Fluorescence assay to predict activity of the glycopeptide antibiotics

J Antibiot (Tokyo). 2019 Feb;72(2):114-117. doi: 10.1038/s41429-018-0120-5. Epub 2018 Nov 30.

Abstract

Here, we describe a fluorescent assay developed to study competitive binding of the glycopeptide antibiotics to live bacteria cells. This assay demonstrated that the mechanism of action of the lipoglycopeptide antibiotics strongly depends on the hydrophobicity of the substitutes, with the best antibacterial activity of the glycopeptide antibiotics equally sharing properties of binding to D-Ala-D-Ala residues of the nascent peptidoglycan and to the membrane.

MeSH terms

  • Anti-Bacterial Agents / metabolism*
  • Cell Wall / microbiology
  • Enterococcus faecium / metabolism*
  • Fluorescence
  • Glycopeptides / metabolism
  • Lipoglycopeptides / chemistry
  • Lipoglycopeptides / metabolism*
  • Microbial Sensitivity Tests
  • Peptidoglycan / metabolism*
  • Protein Binding / physiology
  • Rhodamines / chemistry
  • Staining and Labeling
  • Staphylococcus aureus / metabolism*
  • Teicoplanin / analogs & derivatives*
  • Teicoplanin / chemistry
  • Teicoplanin / metabolism*
  • Vancomycin / chemistry
  • Vancomycin / metabolism*
  • Vancomycin-Resistant Enterococci / metabolism*

Substances

  • Anti-Bacterial Agents
  • Glycopeptides
  • Lipoglycopeptides
  • Peptidoglycan
  • Rhodamines
  • Teicoplanin
  • Vancomycin
  • dalbavancin
  • rhodamine isothiocyanate
  • oritavancin