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The protective effects of the antioxidative compound sesamol against radiation were reported as early as 1991.1 The water-soluble lignan sesamol, a natural phenolic compound derived from Sesamum indicum (sesame) seed oil, has since become known as a potent antioxidant with significant anticancer potential.2,3 As a constituent found in food oils such as sesame and sunflower oil, sesamol has been studied for the dietary benefits that it has been said to impart. Sesame oil, in particular, has been used in Ayurveda, traditional Chinese medicine, as well as in folk medicine in Nigeria and other African countries.Data on its antioxidant and chemopreventive properties also have prompted investigations into its potential in the dermatologic realm because sesamol has demonstrated an increasingly wide array of cutaneous applications.
Antibacterial effects
In 2007, Bankole et al. ascertained the synergistic antimicrobial properties of the essential oils and lignans found in the leaf extracts of S. radiatum and S. indicum. Phytochemical screening of methanolic extracts revealed the presence of phenolic compounds such as the potent antioxidants sesamol, sesamolin, and sesamin, as well as carboxylic acids. Methanolic and ethanolic extracts were shown to exhibit broad-spectrum antimicrobial effects against all of the pathogens tested except Streptococcus pneumoniae (methanolic extracts) and Staphylococcus aureus (ethanolic extracts). The investigators concluded that their results buttressed long-held traditional claims in multiple regions in Nigeria where consumption of sesame leaf extracts has been known to confer antibacterial effects with effectiveness reported for common skin infections.4
Anticancer activity
Kapadia et al. studied the dietary components resveratrol, sesamol, sesame oil, and sunflower oil in various protocols, including a murine two-stage skin cancer model, for their potential as cancer chemopreventive agents. In this 2002 study, the mouse skin tumor model, sesamol was found to provide a 50% reduction in skin papillomas at 20 weeks after promotion with 12-O-tetradecanoylphorbol 13-acetate. The researchers concluded that all of the dietary constituents appeared to provide chemopreventive effects.5
In 2010, Ramachandran et al. observed that pretreating human skin dermal fibroblast adult cells with sesamol before irradiation with UVB yielded significant reductions in cytotoxicity, intracellular reactive oxygen species levels, lipid peroxidation, and apoptosis. In noting increases in enzymatic and nonenzymatic antioxidant activity in sesamol-pretreated UVB-exposed fibroblasts, the investigators ascribed the apparent protective effects of sesamol to its antioxidant scavenging of reactive oxygen species.6
Seven years later, Bhardwaj et al. evaluated the chemopreventive efficacy of free and encapsulated sesamol in a 7,12-dimethylbenz[a]-anthracene–induced skin cancer animal model. The investigators found that in both forms sesamol significantly reduced tumor burden and lipid peroxidation while raising antioxidant levels. This resulted in the inhibition of skin tumor development and promotion. Apoptosis in tumor cells also was found to result from the down-regulation of Bcl-2 and stimulation of Bcl-2–associated X protein expression from administration of both free and encapsulated sesamol. Furthermore, the irritant qualities of sesamol were mitigated by encapsulation, which also aided in direct targeting of the skin.2
Potential cosmeceutical applications: Anti-aging and skin-whitening activity
In 2006, Sharma and Kaur demonstrated in mouse skin, through biochemical and histopathologic evaluations, that a topical sesamol formulation was effective in preventing photodamage (such as alterations in skin integrity, lesions, ulcers) from chronic UV exposure. They suggested the merits of further testing and consideration of sesamol as an antiaging agent.7
Almost a decade later, Srisayam et al. conducted a systematic study of the antimelanogenic and skin protective activities of sesamol. They found that sesamol exhibited significant scavenging activity of the 2,2-Diphenyl-1-picrylhydrazyl hydrate radical with an IC50 value less than 14.48 mcm. The antioxidant also suppressed lipid peroxidation (IC50 value of 6.15 mcm), and displayed a whitening effect via mushroom tyrosinase inhibition as well as inhibition of cellular tyrosinase. In noting the potent antioxidant and antityrosinase activity in comparison to the positive control – kojic acid and beta-arbutin – the researchers highlighted the potential cosmeceutical applications of sesamol.8
