Characterization of estrogen receptor α activities in polychlorinated biphenyls by in vitro dual-luciferase reporter gene assay

Polychlorinated biphenyls (PCBs) are thought to cause adverse health effects, particularly endocrine disruption. However, results on the estrogenic activities of a large set of PCB congeners through hormone receptors have not been fully studied. In this study, we evaluated the anti/estrogenic effects of 20 PCBs using an in vitro dual-luciferase reporter gene assay. PCB 18, 28, 49, 52, 99, 101, 103, 110, and 128 exhibited estrogenic effects, whereas PCB 118, 138, 163, 170, 180, 187, 194, 199 and 203 behaved as anti-estrogens. In particular, PCB 30 and 44 exhibited both agonistic and antagonistic activities in the dual-luciferase reporter gene assay. The results obtained from the dual-luciferase reporter gene assay, yeast two-hybrid assay and E-SCREEN were compared, suggesting that the dual-luciferase reporter gene assay is a useful approach for high-throughput screening. We also predicted the possible relationship between the chemical structures and the estrogenic effects of PCBs. (C) 2014 Elsevier Ltd. All rights reserved.