Cellular internalization and cytotoxicity of the antimicrobial proline-rich peptide Bac7(1-35) in monocytes/macrophages, and its activity against phagocytosed Salmonella typhimurium

Protein Pept Lett. 2014 Apr;21(4):382-90. doi: 10.2174/09298665113206660109.

Abstract

Bac7(1-35) is an active fragment of the bovine cathelicidin antimicrobial peptide Bac7, which selectively inactivates Gram-negative bacteria both in vitro and in mice infected with Salmonella typhimurium. It has a non-lytic mechanism of action, is rapidly internalized by susceptible bacteria and mammalian cells and likely acts by binding to internal targets. In this study we show that Bac7(1-35) accumulates selectively within primed macrophages with respect to resting monocytes. Confocal microscopy analysis showed that the peptide mainly distributes in the cytoplasm and perinuclear region of macrophages within 3 hours of incubation, without affecting cell viability. Cytotoxicity studies showed that the peptide does not induce necrotic or apoptotic damage up to concentrations 50-100-fold higher than minimal inhibitory concentrations (MIC). Moreover, Bac7(1-35) did not affect the ability of macrophages to engulf S. typhimurium, a species that may proliferate within this cell type. Conversely, when added to macrophages after phagocytosis, Bac7(1-35) caused a significant reduction in the number of recovered bacteria, indicating that it can kill the engulfed microorganisms directly and/or indirectly, via activation of the defense response of the cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Infective Agents / pharmacokinetics*
  • Anti-Infective Agents / pharmacology*
  • Cattle
  • Cell Line
  • Cells, Cultured
  • Humans
  • Macrophages / cytology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Macrophages / microbiology*
  • Mice
  • Peptides, Cyclic / pharmacokinetics*
  • Peptides, Cyclic / pharmacology
  • Phagocytosis
  • Salmonella Infections / drug therapy*
  • Salmonella typhimurium / drug effects*

Substances

  • Anti-Infective Agents
  • Peptides, Cyclic
  • bactenecin