Baek and Lee showed in 2015 that sesamol potently suppressed melanin biosynthesis by down-regulating tyrosinase activity and regulating gene expression of melanogenesis-related proteins via microphthalmia-associated transcription factor (MITF) activity modulation. They concluded that sesamol warrants attention in the cosmetic realm as a new skin-whitening agent.9
Formulation issues
Earlier that year, Geetha et al. confirmed the apoptotic characteristics of sesamol in in vitro antiproliferative and DNA-fragmentation studies in HL60 cell lines. Because of its small size, low molecular weight, and easy permeability, its viability in topical applications is considered minimal. The investigators addressed this issue by preparing sesamol-loaded solid-lipid nanoparticles, which, when applied in a cream base in mice, revealed significant retention in the skin. Its use in in vivo anticancer studies performed on tumor production induced by 12-O-tetradecanoylphorbol 13-acetate and initiated by benzo(a)pyrene in mouse epidermis resulted in the normalization of skin cancers.10
More recently, Puglia et al. set out to improve the delivery of the benefits of sesamol to the skin by developing a nanostructured lipid carrier for topical administration. They synthesized two different carrier systems and performed an in vitro percutaneous absorption study in excised human skin to determine antioxidant activity. The carrier systems differed by oil phase: One contained Miglyol 812 (nanostructured lipid carrier–M) and the other contained sesame oil (nanostructured lipid carrier–PLUS). Greater encapsulation efficiency was reported when sesame oil was employed as the oil phase, but both products displayed the capacity in vitro to control the rate of sesamol diffusion through the skin, compared with reference preparations. Both formulations also showed the extended antioxidant activity of sesamol, particularly the nanostructured lipid carrier–PLUS.3
Conclusion
Dr. Baumann is a private practice dermatologist, researcher, author and entrepreneur who practices in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann has written two textbooks: “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and “Cosmeceuticals and Cosmetic Ingredients” (New York: McGraw-Hill, 2014). She also wrote a New York Times Best Sellers book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). Dr. Baumann has received funding for advisory boards and/or clinical research trials from Allergan, Evolus, Galderma, and Revance. She is the founder and CEO of Skin Type Solutions Franchise Systems LLC.
References
1. Sato Y et al. Yakugaku Zasshi. 1991 Jan;111(1):51-8.
2. Bhardwaj R et al. Anticancer Agents Med Chem. 2017;17(5):726-33.
3. Puglia C et al. Planta Med. 2017 Mar;83(5):398-404.
4. Bankole MA et al. Afr J Tradit Complement Altern Med. 2007; 4(4): 427-33.
5. Kapadia GJ et al. Pharmacol Res. 2002 Jun;45(6):499-505.
6. Ramachandran S et al. Arch Dermatol Res. 2010 Dec;302(10):733-44.
7. Sharma S and Kaur IP. Int J Dermatol. 2006 Mar;45(3):200-8.
8. Srisayam M et al. J Cosmet Sci. 2014 Mar-Apr;65(2):69-79.
9. Baek SH and Lee SH. Exp Dermatol. 2015 Oct;24(10):761-6.
10. Geetha T et al. J Drug Target. 2015 Feb;23(2):159-69.
The protective effects of the antioxidative compound sesamol against radiation were reported as early as 1991.1 The water-soluble lignan sesamol, a natural phenolic compound derived from Sesamum indicum (sesame) seed oil, has since become known as a potent antioxidant with significant anticancer potential.2,3 As a constituent found in food oils such as sesame and sunflower oil, sesamol has been studied for the dietary benefits that it has been said to impart. Sesame oil, in particular, has been used in Ayurveda, traditional Chinese medicine, as well as in folk medicine in Nigeria and other African countries.Data on its antioxidant and chemopreventive properties also have prompted investigations into its potential in the dermatologic realm because sesamol has demonstrated an increasingly wide array of cutaneous applications.
