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Quasi-Drugs Developed in Japan for the Prevention or Treatment of Hyperpigmentary Disorders
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Int. J. Mol. Sci. 2010, 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 and Masamitsu Ichihashi 1,2
Skin Aging and Photo-aging Research Center, Doshisha University, Kizugawa, Kyoto 619-0225, Japan
Kobe Skin Research Institute, Kobe, Hyogo 650-0047, Japan
Biological Research Division, The Estee Lauder Companies Inc., Melville, New York 11747, NY, USA
Author to whom correspondence should be addressed; Tel.: +81-78-304-5791; Fax: +81-78-304-5792.
Received: 5 July 2010 / Accepted: 8 July 2010 / Published: 12 July 2010
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.

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].


  1. 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. [Google Scholar]
  2. 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. [Google Scholar]
  3. 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. [Google Scholar]
  4. 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. [Google Scholar]
Table 1. Mechanistic classification of skin lightening QDs approved by the MHLW of Japan.
Table 1. Mechanistic classification of skin lightening QDs approved by the MHLW of Japan.
TargetMechanismDetailSkin Lightening QD

MelanocyteInhibition of tyrosinase activityAnti-oxidationAscorbic acid/derivatives

Chelating copper atomsKojic acidEllagic acid

Competitive inhibitionArbutin 4MSKRucinol® 4-HPB

Decrease of tyrosinase protein levelAcceleration of Tyr degradationLinoleic acid

Inhibition of Tyr maturationMagnolignan®

KeratinocyteInhibition of KC-MC signalingInhibition of UV inflammationChamomilla extract Tranexamic acid/derivative

Melanocyte and KeratinocyteInhibition of melanosome transferInhibition of melanin dispersionNiacinamide

EpidermisAcceleration of epidermal turnoverDesquamation of melaninPlacental extract Adenosine mono-phosphate
KC: keratinocyte; MC: melanocyte; Tyr: tyrosinase; UV: ultraviolet light.
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
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