The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein

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The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein
D S Kim; Sangku Lee; H K Lee; S H Park; In Ja Ryoo; Ick Dong Yoo; S B Kwon; J B Kwang; J I Na; K C Park
Bibliographic Citation
Journal of Pharmacy and Pharmacology, vol. 60, no. 3, pp. 343-348
Publication Year
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.
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