JVI-1 to show that fresh homogenized crude aerial parts of the plant topically applied on excision wound surfaces reduced wound surface areas and increased tensile strength. The best documented contraction was associated with a single dose of 50 mg, followed by two doses of 25 mg each.10
Oral lichen planus treatment
In 2010, Agha-Hosseini et al. conducted a randomized double-blind placebo-controlled 3-month study to assess the effectiveness of purslane in the treatment of oral lichen planus. Thirty-seven symptomatic patients (confirmed by biopsy) were divided into a purslane treatment group (n = 20) and a placebo group (n = 17). The investigators reported that partial to complete clinical improvement was observed in 83% of the treatment group, with no response in the remaining 17%, whereas partial improvement was seen in 17% of the placebo group, 73% had no response, and the condition was aggravated in 10% of the placebo group. No adverse side effects were reported in either group, and the researchers concluded that purslane was clinically effective in treating oral lichen planus and warrants consideration as a treatment option for the disorder.5
Other activities
In 2001, Radhakrishnan et al. identified several neuropharmacological actions, particularly anti-nociceptive and muscle-relaxing activity, with a range of effects on the central and peripheral nervous system observed in animal studies.1 The betacyanins found in P. oleracea have subsequently been found to confer a protective effect against neurotoxicity, specifically, ameliorating the D-galactose-induced cognitive deficits in senescent mice.11P. oleracea also has been shown to efficiently eliminate the endocrine-disrupting chemical bisphenol A from a hydroponic solution.12
In 2012, Yan et al. showed that three newly isolated homoisoflavonoids, known as portulacanones, and the compound 2,2’-dihydroxy-4’,6’-dimethoxychalcone selectively exhibited in vitro cytotoxic activities against four human cancer cell lines.2
Conclusions
This antioxidant-rich plant is found throughout the world and has long been associated with traditional health care. Modern research into its potential dermatologic uses is ongoing, but the evidence is relatively scarce. There are indications that the antioxidant, anti-inflammatory, and wound healing activity reportedly exhibited by purslane may be harnessed for various cutaneous applications. However, much more research is necessary to determine how extensive a role purslane may play in skin care.
References
1.J. Ethnopharmacol. 2001;76:171-6
2.Phytochemistry 2012;80:37-41
3.J. Biosci. Bioeng. 2007;103:420-6
4.J. Ethnopharmacol. 2000;73:445-51
5.Phytother. Res. 2010;24:240-4
6.Biomed. Res. Int. 2014;2014:296063
7.Int. J. Mol. Sci. 2012;13:10257-67
8.Nat Prod. Commun. 2014;9:45-50
9. J. Ethnopharmacol. 2000;73:445-51
10. J. Ethnopharmacol. 2003;88:131-6
11. Phytomedicine. 2010 Jun;17:527-32
12. Biosci. Biotechnol. Biochem. 2012;76:1015-7
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Portulaca oleracea, also known as purslane, has long been used in various traditional medicine systems to relieve pain and edema.1Portulaca oleracea is a warm-climate annual plant originally found in the Middle East, North Africa, and the Indian subcontinent and now cultivated in the Arabian peninsula; Japan, where it is an abundant garden plant from spring to fall;2,3 and throughout the world.
The use of P. oleracea, a member of the Portulacaceae family, as a vegetable as well as herbal medicine dates back several centuries.4 In modern times, purslane has been found to be rich in antioxidants, particularly omega-3 fatty acids, vitamins C and E, beta-carotene, melatonin, and glutathione, as well as several minerals.5,6,7 Currently, it is considered one of the top ten most common plants in the world, and one of the most-used medical plants according to the World Health Organization.6 It is considered a weed in the United States, but is eaten in many parts of the world.
Antioxidant activity
Using two different assays, Uddin et al. determined in 2012 that P. oleracea cultivars exhibited significant antioxidant activity through various growth stages. In addition, the researchers suggested that purslane could provide multiple minerals as well as antioxidants in the context of nutraceutical products and functional food.7 Early this year, Silva et al. studied the antioxidant activity of P. oleracea leaves, flowers, and stems from two different locations in Portugal, with assays revealing significantly greater antioxidant activity in the stems of both samples compared to the leaves and flowers. However, the phenolic extracts of all three plant sections from both samples were found to protect DNA against hydroxyl radicals. The investigators concluded that their findings, particularly related to high antioxidant activity, support the potential benefits of purslane consumption to human health.8
A 2014 analysis of 13 collected purslane accessions revealed significant mineral content (particularly potassium, followed by nitrogen, sodium, calcium, magnesium, phosphorus, iron, zinc, and manganese) and showed that antioxidant activity was more strongly associated with ornamental as opposed to common purslane, the latter of which was richer in mineral content.6
Anti-inflammatory activity
In 2000, Chan et al. found that a 10% ethanolic extract of the dried leaves and stem of a P. oleracea cultivar displayed significant anti-inflammatory and analgesic properties after topical and intraperitoneal, but not oral, administration in comparison to diclofenac sodium, a synthetic drug used as active control. They added that these activities corresponded to the reputed effects of the traditional uses of the wild species.9
Wound healing activity
Rashed et al. reported in 2003 that a crude extract of P. oleracea accelerates wound healing. They used Mus musculus JVI-1 to show that fresh homogenized crude aerial parts of the plant topically applied on excision wound surfaces reduced wound surface areas and increased tensile strength. The best documented contraction was associated with a single dose of 50 mg, followed by two doses of 25 mg each.10
Oral lichen planus treatment
In 2010, Agha-Hosseini et al. conducted a randomized double-blind placebo-controlled 3-month study to assess the effectiveness of purslane in the treatment of oral lichen planus. Thirty-seven symptomatic patients (confirmed by biopsy) were divided into a purslane treatment group (n = 20) and a placebo group (n = 17). The investigators reported that partial to complete clinical improvement was observed in 83% of the treatment group, with no response in the remaining 17%, whereas partial improvement was seen in 17% of the placebo group, 73% had no response, and the condition was aggravated in 10% of the placebo group. No adverse side effects were reported in either group, and the researchers concluded that purslane was clinically effective in treating oral lichen planus and warrants consideration as a treatment option for the disorder.5
Other activities
In 2001, Radhakrishnan et al. identified several neuropharmacological actions, particularly anti-nociceptive and muscle-relaxing activity, with a range of effects on the central and peripheral nervous system observed in animal studies.1 The betacyanins found in P. oleracea have subsequently been found to confer a protective effect against neurotoxicity, specifically, ameliorating the D-galactose-induced cognitive deficits in senescent mice.11P. oleracea also has been shown to efficiently eliminate the endocrine-disrupting chemical bisphenol A from a hydroponic solution.12
In 2012, Yan et al. showed that three newly isolated homoisoflavonoids, known as portulacanones, and the compound 2,2’-dihydroxy-4’,6’-dimethoxychalcone selectively exhibited in vitro cytotoxic activities against four human cancer cell lines.2
Conclusions
This antioxidant-rich plant is found throughout the world and has long been associated with traditional health care. Modern research into its potential dermatologic uses is ongoing, but the evidence is relatively scarce. There are indications that the antioxidant, anti-inflammatory, and wound healing activity reportedly exhibited by purslane may be harnessed for various cutaneous applications. However, much more research is necessary to determine how extensive a role purslane may play in skin care.
References
1.J. Ethnopharmacol. 2001;76:171-6
2.Phytochemistry 2012;80:37-41
3.J. Biosci. Bioeng. 2007;103:420-6
4.J. Ethnopharmacol. 2000;73:445-51
5.Phytother. Res. 2010;24:240-4
6.Biomed. Res. Int. 2014;2014:296063
7.Int. J. Mol. Sci. 2012;13:10257-67
8.Nat Prod. Commun. 2014;9:45-50
9. J. Ethnopharmacol. 2000;73:445-51
10. J. Ethnopharmacol. 2003;88:131-6
11. Phytomedicine. 2010 Jun;17:527-32
12. Biosci. Biotechnol. Biochem. 2012;76:1015-7
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Plantago major
For centuries, the leaves of Plantago major have been used in most regions of the world in traditional medical treatment of wounds and various diseases, including cutaneous conditions (J. Ethnopharmacol. 2000;71:1-21). P. major, also known as broadleaf plantain or greater plantain, is a member of the Plantaginaceae family, which is now widely dispersed throughout the world, though native to much of Europe as well as northern and central Asia. The Norwegian and Swedish name for the plant, groblad, means “healing leaves” (J. Ethnopharmacol. 2000;71:1-21). It was brought to the Americas by Europeans during the colonial period. Native Americans referred to it as the “white man’s footprint,” which inspired the genus name Plantago from the Latin planta (foot) (J. Ethnopharmacol. 2000;71:1-21).
Among the biologically active constituents of P. major are polysaccharides, lipids, caffeic acid derivatives, flavonoids (apigenin, luteolin, scutellarin, baicalein, nepetin, hispidulin, plantagoside), iridoid glycosides (aucubin, catalpol), terpenoids, and alkaloids (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In an ethnopharmacologic and folk medicine survey study of 1,225 residents of the Atlantic coast of Colombia completed in 2011, Gómez-Estrada et al. found that P. major was one of the plants traditionally used to treat inflammation; it also was used to treat kidney pain and eye injuries (J. Ethnobiol. Ethnomed. 2011;7:27). P. major also is traditionally used as a mucilage and bulk laxative (Principles and Practice of Phytotherapy: Modern Herbal Medicine, 2013, Churchill Livingstone).
Extracts of the plant have been associated with myriad biologic activities, including wound healing, anti-inflammatory, antimicrobial, analgesic, antioxidant, immunomodulating, and antiulcerogenic action, which Samuelsen suggested may account for the use of the botanical in traditional medicine (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In fact, the range of biologic properties attributed to P. major also includes astringent, anesthetic, antihelminthic, analeptic, antihistaminic, antirheumatic, antiviral, antitumor, antiulcer, diuretic, hypotensive, and expectorant activity (Exp. Biol. Med. [Maywood] 2012;237:1379-86). Though not the most popular botanical for this indication, P. major is among the plants used in the treatment of cutaneous leishmanial ulcers in Bahia, Brazil, where Leishmania brazilenesis is endemic (Rev. Soc. Bras. Med. Trop. 1996;29:229-32). Other dermatologic uses in traditional medicine include eczema, cuts, hemorrhoids, ulcerations, and wounds (Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press).
Wound healing
The use of P. major for wound healing dates back to the first century, as described by the Greek physician Dioscorides in “De Materia Medica” (J. Ethnopharmacol. 2000;71:1-21).
In 2011, Krasnov et al. developed an experimental model for characterizing proteins and showed that a newly discovered group of tissue-specific biogregulating proteins found previously in animal tissues was also present in P. major and responsible for the wound-healing activity associated with the plant (Prikl Biokhim. Mikrobiol. 2011;47:146-53).
The next year, Thomé et al. investigated and compared the wound-healing effects of P. major and Siparuna guianensis with a commercial product used in Brazil. Mice with cervical dorsal area wounds were treated with the botanical ingredients and the commercial product. Decreases in the wound area occurred earliest in mice treated with P. major, with complete closure (by day 15) seen only in this group. The investigators concluded that their findings support the traditional application of P. major, which shows potential as a viable wound-healing agent (Exp. Biol. Med. [Maywood] 2012;237:1379-86).
Conclusion
The numerous biologic properties of P. major are well established. In addition, use of the plant in traditional medicine for some cutaneous indications warrants consideration for modern therapeutic usage. Much more research is necessary, however, to elucidate the potential incorporation of this botanical into standard topical preparations for any of various skin conditions.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
For centuries, the leaves of Plantago major have been used in most regions of the world in traditional medical treatment of wounds and various diseases, including cutaneous conditions (J. Ethnopharmacol. 2000;71:1-21). P. major, also known as broadleaf plantain or greater plantain, is a member of the Plantaginaceae family, which is now widely dispersed throughout the world, though native to much of Europe as well as northern and central Asia. The Norwegian and Swedish name for the plant, groblad, means “healing leaves” (J. Ethnopharmacol. 2000;71:1-21). It was brought to the Americas by Europeans during the colonial period. Native Americans referred to it as the “white man’s footprint,” which inspired the genus name Plantago from the Latin planta (foot) (J. Ethnopharmacol. 2000;71:1-21).
