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Simmons DB, Trudeau VL, Marlatt VL, Moon TW, Sherry JP, Metcalfe CD: Interaction of stilbene compounds with human and rainbow trout estrogen receptors. Environ Toxicol Chem. 2008 Feb;27(2):442-51.
Compounds with stilbene structures are widely used as pharmaceuticals and personal care products (PPCPs) and are present in plants. A suite of stilbene-related compounds, including PPCPs and plant-derived compounds were tested in vitro for interactions with the human and rainbow trout estrogen receptors and in vivo with rainbow trout using vitellogenin levels as a biomarker. Among the compounds with antagonistic activity, the common structural similarity was (in addition to the stilbene backbone) the presence of 4-hydroxy substitution. Stilbene-related compounds found to act as inhibitors at the estrogen receptor included the plant-derived compound resveratrol and two formulations of fluorescent whitening agents used in detergents, 4,4'-bis (2-sulfostyryl) biphenyl and diaminostilbene-1. In the yeast estrogenicity screening assay, the concentrations which caused a 50% inhibition in estrogenic response (IC50s) with the human estrogen receptor ranged from 2.56 x 10 (-6) to 2.56 x 10 (-6) M. In the rainbow trout estrogen receptor assay, the IC50s ranged from 7.75 x 10 (-8) to 1.11 x 10 (-5) M. However, in the in vivo rainbow trout vitellogenin assay, tamoxifen was the only stilbene of the compounds tested to have a significant effect as an inhibitor of estrogenicity. |
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