Structure-activity studies of echinomycin antibiotics against drug-resistant and biofilm-forming Staphylococcus aureus and Enterococcus faecalis

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1504-7. doi: 10.1016/j.bmcl.2009.01.010. Epub 2009 Jan 10.

Abstract

Four echinomycin antibiotics were isolated from the culture broth of a marine streptomycete, and their structures were determined by a combination of chemical and spectroscopic analyses. Antibiotic activities were measured against drug-resistant and biofilm-forming strains of Staphylococcus aureus and Enterococcus faecalis. Minimum inhibitory concentrations ranging from 0.01 microM to greater than 14 microM clearly defined structure-activity relationships for antibiotic potency. Echinomycin was the most active compound with a MIC of 0.03 microM against methicillin-resistant S. aureus and 0.01 microM against biofilm-forming E. faecalis.

Publication types

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

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Drug Resistance, Multiple, Bacterial / physiology
  • Echinomycin / chemistry*
  • Echinomycin / isolation & purification
  • Echinomycin / pharmacology
  • Enterococcus faecalis / drug effects*
  • Enterococcus faecalis / growth & development
  • HCT116 Cells
  • Humans
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Methicillin-Resistant Staphylococcus aureus / growth & development
  • Microbial Sensitivity Tests / methods
  • Spectrometry, Mass, Electrospray Ionization
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / growth & development
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Echinomycin