title: Xenovulene A, a novel GABA-benzodiazepine receptor binding compound produced by Acremonium strictum.
abstract: 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 40 nM in an in vitro assay using bovine synaptosome membrane preparations.
authors.affiliation: Xenova Ltd, Slough Berkshire, U.K.
authors.forename: A M
authors.initials: AM
authors.lastname: Ainsworth
authors.forename: M I
authors.initials: MI
authors.lastname: Chicarelli-Robinson
authors.forename: B R
authors.initials: BR
authors.lastname: Copp
authors.forename: U
authors.initials: U
authors.lastname: Fauth
authors.forename: P J
authors.initials: PJ
authors.lastname: Hylands
authors.forename: J A
authors.initials: JA
authors.lastname: Holloway
authors.forename: M
authors.initials: M
authors.lastname: Latif
authors.forename: G B
authors.initials: GB
authors.lastname: O'Beirne
authors.forename: N
authors.initials: N
authors.lastname: Porter
authors.forename: D V
authors.initials: DV
authors.lastname: Renno
mesh_terms: D000164:Acremonium / Q000378:metabolism; D000818:Animals; D002417:Cattle; D005285:Fermentation; D005445:Flunitrazepam / Q000378:metabolism; D015394:Molecular Structure; D018079:Receptors, GABA / Q000187:drug effects* / Q000378:metabolism; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: D018079:Receptors, GABA; D012717:Sesquiterpenes; C095333:xenovulene A; D005445:Flunitrazepam