Novel synthetic antimicrobial peptides effective against methicillin-resistant Staphylococcus aureus.
Previously, we identified a core undecapeptide of sapecin B having antimicrobial activity. Based on the structure of this peptide, we systematically synthesized peptides consisting of terminal basic motifs and internal oligo-leucine sequences and examined their antimicrobial activities. Of these peptides, RLKLLLLLRLK-NH2 and KLKLLLLLKLK-NH2 were found to have potent microbicidal activity against Staphylococcus aureus, Escherichia coli, methicillin-resistant S. aureus and Candida albicans in liquid medium. We also synthesized the D-enantiomer of KLKLLLLLKLK-NH2. This enantiomer was resistant to tryptic digestion and persisted longer in the culture medium, showing greater antimicrobial activity than the original peptide.
Alvarez-Bravo
J
J
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Kurata
S
S
Natori
S
S
D000595:Amino Acid Sequence; D000818:Animals; D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000494:pharmacology*; D005947:Glucose / Q000378:metabolism; D008081:Liposomes; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000378:metabolism / Q000494:pharmacology*; D010743:Phospholipids / Q000378:metabolism; D013211:Staphylococcus aureus / Q000187:drug effects*; D013237:Stereoisomerism
D000900:Anti-Bacterial Agents; D008081:Liposomes; D010446:Peptide Fragments; D010743:Phospholipids; D005947:Glucose