Identification of 3',4',5'-trimethoxychalcone analogues as potent inhibitors of Helicobacter pylori-induced inflammation in human gastric epithelial cells.
Efforts to identify potent small molecule inhibitors of Helicobacter pylori led to the evaluation of 23 3',4',5'-trimethoxychalcone analogues. Some of the compounds displayed potent antibacterial activity against H. pylori. Three most active and selective compounds 1, 7, and 13 also showed the bactericide activity against the reference as well as multidrug-resistant strains of H. pylori. Additionally, the aforementioned three compounds potentially inhibited the H. pylori adhesion and invasion to human gastric epithelial (AGS) cells. Furthermore, these selective compounds inhibited the H. pylori-induced gastric inflammation by reduced inflammatory mediator's nuclear factor kappa B activation, and the secretion of interleukin-8.
Lai
Chih-Ho
CH
Department of Microbiology, School of Medicine, China Medical University, Taichung, Taiwan, ROC.
Rao
Yerra Koteswara
YK
Fang
Shih-Hua
SH
Sing
Yu-Ting
YT
Tzeng
Yew-Min
YM
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D004847:Epithelial Cells / Q000187:drug effects / Q000382:microbiology; D005756:Gastritis / Q000188:drug therapy* / Q000209:etiology / Q000382:microbiology; D016481:Helicobacter Infections / Q000150:complications / Q000188:drug therapy*; D016480:Helicobacter pylori / Q000187:drug effects*; D054884:Host-Pathogen Interactions / Q000187:drug effects; D006801:Humans; D016209:Interleukin-8 / Q000276:immunology; D016328:NF-kappa B / Q000276:immunology
D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D047188:Chalcones; D016209:Interleukin-8; D016328:NF-kappa B; C003702:metochalcone