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New antimicrobial cystatin C-based peptide active against gram-positive bacterial pathogens, including methicillin-resistant Staphylococcus aureus and multiresistant coagulase-negative staphylococci

Författare

Summary, in English

We describe the synthesis and antibacterial properties of a novel antimicrobial peptidyl derivative, (2S)-2-(Nalpha-benzyloxycarbonyl-arginyl-leucylamido-1-[(E)-cinnamoylamido]-3-methylbutane, structurally based upon the inhibitory centre of the human cysteine protease inhibitor, cystatin C. The derivative, here called Cystapep 1, displayed antibacterial activity against several clinically important gram-positive bacteria. It displayed minimal inhibitory and bactericidal concentrations of about 16 microg/ml for both Staphylococcus aureus and Streptococcus pyogenes. In radial agar diffusion assays, groups A, B, C and G streptococci as well as staphylococci were generally susceptible to the action of Cystapep 1, whereas pneumococci and enterococci were less susceptible. No activity against gram-negative bacteria was observed. Cystapep 1 also showed high activity against methicillin-resistant S. aureus (MRSA) and multiantibiotic-resistant coagulase-negative staphylococci (CNS), suggesting that its mechanism of action differs from those of most currently used antibiotics.

Publiceringsår

2003-11

Språk

Engelska

Sidor

1004-1010

Publikation/Tidskrift/Serie

APMIS : acta pathologica, microbiologica, et immunologica Scandinavica

Volym

111

Issue

11

Dokumenttyp

Artikel i tidskrift

Förlag

John Wiley & Sons Inc.

Ämne

  • Microbiology in the medical area
  • Medicinal Chemistry
  • Pharmacology and Toxicology

Nyckelord

  • Anti-Bacterial Agents
  • Cystatin C
  • Cystatins
  • Dipeptides
  • Drug Resistance, Multiple, Bacterial
  • Gram-Positive Cocci
  • Humans
  • Methicillin Resistance
  • Microbial Sensitivity Tests
  • Oligopeptides
  • Staphylococcus aureus
  • Streptococcus pyogenes
  • Journal Article
  • Research Support, Non-U.S. Gov't

Status

Published

Forskningsgrupp

  • Cystatin C, renal disease, amyloidosis and antibiotics

ISBN/ISSN/Övrigt

  • ISSN: 1600-0463