Design of antimicrobially active small amphiphilic peptide dendrimers

Molecules. 2009 Sep 29;14(10):3881-905. doi: 10.3390/molecules14103881.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimicrobial Cationic Peptides / chemical synthesis
  • Antimicrobial Cationic Peptides / chemistry*
  • Antimicrobial Cationic Peptides / pharmacology
  • Candida / drug effects*
  • Cells, Cultured
  • Dendrimers / chemical synthesis
  • Dendrimers / chemistry*
  • Dendrimers / pharmacology
  • Drug Design*
  • Gram-Negative Bacteria / drug effects*
  • Gram-Positive Bacteria / drug effects*
  • Hemolytic Agents / chemical synthesis
  • Hemolytic Agents / chemistry
  • Hemolytic Agents / pharmacology
  • Humans

Substances

  • Antimicrobial Cationic Peptides
  • Dendrimers
  • Hemolytic Agents