NIQUA, Federal University of Juiz de Fora, Juiz de Fora, Minas Gerais 36036-900, Brazil.
Molecules. 2012 Oct 9;17(10):11816-25. doi: 10.3390/molecules171011816.
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 (IC(50) = 28.66 µg/mL), two times more active than resveratrol (IC(50) = 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.
皮肤色素沉着障碍通常涉及黑色素的过度产生或不均匀分布，导致皮肤出现斑点。白藜芦醇可以抑制酪氨酸酶，这是黑色素合成的活性酶，但它不会抑制黑色素的合成，使其无法单独用作药物制剂中的美白剂，因此建议将其用作治疗色素沉着过度的辅助剂。六种白藜芦醇类似物在体外进行了酪氨酸酶抑制活性测试。在所测试的类似物中，化合物 D 是最有效的酪氨酸酶抑制剂（IC（50）= 28.66 µg/mL），比白藜芦醇（IC（50）= 57.05 µg/mL）活性高两倍，其次是类似物 A、E、B、F 和 C。这表明苯环上 C4' 的羟基化是对观察到的活性最重要的分子修饰。
