Antibacterial activity of bactenecin 5 fragments and their interaction with phospholipid membranes.
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.
Tokunaga
Y
Y
Department of Applied Chemistry, Faculty of Engineering, Nagasaki University, Japan.
Niidome
T
T
Hatakeyama
T
T
Aoyagi
H
H
D000595:Amino Acid Sequence; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D001120:Arginine / Q000378:metabolism; D002417:Cattle; D002942:Circular Dichroism; D005452:Fluoresceins / Q000378:metabolism; D006461:Hemolysis / Q000187:drug effects; D008051:Lipid Bilayers / Q000737:chemistry / Q000378:metabolism; D008081:Liposomes / Q000737:chemistry / Q000378:metabolism; D008561:Membrane Fusion / Q000187:drug effects; D008970:Molecular Weight; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D010743:Phospholipids / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D005452:Fluoresceins; D008051:Lipid Bilayers; D008081:Liposomes; D010446:Peptide Fragments; D010456:Peptides, Cyclic; D010743:Phospholipids; C056454:bactenecin; D001120:Arginine; C007740:fluorexon