Xenovulene A, a Novel GABA-Benzodiazepine Receptor Binding Compound Produced by Acremonium strictum

Xenovulene A, a novel inhibitor of benzodiazepine binding to the GABA-benzodiazepine receptor is produced by submerged fermentation of Acremonium strictum. It was isolated from the mycelium by solvent extraction and purified by chromatography on Sephadex LH-20 and octadecyl silica. The structure of...

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Bibliographic Details
Published in:Journal of antibiotics 1995/07/25, Vol.48(7), pp.568-573
Main Authors: AINSWORTH, A. MARTYN, CHICARELLI-ROBINSON, M. INÊS, COPP, BRENT R., FAUTH, URSULA, HYLANDS, PETER J., HOLLOWAY, JACQUELINE A., LATIF, MOHAMMED, O'BEIRNE, GERARD B., PORTER, NEIL, RENNO, DIDIER V., RICHARDS, MICHELLE, ROBINSON, NEIL
Format: Article
Language:English
Subjects:
Acremonium - metabolism
Animals
Biological and medical sciences
Cattle
Fermentation
Flunitrazepam - metabolism
General pharmacology
Medical sciences
Molecular Structure
Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
Pharmacology. Drug treatments
Receptors, GABA - drug effects
Receptors, GABA - metabolism
Sesquiterpenes - chemistry
Sesquiterpenes - isolation & purification
Sesquiterpenes - pharmacology
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Summary:Xenovulene A, a novel inhibitor of benzodiazepine binding to the GABA-benzodiazepine receptor is produced by submerged fermentation of Acremonium strictum. It was isolated from the mycelium by solvent extraction and purified by chromatography on Sephadex LH-20 and octadecyl silica. The structure of xenovulene A was determined to be a novel oxygenated sesquiterpene containing a humulene moiety by interpretation of various spectroscopic data, especially from 2D NMR experiments. Xenovulene A inhibited binding of the benzodiazepine, flunitrazepam, with an IC50 of 40nM in an in vitro assay using bovine synaptosome membrane preparations.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.48.568