Revised Structure and Synthesis of Celastramycin A, A Potent Innate Immune Suppressor
Revised Structure and Synthesis of Celastramycin A, A Potent Innate Immune Suppressor
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DOI：
10.1021/ol9002306
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发表时间：
2009-04-16
期刊：
影响因子：
5.2
通讯作者：
Oshima, Yoshiteru
中科院分区：
文献类型：
--
作者：
Kikuchi, Haruhisa;Sekiya, Mizuki;Oshima, Yoshiteru
在利用果蝇体外培养系统寻找调节天然免疫的天然物质后，一种苯甲酰-吡咯型化合物--克拉斯特霉素A被鉴定并分离为一种有效的抑制剂。通过合成先前报道的结构1和日本专利中报道的另一种苯甲酰基吡咯型化合物2，确定了其正确结构为2。化合物2抑制人脐静脉内皮细胞产生IL-8(IC50为0.06µg/mL)。
After searching for natural substances that regulate innate immunity using the ex vivo Drosophila culture system, a benzoyl pyrrole-type compound, celastramycin A, was identified and isolated as a potent suppressor. By synthesizing the previously reported structure 1 and another benzoyl pyrrole-type compound 2 reported in a Japanese patent, the correct structure of celastramycin A was confirmed to be 2. Compound 2 suppressed the production of IL-8 (IC50 0.06 mu g/mL) in human umbilical vein endothelial cells (HUVECs).