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 a...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 2015-06, Vol.461 (3), p.507-512
Main Authors: Lim, Wonchung, Park, Joonwoo, Lee, Yong Hee, Hong, Jiyong, Lee, YoungJoo
Format: Article
Language:English
Subjects:
Antiestrogen
Base Sequence
Diterpenes - pharmacology
DNA Primers
Estrogen receptor
Estrogen Receptor alpha - antagonists & inhibitors
Fusarium - chemistry
Fusarium subglutinans
Humans
Immunosuppressive Agents - pharmacology
MCF-7 Cells
Pyrones - pharmacology
Reverse Transcriptase Polymerase Chain Reaction
Subglutinol
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Summary: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 [3H]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. •Subglutinols act as weak ER antagonists that disrupt ER-mediated pathways.•Subglutinols compete with estrogen binding to ERs.•This is the first report of the antiestrogenic activity of subglutinol.
ISSN:0006-291X
1090-2104
DOI:10.1016/j.bbrc.2015.04.053