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与氯贝丁酯相关或不相关的降血脂药物对大鼠肝脏谷胱甘肽S-转移酶活性的抑制作用。

Inhibition of liver glutathione S-transferase activity in rats by hypolipidemic drugs related or unrelated to clofibrate.

作者信息

Foliot A, Touchard D, Mallet L

出版信息

Biochem Pharmacol. 1986 May 15;35(10):1685-90. doi: 10.1016/0006-2952(86)90324-2.

DOI:10.1016/0006-2952(86)90324-2
PMID:3707598
Abstract

The effects of in vivo administration of six hypolipidemic drugs on rat liver glutathione S-transferase activity were compared. This activity was measured with sulfobromophthalein (BSP), 1,2-dichloro-4-nitrobenzene (DCNB) or 1-chloro-2,4-dinitrobenzene (CDNB) as substrate. Except for the nicotinic acid derivative ethanolamine oxiniacate, all the compounds tested significantly reduced it, whether or not they were related to clofibrate. The hepatic glutathione concentration either remained unchanged or only increased slightly after treatment with the various drugs. When measured, the maximal excretion rate of bile BSP dropped significantly, but not that of phenol-3,6-dibromophthalein (DBSP). Hepatic dye uptake and storage were not impaired. These results show that hypolipidemic drugs of the peroxisome proliferator type inhibit rat liver glutathione S-transferase activity and may reduce transport of anions conjugated with glutathione before excretion.

摘要

比较了六种降血脂药物体内给药对大鼠肝脏谷胱甘肽S-转移酶活性的影响。以磺溴酞钠(BSP)、1,2-二氯-4-硝基苯(DCNB)或1-氯-2,4-二硝基苯(CDNB)为底物测定该活性。除烟酸衍生物奥昔烟酸乙醇胺外,所有受试化合物均显著降低了该活性,无论它们是否与氯贝丁酯有关。用各种药物治疗后,肝脏谷胱甘肽浓度要么保持不变,要么仅略有增加。测量时,胆汁BSP的最大排泄率显著下降,但酚-3,6-二溴酞钠(DBSP)的排泄率未下降。肝脏对染料的摄取和储存未受损害。这些结果表明,过氧化物酶体增殖剂类型的降血脂药物会抑制大鼠肝脏谷胱甘肽S-转移酶活性,并可能在排泄前减少与谷胱甘肽结合的阴离子的转运。

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