Self-assembling lipopeptides with a potent activity against Gram-positive bacteria, including multidrug resistant strains

Nanomedicine (Lond). 2015 Nov;10(22):3359-71. doi: 10.2217/nnm.15.137.


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.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Gram-Positive Bacteria / drug effects*
  • Hemolysis / drug effects
  • Hep G2 Cells
  • Humans
  • Lipopeptides / administration & dosage*
  • Lipopeptides / chemical synthesis
  • Lipopeptides / chemistry*
  • Lipopeptides / ultrastructure
  • Microbial Sensitivity Tests
  • Microscopy, Electron, Transmission
  • Neoplasms / drug therapy


  • Anti-Bacterial Agents
  • Lipopeptides