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Activity of glycopeptides against vancomycin-resistant gram-positive bacteria

T I Nicas1, C T Cole, D A Preston

  • 1Lilly Research Laboratories, Eli Lilly & Co., Indianapolis, Indiana 46285-0438.

Insights

Rare vancomycin-resistant Gram-positive bacteria, including Leuconostoc and emerging Enterococcus strains, show varied resistance. Certain N-substituted vancomycin derivatives effectively combat these resistant bacteria, offering new therapeutic potential.

Area of Science:

  • Microbiology
  • Infectious Diseases
  • Pharmacology

Background:

  • Vancomycin resistance in Gram-positive bacteria is uncommon but includes genera like Leuconostoc, Lactobacillus, Pediococcus, and emerging strains of Enterococcus faecium and Enterococcus faecalis.
  • These resistant strains pose a significant challenge in clinical settings.

Purpose of the Study:

  • To evaluate the activity of vancomycin, teicoplanin, and novel N-substituted vancomycin derivatives against vancomycin-resistant Gram-positive bacteria.
  • To investigate the mechanisms and patterns of vancomycin resistance in different bacterial genera.

Main Methods:

  • Antimicrobial susceptibility testing was performed using vancomycin, teicoplanin, and various vancomycin derivatives.
  • Minimum inhibitory concentrations (MICs) were determined for vancomycin-resistant strains.
  • Antibody-based assays were used to detect specific membrane proteins in resistant bacteria.

Main Results:

  • Vancomycin-resistant Enterococcus faecium and Enterococcus faecalis exhibited cross-resistance to other glycopeptides.
  • Several N-substituted vancomycin derivatives demonstrated potent activity against resistant enterococci, with MICs ranging from 2 to 32 µg/ml.
  • These derivatives also showed activity against intrinsically vancomycin-resistant organisms like Leuconostoc species.
  • Vancomycin resistance was inducible in enterococci but constitutive in Leuconostoc, Lactobacillus, and Pediococcus.
  • No cross-reacting vancomycin-induced membrane protein was detected in non-enterococcal resistant species.

Conclusions:

  • N-substituted vancomycin derivatives represent a promising therapeutic option for infections caused by vancomycin-resistant Gram-positive bacteria.
  • Understanding the distinct mechanisms of vancomycin resistance (inducible vs. constitutive) is crucial for developing targeted treatment strategies.
  • Further research into the specific resistance mechanisms and the development of novel agents is warranted.

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