title: Pyrethroid and their metabolite, 3-phenoxybenzoic acid showed similar (anti)estrogenic activity in human and rat estrogen receptor α-mediated reporter gene assays.
abstract: Pyrethroids are commonly used as pesticides which are suspected as endocrine disruptors in many studies; however, still we do not know their effects on different species. To compare their effects on human estrogen receptor (hERα) and rat estrogen receptor (rERα), we developed a hERα and rERα mediated luciferase reporter assay to investigate the (anti)estrogenic activities of three frequently used pyrethroids (fenvalerate, cypermethrin, permethrin) and their metabolite 3-phenoxybenzoic acid (3-PBA). All three pyrethroids significantly induced expression of the luciferase, while none of them were antagonistic to 1 nM E₂ mediated induction. Interestingly, 3-PBA, showed antagonist activity by decreasing the effect of 1 nM E₂ to 55.12% in hERα assay and to 45.12% in rERα assay. Our results firstly demonstrated that pyrethroids and 3-PBA showed similar response in the hERα and rERα mediated reporter gene assay, which indicated that data derived from reporter gene assay or other receptor mediated assay systems with rat ER system might be used to predict to estrogenic or anti-estrogenic effects to human systems.
authors.affiliation: Jiangsu Provincial Centre for Disease Prevention and Control, Nanjing 210009, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Sun
authors.affiliation: Nanjing Medical University, Nanjing 210029, China.
authors.forename: Wen
authors.initials: W
authors.lastname: Chen
authors.affiliation: Nanjing Municipal Center for Disease Prevention and Control, Nanjing 210009, China.
authors.forename: Xiaolin
authors.initials: X
authors.lastname: Xu
authors.affiliation: Jiangsu Provincial Centre for Disease Prevention and Control, Nanjing 210009, China.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Ding
authors.affiliation: Jiangsu Provincial Centre for Disease Prevention and Control, Nanjing 210009, China; Nanjing Medical University, Nanjing 210029, China. Electronic address: jscxd@126.com.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Chen
authors.affiliation: Nanjing Medical University, Nanjing 210029, China.
authors.forename: Xinru
authors.initials: X
authors.lastname: Wang
mesh_terms: D000818:Animals; D001565:Benzoates / Q000494:pharmacology*; D002460:Cell Line; D002522:Chlorocebus aethiops; D020847:Estrogen Receptor Modulators / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000235:genetics*; D004967:Estrogens / Q000494:pharmacology*; D017930:Genes, Reporter; D006801:Humans; D008156:Luciferases / Q000378:metabolism; D011722:Pyrethrins / Q000494:pharmacology*; D051381:Rats
chemical_list: D001565:Benzoates; D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D004967:Estrogens; D011722:Pyrethrins; C017618:3-phenoxybenzoic acid; D008156:Luciferases
keywords: Endocrine disruptors; Estrogen; Pesticides