Estrogenic activities of two synthetic pyrethroids and their metabolites
Meiqing Jin , Ling Li , Chao Xu , Yuezhong Wen , Meirong Zhao
DOI:
Received May 16, 2009,Revised July 06, 2009, Accepted , Available online
Volume 22,2010,Pages 290-296
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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 -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 -estradiol (E2) of 10??9 mol/L, with the relative
proliferative e ect 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 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 e ects of parent compounds and their metabolites should be taken into consideration in the risk assessment of
SPs.
