Division of Applied Life Science (BK21 Program), IALS, Graduate School of Gyeongsang National University , Jinju 660-701, Republic of Korea.
J Agric Food Chem. 2012 Aug 29;60(34):8372-8. doi: 10.1021/jf3015987. Epub 2012 Aug 16.
Melanogenesis can be controlled by tyrosinase inhibition or by blocking the maturation processes of tyrosinase and its related proteins. Mangostenone F was isolated from the seedcases of Garcinia mangostana . Mangostenone F was shown to be inactive against tyrosinase (IC50 > 200 μM) but was a potent α-glucosidase inhibitor in vitro (IC50 = 21.0 μM). Mangostenone F was found to inhibit production of melanin in the mouse melanoma cell line B16F10. Importantly, unlike most glycosidase inhibitors, mangostenone F displayed very low cytotoxicity (EC50 > 200 μM). The Western blot for expression levels of proteins involved in melanogenesis showed that mangostenone F down-regulated tyrosinase and TRP-2 expression. Treating B16F10 cells with mangostenone F significantly increased the susceptibility of tyrosinase to endoglycosidase H digestion, indicating that tyrosinase was unable to mature fully and pass to the trans-golgi apparatus. Consistent with these data, in lysate assays, mangostenone F was shown to be a better inhibitor of α-glucosidases than deoxynojirimycin, a representative glycosidase inhibitor.
黑色素生成可以通过抑制酪氨酸酶或阻断酪氨酸酶及其相关蛋白的成熟过程来控制。山竹酮 F 是从山竹的种皮中分离出来的。山竹酮 F 对酪氨酸酶没有活性（IC50 > 200 μM），但在体外是一种有效的α-葡萄糖苷酶抑制剂（IC50 = 21.0 μM）。山竹酮 F 被发现能抑制小鼠黑色素瘤细胞系 B16F10 中黑色素的生成。重要的是，与大多数糖苷酶抑制剂不同，山竹酮 F 的细胞毒性非常低（EC50 > 200 μM）。Western blot 分析显示，山竹酮 F 下调了酪氨酸酶和 TRP-2 的表达水平。用山竹酮 F 处理 B16F10 细胞显著增加了内糖苷酶 H 消化酪氨酸酶的敏感性，表明酪氨酸酶不能完全成熟并转运到反式高尔基体。与这些数据一致，在裂解物测定中，山竹酮 F 对α-葡萄糖苷酶的抑制作用优于去氧野尻霉素，后者是一种代表性的糖苷酶抑制剂。
