title: Steroid activities comparison of natural and food wrap compounds in human breast cancer cell lines.
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 17beta-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%.
authors.affiliation: UMR 1234 Toxicologie Alimentaire, University of Burgundy/INRA, 1 Esplanade Erasme, 21000 Dijon, France.
authors.forename: T
authors.initials: T
authors.lastname: Stroheker
authors.forename: K
authors.initials: K
authors.lastname: Picard
authors.forename: J C
authors.initials: JC
authors.lastname: Lhuguenot
authors.forename: M C
authors.initials: MC
authors.lastname: Canivenc-Lavier
authors.forename: M C
authors.initials: MC
authors.lastname: Chagnon
mesh_terms: D016588:Anticarcinogenic Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D047310:Apigenin; D001559:Benzhydryl Compounds; D001943:Breast Neoplasms / Q000473:pathology*; D002273:Carcinogens / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004703:Endocrine System / Q000187:drug effects; D004852:Epoxy Compounds / Q000494:pharmacology; D004968:Estrogens, Non-Steroidal / Q000494:pharmacology; D005260:Female; D047309:Flavones; D005419:Flavonoids / Q000494:pharmacology; D018857:Food Packaging; D019833:Genistein / Q000494:pharmacology; D006801:Humans; D044949:Kaempferols / Q000494:pharmacology; D010636:Phenols / Q000494:pharmacology; D011944:Receptors, Androgen / Q000187:drug effects* / Q000502:physiology; D011960:Receptors, Estrogen / Q000187:drug effects*; D014407:Tumor Cells, Cultured; D000098826:Bisphenol A Compounds
chemical_list: D016588:Anticarcinogenic Agents; D000970:Antineoplastic Agents; D047310:Apigenin; D001559:Benzhydryl Compounds; D002273:Carcinogens; D004852:Epoxy Compounds; D004968:Estrogens, Non-Steroidal; D047309:Flavones; D005419:Flavonoids; D019833:Genistein; D044949:Kaempferols; D010636:Phenols; D011944:Receptors, Androgen; D011960:Receptors, Estrogen; C006552:kaempferol; C019273:bisphenol A diglycidyl ether; D000098826:Bisphenol A Compounds; C059006:tangeretin; C006780:bisphenol A; C423722:bisphenol F diglycidyl ether