Heterogeneous efflux pump expression underpins phenotypic resistance to antimicrobial peptides

Elife. 2025 Jul 3:13:RP99752. doi: 10.7554/eLife.99752.

Abstract

Antimicrobial resistance threatens the viability of modern medical interventions. There is a dire need to develop novel approaches to counter resistance mechanisms employed by starved or slow-growing pathogens that are refractory to conventional antimicrobial therapies. Antimicrobial peptides have been advocated as potential therapeutic solutions due to the low levels of genetic resistance observed in bacteria against these compounds. However, here we show that subpopulations of stationary phase Escherichia coli and Pseudomonas aeruginosa survive tachyplesin treatment without acquiring genetic mutations. These phenotypic variants display enhanced efflux activity to limit intracellular peptide accumulation. Differential regulation of genes involved in outer membrane vesicle secretion, membrane modification, and protease activity was also observed between phenotypically resistant and susceptible cells. We discovered that the formation of these phenotypic variants could be prevented by administering tachyplesin in combination with sertraline, a clinically used antidepressant, suggesting a novel approach for combatting antimicrobial-refractory stationary phase bacteria.

Keywords: E. coli; antibiotic accumulation; antibiotics; antimicrobial peptides; antimicrobial resistance; efflux pump inhibitors; efflux pumps; gene expression; heterogeneity; infectious disease; membrane transport; microbiology; microfluidics; physics of living systems; stationary phase; transcriptomics.

MeSH terms

  • Anti-Bacterial Agents* / pharmacology
  • Antimicrobial Cationic Peptides* / pharmacology
  • Antimicrobial Peptides* / metabolism
  • Antimicrobial Peptides* / pharmacology
  • Drug Resistance, Bacterial*
  • Escherichia coli* / drug effects
  • Escherichia coli* / genetics
  • Escherichia coli* / metabolism
  • Gene Expression Regulation, Bacterial / drug effects
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Peptides, Cyclic* / pharmacology
  • Phenotype
  • Pseudomonas aeruginosa* / drug effects
  • Pseudomonas aeruginosa* / genetics
  • Pseudomonas aeruginosa* / metabolism
  • Sertraline / pharmacology

Substances

  • Antimicrobial Peptides
  • Anti-Bacterial Agents
  • Peptides, Cyclic
  • Sertraline
  • Antimicrobial Cationic Peptides