While the synthetic stilbene diethylstilbestrol is well known as and estrogen agonist with toxic effects after developmental exposure, natural stilbenes such as resveratrol, piceatannol and pterostilbine found in grapes, blueberrys and other plants have been shown to have antineoplastic and other medicinal properties.  In this report, we test the hypothesis that stilbene analogues and isomers have estrogen agonist or antagonist activity.  Presented is the in vitro estrogen activity of 29 stilbene analogues and isomers obtained from Dr. Agnes Rimando of the USDA Natural Products Utilization Research Unit in Mississippi.  Each compound was tested for estrogen agonist and antagonist activity at 10 uM in the T47DkbLuc reporter gene as well as MCF-7 proliferation assays.  For those with activity at high dose, data was obtained over the range of 1 nM to 10 uM.  In addition, estrogen receptor binding assays were performed using the Invitrogen PolarScreen ER alpha method on all compounds shown to have activity.  Bioassay and receptor binding data will be analyzed to identify structure activity relationships responsible for estrogen agonist or antagonist activity.  This data will be used to suggest the potential of stilbenes analogues as hormone replacement in post-menopausal women or as antihormones that might protect against estrogen dependent breast cancer.

In vitro estrogen activity of 29 stilbenes: Structure-activity relationships for agonist and antagonist activity

247th National Meeting (2014)

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