炔脂肪酸对哺乳动物肝脏谷胱甘肽S-转移酶的抑制作用。

Inhibition of mammalian hepatic glutathione S-transferases by acetylenic fatty acids.

作者信息

Datta K, Kulkarni A P

机构信息

Florida Toxicology Research Center, College of Public Health, University of South Florida, Tampa 33612.

出版信息

Toxicol Lett. 1994 Aug;73(2):157-65. doi: 10.1016/0378-4274(94)90105-8.

DOI:10.1016/0378-4274(94)90105-8

PMID:8048084

Abstract

Micromolar concentrations of 2 classical inhibitors of lipoxygenase, 5,8,11-eicosatriynoic acid (ETI) and 5,8,11,14-eicosatetraynoic acid (ETYA), were found to cause a significant inhibition of the mixture of isozymes of affinity purified rat and human liver glutathione S-transferase (GST) with activity towards 1-chloro-2,4-dinitrobenzene (CDNB). ETI was a more potent inhibitor of both rat and human liver GST than ETYA. Analysis of kinetic data suggested noncompetitive inhibition of human liver GST by ETI towards reduced glutathione and CDNB. ETI also inhibited the hepatic GST activity towards 1,2-dichloro-4-nitrobenzene, p-nitrobenzyl chloride and 4-nitropyridine N-oxide.

摘要

发现微摩尔浓度的两种经典脂氧合酶抑制剂，即5,8,11-二十碳三烯酸（ETI）和5,8,11,14-二十碳四烯酸（ETYA），可显著抑制亲和纯化的大鼠和人肝脏谷胱甘肽S-转移酶（GST）同工酶混合物对1-氯-2,4-二硝基苯（CDNB）的活性。ETI对大鼠和人肝脏GST的抑制作用比ETYA更强。动力学数据分析表明，ETI对人肝脏GST对还原型谷胱甘肽和CDNB的抑制作用为非竞争性抑制。ETI还抑制肝脏GST对1,2-二氯-4-硝基苯、对硝基苄基氯和4-硝基吡啶N-氧化物的活性。