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Taurine modulates catalytic activity of cytochrome P450 3A4

机译:牛磺酸调节细胞色素P450 3A4的催化活性

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摘要

The influence of the biologically active compound taurine on the stability and catalytic properties of the hemoprotein cytochrome P450 3A4 has been investigated. The catalytic properties were analyzed by electrochemical methods (cyclic and square-wave voltammetry) using cytochrome P450 3A4 immobilized on the electrode. Taurine at concentrations in the range 10-70 mu M stimulated the electrochemical reduction of cytochrome P450 3A4, and the reduction was the highest (115 +/- 3%) in the presence of 50 mu M taurine. Taurine pronouncedly attenuated the itraconazol-caused inhibition of the P450 isoenzyme P450 3A4. Taurine protected cytochrome P450 3A4 due to stabilizing it during electrolysis at controlled voltage in the presence of erythromycin as a substrate. This protection was manifested by an increase in the amount of the "residual" reduced form of the hemoprotein (52 +/- 5 and 71 +/- 8%, respectively).
机译:研究了生物活性化合物牛磺酸对血红蛋白细胞色素P450 3A4的稳定性和催化性能的影响。通过电化学方法(循环和方波伏安法)使用固定在电极上的细胞色素P450 3A4分析催化性能。浓度在10-70μM范围内的牛磺酸刺激了细胞色素P450 3A4的电化学还原,在50μM牛磺酸存在下,还原度最高(115 +/- 3%)。牛磺酸显着减弱了依他康那唑对P450同工酶P450 3A4的抑制作用。牛磺酸可保护细胞色素P450 3A4,这是因为在存在红霉素作为底物的情况下,在受控电压下电解过程中,牛磺酸可稳定该色素。这种保护通过血药的“残留”还原形式的数量增加(分别为52 +/- 5和71 +/- 8%)来体现。

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