Among the biologically active constituents of P. major are polysaccharides, lipids, caffeic acid derivatives, flavonoids (apigenin, luteolin, scutellarin, baicalein, nepetin, hispidulin, plantagoside), iridoid glycosides (aucubin, catalpol), terpenoids, and alkaloids (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In an ethnopharmacologic and folk medicine survey study of 1,225 residents of the Atlantic coast of Colombia completed in 2011, Gómez-Estrada et al. found that P. major was one of the plants traditionally used to treat inflammation; it also was used to treat kidney pain and eye injuries (J. Ethnobiol. Ethnomed. 2011;7:27). P. major also is traditionally used as a mucilage and bulk laxative (Principles and Practice of Phytotherapy: Modern Herbal Medicine, 2013, Churchill Livingstone).
Extracts of the plant have been associated with myriad biologic activities, including wound healing, anti-inflammatory, antimicrobial, analgesic, antioxidant, immunomodulating, and antiulcerogenic action, which Samuelsen suggested may account for the use of the botanical in traditional medicine (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In fact, the range of biologic properties attributed to P. major also includes astringent, anesthetic, antihelminthic, analeptic, antihistaminic, antirheumatic, antiviral, antitumor, antiulcer, diuretic, hypotensive, and expectorant activity (Exp. Biol. Med. [Maywood] 2012;237:1379-86). Though not the most popular botanical for this indication, P. major is among the plants used in the treatment of cutaneous leishmanial ulcers in Bahia, Brazil, where Leishmania brazilenesis is endemic (Rev. Soc. Bras. Med. Trop. 1996;29:229-32). Other dermatologic uses in traditional medicine include eczema, cuts, hemorrhoids, ulcerations, and wounds (Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press).
Wound healing
The use of P. major for wound healing dates back to the first century, as described by the Greek physician Dioscorides in “De Materia Medica” (J. Ethnopharmacol. 2000;71:1-21).
In 2011, Krasnov et al. developed an experimental model for characterizing proteins and showed that a newly discovered group of tissue-specific biogregulating proteins found previously in animal tissues was also present in P. major and responsible for the wound-healing activity associated with the plant (Prikl Biokhim. Mikrobiol. 2011;47:146-53).
The next year, Thomé et al. investigated and compared the wound-healing effects of P. major and Siparuna guianensis with a commercial product used in Brazil. Mice with cervical dorsal area wounds were treated with the botanical ingredients and the commercial product. Decreases in the wound area occurred earliest in mice treated with P. major, with complete closure (by day 15) seen only in this group. The investigators concluded that their findings support the traditional application of P. major, which shows potential as a viable wound-healing agent (Exp. Biol. Med. [Maywood] 2012;237:1379-86).
Conclusion
The numerous biologic properties of P. major are well established. In addition, use of the plant in traditional medicine for some cutaneous indications warrants consideration for modern therapeutic usage. Much more research is necessary, however, to elucidate the potential incorporation of this botanical into standard topical preparations for any of various skin conditions.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
For centuries, the leaves of Plantago major have been used in most regions of the world in traditional medical treatment of wounds and various diseases, including cutaneous conditions (J. Ethnopharmacol. 2000;71:1-21). P. major, also known as broadleaf plantain or greater plantain, is a member of the Plantaginaceae family, which is now widely dispersed throughout the world, though native to much of Europe as well as northern and central Asia. The Norwegian and Swedish name for the plant, groblad, means “healing leaves” (J. Ethnopharmacol. 2000;71:1-21). It was brought to the Americas by Europeans during the colonial period. Native Americans referred to it as the “white man’s footprint,” which inspired the genus name Plantago from the Latin planta (foot) (J. Ethnopharmacol. 2000;71:1-21).
Among the biologically active constituents of P. major are polysaccharides, lipids, caffeic acid derivatives, flavonoids (apigenin, luteolin, scutellarin, baicalein, nepetin, hispidulin, plantagoside), iridoid glycosides (aucubin, catalpol), terpenoids, and alkaloids (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In an ethnopharmacologic and folk medicine survey study of 1,225 residents of the Atlantic coast of Colombia completed in 2011, Gómez-Estrada et al. found that P. major was one of the plants traditionally used to treat inflammation; it also was used to treat kidney pain and eye injuries (J. Ethnobiol. Ethnomed. 2011;7:27). P. major also is traditionally used as a mucilage and bulk laxative (Principles and Practice of Phytotherapy: Modern Herbal Medicine, 2013, Churchill Livingstone).
Extracts of the plant have been associated with myriad biologic activities, including wound healing, anti-inflammatory, antimicrobial, analgesic, antioxidant, immunomodulating, and antiulcerogenic action, which Samuelsen suggested may account for the use of the botanical in traditional medicine (J. Ethnopharmacol. 2000;71:1-21; Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press). In fact, the range of biologic properties attributed to P. major also includes astringent, anesthetic, antihelminthic, analeptic, antihistaminic, antirheumatic, antiviral, antitumor, antiulcer, diuretic, hypotensive, and expectorant activity (Exp. Biol. Med. [Maywood] 2012;237:1379-86). Though not the most popular botanical for this indication, P. major is among the plants used in the treatment of cutaneous leishmanial ulcers in Bahia, Brazil, where Leishmania brazilenesis is endemic (Rev. Soc. Bras. Med. Trop. 1996;29:229-32). Other dermatologic uses in traditional medicine include eczema, cuts, hemorrhoids, ulcerations, and wounds (Medical Herbalism: The Science and Practice of Herbal Medicine, 2003, Healing Arts Press).
Wound healing
The use of P. major for wound healing dates back to the first century, as described by the Greek physician Dioscorides in “De Materia Medica” (J. Ethnopharmacol. 2000;71:1-21).
In 2011, Krasnov et al. developed an experimental model for characterizing proteins and showed that a newly discovered group of tissue-specific biogregulating proteins found previously in animal tissues was also present in P. major and responsible for the wound-healing activity associated with the plant (Prikl Biokhim. Mikrobiol. 2011;47:146-53).
The next year, Thomé et al. investigated and compared the wound-healing effects of P. major and Siparuna guianensis with a commercial product used in Brazil. Mice with cervical dorsal area wounds were treated with the botanical ingredients and the commercial product. Decreases in the wound area occurred earliest in mice treated with P. major, with complete closure (by day 15) seen only in this group. The investigators concluded that their findings support the traditional application of P. major, which shows potential as a viable wound-healing agent (Exp. Biol. Med. [Maywood] 2012;237:1379-86).
Conclusion
The numerous biologic properties of P. major are well established. In addition, use of the plant in traditional medicine for some cutaneous indications warrants consideration for modern therapeutic usage. Much more research is necessary, however, to elucidate the potential incorporation of this botanical into standard topical preparations for any of various skin conditions.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Kinetin and the skin
Kinetin (N6-furfuryladenine or 6-furfurylaminopurine) is a plant cytokinin or phytohormone that promotes cell division, delays senescence in plants, and is reputed to aid in the restoration of skin barrier function and, possibly, in reducing the signs and symptoms of rosacea (Clin. Exp. Dermatol. 2007;32:693-5; Plant Sci. 1999;148:37-45).
Kinetin is believed to develop in cellular DNA as a product of the oxidative, secondary modification of DNA (Plant Sci. 1999;148:37-45). In 1955, it became the first cytokinin isolated from DNA (from herring sperm) as an artifactual rearrangement product of the autoclaving process (J. Cosmet. Dermatol. 2007;6:243-9; Int. J. Biol. Macromol. 2007;40:182-92).
It has since been found to be present in human urine as well as DNA freshly extracted from human cells (Int. J. Biol. Macromol. 2007;40:182-92). The preponderance of amassed experimental evidence suggests that endogenous kinetin acts in vitro and in vivo as a potent antioxidant (Plant Sci. 1999;148:37-45). Currently, it is used as an anti-aging agent in various cosmetic products (J. Cosmet. Dermatol. 2007;6:243-9; J. Cosmet. Dermatol. 2010;9:218-25). Synthetic kinetin is thought to have the capacity to neutralize free radicals as well as limit the damage to DNA and fibroblasts (Photochem. Photobiol. 2012;88:748-52).
In vitro results
Olsen et al. demonstrated in vitro in 1999 that kinetin dose-dependently protected DNA against oxidative damage mediated by the Fenton reaction, and noted that kinetin had previously been linked to anti-aging activity in plants, fruit flies, and human cells in culture (Biochem. Biophys. Res. Commun. 1999;265:499-502). The following year, Verbeke et al. showed in vitro that kinetin potently inhibited damage caused by oxidation and glycoxidation (Biochem. Biophys. Res. Commun. 2000;276:1265-70).
In 2006, Vicanova et al. analyzed the effects of active ingredients from topical and systemic skin care formulations in vitro, finding that kinetin affected the upper dermis by enhancing deposits of fibrillin-1 and elastin fibers as well as their organization perpendicular to the dermal-epidermal junction. In the epidermis, kinetin stimulated keratinocyte production. Further, the investigators noted that the combination of topically applied kinetin with Imedeen Time Perfection ingredients (i.e., BioMarine Complex, grape seed extract, tomato extract, and vitamin C) supplemented systemically into culture medium yielded complementary benefits to dermal and epidermal development (Ann. N.Y. Acad. Sci. 2006;1067:337-42).
It is worth noting that in a study by Tournas et al. published the same month, investigators found that the topical application of a combination of vitamins C and E and ferulic acid yielded photoprotection to pig skin at 5 times the minimal erythema dose (MED) while individual antioxidants to which it was compared (i.e., coenzyme Q10, idebenone, and kinetin) delivered no photoprotective effects (J. Invest. Dermatol. 2006;126:1185-7). Nevertheless, Barciszewski et al. have observed that kinetin is the first stable secondary DNA damage product characterized by well defined cytokinin and anti-aging activity, with data showing that it has delayed human cellular aging in culture (Int. J. Biol. Macromol. 2007;40:182-92).
Rosacea
In 2007, Wu et al. performed a 12-week open-label study in 15 women and 3 men (aged 30-67 years) to ascertain the tolerability and efficacy of kinetin 0.1% lotion in the treatment of mild to moderate facial rosacea. Patients (17 of whom completed the study) applied the lotion twice daily, also daily applying an SPF 30 sunscreen. By week 4, significant improvements were observed in the reduction of skin roughness and mottled hyperpigmentation. Subject assessments at each 4-week interval after baseline and after 12 weeks revealed that kinetin 0.1% was well tolerated and effective for mild to moderate inflammatory rosacea (Clin. Exp. Dermatol. 2007;32:693-5).
Anti-aging
A 2002 study by J.L. McCullough and G.D. Weinstein represented the first evidence of the efficacy of topical kinetin in human beings, with twice-daily application for 24 weeks found to ameliorate skin texture, color, and blotchiness while diminishing rhytides and transepidermal water loss (J. Cosmet. Dermatol. 2002;15:29-32).
Two years later, T. Kimura and K. Doi showed that topical administration of kinetin improved the texture, wrinkling, and pigmentation of aged skin of hairless descendants of Mexican hairless dogs, resulting in notable depigmentation and rejuvenation after 100 days of treatment (Rejuvenation Res. 2004;7:32-9).In 2007, Chiu et al. conducted a randomized, double-blind, placebo-controlled, split-face comparative study in 52 Taiwanese subjects aged 30-60 years (90% of whom were female, all of whom had Fitzpatrick skin types II, III, or IV) to evaluate the clinical anti-aging effects and efficacy differences between kinetin plus niacinamide (kinetin 0.03%, niacinamide 4%) and niacinamide 4% alone versus vehicle placebo.
