Metabolism of the α,β-Unsaturated Ketones, Chalcone and trans-4-Phenyl-3-buten-2-one, by Rat Liver Microsomes and Estrogenic Activity of the Metabolites

PBO was oxidized by cytochrome P450 1A1, 1A2, 2C6 and 2E1. Chalcone and PBO were negative in an estrogen reporter assay using estrogen-responsive human breast cancer cell line MCF-7. However, 4-hydroxychalcone, 2-hydroxychalcone, 4'-hydroxychalcone and 4-OH-PBO exhibited estrogenic activity. DMD #2634