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大鼠短期间歇性接触松节油对肝脏药物生物转化的增强作用。

Enhancement of hepatic drug biotransformation by a short-term intermittent turpentine exposure in the rat.

作者信息

Järvisalo J, Vainio H

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 Jan;46(1):32-36. doi: 10.1111/j.1600-0773.1980.tb02415.x.

Abstract

An inhalation exposure of male rats to 300 p.p.m. of a commercial turpentine 6 hrs daily 5 days a week for 8 weeks enhanced the activities of drug biotransformation enzymes of liver microsomes considerably. The activities of NADPH cytochrome c reductase and 7-ethoxycoumarin deethylase, and microsomal content of cytochrome P-450 were increased 35-60% during the first weeks of the experiment, but had a tendency to return towards the control values later on. A similar enhancement of activities was also found in liver microsomal epoxide hydratase and UDP glucuronosyltransferase, but these enzyme activities tended to adapt less during the experiment. The turpentine treatment increased the affinity of liver microsomal cytochrome P-450 to alpha-pinene (the main component of the turpentine). The present data suggests that exposure to turpentine is able to modify considerably the biotransformation of drugs.

摘要

雄性大鼠每周5天、每天6小时吸入浓度为300 ppm的商用松节油,持续8周,这大大增强了肝脏微粒体药物生物转化酶的活性。在实验的最初几周,NADPH细胞色素c还原酶和7-乙氧基香豆素脱乙基酶的活性以及细胞色素P-450的微粒体含量增加了35%-60%,但之后有恢复到对照值的趋势。在肝脏微粒体环氧化物水合酶和UDP葡萄糖醛酸基转移酶中也发现了类似的活性增强,但这些酶活性在实验过程中的适应性较差。松节油处理增加了肝脏微粒体细胞色素P-450对α-蒎烯(松节油的主要成分)的亲和力。目前的数据表明,接触松节油能够显著改变药物的生物转化。

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