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Novel Inhibitory Effect of N-(2-Hydroxycyclohexyl)valiolamine on Melanin Production in a Human Skin Model

AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea
Department of Dermatology, Dongguk University Ilsan Hospital, 814 Siksa-dong, Ilsandong-gu, Goyang-si, Gyenoggi-do 410-773, Korea
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2014, 15(7), 12188-12195;
Received: 30 April 2014 / Revised: 24 June 2014 / Accepted: 26 June 2014 / Published: 9 July 2014
PDF [1378 KB, uploaded 9 July 2014]


Hyper-pigmentation causes skin darkness and medical disorders, such as post-inflammatory melanoderma and melasma. Therefore, the development of anti-melanogenic agents is important for treating these conditions and for cosmetic production. In our previous paper, we demonstrated that the anti-diabetic drug voglibose, a valiolamine derivative, is a potent anti-melanogenic agent. In addition, we proposed an alternative screening strategy to identify valiolamine derivatives with high skin permeability that act as anti-melanogenic agents when applied topically. In this study, we synthesized several valiolamine derivatives with enhanced lipophilicity and examined their inhibitory effects in a human skin model. N-(2-hydroxycyclohexyl)valiolamine (HV) possesses a stronger inhibitory effect on melanin production than voglibose in a human skin model, suggesting that HV is a more potent anti-melanogenic agent for the skin. View Full-Text
Keywords: valiolamine derivative; melanin; melanogenesis; tyrosinase valiolamine derivative; melanin; melanogenesis; tyrosinase

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Bin, B.-H.; Joo, Y.H.; Lee, A.-Y.; Shin, S.S.; Cho, E.-G.; Lee, T.R. Novel Inhibitory Effect of N-(2-Hydroxycyclohexyl)valiolamine on Melanin Production in a Human Skin Model. Int. J. Mol. Sci. 2014, 15, 12188-12195.

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