title: Metronidazole-flavonoid derivatives as anti-Helicobacter pylori agents with potent inhibitory activity against HPE-induced interleukin-8 production by AGS cells.
abstract: Three series of metronidazole-flavonoid derivatives were generated and evaluated for antimicrobial activity against H. pylori. Among these compounds, high anti-H. pylori activities were observed in isoflavones derivatives 4-7, 19, and 20 but exhibited no inhibitory activity against other sorts of bacteria and fungi, for example, Streptococcus pneumoniae, Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence, and Aspergillus niger. Genistein derivative 6 with the potent activity (MIC=0.39 microg mL(-1)) was >50-fold more than metronidazole, and comparable to the positive control amoxicillin. Additionally, compound 6 can significantly attenuate the increase in interleukin-8 (IL-8) levels in the AGS cells stimulated by H. pylori water extract (HPE) at concentrations of 15, 30, and 60 micromol L(-1), which did not show any effects on the cell viability.
authors.affiliation: Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China.
authors.forename: Huan-Qiu
authors.initials: HQ
authors.lastname: Li
authors.forename: Chen
authors.initials: C
authors.lastname: Xu
authors.forename: Hong-Sen
authors.initials: HS
authors.lastname: Li
authors.forename: Zhu-Ping
authors.initials: ZP
authors.lastname: Xiao
authors.forename: Lei
authors.initials: L
authors.lastname: Shi
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004797:Enzyme-Linked Immunosorbent Assay; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D016480:Helicobacter pylori / Q000187:drug effects*; D006801:Humans; D016209:Interleukin-8 / Q000096:biosynthesis*; D009682:Magnetic Resonance Spectroscopy; D008795:Metronidazole / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000900:Anti-Bacterial Agents; D005419:Flavonoids; D016209:Interleukin-8; D008795:Metronidazole