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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Pentanol derivatives from basidiomycete Catathelasma imperiale and their 11beta-hydroxysteroid dehydrogenases inhibitory activity.
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Pentanol derivatives from basidiomycete Catathelasma imperiale and their 11beta-hydroxysteroid dehydrogenases inhibitory activity.

机译：来自担子菌Catathelasma imperiale的戊醇衍生物及其11β-羟基类固醇脱氢酶的抑制活性。

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摘要

Five new secondary metabolites derived from pentanol, namely catathelasmols A-E (1-5), were isolated from the fruiting bodies of the basidiomycete Catathelasma imperiale. Their structures were elucidated on the basis of spectroscopic analysis, and the absolute configurations were determined by computational chemistry. Compounds 3, 4 and 5 showed inhibitory activities against two isozymes of 11-hydroxysteroid dehydrogenases (11-HSD1 and 11-HSD2), with IC(50) values of 28.7-62.3 microg ml(-1) (human 11-HSD1), 30.4-149.2 microg ml(-1) (mouse 11-HSD1), 5.1-177 microg ml(-1) (human 11-HSD2) and 32.3-129.1 microg ml(-1) (mouse 11-HSD2), which catalyze the interconversion of cortisol and cortisone.
机译：从担子菌Cathathelasma imperiale的子实体中分离出五种从戊醇衍生的新的次生代谢产物，即catathelasmols A-E（1-5）。在光谱分析的基础上阐明了它们的结构，并通过计算化学确定了其绝对构型。化合物3、4和5对11个羟类固醇脱氢酶的两个同工酶（11-HSD1和11-HSD2）表现出抑制活性，IC（50）值为28.7-62.3 microg ml（-1）（人11-HSD1）， 30.4-149.2 microg ml（-1）（小鼠11-HSD1），5.1-177 microg ml（-1）（人11-HSD2）和32.3-129.1 microg ml（-1）（小鼠11-HSD2）具有催化作用皮质醇和可的松的相互转化。

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