In the combination group, significant and sustained decreases were observed in counts of spots, pores, wrinkles, and evenness as well as persistent reductions in erythema index at weeks 8 and 12. At week 12, stratum corneum hydration status also was significantly enhanced in this group. In the niacinamide-only group, pore and evenness counts were significantly decreased at week 8, with declines in wrinkle counts emerging at week 12. The investigators concluded that kinetin and niacinamide display synergistic and dynamic anti-aging effects, showing substantial potential as topical anti-aging cosmeceutical agents (J. Cosmet. Dermatol. 2007;6:243-9).
However, Levin et al. noted in 2010 that while the effects of kinetin have been established in plants and its antioxidant properties have been displayed in vitro, the anti-aging effects and clinical efficacy ascribed to kinetin have been based on limited evidence, with no studies extant on the percutaneous absorption of kinetin. They added that research elucidating the mechanisms through which kinetin appears to improve skin barrier function, texture, and pigmentation also are lacking (J. Clin. Aesthet. Dermatol. 2010;3:22-41).
In 2012, Campos et al. assessed the effects on hydration, viscoelastic characteristics, and photoprotection of cosmetic preparations containing a dispersion of liposome with magnesium ascorbyl phosphate, alpha-lipoic acid, and kinetin. They observed that the formulation protected hairless mouse skin barrier function against UV harm. After 4 weeks of application on human skin, the combination product was found to have improved moisturization of the stratum corneum, also delivering hydration effects to deeper skin layers. The researchers concluded that the cosmetic formulation containing kinetin shows promise as a cutaneous anti-aging product (Photochem. Photobiol. 2012;88:748-52).
Conclusion
While some experimental and clinical results appear to suggest an anti-aging effect exerted by topically applied kinetin, much more research – particularly randomized controlled and comparison studies – are needed to provide a clearer picture as to the mechanisms and appropriate role of kinetin in the dermatologic armamentarium.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
Kinetin (N6-furfuryladenine or 6-furfurylaminopurine) is a plant cytokinin or phytohormone that promotes cell division, delays senescence in plants, and is reputed to aid in the restoration of skin barrier function and, possibly, in reducing the signs and symptoms of rosacea (Clin. Exp. Dermatol. 2007;32:693-5; Plant Sci. 1999;148:37-45).
Kinetin is believed to develop in cellular DNA as a product of the oxidative, secondary modification of DNA (Plant Sci. 1999;148:37-45). In 1955, it became the first cytokinin isolated from DNA (from herring sperm) as an artifactual rearrangement product of the autoclaving process (J. Cosmet. Dermatol. 2007;6:243-9; Int. J. Biol. Macromol. 2007;40:182-92).
It has since been found to be present in human urine as well as DNA freshly extracted from human cells (Int. J. Biol. Macromol. 2007;40:182-92). The preponderance of amassed experimental evidence suggests that endogenous kinetin acts in vitro and in vivo as a potent antioxidant (Plant Sci. 1999;148:37-45). Currently, it is used as an anti-aging agent in various cosmetic products (J. Cosmet. Dermatol. 2007;6:243-9; J. Cosmet. Dermatol. 2010;9:218-25). Synthetic kinetin is thought to have the capacity to neutralize free radicals as well as limit the damage to DNA and fibroblasts (Photochem. Photobiol. 2012;88:748-52).
In vitro results
Olsen et al. demonstrated in vitro in 1999 that kinetin dose-dependently protected DNA against oxidative damage mediated by the Fenton reaction, and noted that kinetin had previously been linked to anti-aging activity in plants, fruit flies, and human cells in culture (Biochem. Biophys. Res. Commun. 1999;265:499-502). The following year, Verbeke et al. showed in vitro that kinetin potently inhibited damage caused by oxidation and glycoxidation (Biochem. Biophys. Res. Commun. 2000;276:1265-70).
In 2006, Vicanova et al. analyzed the effects of active ingredients from topical and systemic skin care formulations in vitro, finding that kinetin affected the upper dermis by enhancing deposits of fibrillin-1 and elastin fibers as well as their organization perpendicular to the dermal-epidermal junction. In the epidermis, kinetin stimulated keratinocyte production. Further, the investigators noted that the combination of topically applied kinetin with Imedeen Time Perfection ingredients (i.e., BioMarine Complex, grape seed extract, tomato extract, and vitamin C) supplemented systemically into culture medium yielded complementary benefits to dermal and epidermal development (Ann. N.Y. Acad. Sci. 2006;1067:337-42).
It is worth noting that in a study by Tournas et al. published the same month, investigators found that the topical application of a combination of vitamins C and E and ferulic acid yielded photoprotection to pig skin at 5 times the minimal erythema dose (MED) while individual antioxidants to which it was compared (i.e., coenzyme Q10, idebenone, and kinetin) delivered no photoprotective effects (J. Invest. Dermatol. 2006;126:1185-7). Nevertheless, Barciszewski et al. have observed that kinetin is the first stable secondary DNA damage product characterized by well defined cytokinin and anti-aging activity, with data showing that it has delayed human cellular aging in culture (Int. J. Biol. Macromol. 2007;40:182-92).
Rosacea
In 2007, Wu et al. performed a 12-week open-label study in 15 women and 3 men (aged 30-67 years) to ascertain the tolerability and efficacy of kinetin 0.1% lotion in the treatment of mild to moderate facial rosacea. Patients (17 of whom completed the study) applied the lotion twice daily, also daily applying an SPF 30 sunscreen. By week 4, significant improvements were observed in the reduction of skin roughness and mottled hyperpigmentation. Subject assessments at each 4-week interval after baseline and after 12 weeks revealed that kinetin 0.1% was well tolerated and effective for mild to moderate inflammatory rosacea (Clin. Exp. Dermatol. 2007;32:693-5).
Anti-aging
A 2002 study by J.L. McCullough and G.D. Weinstein represented the first evidence of the efficacy of topical kinetin in human beings, with twice-daily application for 24 weeks found to ameliorate skin texture, color, and blotchiness while diminishing rhytides and transepidermal water loss (J. Cosmet. Dermatol. 2002;15:29-32).
Two years later, T. Kimura and K. Doi showed that topical administration of kinetin improved the texture, wrinkling, and pigmentation of aged skin of hairless descendants of Mexican hairless dogs, resulting in notable depigmentation and rejuvenation after 100 days of treatment (Rejuvenation Res. 2004;7:32-9).In 2007, Chiu et al. conducted a randomized, double-blind, placebo-controlled, split-face comparative study in 52 Taiwanese subjects aged 30-60 years (90% of whom were female, all of whom had Fitzpatrick skin types II, III, or IV) to evaluate the clinical anti-aging effects and efficacy differences between kinetin plus niacinamide (kinetin 0.03%, niacinamide 4%) and niacinamide 4% alone versus vehicle placebo.
In the combination group, significant and sustained decreases were observed in counts of spots, pores, wrinkles, and evenness as well as persistent reductions in erythema index at weeks 8 and 12. At week 12, stratum corneum hydration status also was significantly enhanced in this group. In the niacinamide-only group, pore and evenness counts were significantly decreased at week 8, with declines in wrinkle counts emerging at week 12. The investigators concluded that kinetin and niacinamide display synergistic and dynamic anti-aging effects, showing substantial potential as topical anti-aging cosmeceutical agents (J. Cosmet. Dermatol. 2007;6:243-9).
However, Levin et al. noted in 2010 that while the effects of kinetin have been established in plants and its antioxidant properties have been displayed in vitro, the anti-aging effects and clinical efficacy ascribed to kinetin have been based on limited evidence, with no studies extant on the percutaneous absorption of kinetin. They added that research elucidating the mechanisms through which kinetin appears to improve skin barrier function, texture, and pigmentation also are lacking (J. Clin. Aesthet. Dermatol. 2010;3:22-41).
In 2012, Campos et al. assessed the effects on hydration, viscoelastic characteristics, and photoprotection of cosmetic preparations containing a dispersion of liposome with magnesium ascorbyl phosphate, alpha-lipoic acid, and kinetin. They observed that the formulation protected hairless mouse skin barrier function against UV harm. After 4 weeks of application on human skin, the combination product was found to have improved moisturization of the stratum corneum, also delivering hydration effects to deeper skin layers. The researchers concluded that the cosmetic formulation containing kinetin shows promise as a cutaneous anti-aging product (Photochem. Photobiol. 2012;88:748-52).
Conclusion
While some experimental and clinical results appear to suggest an anti-aging effect exerted by topically applied kinetin, much more research – particularly randomized controlled and comparison studies – are needed to provide a clearer picture as to the mechanisms and appropriate role of kinetin in the dermatologic armamentarium.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
Kinetin (N6-furfuryladenine or 6-furfurylaminopurine) is a plant cytokinin or phytohormone that promotes cell division, delays senescence in plants, and is reputed to aid in the restoration of skin barrier function and, possibly, in reducing the signs and symptoms of rosacea (Clin. Exp. Dermatol. 2007;32:693-5; Plant Sci. 1999;148:37-45).
Kinetin is believed to develop in cellular DNA as a product of the oxidative, secondary modification of DNA (Plant Sci. 1999;148:37-45). In 1955, it became the first cytokinin isolated from DNA (from herring sperm) as an artifactual rearrangement product of the autoclaving process (J. Cosmet. Dermatol. 2007;6:243-9; Int. J. Biol. Macromol. 2007;40:182-92).
It has since been found to be present in human urine as well as DNA freshly extracted from human cells (Int. J. Biol. Macromol. 2007;40:182-92). The preponderance of amassed experimental evidence suggests that endogenous kinetin acts in vitro and in vivo as a potent antioxidant (Plant Sci. 1999;148:37-45). Currently, it is used as an anti-aging agent in various cosmetic products (J. Cosmet. Dermatol. 2007;6:243-9; J. Cosmet. Dermatol. 2010;9:218-25). Synthetic kinetin is thought to have the capacity to neutralize free radicals as well as limit the damage to DNA and fibroblasts (Photochem. Photobiol. 2012;88:748-52).
In vitro results
Olsen et al. demonstrated in vitro in 1999 that kinetin dose-dependently protected DNA against oxidative damage mediated by the Fenton reaction, and noted that kinetin had previously been linked to anti-aging activity in plants, fruit flies, and human cells in culture (Biochem. Biophys. Res. Commun. 1999;265:499-502). The following year, Verbeke et al. showed in vitro that kinetin potently inhibited damage caused by oxidation and glycoxidation (Biochem. Biophys. Res. Commun. 2000;276:1265-70).
In 2006, Vicanova et al. analyzed the effects of active ingredients from topical and systemic skin care formulations in vitro, finding that kinetin affected the upper dermis by enhancing deposits of fibrillin-1 and elastin fibers as well as their organization perpendicular to the dermal-epidermal junction. In the epidermis, kinetin stimulated keratinocyte production. Further, the investigators noted that the combination of topically applied kinetin with Imedeen Time Perfection ingredients (i.e., BioMarine Complex, grape seed extract, tomato extract, and vitamin C) supplemented systemically into culture medium yielded complementary benefits to dermal and epidermal development (Ann. N.Y. Acad. Sci. 2006;1067:337-42).
It is worth noting that in a study by Tournas et al. published the same month, investigators found that the topical application of a combination of vitamins C and E and ferulic acid yielded photoprotection to pig skin at 5 times the minimal erythema dose (MED) while individual antioxidants to which it was compared (i.e., coenzyme Q10, idebenone, and kinetin) delivered no photoprotective effects (J. Invest. Dermatol. 2006;126:1185-7). Nevertheless, Barciszewski et al. have observed that kinetin is the first stable secondary DNA damage product characterized by well defined cytokinin and anti-aging activity, with data showing that it has delayed human cellular aging in culture (Int. J. Biol. Macromol. 2007;40:182-92).
