In our previous study,
8-hydroxydaidzein (8-OHDe) was demonstrated to be a potent and unique suicide substrate of mushroom
tyrosinase. In this study, the compound was evaluated for in vitro cellular
tyrosinase and melanogenesis inhibitory activities in mouse
B16 melanoma cells and for in vivo skin-whitening activity in human volunteers.
Tyrosinase activity and melanogenesis in the cell culture incubated with 10 microM of 8-OHDe were decreased to 20.1% and 51.8% of control, respectively, while no obvious cytotoxicity was observed in this concentration. In contrast, a standard
tyrosinase inhibitor,
kojic acid, showed 69.9% and 71.3% of control in cellular
tyrosinase and melanogenesis activity, respectively, at a concentration as high as 100 microM. Hence, 8-OHDe exhibited more than an inhibitory effects on
melanin production in B16 cells 10-fold stronger than
kojic acid. In addition, when a cream containing 4% 8-OHDe was applied to human skin in an in vivo study, significant increases in the dL*-values were observed after three weeks. Moreover, the increase in the dL*-values after 8-week treatment with 4% 8-OHDe (from -0.57 to 1.94) is stronger than those of 2% 8-OHDe treatment (from 0.26 to 0.94) and 2% ascorbic acid-2-glucoside treatment (from 0.07 to 1.54). From the results of the study, it was concluded that 8-OHDe, the potent suicide substrate of mushroom
tyrosinase, has depigmenting activities in both mouse
melanoma cells and in human volunteers. Thus, the compound has significant potential for use in
cosmetics as a skin-whitening ingredient.