Effect of nonsteroidal anti-inflammatory drugs on the cellular membrane fluidity

• Type: Article in International Scientific Journal
• Date: 2008

Authors

Celia Sousa (Author) Other; Claudia Nunes (Author) Other; Marlene Lucio (Author) FFUP; Helena Ferreira (Author) Other; Jose L F C Lima (Author) FFUP; Joana Tavares (Author) FFUP; Anabela Cordeiro Da Silva (Author) FFUP; Salette Reis (Author) FFUP

Journal

Title: Journal of Pharmaceutical Sciences

Vol. 97 No. 8

Pages: 3195-3206

ISSN: 0022-3549

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 29 Citations

ISI Web of Science

Scopus - 31 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

CORDIS: Health sciences

Other information

Authenticus ID: P-003-XFQ

DOI: 10.1002/jps.21218

Resumo (PT): In this work, fluorescence measurements were performed using the fluorescent probe 1,6-diphenyl-1,3,5-hexatriene (DPH) to evaluate the effects of the interaction of nonsteroidal anti-inflammatory drugs - NSAIDs (meloxicam, lornoxicam, and nimesulide) with several membrane systems (liposomes with and without cholesterol, mouse splenocytes, mouse macrophages cell line - J774, human leukemia monocyte cell line - THP-1, and human granulocytes and mononuclear cells). DPH fluorescence quenching studies revealed that the NSAIDs studied were able to efficiently quench the probe located in membrane hydrocarbon region. Fluorescence anisotropy measurements were also made to investigate the effects on membrane fluidity resulting from the interaction between the drugs and membrane systems. All the anti-inflammatory drugs studied show an increase in the membrane fluidity in a concentration dependent manner. Results obtained provide an insight into NSAIDs capacity to be inserted in lipid bilayers and alter the lipid dynamics. The induced changes in lipid dynamics may modulate the activity of inflammatory enzymes or may be related with deleterious topical action of NSAIDs on gastric phospholipid fluidity <br> <br> Keywords fluorescence spectroscopy • in vitro models • liposomes • drug interactions • NSAID <br> <a target="_blank" href="http://www3.interscience.wiley.com/cgi-bin/fulltext/116840035/HTMLSTART"> Texto integral </a> <br> <br>

Abstract (EN): In this work, fluorescence measurements were performed using the fluorescent probe 1,6-diphenyl-1,3,5-hexatriene (DPH) to evaluate the effects of the interaction of nonsteroidal anti-inflammatory drugs-NSAIDs (meloxicam, lornoxicam, and nimesulide) with several membrane systems (liposomes with and without cholesterol, mouse splenocytes, mouse macrophages cell line-J774, human leukemia monocyte cell line-THP-1, and human granulocytes and mononuclear cells). DPH fluorescence quenching studies revealed that the NSAIDs studied were able to efficiently quench the probe located in membrane hydrocarbon region. Fluorescence anisotropy measurements were also made to investigate the effects on membrane fluidity resulting from the interaction between the drugs and membrane systems. All the anti-inflammatory drugs studied show an increase in the membrane fluidity in a concentration dependent manner. Results obtained provide an insight into NSAIDs capacity to be inserted in lipid bilayers and alter the lipid dynamics. The induced changes in lipid dynamics may modulate the activity of inflammatory enzymes or may be related with deleterious topical action of NSAIDs on gastric phospholipid fluidity. (C) 2007 Wiley-Liss, Inc. and the American Pharmacists Association.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 12