Document Detail

A biophysical approach to phospholipase A2 activity and inhibition by anti-inflammatory drugs.
MedLine Citation:
PMID:  20846779     Owner:  NLM     Status:  In-Process    
The present study describes the interaction of two nonsteroidal anti-inflammatory drugs (ibuprofen and piroxicam) with PLA(2) from Naja mossambica mossambica 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(2). 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(2) 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.
Diana Gaspar; Marlene Lúcio; Kerstin Wagner; Gerald Brezesinski; Sandra Rocha; J L F Costa Lima; Salette Reis
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-08-25
Journal Detail:
Title:  Biophysical chemistry     Volume:  152     ISSN:  1873-4200     ISO Abbreviation:  Biophys. Chem.     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-08     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0403171     Medline TA:  Biophys Chem     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  109-17     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Elsevier B.V. All rights reserved.
REQUIMTE, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha 164, 4090-030 Porto, Portugal.
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