6533b7d5fe1ef96bd12652dc

RESEARCH PRODUCT

Steroid activities comparison of natural and food wrap compounds in human breast cancer cell lines

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Abstract In this study, we tested and compared the endocrine disruption activities of compounds in materials used to package foods (bisphenol A, bisphenol F, and bisphenol A diglycidylether BADGE) with natural molecules (genistein, apigenin, kaempferol, and tangeretin) in the human breast cancer cell lines MCF-7 (ER + ) and MDA-MB453 (AR + ; GR + ). Octylphenol was also chosen as a xenoestrogen reference. Two compounds had no estrogenic activity: BADGE and tangeretin. Genistein was the most active compound in the E-Screen assay with MCF-7, followed by octylphenol, bisphenol F, bisphenol A and apigenin, with kaempferol the least potent. All estrogenic compounds competed with 17β-estradiol for binding to the MCF-7 ER and their estrogenic effects were abolished in the presence of tamoxifen, an ER antagonist. In MDA-MB453 cells transfected with pMMTVneo-Luc, all compounds had anti-androgenic activities, with octylphenol the most potent. Kaempferol, genistein, and apigenin were more potent anti-androgens than bisphenols A or F. The natural compounds had a biphasic effect on luciferase activity. At high concentrations, genistein (10 −5 M) and apigenin (10 −6 M) acted as GR agonists in transfected MDA-MB453 cells. Furthermore, apigenin, at a concentration of 10 −5 M, may act as a partial androgen receptor (AR) agonist, as nilutamide, an AR antagonist, inhibited its activity by 26%.