Antibacterial effects
In 2007, Bankole et al. ascertained the synergistic antimicrobial properties of the essential oils and lignans found in the leaf extracts of S. radiatum and S. indicum. Phytochemical screening of methanolic extracts revealed the presence of phenolic compounds such as the potent antioxidants sesamol, sesamolin, and sesamin, as well as carboxylic acids. Methanolic and ethanolic extracts were shown to exhibit broad-spectrum antimicrobial effects against all of the pathogens tested except Streptococcus pneumoniae (methanolic extracts) and Staphylococcus aureus (ethanolic extracts). The investigators concluded that their results buttressed long-held traditional claims in multiple regions in Nigeria where consumption of sesame leaf extracts has been known to confer antibacterial effects with effectiveness reported for common skin infections.4
Anticancer activity
Kapadia et al. studied the dietary components resveratrol, sesamol, sesame oil, and sunflower oil in various protocols, including a murine two-stage skin cancer model, for their potential as cancer chemopreventive agents. In this 2002 study, the mouse skin tumor model, sesamol was found to provide a 50% reduction in skin papillomas at 20 weeks after promotion with 12-O-tetradecanoylphorbol 13-acetate. The researchers concluded that all of the dietary constituents appeared to provide chemopreventive effects.5
In 2010, Ramachandran et al. observed that pretreating human skin dermal fibroblast adult cells with sesamol before irradiation with UVB yielded significant reductions in cytotoxicity, intracellular reactive oxygen species levels, lipid peroxidation, and apoptosis. In noting increases in enzymatic and nonenzymatic antioxidant activity in sesamol-pretreated UVB-exposed fibroblasts, the investigators ascribed the apparent protective effects of sesamol to its antioxidant scavenging of reactive oxygen species.6
Seven years later, Bhardwaj et al. evaluated the chemopreventive efficacy of free and encapsulated sesamol in a 7,12-dimethylbenz[a]-anthracene–induced skin cancer animal model. The investigators found that in both forms sesamol significantly reduced tumor burden and lipid peroxidation while raising antioxidant levels. This resulted in the inhibition of skin tumor development and promotion. Apoptosis in tumor cells also was found to result from the down-regulation of Bcl-2 and stimulation of Bcl-2–associated X protein expression from administration of both free and encapsulated sesamol. Furthermore, the irritant qualities of sesamol were mitigated by encapsulation, which also aided in direct targeting of the skin.2
Potential cosmeceutical applications: Anti-aging and skin-whitening activity
In 2006, Sharma and Kaur demonstrated in mouse skin, through biochemical and histopathologic evaluations, that a topical sesamol formulation was effective in preventing photodamage (such as alterations in skin integrity, lesions, ulcers) from chronic UV exposure. They suggested the merits of further testing and consideration of sesamol as an antiaging agent.7
Almost a decade later, Srisayam et al. conducted a systematic study of the antimelanogenic and skin protective activities of sesamol. They found that sesamol exhibited significant scavenging activity of the 2,2-Diphenyl-1-picrylhydrazyl hydrate radical with an IC50 value less than 14.48 mcm. The antioxidant also suppressed lipid peroxidation (IC50 value of 6.15 mcm), and displayed a whitening effect via mushroom tyrosinase inhibition as well as inhibition of cellular tyrosinase. In noting the potent antioxidant and antityrosinase activity in comparison to the positive control – kojic acid and beta-arbutin – the researchers highlighted the potential cosmeceutical applications of sesamol.8
Baek and Lee showed in 2015 that sesamol potently suppressed melanin biosynthesis by down-regulating tyrosinase activity and regulating gene expression of melanogenesis-related proteins via microphthalmia-associated transcription factor (MITF) activity modulation. They concluded that sesamol warrants attention in the cosmetic realm as a new skin-whitening agent.9
Formulation issues
Earlier that year, Geetha et al. confirmed the apoptotic characteristics of sesamol in in vitro antiproliferative and DNA-fragmentation studies in HL60 cell lines. Because of its small size, low molecular weight, and easy permeability, its viability in topical applications is considered minimal. The investigators addressed this issue by preparing sesamol-loaded solid-lipid nanoparticles, which, when applied in a cream base in mice, revealed significant retention in the skin. Its use in in vivo anticancer studies performed on tumor production induced by 12-O-tetradecanoylphorbol 13-acetate and initiated by benzo(a)pyrene in mouse epidermis resulted in the normalization of skin cancers.10
More recently, Puglia et al. set out to improve the delivery of the benefits of sesamol to the skin by developing a nanostructured lipid carrier for topical administration. They synthesized two different carrier systems and performed an in vitro percutaneous absorption study in excised human skin to determine antioxidant activity. The carrier systems differed by oil phase: One contained Miglyol 812 (nanostructured lipid carrier–M) and the other contained sesame oil (nanostructured lipid carrier–PLUS). Greater encapsulation efficiency was reported when sesame oil was employed as the oil phase, but both products displayed the capacity in vitro to control the rate of sesamol diffusion through the skin, compared with reference preparations. Both formulations also showed the extended antioxidant activity of sesamol, particularly the nanostructured lipid carrier–PLUS.3
Conclusion
Dr. Baumann is a private practice dermatologist, researcher, author and entrepreneur who practices in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann has written two textbooks: “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and “Cosmeceuticals and Cosmetic Ingredients” (New York: McGraw-Hill, 2014). She also wrote a New York Times Best Sellers book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). Dr. Baumann has received funding for advisory boards and/or clinical research trials from Allergan, Evolus, Galderma, and Revance. She is the founder and CEO of Skin Type Solutions Franchise Systems LLC.
