A macrophage-based screen identifies antibacterial compounds selective for intracellular Salmonella Typhimurium

Nat Commun. 2019 Jan 14;10(1):197. doi: 10.1038/s41467-018-08190-x.

Abstract

Salmonella Typhimurium (S. Tm) establishes systemic infection in susceptible hosts by evading the innate immune response and replicating within host phagocytes. Here, we sought to identify inhibitors of intracellular S. Tm replication by conducting parallel chemical screens against S. Tm growing in macrophage-mimicking media and within macrophages. We identify several compounds that inhibit Salmonella growth in the intracellular environment and in acidic, ion-limited media. We report on the antimicrobial activity of the psychoactive drug metergoline, which is specific against intracellular S. Tm. Screening an S. Tm deletion library in the presence of metergoline reveals hypersensitization of outer membrane mutants to metergoline activity. Metergoline disrupts the proton motive force at the bacterial cytoplasmic membrane and extends animal survival during a systemic S. Tm infection. This work highlights the predictive nature of intracellular screens for in vivo efficacy, and identifies metergoline as a novel antimicrobial active against Salmonella.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Cell Membrane / drug effects
  • Cell Membrane / genetics
  • Disease Models, Animal
  • Drug Evaluation, Preclinical / methods
  • Female
  • Gene Deletion
  • High-Throughput Screening Assays / methods
  • Humans
  • Macrophages / immunology
  • Macrophages / microbiology*
  • Macrophages / ultrastructure
  • Metergoline / pharmacology*
  • Metergoline / therapeutic use
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Mice
  • Mice, Inbred C57BL
  • Microbial Sensitivity Tests
  • Microscopy, Atomic Force
  • RAW 264.7 Cells
  • Salmonella Infections / drug therapy*
  • Salmonella Infections / immunology
  • Salmonella Infections / microbiology
  • Salmonella Infections / mortality
  • Salmonella typhimurium / drug effects*
  • Salmonella typhimurium / genetics
  • Salmonella typhimurium / pathogenicity
  • Treatment Outcome

Substances

  • Anti-Bacterial Agents
  • Metergoline