Antiandrogenic activity of pyrethroid pesticides and their metabolite in reporter gene assay

作者:Sun Hong; Xu Xiao Lin; Xu Li Chun; Song Ling; Hong Xia; Chen Jian Feng; Cui Lun Biao; Wang Xin Ru*
来源:Chemosphere, 2007, 66(3): 474-479.
DOI:10.1016/j.chemosphere.2006.05.059

摘要

Many pesticides possess hormonal activity and have thus been classified as endocrine disruptors. Pyrethroids are commonly used pesticides worldwide, but little has been done to characterize their antiandrogenic activity potential. We tested three frequently encountered pyrethroids (fenvalerate, cypermethrim, permethrin) and their metabolite 3-phenoxybenzoic acid (3-PBA) for antiandrogenic and androgenic activity using a human androgen receptor (AR) mediated luciferase reporter gene assay in CV-1 African green monkey kidney cell. The assay displayed appropriate response to the known AR agonist 5 alpha-dihydrotestosterone and AR antagonist nilutamide and flutamide. At 0.1 mM, all the three tested pyrethroids significantly suppressed the luciferase expression. Further, their metabolite 3-PBA also showed antagonist activity. None of the test chemicals showed androgenic activity. Through the antiandrogenic pathways, exposure to certain pyrethroids may contribute to the damage of reproductive system. In conclusion, pyrethroid pesticides can act as antiandrogen in vitro, and metabolizing to 3-PBA cannot eliminate the antagonist activity. This result provides useful information for risk assessment of pyrethroid pesticides.