Subglutinol A, an immunosuppressive α-pyrone diterpenoid from Fusarium subglutinans, acts as an estrogen receptor antagonist.
Subglutinol A is an immunosuppressive α-pyrone diterpenoid isolated from Fusarium subglutinans that exhibits osteogenic activity. Several non-steroid mycotoxins isolated from various strains of Fusarium fungi exhibit female steroid hormone activities. In this study, we characterized the estrogenic activity of subglutinol A (1). Subglutinol A blocked the 17β-estradiol-induced activation of reporter plasmids and endogenous estrogen-responsive target genes in a dose-dependent manner and efficiently destabilized ER proteins as shown using the estrogen receptor antagonist ICI 182,780. Subglutinol A also displaced the specific binding of [(3)H]17β-estradiol from ER in MCF-7 whole-cell ligand binding assays. These data demonstrate the potential of subglutinol A as an ER antagonist though its competition with 17β-estradiol for direct ER association.
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Related Subject Headings
- Reverse Transcriptase Polymerase Chain Reaction
- Pyrones
- MCF-7 Cells
- Immunosuppressive Agents
- Humans
- Fusarium
- Estrogen Receptor alpha
- Diterpenes
- DNA Primers
- Biochemistry & Molecular Biology
Citation
Published In
DOI
EISSN
ISSN
Publication Date
Volume
Issue
Start / End Page
Related Subject Headings
- Reverse Transcriptase Polymerase Chain Reaction
- Pyrones
- MCF-7 Cells
- Immunosuppressive Agents
- Humans
- Fusarium
- Estrogen Receptor alpha
- Diterpenes
- DNA Primers
- Biochemistry & Molecular Biology