Rosacea
In 2007, Wu et al. performed a 12-week open-label study in 15 women and 3 men (aged 30-67 years) to ascertain the tolerability and efficacy of kinetin 0.1% lotion in the treatment of mild to moderate facial rosacea. Patients (17 of whom completed the study) applied the lotion twice daily, also daily applying an SPF 30 sunscreen. By week 4, significant improvements were observed in the reduction of skin roughness and mottled hyperpigmentation. Subject assessments at each 4-week interval after baseline and after 12 weeks revealed that kinetin 0.1% was well tolerated and effective for mild to moderate inflammatory rosacea (Clin. Exp. Dermatol. 2007;32:693-5).
Anti-aging
A 2002 study by J.L. McCullough and G.D. Weinstein represented the first evidence of the efficacy of topical kinetin in human beings, with twice-daily application for 24 weeks found to ameliorate skin texture, color, and blotchiness while diminishing rhytides and transepidermal water loss (J. Cosmet. Dermatol. 2002;15:29-32).
Two years later, T. Kimura and K. Doi showed that topical administration of kinetin improved the texture, wrinkling, and pigmentation of aged skin of hairless descendants of Mexican hairless dogs, resulting in notable depigmentation and rejuvenation after 100 days of treatment (Rejuvenation Res. 2004;7:32-9).In 2007, Chiu et al. conducted a randomized, double-blind, placebo-controlled, split-face comparative study in 52 Taiwanese subjects aged 30-60 years (90% of whom were female, all of whom had Fitzpatrick skin types II, III, or IV) to evaluate the clinical anti-aging effects and efficacy differences between kinetin plus niacinamide (kinetin 0.03%, niacinamide 4%) and niacinamide 4% alone versus vehicle placebo.
In the combination group, significant and sustained decreases were observed in counts of spots, pores, wrinkles, and evenness as well as persistent reductions in erythema index at weeks 8 and 12. At week 12, stratum corneum hydration status also was significantly enhanced in this group. In the niacinamide-only group, pore and evenness counts were significantly decreased at week 8, with declines in wrinkle counts emerging at week 12. The investigators concluded that kinetin and niacinamide display synergistic and dynamic anti-aging effects, showing substantial potential as topical anti-aging cosmeceutical agents (J. Cosmet. Dermatol. 2007;6:243-9).
However, Levin et al. noted in 2010 that while the effects of kinetin have been established in plants and its antioxidant properties have been displayed in vitro, the anti-aging effects and clinical efficacy ascribed to kinetin have been based on limited evidence, with no studies extant on the percutaneous absorption of kinetin. They added that research elucidating the mechanisms through which kinetin appears to improve skin barrier function, texture, and pigmentation also are lacking (J. Clin. Aesthet. Dermatol. 2010;3:22-41).
In 2012, Campos et al. assessed the effects on hydration, viscoelastic characteristics, and photoprotection of cosmetic preparations containing a dispersion of liposome with magnesium ascorbyl phosphate, alpha-lipoic acid, and kinetin. They observed that the formulation protected hairless mouse skin barrier function against UV harm. After 4 weeks of application on human skin, the combination product was found to have improved moisturization of the stratum corneum, also delivering hydration effects to deeper skin layers. The researchers concluded that the cosmetic formulation containing kinetin shows promise as a cutaneous anti-aging product (Photochem. Photobiol. 2012;88:748-52).
Conclusion
While some experimental and clinical results appear to suggest an anti-aging effect exerted by topically applied kinetin, much more research – particularly randomized controlled and comparison studies – are needed to provide a clearer picture as to the mechanisms and appropriate role of kinetin in the dermatologic armamentarium.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera Biopharmaceuticals, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
Kaempferol
Kaempferol (3,5,7,4’-tetrahydroxyflavone; C15H10O6) is among the natural flavonols found in green tea, broccoli, cabbage, kale, endive, beans, leeks, tomatoes, grapes, apples, grapefruit, berries, and propolis, as well as myriad other plant sources, including Brassica and species (J. Agric. Food Chem. 2006;54:2951-6; Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]).
It is one of the most commonly found dietary flavonoids and is also present in beer, particularly hops (Carcinogenesis 2010;31:1338-43; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]). Significantly, kaempferol is known to exhibit anticancer, anti-inflammatory, antioxidant, cytoprotective, and antiapoptotic activity (Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Exp. Mol. Med. 2008;40:208-19), and is believed to play a role in protecting plants from ultraviolet (UV)-induced damage (J. Agric. Food Chem. 2012;60:6966-76).
Skin protection: antioxidant and anti-inflammatory activity
Among 35 flavonoids tested by Cos et al. in 2001 for lipid peroxidation-inhibiting activity, kaempferol was identified as having the highest antioxidant selectivity index (Planta Med. 2001;67:515-9).
Work by Kim et al. in 2002 revealed that four kaempferol glycosides are key active ingredients in the flowers of Prunus persica, which has long been used in traditional Chinese medicine to treat skin disorders (J. Cosmet. Sci. 2002;53:27-34). Kim and colleagues have also shown in animal studies that the topical application of P. persica may be effective at thwarting UVB-induced skin damage (J. Cosmet. Sci. 2002;53:27-34).
In addition, kaempferol is a key component in Punica granatum, which has been found to act as an effective protector against UVB-induced photodamage and aging in cultured skin fibroblasts (Int. J. Dermatol. 2010;49:276-82).
In various tests on the effects of natural flavonoids on matrix metalloproteinase (MMP)-1 activity and expression, Lim et al. reported in 2007 that kaempferol and quercetin potently inhibited recombinant human MMP-1, and both flavonols along with apigenin and wogonin were found to be strong inhibitors of MMP-1 induction in 12-O-tetradecanoylphorbol-13-acetate–treated human dermal fibroblasts. All four flavonoids also suppressed the activation of activator protein (AP)-1. Kaempferol also hindered p38 mitogen-activated protein kinase c-Jun N-terminal kinase (JNK) activation. The investigators concluded that kaempferol is among the flavonoids or plant extracts containing them that may be useful as an agent to protect against photoaging and to treat some cutaneous inflammatory conditions (Planta Med. 2007;73:1267-74).
In 2010, Park et al. demonstrated that kaempferol alleviated burn injuries in mice and that expression of tumor necrosis factor–alpha (TNF-alpha) induced by burn injuries was reduced by kaempferol. They concluded that their findings suggest the possible application of kaempferol to treat thermal burn–induced skin injuries (BMB Rep. 2010;43:46-51).
Anti-inflammatory as well as depigmenting activity was found by Rho et al. in 2011 to be associated with kaempferol and kaempferol rhamnosides isolated from Hibiscus cannabinus (Molecules 2011;16:3338-44).
In 2014, Kim et al. found that extracts of Aceriphyllum rossii (native to Korea and China) and its active constituents, quercetin and kaempferol, blocked secretion of beta-hexosaminidase and histamine; lowered the production and mRNA expression of interleukin-4 and TNF-alpha; and reduced prostaglandin E2 and leukotriene B4 synthesis as well as the expression of cyclooxygenase-2 (COX-2) and 5-lipoxygenase. These and other findings led the investigators to conclude that A. rossii and its active ingredients kaempferol and quercetin may be effective agents for the treatment of immediate-type hypersensitivity (J. Agric. Food Chem. 2014;62:3750-8).
Anticancer activity
Lee et al. reported in 2010 that the inhibition by kaempferol of phosphatidylinositol 3-kinase (PI3K) activity, a key factor in carcinogenesis, and its concomitant effects may account for the chemopreventive activity of the flavonol (Carcinogenesis 2010;31:1338-43).
At the end of that year, Lee et al. found that kaempferol inhibited UVB-induced COX-2 protein expression in mouse skin epidermal JB6 P+ cells, by blocking Src kinase activity and attenuated the UVB-induced transcriptional activities of COX-2 gene and the transcription factor AP-1. They concluded that kaempferol exerts robust chemopreventive activity against skin cancer by suppressing Src (Biochem. Pharmacol. 2010;80:2042-9).
In 2014, Yao et al. found that kaempferol acted as a safe and potent inhibitor of solar ultraviolet-induced mouse skin carcinogenesis that acted by targeting RSK2 and MSK1 (Cancer Prev. Res. (Phila) 2014;7:958-67).
Significantly, in terms of topical delivery, Chao et al. recently showed that submicron emulsions are effective carriers for the transdermal delivery of kaempferol (Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5).
Conclusion
Kaempferol is one among the many natural flavonols found to exert significant salutary effects. Evidence suggests reasons for confidence that kaempferol can play a role in skin health. More research is necessary to determine the effectiveness of topical products intended to harness the benefits of this flavonoid as proper formulation is challenging.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Kaempferol (3,5,7,4’-tetrahydroxyflavone; C15H10O6) is among the natural flavonols found in green tea, broccoli, cabbage, kale, endive, beans, leeks, tomatoes, grapes, apples, grapefruit, berries, and propolis, as well as myriad other plant sources, including Brassica and species (J. Agric. Food Chem. 2006;54:2951-6; Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]).
It is one of the most commonly found dietary flavonoids and is also present in beer, particularly hops (Carcinogenesis 2010;31:1338-43; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]). Significantly, kaempferol is known to exhibit anticancer, anti-inflammatory, antioxidant, cytoprotective, and antiapoptotic activity (Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Exp. Mol. Med. 2008;40:208-19), and is believed to play a role in protecting plants from ultraviolet (UV)-induced damage (J. Agric. Food Chem. 2012;60:6966-76).
Skin protection: antioxidant and anti-inflammatory activity
Among 35 flavonoids tested by Cos et al. in 2001 for lipid peroxidation-inhibiting activity, kaempferol was identified as having the highest antioxidant selectivity index (Planta Med. 2001;67:515-9).
Work by Kim et al. in 2002 revealed that four kaempferol glycosides are key active ingredients in the flowers of Prunus persica, which has long been used in traditional Chinese medicine to treat skin disorders (J. Cosmet. Sci. 2002;53:27-34). Kim and colleagues have also shown in animal studies that the topical application of P. persica may be effective at thwarting UVB-induced skin damage (J. Cosmet. Sci. 2002;53:27-34).
In addition, kaempferol is a key component in Punica granatum, which has been found to act as an effective protector against UVB-induced photodamage and aging in cultured skin fibroblasts (Int. J. Dermatol. 2010;49:276-82).
In various tests on the effects of natural flavonoids on matrix metalloproteinase (MMP)-1 activity and expression, Lim et al. reported in 2007 that kaempferol and quercetin potently inhibited recombinant human MMP-1, and both flavonols along with apigenin and wogonin were found to be strong inhibitors of MMP-1 induction in 12-O-tetradecanoylphorbol-13-acetate–treated human dermal fibroblasts. All four flavonoids also suppressed the activation of activator protein (AP)-1. Kaempferol also hindered p38 mitogen-activated protein kinase c-Jun N-terminal kinase (JNK) activation. The investigators concluded that kaempferol is among the flavonoids or plant extracts containing them that may be useful as an agent to protect against photoaging and to treat some cutaneous inflammatory conditions (Planta Med. 2007;73:1267-74).
In 2010, Park et al. demonstrated that kaempferol alleviated burn injuries in mice and that expression of tumor necrosis factor–alpha (TNF-alpha) induced by burn injuries was reduced by kaempferol. They concluded that their findings suggest the possible application of kaempferol to treat thermal burn–induced skin injuries (BMB Rep. 2010;43:46-51).
Anti-inflammatory as well as depigmenting activity was found by Rho et al. in 2011 to be associated with kaempferol and kaempferol rhamnosides isolated from Hibiscus cannabinus (Molecules 2011;16:3338-44).
