- freely available
Int. J. Mol. Sci. 2010, 11(7), 2699-2700; doi:10.3390/ijms11072699
One additional skin lightening or whitening quasi-drug (QD) has been developed and officially approved by the Ministry of Health, Labor and Welfare of Japan. The active ingredient niacinamide should be included in this review . Its mechanism of skin lightening is based on the inhibition of melanosome transfer from melanocytes to keratinocytes. Niacinamide is listed in Table 1, which classifies compounds according to the mechanism of skin lightening QDs registered in Japan.
2.15. Niacinamide (Obtained by Procter & Gamble Company in 2007)
Niacinamide (also termed nicotinamide), a derivative of vitamin B3, has been shown to act as an anti-inflammatory agent in acne . Niacinamide had no effect on the tyrosinase activity and melanin synthesis of cultured normal human melanocytes, however, it was found that niacinamide significantly decreased hyperpigmentation, such as melasma and solar lentigines, via inhibition of melanosome transfer from melanocytes to keratinocytes [3,4].
- Ando, H; Matsui, MS; Ichihashi, M. Quasi-drugs developed in Japan for the prevention or treatment of hyperpigmentary disorders. Int. J. Mol. Sci 2010, 11, 2566–2575, doi:10.3390/ijms11062566. 20640168
- Shalita, AR; Smith, JG; Parish, LH; Sofman, MS; Chalker, DK. Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris. Int. J. Dermatol 1995, 34, 434–437, doi:10.1111/j.1365-4362.1995.tb04449.x. 7657446
- Hakozaki, T; Minwalla, L; Zhuang, J; Chhoa, M; Matsubara, A; Miyamoto, K; Greatens, A; Hillebrand, GG; Bissett, DL; Boissy, RE. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br. J. Dermatol 2002, 147, 20–31, doi:10.1046/j.1365-2133.2002.04834.x. 12100180
- Greatens, A; Hakozaki, T; Koshoffer, A; Epstein, H; Schwemberger, S; Babcock, G; Bissett, D; Takiwaki, H; Arase, S; Wickett, RR; Boissy, RE. Effective inhibition of melanosome transfer to keratinocytes by lectins and niacinamide is reversible. Exp. Dermatol 2005, 14, 498–508, doi:10.1111/j.0906-6705.2005.00309.x. 15946237
|Table 1. Mechanistic classification of skin lightening QDs approved by the MHLW of Japan.|
|Target||Mechanism||Detail||Skin Lightening QD|
|Melanocyte||Inhibition of tyrosinase activity||Anti-oxidation||Ascorbic acid/derivatives|
|Chelating copper atoms||Kojic acid||Ellagic acid|
|Competitive inhibition||Arbutin 4MSK||Rucinol® 4-HPB|
|Decrease of tyrosinase protein level||Acceleration of Tyr degradation||Linoleic acid|
|Inhibition of Tyr maturation||Magnolignan®|
|Keratinocyte||Inhibition of KC-MC signaling||Inhibition of UV inflammation||Chamomilla extract Tranexamic acid/derivative|
|Melanocyte and Keratinocyte||Inhibition of melanosome transfer||Inhibition of melanin dispersion||Niacinamide|
|Epidermis||Acceleration of epidermal turnover||Desquamation of melanin||Placental extract Adenosine mono-phosphate|
KC: keratinocyte; MC: melanocyte; Tyr: tyrosinase; UV: ultraviolet light.
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