In vitro activity and potency of an intravenously injected antimicrobial peptide and its DL amino acid analog in mice infected with bacteria.
We report that intravenous injection (3 mg/kg of body weight twice daily) of a diastereomer (containing 33% D amino acids) of an antimicrobial peptide, K6L9 (LKLLKKLLKKLLKLL-NH2), but not the all-L-amino-acid parental peptide, cures neutropenic mice infected with gentamicin-sensitive Pseudomonas aeruginosa and gentamicin-resistant Acinetobacter baumannii bacteria. Various biophysical experiments suggest a membranolytic-like effect.
Braunstein
Amir
A
Department of Biological Chemistry, The Weizmann Institute of Science, Rehovot, Israel.
Papo
Niv
N
Shai
Yechiel
Y
D000151:Acinetobacter Infections / Q000188:drug therapy / Q000382:microbiology; D040981:Acinetobacter baumannii / Q000187:drug effects; D000596:Amino Acids / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002462:Cell Membrane / Q000187:drug effects; D024881:Drug Resistance, Bacterial; D005260:Female; D005839:Gentamicins / Q000494:pharmacology; D007275:Injections, Intravenous; D051379:Mice; D018613:Microscopy, Confocal; D009503:Neutropenia / Q000382:microbiology; D010455:Peptides / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D011552:Pseudomonas Infections / Q000188:drug therapy / Q000382:microbiology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013237:Stereoisomerism; D014357:Trypsin / Q000494:pharmacology
D000596:Amino Acids; D000900:Anti-Bacterial Agents; D005839:Gentamicins; D010455:Peptides; D014357:Trypsin