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

• 作者: Thongchai Taechowisan Watcharee Waratchareeyakul Waya S. Phutdhawong Winyou Puckdee
• 来源期刊: 微生物学(英文)
• 学科: 医学
• 关键词: ANTI-INFLAMMATORY Activity GELDANAMYCIN DERIVATIVES STREPTOMYCES zerumbet RAW 264.7 CELLS
• 年，卷（期）: 2019,（4）
• 页码范围: 398-421
• 页数: 24页
• 分类号: R73

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.