Korean J Physiol Pharmacol.  2014 Jun;18(3):249-254. 10.4196/kjpp.2014.18.3.249.

KHG26792 Inhibits Melanin Synthesis in Mel-Ab Cells and a Skin Equivalent Model

Affiliations
  • 1Department of Biochemistry, Chung-Ang University College of Medicine, Seoul 156-756, Korea. ds_kim@cau.ac.kr
  • 2Organic Chemistry Laboratory, Korea Institute of Science & Technology, Seoul 136-791, Korea.
  • 3Department of Herb Industry, Jungwon University, Goesan 367-805, Korea.
  • 4Department of Dermatology, Seoul National University Bundang Hospital, Seongnam 463-707, Korea.

Abstract

The purpose
of this study is to characterize the effects of KHG26792 (3-(naphthalen-2-yl(propoxy) methyl)azetidine hydrochloride), a potential skin whitening agent, on melanin synthesis and identify the underlying mechanism of action. Our data showed that KHG26792 significantly reduced melanin synthesis in a dose-dependent manner. Additionally, KHG26792 downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase, the rate-limiting enzyme in melanogenesis, although tyrosinase was not inhibited directly. KHG26792 activated extracellular signal-regulated kinase (ERK), whereas an ERK pathway inhibitor, PD98059, rescued KHG26792-induced hypopigmentation. These results suggest that KHG26792 decreases melanin production via ERK activation. Moreover, the hypopigmentary effects of KHG26792 were confirmed in a pigmented skin equivalent model using Cervi cornus Colla (deer antler glue), in which the color of the pigmented artificial skin became lighter after treatment with KHG26792. In summary, our findings suggest that KHG26792 is a novel skin whitening agent.

Keyword

ERK; KHG26792; Melanogenesis; Skin equivalent; Tyrosinase
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