New antimicrobial cystatin C-based peptide active against gram-positive bacterial pathogens, including methicillin-resistant Staphylococcus aureus and multiresistant coagulase-negative staphylococci
Author
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.
Publishing year
2003-11
Language
English
Pages
1004-1010
Publication/Series
APMIS : acta pathologica, microbiologica, et immunologica Scandinavica
Volume
111
Issue
11
Full text
- Available as PDF - 73 kB
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Links
Document type
Journal article
Publisher
John Wiley & Sons Inc.
Topic
- Microbiology in the medical area
- Medicinal Chemistry
- Pharmacology and Toxicology
Keywords
- 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
Research group
- Cystatin C, renal disease, amyloidosis and antibiotics
ISBN/ISSN/Other
- ISSN: 1600-0463