title: Estrogenic effects of fusarielins in human breast cancer cell lines.
abstract: The fusarielins are a group of metabolites found in several Aspergillus and Fusarium species that have been reported to have with weak antifungal, antibiotic and cytotoxic effects. This study identifies fusarielin A, F, G and H isolated from Fusarium as mycoestrogens. Mycoestrogens are compounds from fungi that bind to the estrogen receptors and induce an estrogenic response in targeted cells. All four tested fusarielins stimulate MCF-7 cell proliferation with fusarielin H as the most potent, able to stimulate cell proliferation 4-fold in a resazurin metabolism assay at 25μM. MDA-MB-231 cells without the estrogen receptor-α and MCF-10a cells without estrogen receptors were not stimulated by fusarielins. Furthermore, the stimulation was prevented in MCF-7 cells when fusarielins were incubated in the presence of the estrogen receptor antagonist fulvestrant. These observations suggest that fusarielins bind to the estrogen receptor and act as weak mycoestrogens.
authors.affiliation: Department of Biotechnology, Chemistry and Environmental Engineering, Aalborg University, Sohngaardsholmsvej 49, DK-9000 Aalborg, Denmark. tes@bio.aau.dk
authors.forename: Teis Esben
authors.initials: TE
authors.lastname: Sondergaard
authors.forename: Louise Graabæk
authors.initials: LG
authors.lastname: Klitgaard
authors.forename: Stig
authors.initials: S
authors.lastname: Purup
authors.forename: Hisayoshi
authors.initials: H
authors.lastname: Kobayashi
authors.forename: Henriette
authors.initials: H
authors.lastname: Giese
authors.forename: Jens Laurids
authors.initials: JL
authors.lastname: Sørensen
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D016588:Anticarcinogenic Agents / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004852:Epoxy Compounds / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000494:pharmacology; D004968:Estrogens, Non-Steroidal / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D005260:Female; D000077267:Fulvestrant; D005656:Fungal Proteins / Q000494:pharmacology*; D005670:Fusarium / Q000737:chemistry*; D006801:Humans; D007202:Indicators and Reagents / Q000494:pharmacology; D061986:MCF-7 Cells; D010078:Oxazines / Q000494:pharmacology; D010936:Plant Extracts / Q000037:antagonists & inhibitors / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000172:deficiency / Q000378:metabolism; D014966:Xanthenes / Q000494:pharmacology
chemical_list: D016588:Anticarcinogenic Agents; D004852:Epoxy Compounds; D004965:Estrogen Antagonists; D004968:Estrogens, Non-Steroidal; D005656:Fungal Proteins; D007202:Indicators and Reagents; D010078:Oxazines; D010936:Plant Extracts; D011960:Receptors, Estrogen; D014966:Xanthenes; C005843:resazurin; D000077267:Fulvestrant; D004958:Estradiol