Inhibitory Effects of Resveratrol Analogs on Mushroom Tyrosinase Activity

Molecules

Danielle Cristina Zimmermann Franco¹  Gustavo Senra Gon๺lves de Carvalho²  Paula Rafaela Rocha¹  Raquel da Silva Teixeira¹  Adilson David da Silva² 

[1] NIQUA, Federal University of Juiz de Fora, Juiz de Fora, Minas Gerais 36036-900, Brazil;Department of Chemistry, I.C.E., Federal University of Juiz de Fora, Campus Universitário, Juiz de Fora, Minas Gerais 36036-900, Brazil;

关键词: chemical synthesis;    mushroom tyrosinase activity;    structure-activity;    tyrosinase;    activity in vitro;   

DOI  :  10.3390/molecules171011816

来源: mdpi

【 摘 要 】

Skin pigmentation disorders typically involve an overproduction or uneven distribution of melanin, which results in skin spots. Resveratrol can inhibit tyrosinase, the active enzyme in the synthesis of melanin, but it does not inhibit the synthesis of melanin to an extent that enables its use alone as a skin whitening agent in pharmaceutical formulations, so its use as a coadjuvant in treatment of hyperpigmentation is suggested. Six resveratrol analogs were tested for tyrosinase inhibitory activity in vitro. Among the analogs tested, compound D was the most powerful tyrosinase inhibitor (IC₅₀ = 28.66 µg/mL), two times more active than resveratrol (IC₅₀ = 57.05 µg/mL), followed by the analogs A, E, B, F and C, respectively. This demonstrated that the hydroxylation at C4' on the phenolic ring was the molecular modification with most importance for the observed activity.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.