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

被引：36

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

来源：

JOURNAL OF ANTIBIOTICS | 1995年 / 48卷 / 07期

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

页码：568 / 573

页数：6

共 11 条

[1]

Aldridge DC, 1983, FUNGAL METABOLITES, V2

[2]

Haefely W. E., 1985, ADV DRUG RES, V14, P165

[3] BENZODIAZEPINES [J].