In 2014, Kim et al. found that extracts of Aceriphyllum rossii (native to Korea and China) and its active constituents, quercetin and kaempferol, blocked secretion of beta-hexosaminidase and histamine; lowered the production and mRNA expression of interleukin-4 and TNF-alpha; and reduced prostaglandin E2 and leukotriene B4 synthesis as well as the expression of cyclooxygenase-2 (COX-2) and 5-lipoxygenase. These and other findings led the investigators to conclude that A. rossii and its active ingredients kaempferol and quercetin may be effective agents for the treatment of immediate-type hypersensitivity (J. Agric. Food Chem. 2014;62:3750-8).
Anticancer activity
Lee et al. reported in 2010 that the inhibition by kaempferol of phosphatidylinositol 3-kinase (PI3K) activity, a key factor in carcinogenesis, and its concomitant effects may account for the chemopreventive activity of the flavonol (Carcinogenesis 2010;31:1338-43).
At the end of that year, Lee et al. found that kaempferol inhibited UVB-induced COX-2 protein expression in mouse skin epidermal JB6 P+ cells, by blocking Src kinase activity and attenuated the UVB-induced transcriptional activities of COX-2 gene and the transcription factor AP-1. They concluded that kaempferol exerts robust chemopreventive activity against skin cancer by suppressing Src (Biochem. Pharmacol. 2010;80:2042-9).
In 2014, Yao et al. found that kaempferol acted as a safe and potent inhibitor of solar ultraviolet-induced mouse skin carcinogenesis that acted by targeting RSK2 and MSK1 (Cancer Prev. Res. (Phila) 2014;7:958-67).
Significantly, in terms of topical delivery, Chao et al. recently showed that submicron emulsions are effective carriers for the transdermal delivery of kaempferol (Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5).
Conclusion
Kaempferol is one among the many natural flavonols found to exert significant salutary effects. Evidence suggests reasons for confidence that kaempferol can play a role in skin health. More research is necessary to determine the effectiveness of topical products intended to harness the benefits of this flavonoid as proper formulation is challenging.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Kaempferol (3,5,7,4’-tetrahydroxyflavone; C15H10O6) is among the natural flavonols found in green tea, broccoli, cabbage, kale, endive, beans, leeks, tomatoes, grapes, apples, grapefruit, berries, and propolis, as well as myriad other plant sources, including Brassica and species (J. Agric. Food Chem. 2006;54:2951-6; Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]).
It is one of the most commonly found dietary flavonoids and is also present in beer, particularly hops (Carcinogenesis 2010;31:1338-43; J. Eur. Acad. Dermatol. Venereol. 2013 June 27 [doi:10.1111/jdv.12204]). Significantly, kaempferol is known to exhibit anticancer, anti-inflammatory, antioxidant, cytoprotective, and antiapoptotic activity (Cancer Prev. Res. (Phila) 2014;7:958-67; Biochem. Pharmacol. 2010;80:2042-9; Exp. Mol. Med. 2008;40:208-19), and is believed to play a role in protecting plants from ultraviolet (UV)-induced damage (J. Agric. Food Chem. 2012;60:6966-76).
Skin protection: antioxidant and anti-inflammatory activity
Among 35 flavonoids tested by Cos et al. in 2001 for lipid peroxidation-inhibiting activity, kaempferol was identified as having the highest antioxidant selectivity index (Planta Med. 2001;67:515-9).
Work by Kim et al. in 2002 revealed that four kaempferol glycosides are key active ingredients in the flowers of Prunus persica, which has long been used in traditional Chinese medicine to treat skin disorders (J. Cosmet. Sci. 2002;53:27-34). Kim and colleagues have also shown in animal studies that the topical application of P. persica may be effective at thwarting UVB-induced skin damage (J. Cosmet. Sci. 2002;53:27-34).
In addition, kaempferol is a key component in Punica granatum, which has been found to act as an effective protector against UVB-induced photodamage and aging in cultured skin fibroblasts (Int. J. Dermatol. 2010;49:276-82).
In various tests on the effects of natural flavonoids on matrix metalloproteinase (MMP)-1 activity and expression, Lim et al. reported in 2007 that kaempferol and quercetin potently inhibited recombinant human MMP-1, and both flavonols along with apigenin and wogonin were found to be strong inhibitors of MMP-1 induction in 12-O-tetradecanoylphorbol-13-acetate–treated human dermal fibroblasts. All four flavonoids also suppressed the activation of activator protein (AP)-1. Kaempferol also hindered p38 mitogen-activated protein kinase c-Jun N-terminal kinase (JNK) activation. The investigators concluded that kaempferol is among the flavonoids or plant extracts containing them that may be useful as an agent to protect against photoaging and to treat some cutaneous inflammatory conditions (Planta Med. 2007;73:1267-74).
In 2010, Park et al. demonstrated that kaempferol alleviated burn injuries in mice and that expression of tumor necrosis factor–alpha (TNF-alpha) induced by burn injuries was reduced by kaempferol. They concluded that their findings suggest the possible application of kaempferol to treat thermal burn–induced skin injuries (BMB Rep. 2010;43:46-51).
Anti-inflammatory as well as depigmenting activity was found by Rho et al. in 2011 to be associated with kaempferol and kaempferol rhamnosides isolated from Hibiscus cannabinus (Molecules 2011;16:3338-44).
In 2014, Kim et al. found that extracts of Aceriphyllum rossii (native to Korea and China) and its active constituents, quercetin and kaempferol, blocked secretion of beta-hexosaminidase and histamine; lowered the production and mRNA expression of interleukin-4 and TNF-alpha; and reduced prostaglandin E2 and leukotriene B4 synthesis as well as the expression of cyclooxygenase-2 (COX-2) and 5-lipoxygenase. These and other findings led the investigators to conclude that A. rossii and its active ingredients kaempferol and quercetin may be effective agents for the treatment of immediate-type hypersensitivity (J. Agric. Food Chem. 2014;62:3750-8).
Anticancer activity
Lee et al. reported in 2010 that the inhibition by kaempferol of phosphatidylinositol 3-kinase (PI3K) activity, a key factor in carcinogenesis, and its concomitant effects may account for the chemopreventive activity of the flavonol (Carcinogenesis 2010;31:1338-43).
At the end of that year, Lee et al. found that kaempferol inhibited UVB-induced COX-2 protein expression in mouse skin epidermal JB6 P+ cells, by blocking Src kinase activity and attenuated the UVB-induced transcriptional activities of COX-2 gene and the transcription factor AP-1. They concluded that kaempferol exerts robust chemopreventive activity against skin cancer by suppressing Src (Biochem. Pharmacol. 2010;80:2042-9).
In 2014, Yao et al. found that kaempferol acted as a safe and potent inhibitor of solar ultraviolet-induced mouse skin carcinogenesis that acted by targeting RSK2 and MSK1 (Cancer Prev. Res. (Phila) 2014;7:958-67).
Significantly, in terms of topical delivery, Chao et al. recently showed that submicron emulsions are effective carriers for the transdermal delivery of kaempferol (Chem. Pharm. Bull. (Tokyo) 2012;60:1171-5).
Conclusion
Kaempferol is one among the many natural flavonols found to exert significant salutary effects. Evidence suggests reasons for confidence that kaempferol can play a role in skin health. More research is necessary to determine the effectiveness of topical products intended to harness the benefits of this flavonoid as proper formulation is challenging.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook, “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Mango
Mangifera indica (mango) is a member of the Anacardiaceae family with a tradition of use as a medicinal plant. Mango extracts have been characterized as exhibiting antioxidant, anti-inflammatory, analgesic, and immunomodulatory activities (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9; Drug Chem. Toxicol. 2009;32:53-8). Mango is grown in more than 100 countries, primarily in Asia, in tropical as well as subtropical regions (Molecules 2014;19:17107-29). Mango stem bark and leaves have been used in traditional medicine to treat anemia, cutaneous infections, diabetes, diarrhea, scabies, syphilis, and malignant tumors (Pharmacol. Res. 2007;55:351-8). Polyphenols and carotenoids are among the phytonutrients identified as responsible for the biologic activity of mango (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Various biologic activities and traditional uses
Ojewole investigated the anti-inflammatory, analgesic, and antidiabetic activity of M. indica stem bark aqueous extract in rats and mice in 2005. In mice, mango extract dose-dependently delivered significant analgesic effects against thermally and chemically-generated pain. The investigators attributed the observed salutary effects of the plant to its constituent polyphenolics, flavonoids, triterpenoids, and mangiferin. They also noted that their findings support the folkloric uses of the plant for treating arthritic and other inflammatory conditions, as well as type 2 diabetes (Methods Find. Exp. Clin. Pharmacol. 2005;27:547-54).
Another important constituent of mango (also found in olive, strawberry, fig, and various medicinal herbs) is the triterpene lupeol, which has been characterized as exhibiting potent antioxidant, antimutagenic, anti-inflammatory, and antiarthritic activity (Oncogene 2004;23:5203-14). A 2014 study by Sahu et al. also showed that M. indica leaves display some antityrosinase activity, though not as strongly as other medicinal plants, such as Emblica officinalis (Pak. J. Biol. Sci. 2014;17:146-50).
Anticancer, antioxidant, and antiphotoaging activity
In 2004, Saleem et al. demonstrated that topically applied lupeol exhibited anti–tumor-promoting effects in a CD-1 mouse skin tumorigenesis model. Pretreatment with the mango constituent time- and dose-dependently inhibited multiple 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-mediated increases in edema, hyperplasia, epidermal ornithine decarboxylase (ODC) activity, as well as protein expression of ODC, cyclooxygenase 2 (COX-2) and nitric oxide synthase. Pretreated animals also experienced significantly lower tumor incidence and tumor body burden as well as a significant delay in tumor latency period. The researchers concluded that lupeol exerts anti–skin tumor promoting effects on CD-1 mice (Oncogene 2004;23:5203-14).
Three years later, Núñez-Sellés et al. reported that a mango stem bark extract (Vimang) developed in Cuba exhibited antioxidant, analgesic, anti-inflammatory, and immunomodulating activity in basic, preclinical, and clinical studies (Pharmacol. Res. 2007;55:351-8).
A 2009 toxicological analysis of Vimang, which has been formulated into tablets, creams, capsules, syrup, vaginal oval, and suppositories for various applications, revealed via irritant tests conducted on rabbits that the topical formulation was not irritating to the skin, generally, with minimal irritancy noted after vaginal application. No adverse effects were reported (Drug Chem. Toxicol. 2009;32:53-8).
In 2012, Li et al. discovered norathyriol (1,3,6,7-tetrahydroxy-9H-xanthen-9-one), a plant-derived chemopreventive metabolite of mangiferin, found in mango, Hypericum elegans, and Tripterospermum lanceolatum. They found that norathyriol significantly inhibited solar UV-induced skin carcinogenesis in mouse models. In vitro investigations revealed that the compound suppressed cell growth in mouse skin epidermal JB6 P+ cells at the level of G2-M phase arrest. The investigators concluded that this newly identified substance appears to act as a safe chemopreventive agent against UV-induced skin cancer (Cancer Res. 2012;72:260-70).
A year later, Song et al. assessed the protective effects of orally administered mango extract against UVB-induced cutaneous aging in HR-1 hairless male mice. The animals were divided into control, UVB-treated vehicle, and UVB-treated mango extract groups. The researchers found that mango extract significantly suppressed the increase in epidermal thickness and hypertrophy indicative of UVB treatment, with mean length of wrinkles significantly lower in the mango group compared with the UVB-treated vehicle group. Treatment with mango extract also led to a significant increase in collagen bundles in animals treated with UVB. The authors concluded that mango extract displayed antiphotoaging properties in hairless mice exposed to UVB (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Further, a 2014 in vitro study revealed that extracts of Helicanthus elastica growing on M. indica exhibited antioxidant activity. H. elastica is a hemiparasite that often grows on mango trees in India and is known to be a rich source of phenolic substances (J. Tradit. Complement. Med. 2014;4:285-8).
