Discovery of potent antimicrobial peptide analogs of Ixosin-B

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4185-8. doi: 10.1016/j.bmcl.2012.04.018. Epub 2012 Apr 20.

Abstract

Antimicrobial peptides (AMPs) represent the first defense line against infection when organisms are infected by pathogens. These peptides are generally good targets for the development of antimicrobial agents. Peptide amide analogs of Ixosin-B, an antimicrobial peptide with amino acid sequence of QLKVDLWGTRSGIQPEQHSSGKSDVRRWRSRY, were designed, synthesized and examined for antimicrobial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Within the peptides synthesized, we discovered an 11-mer peptide, KRLRRVWRRWR-amide, which exhibited potent antimicrobial activity while very little hemolytic activity in human erythrocytes was observed even at high dose level (100 μM). With further modifications, this peptide could be developed into a potent antimicrobial agent in the future.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Antimicrobial Cationic Peptides / chemical synthesis*
  • Antimicrobial Cationic Peptides / pharmacology
  • Erythrocytes / drug effects
  • Escherichia coli / drug effects*
  • Escherichia coli / growth & development
  • Hemolysis
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Molecular Sequence Data
  • Protein Structure, Secondary
  • Pseudomonas aeruginosa / drug effects*
  • Pseudomonas aeruginosa / growth & development
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / growth & development
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Antimicrobial Cationic Peptides