Biological properties of low molecular mass peptide dendrimers.
A series of new, low molecular mass, lysine-based peptide dendrimers with varying distribution of cationic and aromatic groups in the structure were synthesized. They expressed antimicrobial activity against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria as well as against fungal pathogens (Candida albicans). Their cytotoxic, haematotoxic, and genotoxic effects were studied. It appears that degree of branching and steric distribution and types of hydrophobic (aromatic) groups and cationic centres are important components of dendrimeric structure and influence both antimicrobial potency and toxicity. Such 3D structure of our dendrimers mimics that of the natural antimicrobial peptides and can be achieved by application of dendrimer chemistry.
Klajnert
B
B
Department of General Biophysics, University of Lodz, 90-237 Lodz, Poland.
Janiszewska
J
J
Urbanczyk-Lipkowska
Z
Z
Bryszewska
M
M
Shcharbin
D
D
Labieniec
M
M
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006224:Cricetinae; D004247:DNA / Q000737:chemistry; D050091:Dendrimers / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008239:Lysine / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D008970:Molecular Weight; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D011487:Protein Conformation; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development
D000890:Anti-Infective Agents; D050091:Dendrimers; D009842:Oligopeptides; D004247:DNA; D008239:Lysine