Inhibition Effects of Mangosenone F from Garcinia mangostana on Melanin Formation in B16F10 Cells

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• 作者：Hyung Won Ryu ; Seong Hun Jeong ; Marcus J. Curtis-Long ; Sunin Jung ; Ji Won Lee ; Hyun Sim Woo ; Jung Keun Cho ; Ki Hun Park
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2012
• 出版时间：August 29, 2012
• 年：2012
• 卷：60
• 期：34
• 页码：8372-8378
• 全文大小：395K
• 年卷期：v.60,no.34(August 29, 2012)
• ISSN：1520-5118

文摘

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 渭M) but was a potent 伪-glucosidase inhibitor in vitro (IC₅₀ = 21.0 渭M). 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 渭M). 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 伪-glucosidases than deoxynojirimycin, a representative glycosidase inhibitor.

Keywords:

mangostenone F; 伪-glucosidase; endo H; cytotoxicity; melanogenesis