Effects of methoxychlor and its metabolite 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane on 11β-hydroxysteroid dehydrogenase activities in vitro

被引：16

作者：

Guo, Jingjing ^{[1
]}

Deng, Haiyun ^{[1
]}

Li, Hongzhi ^{[2
]}

Zhu, Qiqi ^{[1
]}

Zhao, Binghai ^{[2
]}

Chen, Bingbing ^{[3
]}

Chu, Yanhui ^{[2
]}

Ge, Ren-Shan ^{[1
]}

机构：

[1] Wenzhou Med Coll, Affiliated Hosp 2, Wenzhou 325000, Zhejiang, Peoples R China

[2] Mudanjiang Med Univ, Heilongjiang Key Lab Antifibrosis Biotherapy, Mudanjiang, Heilongjiang, Peoples R China

[3] Wenzhou Med Coll, Sch Pharm, Dept Pharmacol, Wenzhou 325000, Zhejiang, Peoples R China

来源：

TOXICOLOGY LETTERS | 2013年 / 218卷 / 01期

关键词：

Methoxychlor; HPTE; Enzyme inhibition; 11 beta-hydroxysteroid dehydrogenase; Glucocorticoid metabolism; RAT LEYDIG-CELLS; BETA-HYDROXYSTEROID DEHYDROGENASE; APPARENT MINERALOCORTICOID EXCESS; VISIBLE BURROW SYSTEM; CORTICOSTEROID; 11-BETA-DEHYDROGENASE; TESTOSTERONE SYNTHESIS; CLONING; ENZYME; MOUSE; RECEPTOR;

D O I：

10.1016/j.toxlet.2013.01.002

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

Methoxychlor (MXC) is primarily used as a pesticide and widely present in the environment. The objective of the present study is to investigate the direct effects of MXC and its metabolite 2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) on two isoforms of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1 and 11 beta-HSD2) in vitro. Human liver microsome, rat testis microsome and adult Leydig cells were used for the measurement of 11 beta-HSD1 activity. Human placental and rat kidney microsomes were used for 11 beta-HSD2 activity. The IC50 values on human 11 beta-HSD1 by MXC and HPTE were 1.91 +/- 0.07 and 8.88 +/- 0.08 mu M, respectively. HPTE inhibited rat 11 beta-HSD1 with IC50 of 9.15 +/- 0.05 mu M, while MXC did not inhibit the enzyme. MXC and HPTE were competitive inhibitors of 11 beta-HSD1. HPTE also inhibited human and rat 11 beta-HSD2 with IC50 values of 55.57 +/- 0.08 and 12.96 +/- 0.11 mu M, respectively, while MXC did not inhibit 11 beta-HSD2. In summary, our results showed that MXC and its metabolite HPTE inhibited both isoforms of 11 beta-HSD in a species-and chemical structure-dependent manner. (C) 2013 Elsevier Ireland Ltd. All rights reserved.

引用

页码：18 / 23

页数：6

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