Synchrotron SAXS and WAXS Study of the Interactions of NSAIDs with Lipid Membranes

• Tipo: Artigo em Revista Científica Internacional
• Data: 2011

Autores

Claudia Nunes (Autor) Outra; Gerald Brezesinski (Autor) Outra; Jose L F C Lima (Autor) FFUP; Salette Reis (Autor) FFUP; Marlene Lucio (Autor) FEUP

Revista

Título: Journal of Physical Chemistry B

Vol. 115 Nº 24

Páginas: 8024-8032

ISSN: 1520-6106

Editora: American Chemical Society

Indexação

ISI Web of Knowledge - 30 Citações

ISI Web of Science

Scopus - 37 Citações

Pubmed / Medline

Classificação Científica

CORDIS: Ciências Físicas > Química > Química analítica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-002-QDH

DOI: 10.1021/jp2025158

Resumo (PT): Cell membranes often constitute the first biological structure encountered by drugs, and binding or interactions of drugs with lipid components of the membrane may explain part of their mechanism of activity or their side effects. The present study provides evidence of alterations in the structural properties of phospholipid bilayers at acidic conditions that can be correlated with the mechanism of action of nonsteroidal anti-inflammatory drugs (NSAIDs) and with their local action effect on the gastrointestinal tract lipids, aiming a molecular biophysical approach to the interaction of these drugs with lipid membranes. In this context, the structural modifications of the 1,2-dipalmitoyl-sn-glycero-3-phosphocholine bilayers at pH 5.0, induced by increasing concentrations of five NSAIDs (piroxicam, meloxicam, tolmetin, indomethacin, and nimesulide), were studied by small-angle and wide-angle X-ray scattering. Results obtained highlight the effect of each NSAID in modulating the membrane structure properties. All the NSAIDs promoted distinct biophysical effects by perturbing the membrane arrangement to different degrees that are intimately related to their different physicochemical properties as well as with the initial organization of the lipids, depending if they are in the gel (Lβˈ) or in the liquid-crystalline phase (Lα). <br> <br> <a target="_blank" href="http://pubs.acs.org/doi/abs/10.1021/jp2025158 "> Texto integral </a> <br> <br>

Abstract (EN): Cell membranes often constitute the first biological structure encountered by drugs, and binding or interactions of drugs with lipid components of the membrane may explain part of their mechanism of activity or their side effects. The present study provides evidence of alterations in the structural properties of phospholipid bilayers at acidic conditions that can be correlated with the mechanism of action of nonsteroidal anti-inflammatory drugs (NSAIDs) and with their local action effect on the gastrointestinal tract lipids, aiming a molecular biophysical approach to the interaction of these drugs with lipid membranes. In this context, the structural modifications of the 1,2-dipalmitoyl-sn-glycero-3-phosphocholine bilayers at pH 5.0, induced by increasing concentrations of five NSAIDs (piroxicam, meloxicam, tolmetin, indomethacin, and nimesulide), were studied by small-angle and wide-angle X-ray scattering. Results obtained highlight the effect of each NSAID in modulating the membrane structure properties. All the NSAIDs promoted distinct biophysical effects by perturbing the membrane arrangement to different degrees that are intimately related to their different physicochemical properties as well as with the initial organization of the lipids, depending if they are in the gel (L-beta) or in the liquid-crystalline phase (L-alpha).

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 9