Antibacterial activity of bactenecin 5 fragments and their interaction with phospholipid membranes

J Pept Sci. 2001 Jun;7(6):297-304. doi: 10.1002/psc.317.

Abstract

Bactenecin 5 (Bac 5) is an antibacterial 43mer peptide isolated from bovine neutrophils. It consists of an Arg-rich N-terminal region and successive repeats of Arg-Pro-Pro-Ile (or Phe). We synthesized Bac 5(1-23) and several related peptides to clarify the roles these regions play in antibacterial activity. An assay of antibacterial activity revealed that such activity requires the presence of Arg residues at or near the N-terminus, as well as a chain length exceeding 15 residues. None of the peptides exhibited haemolytic activity. Polyproline II-like CD curves were observed for most of the peptides. Measurements of the membrane perturbation and fusion indicated that the perturbation and fusogenic activities of the peptides were, generally, parallel to their antibacterial activities. Amino acid substitution in the repeating region had some effect on antibacterial activity.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism*
  • Anti-Bacterial Agents / pharmacology*
  • Arginine / metabolism
  • Cattle
  • Circular Dichroism
  • Fluoresceins / metabolism
  • Hemolysis / drug effects
  • Lipid Bilayers / chemistry
  • Lipid Bilayers / metabolism
  • Liposomes / chemistry
  • Liposomes / metabolism
  • Membrane Fusion / drug effects
  • Molecular Weight
  • Peptide Fragments / chemical synthesis
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism*
  • Peptide Fragments / pharmacology*
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / metabolism*
  • Peptides, Cyclic / pharmacology*
  • Phospholipids / metabolism*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Fluoresceins
  • Lipid Bilayers
  • Liposomes
  • Peptide Fragments
  • Peptides, Cyclic
  • Phospholipids
  • bactenecin
  • Arginine
  • fluorexon