On the inhibitory action of mersalyl on microsomal drug oxidation: a rigid organization of the electron transport chain.
On the inhibitory action of mersalyl on microsomal drug oxidation: a rigid organization of the electron transport chain.
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关于 mersalyl 对微粒体药物氧化的抑制作用：电子传递链的刚性组织。
DOI：
10.1016/0003-9861(71)90213-x
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发表时间：
1971
影响因子：
3.9
通讯作者：
R. Estabrook
中科院分区：
文献类型：
--
作者：
M. Franklin;R. Estabrook
在大鼠肝微粒体中，有机汞汞（汞磺酰）在浓度约为25 mμ mol/mg微粒体蛋白时，对TPNH-细胞色素还原酶活性、TPNH-细胞色素P-450还原酶活性和乙基吗啡N-去甲基化作用的抑制率为50%。TheKi（mersalyl）被证明是独立的整体羟基化活性是否增强通过添加DPNH，或增加离子强度;或抑制一氧化碳。浓度为25 mμ mol/mg蛋白质的Mersalyl不会引起细胞色素P-450向P-420的广泛转化。抑制模式的研究表明，一个刚性的电子传输系统连接一个单一的TPNH-细胞色素还原酶的分子，细胞色素P-450的多组分复合物内所载的一些分子，还原当量只能在一个单一的酶复合物与不同的复合物的组分之间没有明显的电子转移相互作用转移。
The organic mercurial, mersalyl, causes a 50% inhibition of TPNH-cytochromecreductase activity, TPNH-cytochrome P-450 reductase activity, and ethylmorphineN-demethylation in rat liver microsomes at concentrations of about 25 mμmoles/mg microsomal protein. TheKi(mersalyl) proved to be independent of whether the overall hydroxylation activity was enhanced by the addition of DPNH, or an increased ionic strength; or was inhibited by carbon monoxide. Mersalyl, at a concentration of 25 mμmoles/mg protein, caused no extensive conversion of cytochrome P-450 to P-420. Studies on the pattern of inhibition suggest a rigid electron-transport system linking a single molecule of TPNH-cytochromecreductase to a number of molecules of cytochrome P-450 contained within a multicomponent complex and that reducing equivalents can be transferred only within a single enzyme complex with no demonstrable electron transfer interactions between the components of different complexes.