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- Title
The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein.
- Authors
Dong-Seok Kim; Sangku Lee; Hyun-Kyung Lee; Seo-Hyoung Park; In-Ja Ryoo; Ick-Dong Yoo; Sun-Bang Kwon; Kwang Jin Baek; Jung-Im Na; Kyoung-Chan Park
- Abstract
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.
- Subjects
RESORCINOL; MELANOGENESIS; PHENOL oxidase; TRANSCRIPTION factors
- Publication
Journal of Pharmacy & Pharmacology, 2008, Vol 60, Issue 3, p343
- ISSN
0022-3573
- Publication type
Article
- DOI
10.1211/jpp.60.3.0009