Anti-melanogenic effect of (Z)-5-(2,4-dihydroxybenzylidene) thiazolidine-2,4-dione, a novel tyrosinase inhibitor.

摘要: We synthesized (Z)-5-(2,4-dihydroxybenzylidene)thiazolidine-2,4-dione (MHY498) as a potential tyrosinase inhibitor. MHY498 potently inhibited mushroom activity (mean IC50 = 3.55 μM) in dose-dependent manner. was more potent than the well-known inhibitor, kojic acid 22.79 μM). When tested B16F10 melanoma cells treated with α-melanocyte stimulating hormone (α-MSH), murine and decreased melanin production without inducing cytotoxicity. Docking models showed that binding affinity of to higher acid, docking simulation results indicated moieties were similar. Western blotting inhibition by partly resulted from expressional modulations its transcription factor, microphthalmia-associated via cAMP-PKA-CREB pathway. These findings suggest could be useful an antimelanogenic agent for prevention treatment diseases associated skin pigmentation.