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末端烯烃在果蝇微粒体中的命运及其对某些细胞色素P450依赖性活性的抑制作用。

Fate of a terminal olefin with Drosophila microsomes and its inhibitory effects on some P-450 dependent activities.

作者信息

Cuany A, Helvig C, Amichot M, Pflieger P, Mioskowski C, Salaun J P, Pauron D, Larroque C, Berge J B

机构信息

INRA, Laboratoire de Biologie des Invertébrés, Antibes, France.

出版信息

Arch Insect Biochem Physiol. 1995;28(4):325-38. doi: 10.1002/arch.940280403.

Abstract

In vitro bioassays were used to analyze the metabolism of the 11-dodecenoic acid (11-DDNA) by microsomes prepared from Drosophila melanogaster RalDDTR strain. 11-DDNA is metabolized to 11,12-epoxylauric acid (epoxyLA) in a NADPH-dependent way. The microsomal production of epoxyLA reaches a plateau very quickly, suggesting the occurrence of an enzyme inactivation process. After incubation of microsomes with (1-14C)11-DDNA, three proteins of Mr approximately 50 kDa were labeled. 11-DDNA inhibits the microsomal metabolism of lauric acid and 7-ethoxycoumarin in a time and NADPH-dependent process. An inhibition of metabolites generated from DDT and testosterone was also obtained but at higher concentrations. These results are discussed according to the fact that RalDDTR is an insecticide resistant strain characterized as a high metabolizer of the insecticide DDT and also of lauric acid, testosterone, and ethoxycoumarin.

摘要

利用体外生物测定法分析了从黑腹果蝇RalDDTR品系制备的微粒体对11-十二碳烯酸(11-DDNA)的代谢情况。11-DDNA以NADPH依赖的方式代谢为11,12-环氧月桂酸(epoxyLA)。微粒体产生epoxyLA的过程很快达到平稳状态,这表明存在酶失活过程。用(1-14C)11-DDNA孵育微粒体后,标记了三种分子量约为50 kDa的蛋白质。11-DDNA在时间和NADPH依赖的过程中抑制月桂酸和7-乙氧基香豆素的微粒体代谢。在较高浓度下,也观察到对滴滴涕和睾酮产生的代谢物的抑制作用。鉴于RalDDTR是一个抗杀虫剂品系,其特点是对杀虫剂滴滴涕以及月桂酸、睾酮和乙氧基香豆素具有高代谢能力,对这些结果进行了讨论。

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