Substitutions of amino acids in alpha-helix-4 of gyrase A confer fluoroquinolone resistance on Clostridium perfringens

Arch Microbiol. 2007 Feb;187(2):137-44. doi: 10.1007/s00203-006-0180-y. Epub 2006 Oct 19.

Abstract

DNA gyrase, an essential enzyme that regulates DNA topology in bacteria, is the target of fluoroquinolones. Three fluoroquinolone-resistant mutants derived from one strain of Clostridium perfringens had amino acid substitutions of glycine 81 to cysteine, aspartic acid 87 to tyrosine, or both, in alpha-helix-4 of gyrase A. The gyrase mutations affected the growth kinetics of mutants differently when the mutants were exposed to increasing concentrations of gatifloxacin and ciprofloxacin. Fluoroquinolone concentration-dependent effects observed during growth in the exponential and stationary phases depended on the presence of particular gyrA mutations. Introduction of a wild-type gyrA gene into the mutants enhanced their susceptibility to fluoroquinolones and decreased their growth rates proportional to increases in fluoroquinolone concentrations. Amino acid substitutions in alpha-helix-4 of gyrase A protected C. perfringens from fluoroquinolones, and a strain with two substitutions was the most resistant.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Substitution / drug effects
  • Amino Acid Substitution / genetics
  • Anti-Infective Agents / pharmacology*
  • Clostridium perfringens / drug effects*
  • Clostridium perfringens / enzymology
  • Clostridium perfringens / metabolism
  • DNA Gyrase / genetics
  • DNA Gyrase / physiology*
  • DNA, Bacterial / chemistry
  • DNA, Bacterial / genetics
  • Drug Resistance, Bacterial / genetics*
  • Fluoroquinolones / pharmacology
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • DNA, Bacterial
  • Fluoroquinolones
  • DNA Gyrase