Self-assembling lipopeptides with a potent activity against Gram-positive bacteria, including multidrug resistant strains. (November 2015)

• Record Type: Journal Article
• Authors: Azmi, Fazren; Elliott, Alysha G; Khalil, Zeinab G; Hussein, Waleed M; Kavanagh, Angela; Huang, Johnny X; Quezada, Michelle; Blaskovich, Mark AT; Capon, Robert J; Cooper, Matthew A; Skwarczynski, Mariusz; Toth, Istvan
• Is Part Of: Nanomedicine. Volume 10:Number 22(2015)
• Page Start: 3359
• Page End: 3371
• Publication Date: 2015-11
• Subjects: antibacterial activity -- Gram-positive bacteria -- lipopeptides -- multidrug resistant -- nanoparticles -- self-assembly; Nanotechnology -- Periodicals; Medical technology -- Periodicals; Nanotechnology -- Therapeutic use -- Periodicals; 610.28
• DOI: 10.2217/nnm.15.137
• Languages: English
• ISSNs: 1743-5889

Abstract

Aim: To explore the potential of de novo designed cyclic lipopeptides and its linear counterparts as antibacterial agents.Materials & methods: The lipopeptides were synthesized via solid-phase peptide synthesis and the cyclization was achieved by using succinic acid linker. The antimicrobial activities of the lipopeptides were evaluated in vitro against a variety selection of Gram-negative and Gram-positive bacteria including clinical isolates of multidrug-resistant strains.Results: The synthesized lipopeptides were able to self-assemble into nanoparticles in an aqueous environment, with three exhibiting potent antibacterial activity against Gram-positive bacteria, including clinically relevant multidrug-resistant bacteria.Conclusion: The lead compounds have the potential to be developed as new antibacterials that are effective against Gram-positive bacteria, including multidrug-resistant isolates.