Pyrethroid and their metabolite, 3-phenoxybenzoic acid showed similar (anti)estrogenic activity in human and rat estrogen receptor α-mediated reporter gene assays

• Pyrethroids possess weaker estrogenic activity.
• The metabolite of pyrethroid possessed antiestrogenic activity.
• Pyrethroid showed similar response on the function of rat and human estrogen receptors in vitro assay.

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.