In Vitro Activity of the Arylaminoartemisinin GC012 against Helicobacter pylori and Its Effects on Biofilm

This study evaluated the in vitro activity of the arylaminoartemisinin GC012, readily obtained from dihydroartemisinin (DHA), against clinical strains of Helicobacter pylori (H. pylori) with different antibiotic susceptibilities in the planktonic and sessile state. The activity was assessed in terms of bacteriostatic and bactericidal potential. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined by the broth microdilution method. After treatment with GC012, all bacterial strains showed significantly lower MIC and MBC values compared to those of DHA. The effect of combination of GC012 with antibiotics was examined using the checkerboard method. GC012 displayed synergistic interactions with metronidazole, clarithromycin, and amoxicillin in all the strains. The antibiofilm activity was evaluated via crystal violet staining, AlamarBlue (R) assay, colony-forming unit count, and fluorescence microscopy. At 1/2 MIC and 1/4 MIC concentration, both GC012 and DHA inhibited biofilm formation, but only GC012 showed a minimal biofilm eradication concentration (MBEC) on mature biofilm. Furthermore, both compounds induced structural changes in the bacterial membrane, as observed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM). It is thereby demonstrated that GC012 has the potential to be efficacious against H. pylori infection.

Automated summary

This study evaluated the in vitro activity of arylaminoartemisinin GC012 against clinical strains of H. pylori with different antibiotic susceptibilities. GC012 showed significantly lower MIC and MBC values compared to DHA, indicating its potential as an effective treatment for H. pylori infection. Combination of GC012 with metronidazole, clarithromycin, and amoxicillin displayed synergistic interactions. Additionally, GC012 inhibited biofilm formation and showed minimal biofilm eradication concentration (MBEC) on mature biofilm. Structural changes in the bacterial membrane were observed for both GC012 and DHA.