The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein.
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.
Kim
Dong-Seok
DS
Department of Biochemistry, College of Medicine, Chung-Ang University, 221 Heukseok-Dong Dongjak-Gu, Seoul 156-756, Republic of Korea.
Lee
Sangku
S
Lee
Hyun-Kyung
HK
Park
Seo-Hyoung
SH
Ryoo
In-Ja
IJ
Yoo
Ick-Dong
ID
Kwon
Sun-Bang
SB
Baek
Kwang Jin
KJ
Na
Jung-Im
JI
Park
Kyoung-Chan
KC
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
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