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角鲨烯合酶的新型抑制剂——茎点霉属真菌产生的角鲨他汀。I. 分类学、发酵、分离、理化性质及生物活性

The squalestatins, novel inhibitors of squalene synthase produced by a species of Phoma. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activity.

作者信息

Dawson M J, Farthing J E, Marshall P S, Middleton R F, O'Neill M J, Shuttleworth A, Stylli C, Tait R M, Taylor P M, Wildman H G

机构信息

Department of Natural Products Discovery, Glaxo Group Research Ltd., Greenford, Middlesex, UK.

出版信息

J Antibiot (Tokyo). 1992 May;45(5):639-47. doi: 10.7164/antibiotics.45.639.

Abstract

During the screening of fungi for inhibitors of squalene synthase, Phoma sp. C2932 was found to produce three structurally related novel inhibitors. These compounds, designated the squalestatins, exhibited potent activity against both mammalian (rat liver) and fungal (Candida albicans) squalene synthase. Furthermore, they also had broad spectrum in vitro antifungal activity.

摘要

在筛选能够抑制角鲨烯合酶的真菌时,发现茎点霉属真菌C2932能产生三种结构相关的新型抑制剂。这些化合物被命名为角鲨烯抑素,对哺乳动物(大鼠肝脏)和真菌(白色念珠菌)的角鲨烯合酶均表现出强效活性。此外,它们还具有广谱的体外抗真菌活性。

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