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吲哚咔唑和双吲哚蛋白激酶C抑制剂的抗菌活性。

Antimicrobial activities of indolocarbazole and bis-indole protein kinase C inhibitors.

作者信息

Sancelme M, Fabre S, Prudhomme M

机构信息

Université Blaise Pascal, Laboratoire de Chimie Organique Biologique, URA 485, Aubière, France.

出版信息

J Antibiot (Tokyo). 1994 Jul;47(7):792-8. doi: 10.7164/antibiotics.47.792.

Abstract

The antimicrobial activities of twenty-two substances structurally related to staurosporine, aglycone in the indolocarbazole and bis-indole series were examined against Streptomyces chartreusis and Streptomyces griseus, Bacillus cereus, Escherichia coli, Candida albicans and Botrytis cinerea. Inhibition of sporulation was examined also on the two species of Streptomyces. Unlike literature reports for efficient protein kinase inhibitors, staurosporine and K-252a, no evident correlation could be found either between protein kinase inhibitory potencies and inhibition of sporulation of the Streptomyces species, or protein kinase inhibitory potencies and growth of all microorganisms tested. A weak activity against C. albicans was observed for the chloro-indolocarbazole compounds as already reported for structurally related substances from the cyanobacterium Tolypothrix tjipanasensis.

摘要

检测了二十二种与星形孢菌素结构相关的物质(吲哚咔唑和双吲哚系列的苷元)对绿产色链霉菌、灰色链霉菌、蜡样芽孢杆菌、大肠杆菌、白色念珠菌和灰葡萄孢的抗菌活性。还检测了这两种链霉菌的孢子形成抑制情况。与高效蛋白激酶抑制剂星形孢菌素和K-252a的文献报道不同,在蛋白激酶抑制效力与链霉菌孢子形成抑制之间,或者蛋白激酶抑制效力与所有受试微生物的生长之间,均未发现明显的相关性。如之前报道的来自蓝藻托利枝孢的结构相关物质一样,氯代吲哚咔唑化合物对白色念珠菌表现出较弱的活性。

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