Liposome destabilization by a 2,7-diazapyrenium derivative through formation of transient pores in the lipid bilayer

Small. 2010 Apr 23;6(8):952-9. doi: 10.1002/smll.200902306.

Abstract

The effect of the luminescent heteroaromatic electron acceptor N,N'-dimethyl-2,7-diazapyrenium dichloride (DM-DAP(2+)) on the stability of 1-palmitoyl-2-oleoylphosphatydilcholine (POPC) liposomes is determined on the basis of the rate of release of different fluorescent probes entrapped within the liposome. The experiments show that DM-DAP(2+) exerts a substantial destabilizing action on the liposomal bilayer, particularly at low concentrations. Molecular dynamics simulations suggest that the activity of DM-DAP(2+) is related to its tendency to surround itself with water molecules, conceivably favoring the formation of transient pores across the bilayer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chromatography, Gel
  • Fluoresceins / chemistry
  • Kinetics
  • Lipid Bilayers / chemistry*
  • Liposomes / chemistry*
  • Molecular Dynamics Simulation
  • Phenanthrolines / chemistry*
  • Phosphatidylcholines / chemistry
  • Physical Phenomena
  • Porosity
  • Rotation
  • Spectrometry, Fluorescence
  • Spectrophotometry, Ultraviolet
  • Water / chemistry

Substances

  • 2,7-diazapyrenium
  • Fluoresceins
  • Lipid Bilayers
  • Liposomes
  • Phenanthrolines
  • Phosphatidylcholines
  • Water
  • 6-carboxyfluorescein
  • 1-palmitoyl-2-oleoylphosphatidylcholine
  • fluorexon