Assessing Hormone Receptor Activities of Pyrethroid Insecticides and Their Metabolites in Reporter Gene Assays

• DOI: 10.1093/toxsci/kfq120
• Publication Date: 2010-04-22T00:56:00Z
• Authors: Guizhen Du; Ouxi Shen; Hong Sun; Juan Fei; Chuncheng Lu; Ling Song; Yankai Xia; Shoulin Wang; Xinru Wang
• Keywords: Insecticides; Receptors, Cell Surface; Endocrine Disruptors; 01 natural sciences; Hormones; Cell Line; 3. Good health; Xenopus laevis; Genes, Reporter; Pyrethrins; Animals; 0105 earth and related environmental sciences

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.