Design of antimicrobially active small amphiphilic peptide dendrimers.
Novel polyfunctional small amphiphilic peptide dendrimers characterized by incorporation of a new core compounds - tris-amino acids or tetrakis-amino alcohols that originated from a series of basic amino acids - were efficiently synthesized. These new core elements yielded molecules with multiple branching and (+5)/(+6) charge at the 1-st dendrimer generation. Dendrimers exhibited significant antimicrobial potency against Gram(+) and Gram(-) strains involving also multiresistant reference strains (S. aureus ATCC 43300 and E. coli ATCC BAA-198). In addition, high activity against fungi from the Candida genus was detected. More charged and more hydrophobic peptide dendrimers expressed hemolytic properties.
Polcyn
Piotr
P
Institute of Organic Chemistry PAS, Kasprzaka Str. 44/52 01-224 Warsaw, Poland. polcynp@icho.edu.pl
Jurczak
Margarita
M
Rajnisz
Aleksandra
A
Solecka
Jolanta
J
Urbanczyk-Lipkowska
Zofia
Z
D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002175:Candida / Q000187:drug effects*; D002478:Cells, Cultured; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D053878:Hemolytic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans
D023181:Antimicrobial Cationic Peptides; D050091:Dendrimers; D053878:Hemolytic Agents