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有机氯农药作为睾酮和苯并[a]芘羟化酶诱导剂的作用。

The effects of organochlorine pesticides as inducers of testosterone and benzo[a]pyrene hydroxylases.

作者信息

Haake J, Kelley M, Keys B, Safe S

出版信息

Gen Pharmacol. 1987;18(2):165-9. doi: 10.1016/0306-3623(87)90244-8.

DOI:10.1016/0306-3623(87)90244-8
PMID:3569844
Abstract

p,p'-DDE, phenobarbital, dieldrin heptachlor, chlordane and toxaphene induced rat liver microsomes exhibited increased formation of the 4,5-dihydrodiol, 3,6-quinone, 9- and 3-hydroxymetabolites of benzo[a]pyrene and the latter three compounds also induced an increase in the rate of formation of the 9,10-dihydrodiol metabolite. Lindane was inactive as an inducer of benzo[a]pyrene hydroxylase. With the exception of lindane, all the organochlorine pesticides and PB induced testosterone 16 alpha- and 16 beta-hydroxylases; in contrast lindane induced testosterone 6 alpha-, 7 alpha- and 6 beta-hydroxylases and PB also induced testosterone 15 beta-hydroxylase and androstenedione formation. Using a battery of monooxygenase enzyme assays it was evident that there were significant differences between PB and several organochlorine pesticides as inducers of rat hepatic cytochrome P-450-dependent monooxygenases.

摘要

p,p'-滴滴伊、苯巴比妥、狄氏剂、七氯、氯丹和毒杀芬诱导的大鼠肝微粒体表现出苯并[a]芘的4,5-二氢二醇、3,6-醌、9-和3-羟基代谢物形成增加,后三种化合物还诱导9,10-二氢二醇代谢物的形成速率增加。林丹作为苯并[a]芘羟化酶的诱导剂无活性。除林丹外,所有有机氯农药和苯巴比妥均诱导睾酮16α-和16β-羟化酶;相比之下,林丹诱导睾酮6α-、7α-和6β-羟化酶,苯巴比妥还诱导睾酮15β-羟化酶和雄烯二酮形成。使用一系列单加氧酶测定法明显看出,苯巴比妥和几种有机氯农药作为大鼠肝细胞色素P-450依赖性单加氧酶的诱导剂存在显著差异。

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