Antimicrobial activities of indolocarbazole and bis-indole protein kinase C inhibitors.
作者:MARTINE SANCELME、SERGE FABRE、MICHELLE PRUDHOMME
DOI:10.7164/antibiotics.47.792
日期:——
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.
研究了 22 种在结构上与石杉碱(吲哚咔唑和双吲哚系列中的苷元)相关的物质对图链霉和灰葡萄孢链霉菌、蜡样芽孢杆菌、大肠杆菌、白色念珠菌和灰葡萄孢菌的抗菌活性。还研究了这两种链霉菌的孢子抑制作用。与文献报道的高效蛋白激酶抑制剂staurosporine 和 K-252a 不同,在蛋白激酶抑制效力和对链霉菌孢子的抑制之间,或在蛋白激酶抑制效力和所有受试微生物的生长之间,都没有发现明显的相关性。氯代吲哚咔唑化合物对白僵菌的活性较弱,这与 Tolypothrix tjipanasensis 蓝藻中结构相关物质的活性相同。