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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Novel Isoflavone Glucosides in Groundnut (Apios americana Medik) and Their Antiandrogenic Activities
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Novel Isoflavone Glucosides in Groundnut (Apios americana Medik) and Their Antiandrogenic Activities

机译:花生中的新型异黄酮葡糖苷及其抗雄激素活性

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摘要

Isoflavone glucosides (2'-hydroxy,5-methoxy genistein-7-O-glucoside (1), 2'-hydroxy genistein-7-O-gentibioside (2), 5-methbxy genistein-7-O-glucoside (3), 3',S-dimethoxy genistein-7-O-glucoside (4), 2'-hydroxy genistein-7-O-glucoside (5), genistein-7-O-gentibioside (6), 2'-hydroxy,5-methoxy genistein-4',7-O-diglucoside (7), and 2'-hydroxy genistein-4',7-O-diglucoside (8)) were isolated from the groundnut of Apios americana Medik. Their structures were elucidated on the basis of HR-ESI-MS and 1D- and 2D-NMR analyses. Compounds 1, 2,4, and 7 are new compounds presented here for the first time. Compounds 2 and 5 were proven to be androgen receptor antagonists due to their binding activities for androgen receptors (IC_(50) 280 and 160 μM, respectively) and the inhibitory activity of androgen-induced expression of prostate-specific antigen (PSA) mRNA in LNCaP (prostate adenocarcinoma) cells (IC_(50) 20 and 18 //M, respectively).
机译:异黄酮葡萄糖苷(2'-羟基,5-甲氧基染料木黄酮7-O-葡糖苷(1),2'-羟基染料木黄酮-7-O-龙胆二糖苷(2),5-甲基丁香木酮7-O-葡糖苷(3) ,3',S-二甲氧基染料木素-7-O-葡糖苷(4),2'-羟基染料木素-7-O-葡糖苷(5),染料木素-7-O-龙胆苷(6),2'-羟基,5从美洲蜜蜂的花生中分离了-甲氧基染料木黄酮-4',7-O-二葡糖苷(7)和2'-羟基染料木黄酮4',7-O-二葡糖苷(8)。根据HR-ESI-MS以及1D-和2D-NMR分析阐明了它们的结构。化合物1、2、4和7是首次在此展示的新化合物。由于化合物2和5对雄激素受体的结合活性(分别为IC_(50)280和160μM)和雄激素诱导的前列腺特异性抗原(PSA)mRNA的抑制活性,因此它们被证明是雄激素受体拮抗剂。 LNCaP(前列腺腺癌)细胞(分别为IC_(50)20和18 // M)。

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