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.

Synthesis, inhibitory activity and molecular docking studies of two Cu(II) complexes against Helicobacter pylori urease

“…pylori (ATCC 43504; American Type Culture Collection, Manassas, VA) was grown on Columbia Agar supplemented with 7% sheep blood and cultured for 3 days at 37°C under microaerobic conditions (5% O 2 , 10% CO 2 and 85% N 2 ), as previously described 15 . The method of preparation of H. pylori urease was followed by Mao 16 .…”

Phytoceuticals: Mighty but ignored weapons against Helicobacter pylori infection

“…Different levels of anti‐ H. pylori activities might be observed in various isoflavones. A study evaluated three series of metronidazole‐flavonoid derivatives for antimicrobial activity against H. pylori 39 . Only one compound could significantly attenuate the increase in IL‐8 levels in the gastric cancer cells stimulated with a H. pylori water extract, which did not show any effects on the cell viability.…”

6,6′-Oxydichroman

“…For related literature, see: Allen et al (1987); Li et al (2006Li et al ( , 2007; Xiao, Shi et al (2007); Xiao, Xue et al (2007); Huang et al (2007); Zhang et al (2007); Shi et al (2007); Cao et al (2007); Ruan et al (2006).…”