terrein and Hypopigmentation

Resorcinol derivatives are known to inhibit melanin synthesis. In this study, resorcinol derivatives were synthesized and screened for their activity on melanogenesis. KI-063 (a tyrosinase inhibitor) was examined for its effects on melanogenesis using a spontaneously immortalized mouse melanocyte cell line (Mel-Ab). In a cell-free system, KI-063 directly inhibited tyrosinase, the rate-limiting melanogenic enzyme. Moreover, in a cell system, it inhibited melanin synthesis in a concentration-dependent manner. In addition, KI-063 inhibited the activity of cellular tyrosinase. Thus, this study examined the effects of a combination of KI-063 with terrein, an agent that down-regulates microphthalmia-associated transcription factor. The data suggest that KI-063 has an additive effect in combination with terrein. Thus, the suppression of tyrosinase activity by KI-063 and the inhibition of tyrosinase production by terrein appear to be an optimal combination for skin whitening.

Topics: Agaricales; Animals; Caffeic Acids; Cell Line; Cell Survival; Cyclopentanes; Dose-Response Relationship, Drug; Down-Regulation; Drug Synergism; Enzyme Inhibitors; Hypopigmentation; Melanins; Melanocytes; Mice; Microphthalmia-Associated Transcription Factor; Monophenol Monooxygenase