title: Assessing hormone receptor activities of pyrethroid insecticides and their metabolites in reporter gene assays.
abstract: Pyrethroid insecticides, the most commonly used insecticides worldwide, are suspected endocrine-disrupting chemicals. But their interactions with hormone receptors are still unclear. The present study intended to evaluate and compare the hormone receptor (estrogen receptor [ER], androgen receptor [AR], and thyroid hormone receptor [TR]) activities of nine pyrethroids (cycloprothrin, cyfluthrin, cyhalothrin, cypermethrin, deltamethrin, etofenprox, fenvalerate, permethrin, and tetramethrin) and their metabolites (3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropne carboxylic acid [DCCA] and 3-phenoxybenzoic acid [3-PBA]) using receptor-mediated luciferase reporter gene assays. Of the 11 compounds tested, four showed very weak ER agonistic activities and six displayed antiestrogenic effects, among which cyhalothrin and DCCA possessed the most potent estrogenic and antiestrogenic activity respectively. Antagonistic effects to AR were found in 7 compounds, with cyfluthrin and deltamethrin exhibiting stronger AR antagonistic capacity. In the TR assay, all of tested chemicals except DCCA showed antagonistic effects. In this study, we provided evidence that a variety of pyrethroids and their metabolites might disrupt the function of multiple nuclear hormone receptors and thus have the potentials to affect the endocrine and the reproductive systems in humans.
authors.affiliation: Key Laboratory of Reproductive Medicine, Institute of Toxicology, Nanjing Medical University, Nanjing, China.
authors.forename: Guizhen
authors.initials: G
authors.lastname: Du
authors.forename: Ouxi
authors.initials: O
authors.lastname: Shen
authors.forename: Hong
authors.initials: H
authors.lastname: Sun
authors.forename: Juan
authors.initials: J
authors.lastname: Fei
authors.forename: Chuncheng
authors.initials: C
authors.lastname: Lu
authors.forename: Ling
authors.initials: L
authors.lastname: Song
authors.forename: Yankai
authors.initials: Y
authors.lastname: Xia
authors.forename: Shoulin
authors.initials: S
authors.lastname: Wang
authors.forename: Xinru
authors.initials: X
authors.lastname: Wang
mesh_terms: D000818:Animals; D002460:Cell Line; D052244:Endocrine Disruptors / Q000633:toxicity*; D017930:Genes, Reporter; D006728:Hormones / Q000378:metabolism*; D007306:Insecticides / Q000633:toxicity*; D011722:Pyrethrins / Q000633:toxicity*; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D014982:Xenopus laevis
chemical_list: D052244:Endocrine Disruptors; D006728:Hormones; D007306:Insecticides; D011722:Pyrethrins; D011956:Receptors, Cell Surface