Estrogenic activities of two synthetic pyrethroids and their metabolites
Estrogenic activities of two synthetic pyrethroids and their metabolites
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两种合成拟除虫菊酯及其代谢物的雌激素活性
DOI：
10.1016/s1001-0742(09)60107-8
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发表时间：
2010-01-01
影响因子：
6.9
通讯作者：
Zhao, Meirong
中科院分区：
文献类型：
--
作者：
Jin, Meiqing;Li, Ling;Zhao, Meirong
拟除虫菊酯是目前最常用的农药之一，迄今为止，已通过各种方法评估了几种拟除虫菊酯的潜在雌激素活性。以往的研究表明，雌激素活性部分来自其代谢产物。虽然有相当多的资料，关于SP的代谢和环境降解，很少有人知道的代谢产物的雌激素活性。本文研究了氯菊酯（PM）、高效氯氰菊酯（CP）及其代谢产物3-苯氧基苯甲醇（PBCOH）、3-苯氧基苯甲醛（PBCHO）和3-苯氧基苯甲酸（PBCOOH）对人乳腺癌MCF-7细胞的雌激素样活性。在MCF-7细胞增殖实验中，PM和CP在10（-7）mol/L时表现出明显的雌激素样活性，与17 β-雌二醇（E-2）在10（-9）mol/L时相当，相对增殖效应比分别为55.4%和56.3%。实时定量聚合酶链反应（qRT-PCR）结果证实了PM和CP的雌激素样活性，在10（-6）mol/L时观察到pS2和ER α mRNA水平的显著变化。对于三种主要代谢产物，PBCOH和PBCOOH在所有试验中均表现出雌激素活性，而与溶剂对照相比，PBCHO未观察到显著的雌激素反应。特别是PBCOH的雌激素活性甚至略强于其母体化合物，表明代谢可能是SPs雌激素活性的原因之一。鉴于五氯苯酚的广泛使用，在对五氯苯酚进行风险评估时应考虑母体化合物及其代谢物的毒理学效应。
Synthetic pyrethroids (SPs) are among the most common pesticides in current use, and so far, several SPs have been assessed for their potential estrogenicities by various methods. Previous studies have shown that the estrogenicities partly come from their metabolites. Although considerable information is available with respect to the metabolism and environmental degradation of SPs, little is known about the estrogenicities of the metabolites. In this study, permethrin (PM) and beta-cypermethrin (CP), as well as their metabolites (3-phenoxybenzoic alcohol (PBCOH), 3-phenoxybenzaldehyde (PBCHO) and 3-phenoxybenzoic acid (PBCOOH) were evaluated for their estrogenic activities in the MCF-7 human breast carcinoma cell line. In the MCF-7 cell proliferation assay, PM and CP exhibited significant estrogenic activities at 10(-7) mol/L, comparable to 17 beta-estradiol (E-2) of 10(-9) mol/L, with the relative proliferative effect ratios of 55.4% and 56.3%, respectively. The real-time quantitative polymerase chain reaction (qRT-PCR) results confirmed the estrogenicities of PM and CP with significant alteration of pS2 and ER alpha mRNA levels observed at 10(-6) mol/L. For the three major metabolites, PBCOH and PBCOOH exhibited estrogenic activities in all assays, while no significant estrogenic responses was observed for PBCHO compared to the vehicle control. In particular, PBCOH had even slightly stronger estrogenic activity than its parent compounds, indicating that metabolism may be one of the reasons for the estrogenicities of the SPs. Given the widespread use of SPs, the toxicological effects of parent compounds and their metabolites should be taken into consideration in the risk assessment of SPs.