A biophysical approach to Phospholipase A activity and inhibition by anti-inflammatory drugs

Diana Gaspar , Marlene Lúcio , Kerstin Wagner (1) , Gerald Brezesinski (1) , Sandra Rocha , J.L.F. Costa Lima , Salette Reis

1 Max Planck Institute of Colloids and Interfaces

The present study describes the interaction of two nonsteroidal anti-inflammatory drugs (ibuprofen and piroxicam) with PLA from and seeks to deepen the knowledge about the influence of the biophysical properties of biomembranes, and the inhibitory effect of the drugs on the enzymatic activity. Fluorescent techniques with and without the use of probes, surface pressure/molecular area isotherms, surface pressure/time and molecular area/time measurements combined with circular dichroism spectroscopy and direct techniques of visualization of lipid membranes (Brewster angle microscopy), revealed that both drugs inhibit PLA. Additionally, the structure and characteristics of the lipid bilayer, as well as, the direct interaction of drugs with the enzyme seem to play an important role on the hydrolytic activity of PLA towards membrane model systems. These results open a way of finding new and better strategies that can contribute to the development of suitable agents for relieving inflammatory conditions.

Mots clés: sPLA; NSAIDs; enzymatic inhibition; membrane model systems; membrane biophysical properties

Domaines: Chimie-Physique [physics.chem-ph]

Diana Gaspar, Marlene Lúcio, Kerstin Wagner, Gerald Brezesinski, Sandra Rocha, et al.. A biophysical approach to Phospholipase A activity and inhibition by anti-inflammatory drugs. Biophysical Chemistry, 2010, 152 (1-3), pp.109. ⟨10.1016/j.bpc.2010.08.006⟩. ⟨hal-00694282⟩