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首页> 外文期刊>Comparative biochemistry and physiology, Part C. Pharmacology, toxicology and endocrinology: An international journal >Effect of three structurally related antimalarial drugs on liver microsomal components and lipid peroxidation in rats
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Effect of three structurally related antimalarial drugs on liver microsomal components and lipid peroxidation in rats

机译:三种结构相关的抗疟药对大鼠肝微粒体成分和脂质过氧化的影响

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摘要

Changes in microsomal drug oxidizing enzymes, microsomal lipids, hepatic glutathione (GSH), glutathione S-transferase (GST) and malondialdehyde (MDA) formation following administration of rats with therapeutic doses of three structurally related antimalarial drugs, amodiaquine (AQ). mefloquine (MQ) and halofantrine (HF) were investigated. There was a significant decrease in the activities of aniline hydroxylase, p-nitroanisole O-demethylase and pentoxyresorufin O-dealkylase in AQ, MQ and HF treated rats. AQ elicited the greatest effect with 50, 37 and 67% reductions in the activities of aniline hydroxylase, p-nitroanisole O-demethylase and pentoxyresorufin O-dealkylase, respectively. All the drugs prolonged hexobarbital-sleeping time to varying extents. The three drugs increased significantly the cholesterol pet phospholipid ratio. AQ, MQ and HF decreased significantly the GSH level, GST activity and increased the formation of MDR. The results indicate that the alterations in hepatic microsomal components and lipid peroxidation caused by the antimalarials are related to the structural differences in the compounds. (C) 2000 Elsevier Science Inc. All rights reserved. [References: 34]
机译:给大鼠施用治疗剂量的三种结构相关抗疟药物阿莫地喹(AQ)后,微粒体药物氧化酶,微粒体脂质,肝谷胱甘肽(GSH),谷胱甘肽S-转移酶(GST)和丙二醛(MDA)形成的变化。研究了甲氟喹(MQ)和氟丁胺(HF)。在AQ,MQ和HF处理的大鼠中,苯胺羟化酶,对硝基苯甲醚O-脱甲基酶和戊氧基试卤灵O-脱烷基酶的活性显着降低。 AQ引起的最大影响是苯胺羟化酶,对硝基苯甲醚O-脱甲基酶和戊氧基试卤灵O-脱烷基酶活性分别降低50%,37%和67%。所有的药物都不同程度地延长了己烯巴比妥的睡眠时间。这三种药物显着增加了胆固醇宠物磷脂的比例。 AQ,MQ和HF显着降低了GSH水平,GST活性并增加了MDR的形成。结果表明,抗疟疾药物引起的肝微粒体组分的改变和脂质过氧化与化合物的结构差异有关。 (C)2000 Elsevier Science Inc.保留所有权利。 [参考:34]

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