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The Development of Sugar-Based Anti-Melanogenic Agents

AmorePacific Corporation Research & Deveolopment Center, Yongin, Gyeonggi-do 446-729, Korea
Department of Chemical Engineering, POSTECH, Pohang 790-784, Korea
Authors to whom correspondence should be addressed.
Academic Editor: Manickam Sugumaran
Int. J. Mol. Sci. 2016, 17(4), 583;
Received: 17 March 2016 / Revised: 12 April 2016 / Accepted: 14 April 2016 / Published: 16 April 2016
(This article belongs to the Special Issue Biochemistry and Mechanisms of Melanogenesis)
The regulation of melanin production is important for managing skin darkness and hyperpigmentary disorders. Numerous anti-melanogenic agents that target tyrosinase activity/stability, melanosome maturation/transfer, or melanogenesis-related signaling pathways have been developed. As a rate-limiting enzyme in melanogenesis, tyrosinase has been the most attractive target, but tyrosinase-targeted treatments still pose serious potential risks, indicating the necessity of developing lower-risk anti-melanogenic agents. Sugars are ubiquitous natural compounds found in humans and other organisms. Here, we review the recent advances in research on the roles of sugars and sugar-related agents in melanogenesis and in the development of sugar-based anti-melanogenic agents. The proposed mechanisms of action of these agents include: (a) (natural sugars) disturbing proper melanosome maturation by inducing osmotic stress and inhibiting the PI3 kinase pathway and (b) (sugar derivatives) inhibiting tyrosinase maturation by blocking N-glycosylation. Finally, we propose an alternative strategy for developing anti-melanogenic sugars that theoretically reduce melanosomal pH by inhibiting a sucrose transporter and reduce tyrosinase activity by inhibiting copper incorporation into an active site. These studies provide evidence of the utility of sugar-based anti-melanogenic agents in managing skin darkness and curing pigmentary disorders and suggest a future direction for the development of physiologically favorable anti-melanogenic agents. View Full-Text
Keywords: sugar; melanin; anti-melanogenic agent; stress N-glycosylation; osmotic stress sugar; melanin; anti-melanogenic agent; stress N-glycosylation; osmotic stress
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MDPI and ACS Style

Bin, B.-H.; Kim, S.T.; Bhin, J.; Lee, T.R.; Cho, E.-G. The Development of Sugar-Based Anti-Melanogenic Agents. Int. J. Mol. Sci. 2016, 17, 583.

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