References
1. Sato Y et al. Yakugaku Zasshi. 1991 Jan;111(1):51-8.
2. Bhardwaj R et al. Anticancer Agents Med Chem. 2017;17(5):726-33.
3. Puglia C et al. Planta Med. 2017 Mar;83(5):398-404.
4. Bankole MA et al. Afr J Tradit Complement Altern Med. 2007; 4(4): 427-33.
5. Kapadia GJ et al. Pharmacol Res. 2002 Jun;45(6):499-505.
6. Ramachandran S et al. Arch Dermatol Res. 2010 Dec;302(10):733-44.
7. Sharma S and Kaur IP. Int J Dermatol. 2006 Mar;45(3):200-8.
8. Srisayam M et al. J Cosmet Sci. 2014 Mar-Apr;65(2):69-79.
9. Baek SH and Lee SH. Exp Dermatol. 2015 Oct;24(10):761-6.
10. Geetha T et al. J Drug Target. 2015 Feb;23(2):159-69.
The protective effects of the antioxidative compound sesamol against radiation were reported as early as 1991.1 The water-soluble lignan sesamol, a natural phenolic compound derived from Sesamum indicum (sesame) seed oil, has since become known as a potent antioxidant with significant anticancer potential.2,3 As a constituent found in food oils such as sesame and sunflower oil, sesamol has been studied for the dietary benefits that it has been said to impart. Sesame oil, in particular, has been used in Ayurveda, traditional Chinese medicine, as well as in folk medicine in Nigeria and other African countries.Data on its antioxidant and chemopreventive properties also have prompted investigations into its potential in the dermatologic realm because sesamol has demonstrated an increasingly wide array of cutaneous applications.
Antibacterial effects
In 2007, Bankole et al. ascertained the synergistic antimicrobial properties of the essential oils and lignans found in the leaf extracts of S. radiatum and S. indicum. Phytochemical screening of methanolic extracts revealed the presence of phenolic compounds such as the potent antioxidants sesamol, sesamolin, and sesamin, as well as carboxylic acids. Methanolic and ethanolic extracts were shown to exhibit broad-spectrum antimicrobial effects against all of the pathogens tested except Streptococcus pneumoniae (methanolic extracts) and Staphylococcus aureus (ethanolic extracts). The investigators concluded that their results buttressed long-held traditional claims in multiple regions in Nigeria where consumption of sesame leaf extracts has been known to confer antibacterial effects with effectiveness reported for common skin infections.4
Anticancer activity
Kapadia et al. studied the dietary components resveratrol, sesamol, sesame oil, and sunflower oil in various protocols, including a murine two-stage skin cancer model, for their potential as cancer chemopreventive agents. In this 2002 study, the mouse skin tumor model, sesamol was found to provide a 50% reduction in skin papillomas at 20 weeks after promotion with 12-O-tetradecanoylphorbol 13-acetate. The researchers concluded that all of the dietary constituents appeared to provide chemopreventive effects.5
In 2010, Ramachandran et al. observed that pretreating human skin dermal fibroblast adult cells with sesamol before irradiation with UVB yielded significant reductions in cytotoxicity, intracellular reactive oxygen species levels, lipid peroxidation, and apoptosis. In noting increases in enzymatic and nonenzymatic antioxidant activity in sesamol-pretreated UVB-exposed fibroblasts, the investigators ascribed the apparent protective effects of sesamol to its antioxidant scavenging of reactive oxygen species.6
Seven years later, Bhardwaj et al. evaluated the chemopreventive efficacy of free and encapsulated sesamol in a 7,12-dimethylbenz[a]-anthracene–induced skin cancer animal model. The investigators found that in both forms sesamol significantly reduced tumor burden and lipid peroxidation while raising antioxidant levels. This resulted in the inhibition of skin tumor development and promotion. Apoptosis in tumor cells also was found to result from the down-regulation of Bcl-2 and stimulation of Bcl-2–associated X protein expression from administration of both free and encapsulated sesamol. Furthermore, the irritant qualities of sesamol were mitigated by encapsulation, which also aided in direct targeting of the skin.2
Potential cosmeceutical applications: Anti-aging and skin-whitening activity
