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首页> 外文期刊>Life sciences >Differential effects of flavonoids on testosterone-metabolizing cytochrome P450s.
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Differential effects of flavonoids on testosterone-metabolizing cytochrome P450s.

机译：黄酮类化合物对睾丸激素代谢细胞色素P450的差异作用。

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Flavonoids are widely distributed phytochemicals, whose modulation of cytochrome P450 mediated carcinogen metabolism is well established. Less well studied is their effect on P450 dependent metabolism of endogenous substrates. To address this question we evaluated a series of twelve flavonoids and hematoxylin for their effect on P450-mediated steroid hydroxylation by rat liver microsomes. Site-specific 7alpha-, 6beta- and 2alpha-hydroxylation of testosterone by P450s 2A1, 3A2 and 2C11, respectively, was measured. Highly selective patterns of inhibition or activation of these P450s were observed. 3,6-dichloro-2'-isopropyloxy-4'-methylflavone was the most potent inhibitor of P450 2C11 while cyanidin chloride most potently inhibited P450s 2A1 and 3A2. The flavonoid analogue hematoxylin was unique in that it activated 2C11 (by 2.5 fold) yet inhibited both 2A1 and 3A2 (by 60%). These results indicate that consumption of dietary flavonoids may likewise alter the metabolite profile of steroids and other physiological P450 substrates.
机译：黄酮类化合物是分布广泛的植物化学物质，其对细胞色素P450介导的致癌物代谢的调节已得到很好的确立。研究较少的是它们对内源性底物的P450依赖性代谢的影响。为了解决这个问题，我们评估了一系列十二种类黄酮和苏木精对大鼠肝微粒体对P450介导的甾体羟基化的影响。测量了分别由P450 2A1、3A2和2C11引起的睾丸激素的位点特异性7α-，6β-和2α-羟基化。观察到抑制或激活这些P450的高度选择性模式。 3,6-二氯-2'-异丙氧基-4'-甲基黄酮是P450 2C11的最强抑制剂，而花青素氯化物最有效地抑制P450 2A1和3A2。类黄酮类似物苏木精的独特之处在于它激活2C11（2.5倍），但同时抑制2A1和3A2（60％）。这些结果表明，食用类黄酮可能同样会改变类固醇和其他生理性P450底物的代谢特性。

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