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首页> 外文期刊>Life sciences >Resveratrol, a red wine constituent, is a mechanism-based inactivator of cytochrome P450 3A4.
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Resveratrol, a red wine constituent, is a mechanism-based inactivator of cytochrome P450 3A4.

机译：白藜芦醇是一种红酒成分，是一种基于机理的细胞色素P450 3A4灭活剂。

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摘要

Resveratrol, a phytoalexin found in red wine, has been shown to possess antioxidant and antimutagenic properties. Incubation of resveratrol with Sf9 insect microsomes containing baculovirus-derived human cytochrome P450 3A4 (CYP3A4) and NADPH-cytochrome P450 reductase showed that resveratrol inactivated CYP3A4 in a time- and NADPH-dependent manner. Resveratrol, erythromycin and troleandomycin inactivated CYP3A4 at a similar rate (as reflected by k(inact)) whereas the binding affinity to CYP3A4 (as reflected by K(I)) was in the order of: troleandomycin > erythromycin > resveratrol. (K(I) and k(inact) for CYP3A4 inactivation by resveratrol, erythromycin and troleandomycin are 20 microM and 0.20 min(-1), 5.3 microM and 0.12 min(-1) and 0.18 microM and 0.15 min(-1), respectively.) Fractionation studies of red wine showed that fractions that did not contain resveratrol inactivated CYP3A4 significantly. In addition, the resveratrol content in red wine used in the study was too low to account for the degree of CYP3A4 inactivation observed after red wine treatment. Inactivation studies using a variety of red wine types showed that the CYP3A4 inactivation did not correlate to their resveratrol content. In summary, data here showed that resveratrol is an effective mechanism-based inactivator of CYP3A4; however, it is not one of the main red wine constituents that are responsible for CYP3A4 inactivation by red wine. Nevertheless, inactivation of CYP3A4 by resveratrol may cause clinically relevant drug interactions with CYP3A4 substrates.
机译：白藜芦醇，一种在红酒中发现的植物抗毒素，已被证明具有抗氧化和抗诱变特性。将白藜芦醇与含有杆状病毒衍生的人细胞色素P450 3A4（CYP3A4）和NADPH-细胞色素P450还原酶的Sf9昆虫微粒体一起温育，表明白藜芦醇以时间和NADPH依赖性方式灭活CYP3A4。白藜芦醇，红霉素和troleandomycin以相似的速率使CYP3A4失活（如k（inact）所示），而与CYP3A4的结合亲和力（如K（I）所示）则依次为troleandomycin> erythromycin>白藜芦醇。 （K（I）和k（inact）用于白藜芦醇，红霉素和曲安霉素的CYP3A4灭活分别为20 microM和0.20 min（-1），5.3 microM和0.12 min（-1）和0.18 microM和0.15 min（-1），红酒的分馏研究表明，不含白藜芦醇的馏分会显着灭活CYP3A4。此外，研究中使用的红酒中白藜芦醇含量过低，无法解释红酒处理后CYP3A4失活的程度。使用各种红酒进行的灭活研究表明，CYP3A4的灭活与其白藜芦醇含量无关。总之，这里的数据显示白藜芦醇是一种有效的基于机制的CYP3A4灭活剂;然而，它不是导致红酒中CYP3A4失活的主要红酒成分之一。然而，白藜芦醇对CYP3A4的灭活可能引起与CYP3A4底物的临床相关药物相互作用。

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