Abstract
A novel dermaseptin peptide, dermaseptin-PT9 (DPT9), was isolated and identified from Phyllomedusa tarsius by the combination of molecular cloning and LC-MS analysis. Chemically synthesised DPT9 was broadly effective against the tested microorganisms through the disruption of cell membranes and showed weak haemolytic activity towards horse erythrocytes. It also exhibited anti-proliferative effect against various human cancer cells. Moreover, an analogue with enhanced cationicity, K8, 23-DPT9, in which Asp8 and Glu23 were substituted by lysine residues, had a markedly increased antimicrobial effect against all tested microorganisms and disrupted microbial cell membranes. This analogue also showed no haemolysis at its effective antimicrobial concentrations. In addition, K8, 23-DPT9 displayed an enhanced anti-proliferative effect against cancer cells, while displayed weak activity against the normal human cell line, HMEC-1.
Keywords:
antimicrobial peptide; dermaseptin; frog skin secretion.
MeSH terms
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Amphibian Proteins / chemistry
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Amphibian Proteins / isolation & purification
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Amphibian Proteins / pharmacology*
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Animals
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / isolation & purification
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Anti-Bacterial Agents / pharmacology*
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Antifungal Agents / chemistry
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Antifungal Agents / isolation & purification
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Antifungal Agents / pharmacology*
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Antimicrobial Cationic Peptides / chemistry
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Antimicrobial Cationic Peptides / isolation & purification
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Antimicrobial Cationic Peptides / pharmacology*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / pharmacology*
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Anura
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Biofilms / drug effects
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Candida albicans / drug effects
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects
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Humans
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Microbial Sensitivity Tests
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Skin / chemistry*
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Skin / metabolism
Substances
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Amphibian Proteins
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Anti-Bacterial Agents
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Antifungal Agents
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Antimicrobial Cationic Peptides
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Antineoplastic Agents
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dermaseptin