In vitro activity of artemisone and artemisinin derivatives against extracellular and intracellular Helicobacter pylori

Francesca Sisto, Maria Maddalena Scaltrito, Carla Masia, Arianna Bonomi, Valentina Coccè, Giuseppe Marano, Richard K. Haynes, Alessandro Miani, Giampietro Farronato, Donatella Taramelli

Research output: Contribution to journalArticle

Abstract

The in vitro activity of the new artemisinin derivative artemisone as well as other molecules of the same class against Helicobacter pylori and their effects when combined with standard antibiotics were evaluated. Since H. pylori can be internalised into gastric epithelial cells, the effects of artemisinin, dihydroartemisinin and artemisone against intracellular H. pylori were also investigated. Bacteriostatic [minimum inhibitory concentration (MIC)] and bactericidal [minimum bactericidal concentration (MBC)] activities were assessed against 24 clinical strains of H. pylori with different antibiotics susceptibilities. Artemisone showed MIC50 and MIC90 values of 0.25 mg/L and 0.5 mg/L, respectively, and an MBC50 value of 0.5 mg/L. Artemisone was synergistic with amoxicillin in 60% of strains, with clarithromycin in 40% and with metronidazole in 20%. There was no interaction between artemisone and omeprazole or bismuth citrate. Against intracellular H. pylori, only dihydroartemisinin at 2× MIC caused a 1 log10 CFU decrease after 18 h and 24 h of incubation. This is the first demonstration in vitro of the activity of artemisinin derivatives against intracellular H. pylori and indicates that artemisone has the potential to be efficacious for the treatment of H. pylori infection, especially in combination with antibiotics.

Original languageEnglish
Pages (from-to)101-5
Number of pages5
JournalInternational Journal of Antimicrobial Agents
Volume48
Issue number1
DOIs
Publication statusPublished - Jul 2016
Externally publishedYes

Keywords

  • Anti-Infective Agents
  • Artemisinins
  • Drug Synergism
  • Helicobacter Infections
  • Helicobacter pylori
  • Humans
  • Microbial Sensitivity Tests
  • Microbial Viability
  • Journal Article

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  • Cite this

    Sisto, F., Scaltrito, M. M., Masia, C., Bonomi, A., Coccè, V., Marano, G., Haynes, R. K., Miani, A., Farronato, G., & Taramelli, D. (2016). In vitro activity of artemisone and artemisinin derivatives against extracellular and intracellular Helicobacter pylori. International Journal of Antimicrobial Agents, 48(1), 101-5. https://doi.org/10.1016/j.ijantimicag.2016.03.018