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2,4,3',5'-四羟基二苯乙烯对线粒体ATP酶的抑制作用。

Inhibition of mitochondrial ATPase by 2,4,3',5'-tetrahydroxystilbene.

作者信息

Janthasoot W, Ratanabanangkoon K, Chudapongse P

出版信息

Chem Biol Interact. 1977 Sep;18(3):355-64. doi: 10.1016/0009-2797(77)90021-7.

Abstract

2,4,3',5'-tetrahydroxystilbene (THS) wa s found to inhibit rat liver mitochondrial adenosine triphosphatase (ATPase) activity induced by various concentrations of 2,4-dinitrophenol (DNP). The I50 was found to be 17 nmoles/mg mitochondrial protein. The maximum inhibitory effects of oligomycin and atractyloside on the DNP-activated mitochondrial ATPase activity can be enhanced by adding THS. The atractyloside-insensitive ATPase activity of Lubrol-treated rat liver mitochondria was also inhibited by low concentration of THS. The tetramethoxyderivative of THS was much less effective than the parent compound in depressing the ATPase activity of both intact and Lubrol-treated mitochondria. These observations suggest that the phenolic groups are essential for the mitochondrial actions of THS, and this compound most probably acts by a mechanism different from oligomycin on the mitochondrial ATPase complex.

摘要

发现2,4,3',5'-四羟基二苯乙烯(THS)可抑制由不同浓度的2,4-二硝基苯酚(DNP)诱导的大鼠肝脏线粒体腺苷三磷酸酶(ATPase)活性。发现其半数抑制浓度(I50)为17纳摩尔/毫克线粒体蛋白。添加THS可增强寡霉素和苍术苷对DNP激活的线粒体ATPase活性的最大抑制作用。低浓度的THS也可抑制经Lubrol处理的大鼠肝脏线粒体对苍术苷不敏感的ATPase活性。THS的四甲氧基衍生物在抑制完整和经Lubrol处理的线粒体的ATPase活性方面比母体化合物的效果要差得多。这些观察结果表明,酚羟基对于THS的线粒体作用至关重要,并且该化合物对线粒体ATPase复合物的作用机制很可能与寡霉素不同。

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