Anti-Inflammatory Activity of Geldanamycin and Its Derivatives in LPS-Induced RAW 264.7 Cells

作     者：Thongchai Taechowisan Winyou Puckdee Watcharee Waratchareeyakul Waya S. Phutdhawong 

作者机构：Department of Microbiology Faculty of Science Silpakorn University Nakhon Pathom Thailand Department of Biology Faculty of Science and Technology Rambhai Barni Rajabhat University Chanthaburi Thailand Department of Chemistry Faculty of Science and Technology Rambhai Barni Rajabhat University Chanthaburi Thailand Department of Chemistry Faculty of Science Silpakorn University Nakhon Pathom Thailand 

出 版 物：《Advances in Microbiology》 (微生物学（英文）)

年 卷 期：2019年第9卷第4期

页      面：398-421页

学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学] 

主　　题：Anti-Inflammatory Activity Geldanamycin Derivatives Streptomyces zerumbet RAW 264.7 Cells 

摘      要：Geldanamycin (1) had been isolated as a major compound from Streptomyces zerumbet W14;an endophyte of Zingiber zerumbet (L.) Smith. Two new geldanamycin derivatives;17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5’-methoxytryptamine)-17-demethoxygeldanamycin (3) were synthe- sized and their anti-inflammatory activity was evaluated in LPS-induced macrophage RAW 264.7 cells by investigating their effects on the inhibition of production of NO, PGE2, TNF-α, IL-1β, IL-6 and IL-10. The data obtained were consistent with the modulation of TNF-α, IL-1β, IL-6, IL-10 production by these derivatives at concentration of 1 to 5 μg/ml. A similar effect was also observed when LPS-induced NO release and PGE2 production were tested. The inhibitory effects were shown in concentration-dependent manners. From the obtained results, it was concluded that two new gelda- namycin derivatives possess anti-inflammatory activity on LPS-induced RAW 264.7 cells. They could be useful for the management of inflammatory diseases.