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

Title
Effect of nonsteroidal anti-inflammatory drugs on the cellular membrane fluidity
Type
Article in International Scientific Journal
Year
2008
Authors
Celia Sousa
(Author)
Other
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Claudia Nunes
(Author)
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Marlene Lucio
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Helena Ferreira
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Joana Tavares
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Anabela Cordeiro Da Silva
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Salette Reis
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Journal
Vol. 97 No. 8
Pages: 3195-3206
ISSN: 0022-3549
Publisher: Elsevier
Indexing
Scientific classification
FOS: Natural sciences > Chemical sciences
CORDIS: Health sciences
Other information
Authenticus ID: P-003-XFQ
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
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