In 2006, Sharma and Kaur demonstrated in mouse skin, through biochemical and histopathologic evaluations, that a topical sesamol formulation was effective in preventing photodamage (such as alterations in skin integrity, lesions, ulcers) from chronic UV exposure. They suggested the merits of further testing and consideration of sesamol as an antiaging agent.7
Almost a decade later, Srisayam et al. conducted a systematic study of the antimelanogenic and skin protective activities of sesamol. They found that sesamol exhibited significant scavenging activity of the 2,2-Diphenyl-1-picrylhydrazyl hydrate radical with an IC50 value less than 14.48 mcm. The antioxidant also suppressed lipid peroxidation (IC50 value of 6.15 mcm), and displayed a whitening effect via mushroom tyrosinase inhibition as well as inhibition of cellular tyrosinase. In noting the potent antioxidant and antityrosinase activity in comparison to the positive control – kojic acid and beta-arbutin – the researchers highlighted the potential cosmeceutical applications of sesamol.8
Baek and Lee showed in 2015 that sesamol potently suppressed melanin biosynthesis by down-regulating tyrosinase activity and regulating gene expression of melanogenesis-related proteins via microphthalmia-associated transcription factor (MITF) activity modulation. They concluded that sesamol warrants attention in the cosmetic realm as a new skin-whitening agent.9
Formulation issues
Earlier that year, Geetha et al. confirmed the apoptotic characteristics of sesamol in in vitro antiproliferative and DNA-fragmentation studies in HL60 cell lines. Because of its small size, low molecular weight, and easy permeability, its viability in topical applications is considered minimal. The investigators addressed this issue by preparing sesamol-loaded solid-lipid nanoparticles, which, when applied in a cream base in mice, revealed significant retention in the skin. Its use in in vivo anticancer studies performed on tumor production induced by 12-O-tetradecanoylphorbol 13-acetate and initiated by benzo(a)pyrene in mouse epidermis resulted in the normalization of skin cancers.10
More recently, Puglia et al. set out to improve the delivery of the benefits of sesamol to the skin by developing a nanostructured lipid carrier for topical administration. They synthesized two different carrier systems and performed an in vitro percutaneous absorption study in excised human skin to determine antioxidant activity. The carrier systems differed by oil phase: One contained Miglyol 812 (nanostructured lipid carrier–M) and the other contained sesame oil (nanostructured lipid carrier–PLUS). Greater encapsulation efficiency was reported when sesame oil was employed as the oil phase, but both products displayed the capacity in vitro to control the rate of sesamol diffusion through the skin, compared with reference preparations. Both formulations also showed the extended antioxidant activity of sesamol, particularly the nanostructured lipid carrier–PLUS.3
Conclusion
Dr. Baumann is a private practice dermatologist, researcher, author and entrepreneur who practices in Miami. She founded the Cosmetic Dermatology Center at the University of Miami in 1997. Dr. Baumann has written two textbooks: “Cosmetic Dermatology: Principles and Practice” (New York: McGraw-Hill, 2002) and “Cosmeceuticals and Cosmetic Ingredients” (New York: McGraw-Hill, 2014). She also wrote a New York Times Best Sellers book for consumers, “The Skin Type Solution” (New York: Bantam Dell, 2006). Dr. Baumann has received funding for advisory boards and/or clinical research trials from Allergan, Evolus, Galderma, and Revance. She is the founder and CEO of Skin Type Solutions Franchise Systems LLC.
References
1. Sato Y et al. Yakugaku Zasshi. 1991 Jan;111(1):51-8.
2. Bhardwaj R et al. Anticancer Agents Med Chem. 2017;17(5):726-33.
3. Puglia C et al. Planta Med. 2017 Mar;83(5):398-404.
4. Bankole MA et al. Afr J Tradit Complement Altern Med. 2007; 4(4): 427-33.
5. Kapadia GJ et al. Pharmacol Res. 2002 Jun;45(6):499-505.
6. Ramachandran S et al. Arch Dermatol Res. 2010 Dec;302(10):733-44.
7. Sharma S and Kaur IP. Int J Dermatol. 2006 Mar;45(3):200-8.
8. Srisayam M et al. J Cosmet Sci. 2014 Mar-Apr;65(2):69-79.
9. Baek SH and Lee SH. Exp Dermatol. 2015 Oct;24(10):761-6.
10. Geetha T et al. J Drug Target. 2015 Feb;23(2):159-69.