Topical delivery
Mandawgade and Patravale developed a mango butter skin care formulation in 2008 that was used to test skin repair in rat excision and incision wound models. A healing response was noted in both animal models. The formulation also was found to be effective in achieving complete repair of worn and cracked skin on the feet of all human volunteers in the study. The investigators concluded that the mango butter preparation delivers superlative emolliency and warrants consideration as an excipient agent in cosmeceutical products (Indian J. Pharm. Sci. 2008;70:539-42).
It is worth noting that cases of “mango dermatitis” (allergic contact dermatitis to the sap or skin of M. indica), manifesting in urticaria and eczematous rashes, have been reported (Australas. J. Dermatol. 1996;37:59-60; Int. J. Dermatol. 2004;43:195-6).
In 2014, Leanpolchareanchai et al. developed a microemulsion system containing Thai mango seed kernel extract that displayed strong skin enhancement results in ex vivo skin permeation studies (penetrating skin layers up to 60-fold higher than controls) and physicochemical stability over 6 months (Drug Chem. Toxicol. 2009;32:53-8). Thai mango seed kernel extract had previously been shown to exhibit anti–methicillin-resistant Staphylococcus aureus and antityrosinase characteristics, as well as strong free radical scavenging, antioxidant, anti-inflammatory, and hepatoprotective activities.(Molecules 2014;19:17107-29).
Conclusion
Evidence on the cutaneous applications of mango is emerging, but does not have a significant track record. That said, this fruit has long been used in traditional medicine for a range of indications, including skin disorders. Much more research is necessary, however, to ascertain how beneficial this fruit and its extracts may be. At the very least, there are few reports of adverse events associated with topical application.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Mangifera indica (mango) is a member of the Anacardiaceae family with a tradition of use as a medicinal plant. Mango extracts have been characterized as exhibiting antioxidant, anti-inflammatory, analgesic, and immunomodulatory activities (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9; Drug Chem. Toxicol. 2009;32:53-8). Mango is grown in more than 100 countries, primarily in Asia, in tropical as well as subtropical regions (Molecules 2014;19:17107-29). Mango stem bark and leaves have been used in traditional medicine to treat anemia, cutaneous infections, diabetes, diarrhea, scabies, syphilis, and malignant tumors (Pharmacol. Res. 2007;55:351-8). Polyphenols and carotenoids are among the phytonutrients identified as responsible for the biologic activity of mango (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Various biologic activities and traditional uses
Ojewole investigated the anti-inflammatory, analgesic, and antidiabetic activity of M. indica stem bark aqueous extract in rats and mice in 2005. In mice, mango extract dose-dependently delivered significant analgesic effects against thermally and chemically-generated pain. The investigators attributed the observed salutary effects of the plant to its constituent polyphenolics, flavonoids, triterpenoids, and mangiferin. They also noted that their findings support the folkloric uses of the plant for treating arthritic and other inflammatory conditions, as well as type 2 diabetes (Methods Find. Exp. Clin. Pharmacol. 2005;27:547-54).
Another important constituent of mango (also found in olive, strawberry, fig, and various medicinal herbs) is the triterpene lupeol, which has been characterized as exhibiting potent antioxidant, antimutagenic, anti-inflammatory, and antiarthritic activity (Oncogene 2004;23:5203-14). A 2014 study by Sahu et al. also showed that M. indica leaves display some antityrosinase activity, though not as strongly as other medicinal plants, such as Emblica officinalis (Pak. J. Biol. Sci. 2014;17:146-50).
Anticancer, antioxidant, and antiphotoaging activity
In 2004, Saleem et al. demonstrated that topically applied lupeol exhibited anti–tumor-promoting effects in a CD-1 mouse skin tumorigenesis model. Pretreatment with the mango constituent time- and dose-dependently inhibited multiple 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-mediated increases in edema, hyperplasia, epidermal ornithine decarboxylase (ODC) activity, as well as protein expression of ODC, cyclooxygenase 2 (COX-2) and nitric oxide synthase. Pretreated animals also experienced significantly lower tumor incidence and tumor body burden as well as a significant delay in tumor latency period. The researchers concluded that lupeol exerts anti–skin tumor promoting effects on CD-1 mice (Oncogene 2004;23:5203-14).
Three years later, Núñez-Sellés et al. reported that a mango stem bark extract (Vimang) developed in Cuba exhibited antioxidant, analgesic, anti-inflammatory, and immunomodulating activity in basic, preclinical, and clinical studies (Pharmacol. Res. 2007;55:351-8).
A 2009 toxicological analysis of Vimang, which has been formulated into tablets, creams, capsules, syrup, vaginal oval, and suppositories for various applications, revealed via irritant tests conducted on rabbits that the topical formulation was not irritating to the skin, generally, with minimal irritancy noted after vaginal application. No adverse effects were reported (Drug Chem. Toxicol. 2009;32:53-8).
In 2012, Li et al. discovered norathyriol (1,3,6,7-tetrahydroxy-9H-xanthen-9-one), a plant-derived chemopreventive metabolite of mangiferin, found in mango, Hypericum elegans, and Tripterospermum lanceolatum. They found that norathyriol significantly inhibited solar UV-induced skin carcinogenesis in mouse models. In vitro investigations revealed that the compound suppressed cell growth in mouse skin epidermal JB6 P+ cells at the level of G2-M phase arrest. The investigators concluded that this newly identified substance appears to act as a safe chemopreventive agent against UV-induced skin cancer (Cancer Res. 2012;72:260-70).
A year later, Song et al. assessed the protective effects of orally administered mango extract against UVB-induced cutaneous aging in HR-1 hairless male mice. The animals were divided into control, UVB-treated vehicle, and UVB-treated mango extract groups. The researchers found that mango extract significantly suppressed the increase in epidermal thickness and hypertrophy indicative of UVB treatment, with mean length of wrinkles significantly lower in the mango group compared with the UVB-treated vehicle group. Treatment with mango extract also led to a significant increase in collagen bundles in animals treated with UVB. The authors concluded that mango extract displayed antiphotoaging properties in hairless mice exposed to UVB (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Further, a 2014 in vitro study revealed that extracts of Helicanthus elastica growing on M. indica exhibited antioxidant activity. H. elastica is a hemiparasite that often grows on mango trees in India and is known to be a rich source of phenolic substances (J. Tradit. Complement. Med. 2014;4:285-8).
Topical delivery
Mandawgade and Patravale developed a mango butter skin care formulation in 2008 that was used to test skin repair in rat excision and incision wound models. A healing response was noted in both animal models. The formulation also was found to be effective in achieving complete repair of worn and cracked skin on the feet of all human volunteers in the study. The investigators concluded that the mango butter preparation delivers superlative emolliency and warrants consideration as an excipient agent in cosmeceutical products (Indian J. Pharm. Sci. 2008;70:539-42).
It is worth noting that cases of “mango dermatitis” (allergic contact dermatitis to the sap or skin of M. indica), manifesting in urticaria and eczematous rashes, have been reported (Australas. J. Dermatol. 1996;37:59-60; Int. J. Dermatol. 2004;43:195-6).
In 2014, Leanpolchareanchai et al. developed a microemulsion system containing Thai mango seed kernel extract that displayed strong skin enhancement results in ex vivo skin permeation studies (penetrating skin layers up to 60-fold higher than controls) and physicochemical stability over 6 months (Drug Chem. Toxicol. 2009;32:53-8). Thai mango seed kernel extract had previously been shown to exhibit anti–methicillin-resistant Staphylococcus aureus and antityrosinase characteristics, as well as strong free radical scavenging, antioxidant, anti-inflammatory, and hepatoprotective activities.(Molecules 2014;19:17107-29).
Conclusion
Evidence on the cutaneous applications of mango is emerging, but does not have a significant track record. That said, this fruit has long been used in traditional medicine for a range of indications, including skin disorders. Much more research is necessary, however, to ascertain how beneficial this fruit and its extracts may be. At the very least, there are few reports of adverse events associated with topical application.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Mangifera indica (mango) is a member of the Anacardiaceae family with a tradition of use as a medicinal plant. Mango extracts have been characterized as exhibiting antioxidant, anti-inflammatory, analgesic, and immunomodulatory activities (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9; Drug Chem. Toxicol. 2009;32:53-8). Mango is grown in more than 100 countries, primarily in Asia, in tropical as well as subtropical regions (Molecules 2014;19:17107-29). Mango stem bark and leaves have been used in traditional medicine to treat anemia, cutaneous infections, diabetes, diarrhea, scabies, syphilis, and malignant tumors (Pharmacol. Res. 2007;55:351-8). Polyphenols and carotenoids are among the phytonutrients identified as responsible for the biologic activity of mango (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Various biologic activities and traditional uses
Ojewole investigated the anti-inflammatory, analgesic, and antidiabetic activity of M. indica stem bark aqueous extract in rats and mice in 2005. In mice, mango extract dose-dependently delivered significant analgesic effects against thermally and chemically-generated pain. The investigators attributed the observed salutary effects of the plant to its constituent polyphenolics, flavonoids, triterpenoids, and mangiferin. They also noted that their findings support the folkloric uses of the plant for treating arthritic and other inflammatory conditions, as well as type 2 diabetes (Methods Find. Exp. Clin. Pharmacol. 2005;27:547-54).
Another important constituent of mango (also found in olive, strawberry, fig, and various medicinal herbs) is the triterpene lupeol, which has been characterized as exhibiting potent antioxidant, antimutagenic, anti-inflammatory, and antiarthritic activity (Oncogene 2004;23:5203-14). A 2014 study by Sahu et al. also showed that M. indica leaves display some antityrosinase activity, though not as strongly as other medicinal plants, such as Emblica officinalis (Pak. J. Biol. Sci. 2014;17:146-50).
Anticancer, antioxidant, and antiphotoaging activity
In 2004, Saleem et al. demonstrated that topically applied lupeol exhibited anti–tumor-promoting effects in a CD-1 mouse skin tumorigenesis model. Pretreatment with the mango constituent time- and dose-dependently inhibited multiple 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-mediated increases in edema, hyperplasia, epidermal ornithine decarboxylase (ODC) activity, as well as protein expression of ODC, cyclooxygenase 2 (COX-2) and nitric oxide synthase. Pretreated animals also experienced significantly lower tumor incidence and tumor body burden as well as a significant delay in tumor latency period. The researchers concluded that lupeol exerts anti–skin tumor promoting effects on CD-1 mice (Oncogene 2004;23:5203-14).
Three years later, Núñez-Sellés et al. reported that a mango stem bark extract (Vimang) developed in Cuba exhibited antioxidant, analgesic, anti-inflammatory, and immunomodulating activity in basic, preclinical, and clinical studies (Pharmacol. Res. 2007;55:351-8).
A 2009 toxicological analysis of Vimang, which has been formulated into tablets, creams, capsules, syrup, vaginal oval, and suppositories for various applications, revealed via irritant tests conducted on rabbits that the topical formulation was not irritating to the skin, generally, with minimal irritancy noted after vaginal application. No adverse effects were reported (Drug Chem. Toxicol. 2009;32:53-8).
In 2012, Li et al. discovered norathyriol (1,3,6,7-tetrahydroxy-9H-xanthen-9-one), a plant-derived chemopreventive metabolite of mangiferin, found in mango, Hypericum elegans, and Tripterospermum lanceolatum. They found that norathyriol significantly inhibited solar UV-induced skin carcinogenesis in mouse models. In vitro investigations revealed that the compound suppressed cell growth in mouse skin epidermal JB6 P+ cells at the level of G2-M phase arrest. The investigators concluded that this newly identified substance appears to act as a safe chemopreventive agent against UV-induced skin cancer (Cancer Res. 2012;72:260-70).
