The Quinone-Derived Small Molecule M5N32 Is an Effective Anti–Helicobacter pylori Agent Both In Vivo and In Vitro

Abstract

Abstract Background Helicobacter pylori has become increasingly resistant to all commonly used clinical antibiotics. Therefore, new anti–H. pylori drugs need to be identified. Recently, quinones were found to inhibit growth of H. pylori with quinone-derived small-molecule compounds identified as having antitumor effects. Methods The minimum inhibitory concentrations of the compounds against H. pylori were measured by agar plate dilution method. The inhibition of biofilm formation by the compounds was assessed by SYTO9-PI double staining. The reactive oxygen species induced by the compounds were detected by DCFH-DA stain. The clearance effects of the compounds for H. pylori in mouse were evaluated by counting colony-forming units and hematoxylin and eosin staining. Results Our results revealed strong inhibition of M5N32 in vitro against H. pylori in both the planktonic and biofilm-forming states. Resistance to M5N32 was not developed in successive generations of the bacteria. In vivo, the combination of M5N32 and omeprazole showed enhanced effects in comparison to the standard triple therapy. M5N32 was nontoxic to normal tissues. Conclusions M5N32 is effective in the treatment of H. pylori infections, providing potential development of anti–H. pylori medicines in the treatment of H. pylori infections.