J. Cosmet. Sci., 64, 133–144 (March/April 2013) 133 In vitro melanogenesis inhibitory effects of N-feruloyldopamine S. LEOTY-OKOMBI, S. BONNET, D. RIVAL, V. DEGRAVE, X. LIN, B. VOGELGESANG, and V. ANDRÉ-FREI, BASF Beauty Care Solutions, 69366 Lyon Cedex 07, France (S.L.-O., S.B., D.R., V.D., B.V., V.A.-F.), and BASF Beauty Care Solutions, Stony Brook, NY 11790 (X.L.). Accepted for publication July 23, 2012. The author’s of this article are the employees of BASF. S.L.-O and D.R. are both inventors of U.S. patent US 20110237551 owned by BASF Beauty Care Solutions France S.A.S that protects the use of N-feruloyldopamine in cosmetic preparations. Synopsis Tyrosinase is the rate-limiting enzyme in the melanogenesis process. It remains the most effi cient way to downregulate melanin production and improve unsightly pigmentary disorders. The aim of our investiga- tions was to fi nd a structurally characterized molecule with better effi cacy than existing molecules without cell toxicity. We focused our investigations on compounds that could act as substrate-mimicking inhibitors of tyrosinase and identifi ed N-feruloyldopamine as the best candidate. In vitro, N-feruloyldopamine inhibited human tyrosinase with higher effi cacy than the reference inhibitor arbutin without cell toxicity at least up to 100 μM as measured in cultured normal human epidermal melanocytes (NHEMs). Moreover, the inhibition appeared to be specifi c to mammalian tyrosinases as shown by a very poor inhibition of mushroom tyrosinase, but a signifi cant decrease of total melanin in B16-F10 cells. The antioxidant capacity assessed using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay was comparable to that of vitamin C and fi nally, N-feruloyldopamine exerted a signifi cant inhibition of Pmel17 gene expression when used at 100 μM on cultured NHEM. Taken together, these results suggest that N-feruloyldopamine is a serious candidate for in vivo application as complexion-brightening ingredient. INTRODUCTION Besides increasing concerns about deleterious effects of excessive sun exposure, skin complexion color has become a crucial parameter in the perception of health and beauty (1). Pigmentation disorders that can occur at different moments of a lifetime (pregnancy, old age …), e.g., melasma, freckles, or age spots, can dramatically affect one’s self-confi dence. Medicinal or cosmetic complexion-lightening agents have proved growing popularity. Address all correspondence to Sabrina Leoty-Okombi at sabrina.leoty-okombi@basf.com
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