Synthesis and Biological Evaluation of Resveratrol Derivatives as Melanogenesis InhibitorsReport as inadecuate




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1

College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 28644, Korea

2

RNS Inc., Yuseong-Gu, Daejeon 34182, Korea





*

Author to whom correspondence should be addressed.



Academic Editor: Derek J. McPhee

Abstract Resveratrol 1, a naturally occurring stilbene compound, has been suggested as a potential whitening agent with strong inhibitory activity on melanin synthesis. However, the use of resveratrol in cosmetics has been limited due to its chemical instability and poor bioavailability. Therefore, resveratrol derivatives were prepared to improve bioavailability and anti-melanogenesis activity. Nine resveratrol derivatives including five alkyl ether derivatives with C2H5, C4H9, C5H11, C6H13, and C8H17 2a–2e and four ester derivatives with CH3, CH=CCH32, CHC2H5C4H9, C7H15 3a–3d were newly synthesized and their effect on melanin synthesis were assessed. All the synthetic derivatives efficiently reduced the melanin content in α-MSH stimulated B16F10 melanoma cells. Further investigation showed that the inhibitory effect of 2a on melanin synthesis was achieved not by the inhibition of tyrosinase activity but by the inhibition of melanogenic enzyme expressions such as tyrosinase and tyrosinase-related protein TRP-1. Our synthetic resveratrol derivatives have more lipophilic properties than resveratrol by the addition of alkyl or acyl chains to free hydroxyl moiety of resveratrol; thus, they are expected to show better bioavailability in skin application. Therefore, we suggest that our synthetic resveratrol derivatives might be promising candidates for better practical application to skin-whitening cosmetics. View Full-Text

Keywords: melanin; resveratrol derivatives; tyrosinase; tyrosinase-related protein TRP-1 melanin; resveratrol derivatives; tyrosinase; tyrosinase-related protein TRP-1





Author: Qing Liu 1, CheongTaek Kim 2, Yang Hee Jo 1, Seon Beom Kim 1, Bang Yeon Hwang 1 and Mi Kyeong Lee 1,*

Source: http://mdpi.com/



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