XENOVULENE-A, A NOVEL GABA-BENZODIAZEPINE RECEPTOR-BINDING COMPOUND PRODUCED BY ACREMONIUM-STRICTUM

被引:35
作者
AINSWORTH, AM [1 ]
CHICARELLIROBINSON, MI [1 ]
COPP, BR [1 ]
FAUTH, U [1 ]
HYLANDS, PJ [1 ]
HOLLOWAY, JA [1 ]
LATIF, M [1 ]
OBEIRNE, GB [1 ]
PORTER, N [1 ]
RENNO, DV [1 ]
RICHARDS, M [1 ]
ROBINSON, N [1 ]
机构
[1] XENOVA LTD,SLOUGH SL1 4EF,BERKS,ENGLAND
关键词
D O I
10.7164/antibiotics.48.568
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
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.
引用
收藏
页码:568 / 573
页数:6
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