Some flame retardants and the antimicrobials triclosan and triclocarban enhance the androgenic activity in vitro
Some flame retardants and the antimicrobials triclosan and triclocarban enhance the androgenic activity in vitro
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DOI：
10.1016/j.chemosphere.2010.09.031
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发表时间：
2010-11-01
期刊：
影响因子：
8.8
通讯作者：
Fent, Karl
中科院分区：
文献类型：
--
作者：
Christen, Verena;Crettaz, Pierre;Fent, Karl
在我们的研究中，我们分析了阻燃剂四溴双酚A（TBBPA）、六溴环癸烷（HBCD）、五溴二苯醚（BDE-100）和六溴二苯醚（BDE-155）、抗菌化合物三氯生（TCS）和三氯卡班（TCC）。和八种邻苯二甲酸酯在体外MDA-kb 2细胞系中的雄激素和抗雄激素活性，所有测试化合物均未观察到雄激素活性或仅观察到弱雄激素活性，TBBPA显示出弱抗雄激素活性，这是首次得到证实。155增强了雄激素受体反应基因表达的双氢睾酮依赖性激活，但表现出很少或没有激动活性，增强达到150%，这与抗菌剂相似（TCS高达180%，TCC高达130%）这种雄激素活性的增强代表了阻燃剂内分泌活性的一种新的作用模式，相反，大多数邻苯二甲酸酯显示出抗雄激素活性。邻苯二甲酸丁基苄酯（BBP）、邻苯二甲酸二丁酯（DBP）和邻苯二甲酸二乙酯（DEP）显示出较强的抗雄激素活性，而邻苯二甲酸二乙基己酯（DEHP）、邻苯二甲酸二戊酯（DPP）、邻苯二甲酸二甲酯（DBP）和DEHP代谢物邻苯二甲酸单乙基己酯（MEHP）的作用较低。100和BDE 155代表阻燃剂激素活性的新机制（C）2010 Elsevier Ltd版权所有
Contaminants including flame retardants antimicrobial agents and phthalates occurring as residues in human tissues were associated with altered endocrine function In our study we analysed the flame retardants tetrabromobisphenol A (TBBPA) hexabromocyclodecane (HBCD) penta-bromodiphenylether (BDE-100) and hexa-BDE (BDE-155) the antimicrobial compounds triclosan (TCS) and triclocarban (TCC) and eight phthalates for their androgenic and antiandrogenic activity in vitro in the MDA-kb2 cell line No or only weak androgenic activity was observed for all the tested compounds TBBPA showed weak antiandrogenic activity which was demonstrated for the first time The flame retardants HBCD BDE 100 and BDE-155 enhanced the dihydrotestosterone dependent activation of androgen receptor-responsive gene expression but exhibited little or no agonistic activity The enhancement reached 150% which was similar to the antimicrobials (TCS up to 180% and TCC up to 130%) This enhancement of androgenic activity represents a novel mode of action of the endocrine activity of flame retardants In contrast most phthalates showed antiandrogenic activity Butylbenzyl phthalate (BBP) dibutyl phthalate (DBP) and diethyl phthalate (DEP) showed strong antiandrogenicity whereas the action of diethylhexyl phthalate (DEHP) dipentyl phthalate (DPP) dimethyl phthalate (DMP) and the DEHP metabolite monoethylhexyl phthalate (MEHP) was lower Our in vitro study demonstrates for the first time a weak antiandrogenic activity of TBBPA and a significant enhancement of the androgenic activity of HBCD BDE-100 and BDE 155 which represents a novel mechanism of hormonal activity of flame retardants (C) 2010 Elsevier Ltd All rights reserved