大鼠体内1-¹⁴C-丙烯腈的生物转化及胆汁排泄

In vivo biotransformation and biliary excretion of 1-14C-acrylonitrile in rats.

作者信息

Ghanayem B I, Ahmed A E

出版信息

Arch Toxicol. 1982 Jul;50(2):175-85. doi: 10.1007/BF00373400.

DOI:10.1007/BF00373400

Abstract

1-14C-Acrylonitrile (VCN) was give orally to rats, 27% of the given dose was excreted in bile in 6 h. When 1-14C-VCN was given to overnight fasted or cobaltous chloride treated rats, a significant increase in the biliary excretion occurred. Pretreatment of rats with phenobarbital produced no change, while diethyl maleate pretreatment significantly decreased the portion of the dose excreted in bile in 6 h. Four metabolites of 1-14C-VCN have been isolated from the collected bile, and characterized. The two major biliary metabolites were found to be glutathione (GSH) conjugates of VCN, indicating the importance of GSH in VCN biotransformation.

摘要

将1-¹⁴C-丙烯腈（VCN）经口给予大鼠，给药剂量的27%在6小时内随胆汁排出。当将1-¹⁴C-VCN给予禁食过夜或经氯化钴处理的大鼠时，胆汁排泄显著增加。用苯巴比妥预处理大鼠没有变化，而用马来酸二乙酯预处理则显著降低了6小时内随胆汁排出的剂量比例。已从收集的胆汁中分离并鉴定出1-¹⁴C-VCN的四种代谢产物。发现两种主要的胆汁代谢产物是VCN的谷胱甘肽（GSH）共轭物，表明GSH在VCN生物转化中的重要性。

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