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International Journal of Molecular Sciences logoLink to International Journal of Molecular Sciences
. 2010 Jul 12;11(7):2699–2700. doi: 10.3390/ijms11072699

Quasi-Drugs Developed in Japan for the Prevention or Treatment of Hyperpigmentary Disorders. Int. J. Mol. Sci. 2010, 11, 2566–2575

Hideya Ando 1,2,*, Mary S Matsui 3, Masamitsu Ichihashi 1,2
PMCID: PMC2920561

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 [1]. 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.

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.

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 [2]. 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].

References

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