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取代酚的质子载体活性与解偶联活性之间的定量关系。

Quantitative relationship between protonophoric and uncoupling activities of substituted phenols.

作者信息

Miyoshi H, Nishioka T, Fujita T

出版信息

Biochim Biophys Acta. 1987 Apr 15;891(2):194-204. doi: 10.1016/0005-2728(87)90011-9.

DOI:10.1016/0005-2728(87)90011-9
PMID:3828329
Abstract

The protonophoric activity through liposomal membranes was measured and compared with the uncoupling activity with the oxidative phosphorylation of rat-liver mitochondria for 19 substituted phenols. Quantitative analyses of the protonophoric activity of the phenols in terms of physicochemical molecular parameters showed that the activity was mostly decided by two factors: the partition coefficient between the liposome and aqueous buffer phases and the acid dissociation constant. Correlation was excellent between protonophoric and uncoupling activities when the difference in the effect of acidity of phenols between liposomal and mitochondrial membranes was taken into account. The results were further evidence for the shuttle-type of mechanism of weakly acidic uncouplers based on the Mitchell chemiosmotic hypothesis.

摘要

测定了19种取代酚通过脂质体膜的质子载体活性,并将其与对大鼠肝脏线粒体氧化磷酸化的解偶联活性进行了比较。根据物理化学分子参数对酚类的质子载体活性进行定量分析表明,该活性主要由两个因素决定:脂质体与水性缓冲液相之间的分配系数和酸解离常数。当考虑到酚类在脂质体膜和线粒体膜之间酸度效应的差异时,质子载体活性和解偶联活性之间的相关性非常好。这些结果进一步证明了基于米切尔化学渗透假说的弱酸性解偶联剂的穿梭型机制。

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