A biophysical approach to phospholipase A(2) activity and inhibition by anti-inflammatory drugs

• Type: Article in International Scientific Journal
• Date: 2010

Authors

Diana Gaspar (Author) Other; Marlene Lucio (Author) FEUP; Kerstin Wagner (Author) Other; Gerald Brezesinski (Author) Other; Sandra Rocha (Author) Other; Costa Lima, JLFC (Author) FFUP; Salette Reis (Author) FFUP

Journal

Title: Biophysical Chemistry

Vol. 152 No. 1-3

Pages: 109-117

ISSN: 0301-4622

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 11 Citations

ISI Web of Science

Scopus - 13 Citations

Pubmed / Medline

Scientific classification

FOS: Natural sciences > Chemical sciences

CORDIS: Health sciences > Pharmacological sciences > Pharmacy

Other information

Authenticus ID: P-003-18A

DOI: 10.1016/j.bpc.2010.08.006

Resumo (PT): The present study describes the interaction of two nonsteroidal anti-inflammatory drugs (ibuprofen and piroxicam) with PLA2 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 PLA2. 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 PLA2 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. <br> <br> Keywords: sPLA2; NSAIDs; Enzymatic inhibition; Membrane model systems; Membrane biophysical properties <br> <a target="_blank" href="http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TFB-50VTWPS-1&_user=2460038&_coverDate=11%2F30%2F2010&_rdoc=14&_fmt=high&_orig=browse&_origin=browse&_zone=rslt_list_item&_srch=doc-info(%23toc%235222%232010%23998479998%232591770%23FLA%23display%23Volume)&_cdi=5222&_sort=d&_docanchor=&_ct=23&_acct=C000057398&_version=1&_urlVersion=0&_userid=2460038&md5=68065802c6c489427c34957b2d303256&searchtype=a "> Texto integral </a> <br> <br>

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9