A year later, Song et al. assessed the protective effects of orally administered mango extract against UVB-induced cutaneous aging in HR-1 hairless male mice. The animals were divided into control, UVB-treated vehicle, and UVB-treated mango extract groups. The researchers found that mango extract significantly suppressed the increase in epidermal thickness and hypertrophy indicative of UVB treatment, with mean length of wrinkles significantly lower in the mango group compared with the UVB-treated vehicle group. Treatment with mango extract also led to a significant increase in collagen bundles in animals treated with UVB. The authors concluded that mango extract displayed antiphotoaging properties in hairless mice exposed to UVB (Photodermatol. Photoimmunol. Photomed. 2013;29:84-9).
Further, a 2014 in vitro study revealed that extracts of Helicanthus elastica growing on M. indica exhibited antioxidant activity. H. elastica is a hemiparasite that often grows on mango trees in India and is known to be a rich source of phenolic substances (J. Tradit. Complement. Med. 2014;4:285-8).
Topical delivery
Mandawgade and Patravale developed a mango butter skin care formulation in 2008 that was used to test skin repair in rat excision and incision wound models. A healing response was noted in both animal models. The formulation also was found to be effective in achieving complete repair of worn and cracked skin on the feet of all human volunteers in the study. The investigators concluded that the mango butter preparation delivers superlative emolliency and warrants consideration as an excipient agent in cosmeceutical products (Indian J. Pharm. Sci. 2008;70:539-42).
It is worth noting that cases of “mango dermatitis” (allergic contact dermatitis to the sap or skin of M. indica), manifesting in urticaria and eczematous rashes, have been reported (Australas. J. Dermatol. 1996;37:59-60; Int. J. Dermatol. 2004;43:195-6).
In 2014, Leanpolchareanchai et al. developed a microemulsion system containing Thai mango seed kernel extract that displayed strong skin enhancement results in ex vivo skin permeation studies (penetrating skin layers up to 60-fold higher than controls) and physicochemical stability over 6 months (Drug Chem. Toxicol. 2009;32:53-8). Thai mango seed kernel extract had previously been shown to exhibit anti–methicillin-resistant Staphylococcus aureus and antityrosinase characteristics, as well as strong free radical scavenging, antioxidant, anti-inflammatory, and hepatoprotective activities.(Molecules 2014;19:17107-29).
Conclusion
Evidence on the cutaneous applications of mango is emerging, but does not have a significant track record. That said, this fruit has long been used in traditional medicine for a range of indications, including skin disorders. Much more research is necessary, however, to ascertain how beneficial this fruit and its extracts may be. At the very least, there are few reports of adverse events associated with topical application.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy, Topix Pharmaceuticals, and Unilever.
Alpinia officinarum
Alpinia officinarum (and its close relative Alpinia galanga), a member of the Zingiberaceae family (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5), has long been used in Chinese medicinals (Bioorg. Med. Chem. 2009;17:6048-53). Specifically, the plant is used in traditional Chinese medicine as an aphrodisiac, abortifacient, carminative, antipyretic, anti-inflammatory, and emmenagogue as well as to treat disorders of the heart and kidneys, bronchitis, chronic enteritis, renal calculus, diabetes, and rheumatism (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53). Stomach ailments are the most typical application of the herb in traditional Chinese and Thai medicine; it is also used in Ayurveda and Sidda medicine. A. officinarum is widely cultivated throughout Asia, including China, Thailand, India, Sri Lanka, Malaysia, and Indonesia, as well as the Middle East and Northern Africa (Saudi Arabia and Egypt, respectively) (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5).
The flavonoid galangin (3,5,7-trihydroxyflavone) is the primary active constituent of A. officinarum (Phytother. Res. 2014;28:1533-8; J. Cell Biochem. 2013;114:152-61). In vitro, it has demonstrated a cytotoxic effect on multiple cancer cell lines (J. Cell Biochem. 2013;114[1]:152-61). Traditional Uighur medicine in China has incorporated galangin for the treatment of vitiligo (Phytother. Res. 2014;28:1533-8). Overall, A. officinarum rhizomes have been associated with antiemetic, antigenotoxic, antimutagenic, and antioxidant activity, as well as inhibitory effects on prostaglandin and leukotriene biosynthesis, and modulatory effects on cytochrome P450 enzymes (Bioorg. Med. Chem. 2009;17:6048-53; J. Cell Biochem. 2013;114:152-61). The rhizomes of A. officinarum have been used externally to treat skin infections, gum diseases, and skin cancer (J. Nat. Med. 2008;62:374-8).
Constituents
The rhizomes of the plant, commonly referred to as galangal, contain several key active constituents, including essential oils, tannins, neolignans, phenol, glycosides, monoterpenes, diarylheptanoids, phenylpropanoids, carbohydrates, gallic acid glycoside, galangoisoflavonoid, beta-sitosterol, galangin, alpinin, zerumbone, and kampferide (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53; J. Nat. Med. 2008;62:374-8).
In 2009, Matsuda et al. reported that the 80% aqueous acetone extract of the rhizomes of A. officinarum suppressed melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. They found that several isolated constituents had significant IC50 values (10-48 mcm) for inhibiting melanogenesis, including four diarylheptanoids (5-hydroxy-1,7-diphenyl-3-heptanone, 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, 5-hydroxy-7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenyl-3-heptanone, and 3,5-dihydroxy-1,7-diphenylheptane) and two flavonol constituents (kaempferide and galangin). The mRNA expression of tyrosinase and tyrosinase-related proteins-1 and -2 was also hindered by 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, kaempferide, and galangin, as was the protein level of a microphthalmia-associated transcription factor, the authors noted (Bioorg. Med. Chem. 2009;17:6048-53).
Biologic activity
Penetration enhancement: In 2000, Shen et al. found that volatile oils from galangal, among other herbs, were effective in enhancing the skin permeation of 5-fluorouracil and notably more effective than azone (Zhong Yao Cai 2000;23:697-9).
Anti-inflammatory effects: In 2008, Yasukawa et al. examined the inhibitory effect of galangal in a two-stage in vivo carcinogenesis model in mice. They observed that the A. officinarum rhizomes displayed significant antitumor-promoting activity against 7,12-dimethylbenz[a]anthracene (DMBA)-initiated and 12-O-tetradecanoylphorbol-13-acetate (TPA)–promoted lesions. Seven diarylheptanoids isolated from the active fraction of the methanol extracts demonstrated significant anti-inflammatory effects against TPA-induced inflammation (J. Nat. Med. 2008;62:374-8).
Cancer prevention and pigmentary effects: Heo et al. reported in 2001 that in vitro and in vivo studies have demonstrated that the flavonoid galangin, found in high concentrations in A. officinarum, as well as the bee product propolis, exhibits significant antioxidant activity and can influence enzyme activities and inhibit genotoxicity without introducing a pro-oxidant effect. They concluded that galangin warrants consideration for its potential as a chemical cancer-preventing agent (Mutat. Res. 2001;488:135-50).
In 2007, Lu et al. investigated the whitening effects of the flavonoid components of A. officinarum on melanin biosynthesis in B16 mouse melanoma cells, tyrosinase inhibition, and UV absorption. They found that galangin and the flavonoid mixture both decreased melanin content more than controls and also lowered melanin production, with galangin more effective than the flavonoid mixture. In addition, galangin and the flavonoid mixture exerted greater tyrosinase inhibition at lower concentrations. The A. officinarum constituents also displayed a broad absorption band in the UVB area (270 to 290 nm). The researchers concluded that galangin may be a viable whitening agent with the potential to prevent skin cancer (J. Enzyme Inhib. Med. Chem. 2007;22:433-8).
Six years later, Zhang et al. noted that various doses of galangin resulted in the inhibition of B16F10 melanoma cell proliferation. The investigators also showed that galangin achieved an antimetastatic effect in vivo in C57BL/6J mice, reducing focal adhesion kinase. They concluded that focal adhesion kinase is a viable target in melanoma therapy, with B16F10 melanoma metastasis apparently checked by galangin in mice and in cell cultures (J. Cell Biochem. 2013;114:152-61).
In 2014, Huo et al. tested galangin in a mouse model of vitiligo induced in C57BL/6 mice through the daily topical application of hydroquinone (2.5%) on shaved dorsal skin for 60 days. Thirty days after the final hydroquinone application, investigators began oral administration of galangin for 30 days. Hair grew back after treatment darker than the original color, with histologic analysis revealing that mice treated with galangin and the positive control 8-methoxypsoralen had an increased number of melanin-containing hair follicles, compared with untreated animals. In addition, galangin treatment was associated with significant increases in the number of cutaneous basal layer melanocytes and melanin-containing epidermal cells. Compared with controls, treatment with galangin and 8-methoxypsoralen led to increased serum levels of tyrosinase and decreased levels of malondialdehyde and lower cholinesterase activity. Galangin and 8-methoxypsoralen use also increased the expression of tyrosinase protein in treated skin. The investigators concluded that galangin improved hydroquinone-induced vitiligo in mice and warrants further study as a potential vitiligo treatment in humans (Phytother. Res. 2014 28:1533-8).
Conclusion
Alpinia officinarum is one of many botanical agents with a long history of applications in traditional folk medicine, particularly in Asia. There is a relative paucity of evidence regarding the dermatologic applications of this plant, but recent findings support continued research into its various potential cutaneous benefits, with particular focus on the main active ingredient galangin.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
Alpinia officinarum (and its close relative Alpinia galanga), a member of the Zingiberaceae family (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5), has long been used in Chinese medicinals (Bioorg. Med. Chem. 2009;17:6048-53). Specifically, the plant is used in traditional Chinese medicine as an aphrodisiac, abortifacient, carminative, antipyretic, anti-inflammatory, and emmenagogue as well as to treat disorders of the heart and kidneys, bronchitis, chronic enteritis, renal calculus, diabetes, and rheumatism (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53). Stomach ailments are the most typical application of the herb in traditional Chinese and Thai medicine; it is also used in Ayurveda and Sidda medicine. A. officinarum is widely cultivated throughout Asia, including China, Thailand, India, Sri Lanka, Malaysia, and Indonesia, as well as the Middle East and Northern Africa (Saudi Arabia and Egypt, respectively) (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5).
The flavonoid galangin (3,5,7-trihydroxyflavone) is the primary active constituent of A. officinarum (Phytother. Res. 2014;28:1533-8; J. Cell Biochem. 2013;114:152-61). In vitro, it has demonstrated a cytotoxic effect on multiple cancer cell lines (J. Cell Biochem. 2013;114[1]:152-61). Traditional Uighur medicine in China has incorporated galangin for the treatment of vitiligo (Phytother. Res. 2014;28:1533-8). Overall, A. officinarum rhizomes have been associated with antiemetic, antigenotoxic, antimutagenic, and antioxidant activity, as well as inhibitory effects on prostaglandin and leukotriene biosynthesis, and modulatory effects on cytochrome P450 enzymes (Bioorg. Med. Chem. 2009;17:6048-53; J. Cell Biochem. 2013;114:152-61). The rhizomes of A. officinarum have been used externally to treat skin infections, gum diseases, and skin cancer (J. Nat. Med. 2008;62:374-8).
Constituents
The rhizomes of the plant, commonly referred to as galangal, contain several key active constituents, including essential oils, tannins, neolignans, phenol, glycosides, monoterpenes, diarylheptanoids, phenylpropanoids, carbohydrates, gallic acid glycoside, galangoisoflavonoid, beta-sitosterol, galangin, alpinin, zerumbone, and kampferide (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53; J. Nat. Med. 2008;62:374-8).
