Evaluation of estrogenic effects of POPs by OECD TG455 and estrogen receptor binding assay

Program: Abstracts - Orals, Featured Poster Presentations, and Posters
Session: MON 338-354-Physiological Impacts of Endocrine Disrupting Chemicals
Basic/Translational
Monday, June 17, 2013: 1:45 PM-3:45 PM
Expo Halls ABC (Moscone Center)

Poster Board MON-351
Sang-Yub Kim*, HeeSeok Lee, Eun-Jung Park, Seung-Yul Lee, Min-Ki Shin, Chi-Young Kim and Young-Mi Jang
Health Effect Analysis Team, Institute of Food and Drug Safety Evaluation, Korea FDA
The estrogenic activities of industrial chemicals, persistant organic pollutants (linden, arochlor, dieldrin, heptachlor, chlordane, PBDEs, PFOA, PFOS, p’p-DDT, p’p-DDE) as well as reference chemical, 17β-estradiol were carried out by fluorescence polarization competitive binding assay and stably transfected human estrogen receptor-α transcriptional activation assay (OECD TG455). These compounds were tested with full-length human recombinant estrogen receptor-α and -β proteins respectively. The relative binding affinities of test compounds with full length human estrogen receptor-α ligand could be ranked PFOS, arochlor> p’p-DDT > lindane, chlordane> p’p-DDE≥ dieldrin, PBDEs > and PFOA. Besides the rank of the relative binding affinities against estrogen receptor-β was p’p-DDT > chlordane > arochlor, p’p-DDE > PFOS > heptachlor> lindane> arochlor and PFOA. The pattern of relative binding affinity to estrogen receptor-α of POPs was very similar to that estrogen receptor-β. However, dieldrin, p’p-DDT and p’p-DDE exhibited estrogenic effects with PC50 values of 3.98☓10-10, 7.31☓10-8 and 6.57☓10-8 M, respectively in OECD TG455 assay among the tested chemicals. These activities of dieldrin, p’p-DDT and p’p-DDE are approximately 10-, 300- and 400-fold less than 17β-estradiol(2.43☓10-8 M). Our results suggested that estrogen receptor competitive binding assay and stably transfected human estrogen receptor-α transcriptional activation assay are useful as a fast screening test for potential endocrine disruptors.

Nothing to Disclose: SYK, HL, EJP, SYL, MKS, CYK, YMJ

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