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- Title
Effects of Phospholipase A2 Inhibitors on Bilayer Lipid Membranes.
- Authors
Dubinin, Mikhail; Astashev, Maxim; Penkov, Nikita; Gudkov, Sergey; Dyachenko, Igor; Samartsev, Victor; Belosludtsev, Konstantin; Dubinin, Mikhail V; Astashev, Maxim E; Penkov, Nikita V; Gudkov, Sergey V; Dyachenko, Igor A; Samartsev, Victor N; Belosludtsev, Konstantin N
- Abstract
The work examines the effect of inhibitors of cytosolic Ca(2+)-dependent and Ca(2+)-independent phospholipases A2 on bilayer lipid membranes. It was established that trifluoroperazine (TFP) and, to a lesser extent, arachidonyl trifluoromethyl ketone (AACOCF3) and palmitoyl trifluoromethyl ketone (PACOCF3) were able to permeabilize artificial lipid membranes (BLM and liposomes). It was shown that AACOCF3 lowered the temperature of phase transition of DMPC liposomes, inducing disordering of the hydrophobic region of lipid bilayer. TFP disordered membranes both in the hydrophobic region and in the region of hydrophilic heads, this being accompanied by changes in the membrane permeability: appearance of a channel-like BLM activity and leakage of sulforhodamine B from liposomes. In contrast to AACOCF3 and TFP, PACOCF3 increased membrane orderliness in the hydrophobic region (heightened the temperature of phase transition of DMPC liposomes) and in the region of lipid heads. The effectiveness of AACOCF3 and PACOCF3 as inductors of BLM and liposome permeabilization was considerably lower comparatively to TFP. As revealed by dynamic light scattering, incorporation of TFP, AACOCF3 and PACOCF3 into the membrane of liposomes resulted in the increase of the average size of particles in the suspension, presumably due to their aggregation or fusion. The paper discusses possible mechanisms of the influence of phospholipase A2 inhibitors on bilayer lipid membranes.
- Subjects
PHOSPHOLIPASE A2; ENZYME inhibitors; BILAYER lipid membranes; TRIFLUOPERAZINE; PERMEABILITY (Biology); PHASE transitions; HYDROPHOBIC interactions; CELL physiology; ELECTROPHYSIOLOGY; ESTERASES; FLUORESCENCE spectroscopy; LECITHIN; LIPIDS; ARTIFICIAL membranes; MOLECULAR structure; TEMPERATURE; FLUORESCENT dyes
- Publication
Journal of Membrane Biology, 2016, Vol 249, Issue 3, p339
- ISSN
0022-2631
- Publication type
journal article
- DOI
10.1007/s00232-016-9872-7