Repurposing the antimycotic drug flucytosine for suppression of Pseudomonas aeruginosa pathogenicity

Proc Natl Acad Sci U S A. 2013 Apr 30;110(18):7458-63. doi: 10.1073/pnas.1222706110. Epub 2013 Apr 8.

Abstract

Although antibiotic resistance represents a public health emergency, the pipeline of new antibiotics is running dry. Repurposing of old drugs for new clinical applications is an attractive strategy for drug development. We used the bacterial pathogen Pseudomonas aeruginosa as a target for the screening of antivirulence activity among marketed drugs. We found that the antimycotic agent flucytosine inhibits the expression of the iron-starvation σ-factor PvdS, thereby repressing the production of major P. aeruginosa virulence factors, namely pyoverdine, PrpL protease, and exotoxin A. Flucytosine administration at clinically meaningful dosing regimens suppressed P. aeruginosa pathogenicity in a mouse model of lung infection. The in vitro and in vivo activity of flucytosine against P. aeruginosa, combined with its desirable pharmacological properties, paves the way for clinical trials on the anti-P. aeruginosa efficacy of flucytosine in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / pharmacology*
  • Antifungal Agents / therapeutic use
  • Bacterial Proteins / metabolism
  • Down-Regulation / drug effects
  • Flucytosine / pharmacology*
  • Flucytosine / therapeutic use
  • Fluorouracil / metabolism
  • Gene Expression Regulation, Bacterial / drug effects
  • Genes, Bacterial / genetics
  • Humans
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Microbial Sensitivity Tests
  • Oligopeptides / biosynthesis
  • Pseudomonas Infections / drug therapy
  • Pseudomonas Infections / microbiology
  • Pseudomonas Infections / pathology
  • Pseudomonas aeruginosa / drug effects*
  • Pseudomonas aeruginosa / genetics
  • Pseudomonas aeruginosa / pathogenicity*
  • Sigma Factor / metabolism
  • Transcription, Genetic / drug effects
  • Virulence / drug effects
  • Virulence / genetics

Substances

  • Antifungal Agents
  • Bacterial Proteins
  • Oligopeptides
  • PvdS protein, Pseudomonas aeruginosa
  • Sigma Factor
  • pyoverdin
  • Flucytosine
  • Fluorouracil