Antimicrobial activity of short, synthetic cationic lipopeptides.
The increasing emergence of multidrug-resistant micro-organisms presents one of the greatest challenges in the clinical management of infectious diseases. Therefore, novel antimicrobial agents are urgently required to address this issue. In this report, we describe the solid phase synthesis, characterization, microbiological and toxicological evaluation of a library of ultrashort cationic antimicrobial lipopeptides based on the previously described tetrapeptide amide H-Orn-Orn-Trp-Trp-NH2 conjugated with saturated fatty acids which have inherent antimicrobial activity. The microbiological activity of these ultrashort cationic lipopeptides, which exhibit excellent, broad-spectrum antimicrobial activity against a number of clinically important pathogenic bacteria and fungi, including multidrug resistant micro-organisms in both planktonic and sessile (biofilm) cultures is reported.
Laverty
Garry
G
Biomaterials Research Group, School of Pharmacy, Queens University of Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT97BL, UK.
McLaughlin
Martin
M
Shaw
Christopher
C
Gorman
Sean P
SP
Gilmore
Brendan F
BF
D000595:Amino Acid Sequence; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D026141:Drug Resistance, Multiple, Fungal / Q000187:drug effects; D006461:Hemolysis; D006801:Humans; D055666:Lipopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests
D000890:Anti-Infective Agents; D055666:Lipopeptides