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 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.
Ainsworth
A M
AM
Xenova Ltd, Slough Berkshire, U.K.
Chicarelli-Robinson
M I
MI
Copp
B R
BR
Fauth
U
U
Hylands
P J
PJ
Holloway
J A
JA
Latif
M
M
O'Beirne
G B
GB
Porter
N
N
Renno
D V
DV
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
D018079:Receptors, GABA; D012717:Sesquiterpenes; C095333:xenovulene A; D005445:Flunitrazepam