S-Space College of Medicine/School of Medicine (의과대학/대학원) Molecular and Genomic Medicine (분자유전체의학전공) Journal Papers (저널논문_분자유전체의학전공)
Inhibitory effects of 4-n-butylresorcinol on tyrosinase activity and melanin synthesis
- Kim, Dong-Seok; Kim, So-Young; Park, Seo-Hyoung; Choi, Yeong-Gon; Kwon, Sun-Bang; Kim, Myo-Kyoung; Na, Jung-Im; Youn, Sang-Woong; Park, Kyoung-Chan
- Issue Date
- Pharmaceutical Society of Japan
- Biol Pharm Bull. 2005 Dec;28(12):2216-9.
- Animals; Blotting, Western; Cell Line; Cell Survival/drug effects; Dose-Response Relationship, Drug; Down-Regulation/drug effects; Drug Combinations; Drug Synergism; Humans; Hypopigmentation/chemically induced/metabolism; Melanins/*antagonists & inhibitors/*biosynthesis/chemistry; Mice; Microphthalmia-Associated Transcription Factor/antagonists &; inhibitors/chemistry/drug effects; Monophenol Monooxygenase/*antagonists & inhibitors/drug effects/metabolism; Monoterpenes/chemistry/pharmacology; Resorcinols/chemistry/*pharmacology; Signal Transduction/drug effects; Skin Pigmentation; Tropolone/analogs & derivatives/chemistry/pharmacology
- In this study, we investigated the effects of 4-n-butylresorcinol on melanogenesis in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Our results show that 4-n-butylresorcinol significantly inhibits melanin synthesis in a concentration-dependent manner. In addition, it was also found to inhibit the activity of tyrosinase, the rate-limiting melanogenic enzyme. Several reports have indicated that the activation of extracellular signal-regulated kinase (ERK) or of Akt reduces melanin synthesis via microphthalmia-associated transcription factor (MITF) down-regulation. Accordingly, we examined the effects of 4-n-butylresorcinol on the ERK and Akt signaling pathways. 4-n-Butylresorcinol did not induce ERK, Akt activation, or MITF degradation, and had no effect on cAMP response element binding protein (CREB) phosphorylation, which stimulates MITF expression. In contrast, 4-n-butylresorcinol strongly reduced tyrosinase activity in a cell-free system. Moreover, 4-n-butylresorcinol showed an additive effect in combination with hinokitiol, which reduces MITF expression. These results show that the hypopigmentary effect of 4-n-butylresorcinol results from its direct inhibition of tyrosinase.
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