A Novel Role of Serotonin Receptor 2B Agonist as an Anti-Melanogenesis Agent

被引：17

作者：

Oh, Eun Ju ^{[1
]}

Park, Jong Il ^{[1
]}

Lee, Ji Eun ^{[1
]}

Myung, Cheol Hwan ^{[1
]}

Kim, Su Yeon ^{[2
]}

Chang, Sung Eun ^{[2
]}

Hwang, Jae Sung ^{[1
]}

机构：

[1] Kyung Hee Univ, Grad Sch Biotechnol, Dept Genet Engn, Yongin 446701, South Korea

[2] Univ Ulsan, Coll Med, Asan Med Ctr, Dept Dermatol, 388-1 Pungnap Dong, Seoul 138736, South Korea

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2016年 / 17卷 / 04期

关键词：

BW723C86; melanogenesis; PKA; CREB; MITF; MELATONINERGIC SYSTEMS; BW; 723C86; SKIN; INHIBITION; EXPRESSION; ACTIVATION; TRYPTOPHAN; MITF; ACID; CAMP;

D O I：

10.3390/ijms17040546

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

BW723C86, a serotonin receptor 2B agonist, has been investigated as a potential therapeutic for various conditions such as anxiety, hyperphagia and hypertension. However, the functional role of BW723C86 against melanogenesis remains unclear. In this study, we investigate the effect of serotonin receptor 2B (5-HTR2B) agonist on melanogenesis and elucidate the mechanism involved. BW723C86 reduced melanin synthesis and intracellular tyrosinase activity in melan-A cells and normal human melanocytes. The expression of melanogenesis-related proteins (tyrosinase, TRP-1 and TRP-2) and microphthalmia-associated transcription factor (MITF) in melan-A cells decreased after BW723C86 treatment. The promoter activity of MITF was also reduced by BW723C86 treatment. The reduced level of MITF was associated with inhibition of protein kinase A (PKA) and cAMP response element-binding protein (CREB) activation by BW723C86 treatment. These results suggest that the serotonin agonist BW723C86 could be a potential therapeutic agent for skin hyperpigmentation disorders.

引用

页数：10

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