Impact of qnrA1, qnrB1 and qnrS1 on the efficacy of ciprofloxacin and levofloxacin in an experimental pneumonia model caused by Escherichia coli with or without the GyrA mutation Ser83Leu

J Antimicrob Chemother. 2013 Jul;68(7):1609-15. doi: 10.1093/jac/dkt063. Epub 2013 Mar 14.

Abstract

Objectives: The aim of this study was to evaluate the impact of qnrA1, qnrB1 and qnrS1 on the in vivo efficacies of ciprofloxacin and levofloxacin in an experimental model of pneumonia caused by Escherichia coli.

Methods: Two isogenic groups of E. coli transformants, based on two ATCC 25922 strains, with or without the GyrA mutation Ser83Leu, and carrying qnrA1, qnrB1 or qnrS1, were used in an experimental pneumonia model. The efficacies of ciprofloxacin (40 mg/kg/day) and levofloxacin (50 and 150 mg/kg/day) were evaluated.

Results: For the pneumonia caused by the parental strains lacking qnr genes, both fluoroquinolones significantly (P<0.05) reduced the bacterial lung concentration by >7 log10 cfu/g against E. coli ATCC/pBK and between 5.09 and 6.34 log10 cfu/g against E. coli ATCC-S83L/pBK. The presence of any qnr genes in the strains of both isogenic groups diminished the reduction of bacterial lung concentration with any therapy (P<0.05). Furthermore, all therapeutic schemes reduced the percentage of positive blood cultures in both isogenic groups (P<0.05). Finally, the survival results suggest a higher mortality with the strains expressing qnr genes.

Conclusions: The presence of qnrA1, qnrB1 and qnrS1 in E. coli reduced the efficacy of ciprofloxacin and levofloxacin in a murine pneumonia model.

Keywords: Enterobacteriaceae; mouse model; pharmacodynamics; pharmacokinetics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Ciprofloxacin / administration & dosage*
  • DNA Gyrase / genetics
  • Disease Models, Animal
  • Drug Resistance, Bacterial
  • Escherichia coli / drug effects*
  • Escherichia coli / genetics
  • Escherichia coli Infections / drug therapy*
  • Escherichia coli Infections / microbiology
  • Escherichia coli Proteins / genetics*
  • Female
  • Levofloxacin / administration & dosage*
  • Mice
  • Mice, Inbred C57BL
  • Mutant Proteins / genetics
  • Pneumonia, Bacterial / drug therapy*
  • Pneumonia, Bacterial / microbiology
  • Treatment Outcome

Substances

  • Anti-Bacterial Agents
  • Escherichia coli Proteins
  • Mutant Proteins
  • Qnr protein, E coli
  • Ciprofloxacin
  • Levofloxacin
  • DNA Gyrase