Abstract
Alkylphenols (APs) are widely used as important industrial materials and have attracted lots of attention because of their potential estrogenic activities. In this study, we developed human estrogen receptor α (hERα) and rat estrogen receptor α (rERα) mediated reporter gene assays and compared the estrogenic activity of APs and related chemicals based on the two ERα. Human breast cancer cell line MCF-7 was co-transfected with Gal4-fused hERα and corresponding reporter plasmid; African green monkey kidney cell line CV-1 was co-transfected with rERα and reporter gene. Both assays showed acceptable response to natural estrogen 17β-estradiol (E2) with EC 50 of 0.16 nM and 4.7 nM. Then the estrogenic activity of 4-APs, 4-phenylphenol and bisphenol-A were evaluated and compared with the effects of E2. The data suggested that test APs and related chemicals possessed weakly estrogenic activity and the activity of test APs increased with the increase of substituent size. This structure–activity relationship helped to infer the activity of chemicals with similar feature. Furthermore, test APs showed similar effect on the function of hERα and rERα. This consistency helped to extrapolate in vivo rodent data to human being when performing risk assessment of endocrine disruptors.
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