In 2009, Matsuda et al. reported that the 80% aqueous acetone extract of the rhizomes of A. officinarum suppressed melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. They found that several isolated constituents had significant IC50 values (10-48 mcm) for inhibiting melanogenesis, including four diarylheptanoids (5-hydroxy-1,7-diphenyl-3-heptanone, 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, 5-hydroxy-7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenyl-3-heptanone, and 3,5-dihydroxy-1,7-diphenylheptane) and two flavonol constituents (kaempferide and galangin). The mRNA expression of tyrosinase and tyrosinase-related proteins-1 and -2 was also hindered by 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, kaempferide, and galangin, as was the protein level of a microphthalmia-associated transcription factor, the authors noted (Bioorg. Med. Chem. 2009;17:6048-53).
Biologic activity
Penetration enhancement: In 2000, Shen et al. found that volatile oils from galangal, among other herbs, were effective in enhancing the skin permeation of 5-fluorouracil and notably more effective than azone (Zhong Yao Cai 2000;23:697-9).
Anti-inflammatory effects: In 2008, Yasukawa et al. examined the inhibitory effect of galangal in a two-stage in vivo carcinogenesis model in mice. They observed that the A. officinarum rhizomes displayed significant antitumor-promoting activity against 7,12-dimethylbenz[a]anthracene (DMBA)-initiated and 12-O-tetradecanoylphorbol-13-acetate (TPA)–promoted lesions. Seven diarylheptanoids isolated from the active fraction of the methanol extracts demonstrated significant anti-inflammatory effects against TPA-induced inflammation (J. Nat. Med. 2008;62:374-8).
Cancer prevention and pigmentary effects: Heo et al. reported in 2001 that in vitro and in vivo studies have demonstrated that the flavonoid galangin, found in high concentrations in A. officinarum, as well as the bee product propolis, exhibits significant antioxidant activity and can influence enzyme activities and inhibit genotoxicity without introducing a pro-oxidant effect. They concluded that galangin warrants consideration for its potential as a chemical cancer-preventing agent (Mutat. Res. 2001;488:135-50).
In 2007, Lu et al. investigated the whitening effects of the flavonoid components of A. officinarum on melanin biosynthesis in B16 mouse melanoma cells, tyrosinase inhibition, and UV absorption. They found that galangin and the flavonoid mixture both decreased melanin content more than controls and also lowered melanin production, with galangin more effective than the flavonoid mixture. In addition, galangin and the flavonoid mixture exerted greater tyrosinase inhibition at lower concentrations. The A. officinarum constituents also displayed a broad absorption band in the UVB area (270 to 290 nm). The researchers concluded that galangin may be a viable whitening agent with the potential to prevent skin cancer (J. Enzyme Inhib. Med. Chem. 2007;22:433-8).
Six years later, Zhang et al. noted that various doses of galangin resulted in the inhibition of B16F10 melanoma cell proliferation. The investigators also showed that galangin achieved an antimetastatic effect in vivo in C57BL/6J mice, reducing focal adhesion kinase. They concluded that focal adhesion kinase is a viable target in melanoma therapy, with B16F10 melanoma metastasis apparently checked by galangin in mice and in cell cultures (J. Cell Biochem. 2013;114:152-61).
In 2014, Huo et al. tested galangin in a mouse model of vitiligo induced in C57BL/6 mice through the daily topical application of hydroquinone (2.5%) on shaved dorsal skin for 60 days. Thirty days after the final hydroquinone application, investigators began oral administration of galangin for 30 days. Hair grew back after treatment darker than the original color, with histologic analysis revealing that mice treated with galangin and the positive control 8-methoxypsoralen had an increased number of melanin-containing hair follicles, compared with untreated animals. In addition, galangin treatment was associated with significant increases in the number of cutaneous basal layer melanocytes and melanin-containing epidermal cells. Compared with controls, treatment with galangin and 8-methoxypsoralen led to increased serum levels of tyrosinase and decreased levels of malondialdehyde and lower cholinesterase activity. Galangin and 8-methoxypsoralen use also increased the expression of tyrosinase protein in treated skin. The investigators concluded that galangin improved hydroquinone-induced vitiligo in mice and warrants further study as a potential vitiligo treatment in humans (Phytother. Res. 2014 28:1533-8).
Conclusion
Alpinia officinarum is one of many botanical agents with a long history of applications in traditional folk medicine, particularly in Asia. There is a relative paucity of evidence regarding the dermatologic applications of this plant, but recent findings support continued research into its various potential cutaneous benefits, with particular focus on the main active ingredient galangin.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
Alpinia officinarum (and its close relative Alpinia galanga), a member of the Zingiberaceae family (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5), has long been used in Chinese medicinals (Bioorg. Med. Chem. 2009;17:6048-53). Specifically, the plant is used in traditional Chinese medicine as an aphrodisiac, abortifacient, carminative, antipyretic, anti-inflammatory, and emmenagogue as well as to treat disorders of the heart and kidneys, bronchitis, chronic enteritis, renal calculus, diabetes, and rheumatism (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53). Stomach ailments are the most typical application of the herb in traditional Chinese and Thai medicine; it is also used in Ayurveda and Sidda medicine. A. officinarum is widely cultivated throughout Asia, including China, Thailand, India, Sri Lanka, Malaysia, and Indonesia, as well as the Middle East and Northern Africa (Saudi Arabia and Egypt, respectively) (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5).
The flavonoid galangin (3,5,7-trihydroxyflavone) is the primary active constituent of A. officinarum (Phytother. Res. 2014;28:1533-8; J. Cell Biochem. 2013;114:152-61). In vitro, it has demonstrated a cytotoxic effect on multiple cancer cell lines (J. Cell Biochem. 2013;114[1]:152-61). Traditional Uighur medicine in China has incorporated galangin for the treatment of vitiligo (Phytother. Res. 2014;28:1533-8). Overall, A. officinarum rhizomes have been associated with antiemetic, antigenotoxic, antimutagenic, and antioxidant activity, as well as inhibitory effects on prostaglandin and leukotriene biosynthesis, and modulatory effects on cytochrome P450 enzymes (Bioorg. Med. Chem. 2009;17:6048-53; J. Cell Biochem. 2013;114:152-61). The rhizomes of A. officinarum have been used externally to treat skin infections, gum diseases, and skin cancer (J. Nat. Med. 2008;62:374-8).
Constituents
The rhizomes of the plant, commonly referred to as galangal, contain several key active constituents, including essential oils, tannins, neolignans, phenol, glycosides, monoterpenes, diarylheptanoids, phenylpropanoids, carbohydrates, gallic acid glycoside, galangoisoflavonoid, beta-sitosterol, galangin, alpinin, zerumbone, and kampferide (Zhong Xi Yi Jie He Xue Bao 2011;9:1061-5; Bioorg. Med. Chem. 2009;17:6048-53; J. Nat. Med. 2008;62:374-8).
In 2009, Matsuda et al. reported that the 80% aqueous acetone extract of the rhizomes of A. officinarum suppressed melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. They found that several isolated constituents had significant IC50 values (10-48 mcm) for inhibiting melanogenesis, including four diarylheptanoids (5-hydroxy-1,7-diphenyl-3-heptanone, 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, 5-hydroxy-7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenyl-3-heptanone, and 3,5-dihydroxy-1,7-diphenylheptane) and two flavonol constituents (kaempferide and galangin). The mRNA expression of tyrosinase and tyrosinase-related proteins-1 and -2 was also hindered by 7-(4(‘’)-hydroxy-3(‘’)-methoxyphenyl)-1-phenylhept-4-en-3-one, kaempferide, and galangin, as was the protein level of a microphthalmia-associated transcription factor, the authors noted (Bioorg. Med. Chem. 2009;17:6048-53).
Biologic activity
Penetration enhancement: In 2000, Shen et al. found that volatile oils from galangal, among other herbs, were effective in enhancing the skin permeation of 5-fluorouracil and notably more effective than azone (Zhong Yao Cai 2000;23:697-9).
Anti-inflammatory effects: In 2008, Yasukawa et al. examined the inhibitory effect of galangal in a two-stage in vivo carcinogenesis model in mice. They observed that the A. officinarum rhizomes displayed significant antitumor-promoting activity against 7,12-dimethylbenz[a]anthracene (DMBA)-initiated and 12-O-tetradecanoylphorbol-13-acetate (TPA)–promoted lesions. Seven diarylheptanoids isolated from the active fraction of the methanol extracts demonstrated significant anti-inflammatory effects against TPA-induced inflammation (J. Nat. Med. 2008;62:374-8).
Cancer prevention and pigmentary effects: Heo et al. reported in 2001 that in vitro and in vivo studies have demonstrated that the flavonoid galangin, found in high concentrations in A. officinarum, as well as the bee product propolis, exhibits significant antioxidant activity and can influence enzyme activities and inhibit genotoxicity without introducing a pro-oxidant effect. They concluded that galangin warrants consideration for its potential as a chemical cancer-preventing agent (Mutat. Res. 2001;488:135-50).
In 2007, Lu et al. investigated the whitening effects of the flavonoid components of A. officinarum on melanin biosynthesis in B16 mouse melanoma cells, tyrosinase inhibition, and UV absorption. They found that galangin and the flavonoid mixture both decreased melanin content more than controls and also lowered melanin production, with galangin more effective than the flavonoid mixture. In addition, galangin and the flavonoid mixture exerted greater tyrosinase inhibition at lower concentrations. The A. officinarum constituents also displayed a broad absorption band in the UVB area (270 to 290 nm). The researchers concluded that galangin may be a viable whitening agent with the potential to prevent skin cancer (J. Enzyme Inhib. Med. Chem. 2007;22:433-8).
Six years later, Zhang et al. noted that various doses of galangin resulted in the inhibition of B16F10 melanoma cell proliferation. The investigators also showed that galangin achieved an antimetastatic effect in vivo in C57BL/6J mice, reducing focal adhesion kinase. They concluded that focal adhesion kinase is a viable target in melanoma therapy, with B16F10 melanoma metastasis apparently checked by galangin in mice and in cell cultures (J. Cell Biochem. 2013;114:152-61).
In 2014, Huo et al. tested galangin in a mouse model of vitiligo induced in C57BL/6 mice through the daily topical application of hydroquinone (2.5%) on shaved dorsal skin for 60 days. Thirty days after the final hydroquinone application, investigators began oral administration of galangin for 30 days. Hair grew back after treatment darker than the original color, with histologic analysis revealing that mice treated with galangin and the positive control 8-methoxypsoralen had an increased number of melanin-containing hair follicles, compared with untreated animals. In addition, galangin treatment was associated with significant increases in the number of cutaneous basal layer melanocytes and melanin-containing epidermal cells. Compared with controls, treatment with galangin and 8-methoxypsoralen led to increased serum levels of tyrosinase and decreased levels of malondialdehyde and lower cholinesterase activity. Galangin and 8-methoxypsoralen use also increased the expression of tyrosinase protein in treated skin. The investigators concluded that galangin improved hydroquinone-induced vitiligo in mice and warrants further study as a potential vitiligo treatment in humans (Phytother. Res. 2014 28:1533-8).
Conclusion
Alpinia officinarum is one of many botanical agents with a long history of applications in traditional folk medicine, particularly in Asia. There is a relative paucity of evidence regarding the dermatologic applications of this plant, but recent findings support continued research into its various potential cutaneous benefits, with particular focus on the main active ingredient galangin.
Dr. Baumann is chief executive officer of the Baumann Cosmetic & Research Institute in the Design District in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann wrote the textbook “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002), and a book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). She has contributed to the Cosmeceutical Critique column in Dermatology News since January 2001. Her latest book, “Cosmeceuticals and Cosmetic Ingredients,” was published in November 2014. Dr. Baumann has received funding for clinical grants from Allergan, Aveeno, Avon Products, Evolus, Galderma, GlaxoSmithKline, Kythera, Mary Kay, Medicis Pharmaceuticals, Neutrogena, Philosophy,Topix Pharmaceuticals, and Unilever.
