Validation and application of a rapid in vitro assay for assessing the estrogenic potency of halogenated phenolic chemicals.
The E-Screen assay serves as an in vitro tool for the detection of estrogenic activity of chemicals and extracts of environmental samples. Based on the induction of proliferation in human estrogen receptor-positive MCF-7 breast cancer cells we could substantially simplify the assay. As one important step of validation we applied the modified assay for testing nine known xenoestrogens. We could confirm the results of other groups assuring the reproducibility of the E-Screen assay. The results provide evidence that the E-Screen assay is suitable for determination of estradiol equivalency factors (EEFs) for environmental estrogens to rank their estrogenic potency relative to the natural estrogen 17 beta-estradiol. Further, we used the optimized proliferation test to screen nine halogenated phenolic compounds for their possible estrogenic potency. Three widely applied chemicals expressed a weak receptor-mediated estrogenic activity: the flame retardant Tetrabromo-Bisphenol-A, the disinfectant 4-chloro-3-methylphenol, and the herbicide educt 4-chloro-2-methylphenol. Their estrogenic potencies were five to six orders of magnitude lower than that of 17 beta-estradiol.
Körner
W
W
Institute of Organic Chemistry, University of Tübingen, Germany.
Hanf
V
V
Schuller
W
W
Bartsch
H
H
Zwirner
M
M
Hagenmaier
H
H
D001681:Biological Assay / Q000379:methods; D001943:Breast Neoplasms; D004967:Estrogens / Q000494:pharmacology*; D005260:Female; D006219:Halogens; D006801:Humans; D010636:Phenols / Q000633:toxicity*; D011960:Receptors, Estrogen / Q000187:drug effects*; D015203:Reproducibility of Results; D018675:Toxicity Tests / Q000379:methods; D014407:Tumor Cells, Cultured
D004967:Estrogens; D006219:Halogens; D010636:Phenols; D011960:Receptors, Estrogen