Madindoline, a novel inhibitor of IL-6 activity from Streptomyces sp K93-0711 .1. Taxonomy, fermentation, isolation and biological activities
Madindoline, a novel inhibitor of IL-6 activity from Streptomyces sp K93-0711 .1. Taxonomy, fermentation, isolation and biological activities
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DOI：
10.7164/antibiotics.49.1091
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发表时间：
1996-11-01
影响因子：
3.3
通讯作者：
Omura, S
中科院分区：
文献类型：
--
作者：
Hayashi, M;Kim, YP;Omura, S
微生物菌株K93-0711的发酵液对依赖IL-6的细胞有选择性抑制作用，该菌株属于链霉菌属。分离得到两个活性代谢物，分别命名为马吲哚A、B，确定其结构为N位含二酮环戊烯的3a-羟基吲哚。0.1U/mlIL-6对MH60细胞呈剂量依赖性抑制作用。对该细胞株的IC50分别为8mM和30mM。这些化合物对不依赖IL-6的细胞株的生长无抑制作用，过量的IL-6(0.4U/ml)可逆转对MH60细胞的生长抑制作用。这些化合物在1000微克/毫升的浓度下没有表现出任何抗菌活性。
Selective growth inhibition against IL-6-dependent cells was detected in fermentation extracts of a microbial strain, K93-0711, which was characterized as Streptomyces species. Active metabolite, termed madindoline A and B, were isolated, and the structure was determined to be 3a-hydroxyindoline with diketocyclopentene at the N position. Madindoline A and B displayed dose-dependent inhibition of MH60 cells, an IL-6-dependent cell line, in presence of 0.1 U/ml IL-6. The IC50 for madindoline A and B against this cell line was 8 mu M and 30 mu M, respectively. These compounds did not inhibit the growth of cell lines which are not IL-6 dependent and the growth inhibition bf the MH60 cell line was reversed by addition of excess, 0.4 U/ml of IL-6 to the culture media. These compounds did not show any antimicrobial activity at a concentration Of 1,000 mu g/ml.