title: The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein.
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.
authors.affiliation: Department of Biochemistry, College of Medicine, Chung-Ang University, 221 Heukseok-Dong Dongjak-Gu, Seoul 156-756, Republic of Korea.
authors.forename: Dong-Seok
authors.initials: DS
authors.lastname: Kim
authors.forename: Sangku
authors.initials: S
authors.lastname: Lee
authors.forename: Hyun-Kyung
authors.initials: HK
authors.lastname: Lee
authors.forename: Seo-Hyoung
authors.initials: SH
authors.lastname: Park
authors.forename: In-Ja
authors.initials: IJ
authors.lastname: Ryoo
authors.forename: Ick-Dong
authors.initials: ID
authors.lastname: Yoo
authors.forename: Sun-Bang
authors.initials: SB
authors.lastname: Kwon
authors.forename: Kwang Jin
authors.initials: KJ
authors.lastname: Baek
authors.forename: Jung-Im
authors.initials: JI
authors.lastname: Na
authors.forename: Kyoung-Chan
authors.initials: KC
authors.lastname: Park
mesh_terms: D000363:Agaricales / Q000201:enzymology; D000818:Animals; D002109:Caffeic Acids / Q000008:administration & dosage / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003517:Cyclopentanes / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation / Q000187:drug effects; D004357:Drug Synergism; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D017496:Hypopigmentation / Q000378:metabolism*; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D051739:Microphthalmia-Associated Transcription Factor / Q000187:drug effects / Q000378:metabolism; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors
chemical_list: C527982:2-butyl-5-hydroxyphenyl dihydrocaffeate; D002109:Caffeic Acids; D003517:Cyclopentanes; D004791:Enzyme Inhibitors; D008543:Melanins; D051739:Microphthalmia-Associated Transcription Factor; C439087:terrein; D014442:Monophenol Monooxygenase