Structural effects in vitro of the anti-inflammatory drug diclofenac on human erythrocytes and molecular models of cell membranes |
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Authors: | Mario Suwalsky Marcela Manrique Fernando Villena Carlos P. Sotomayor |
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Affiliation: | 1. Faculty of Chemical Sciences, University of Concepción, Concepción, Chile;2. University of Antioquia, Faculty of Exact and Natural Sciences, Medellín, Colombia;3. Faculty of Biological Sciences, University of Concepción, Concepción, Chile;4. Institute of Chemistry, Catholic University of Valparaíso, Valparaíso, Chile |
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Abstract: | Diclofenac, a nonsteroidal anti-inflammatory drug (NSAID), has been widely investigated in terms of its pharmacological action, but less is known about its effects on cell membranes and particularly on those of human erythrocytes. In the present work, the structural effects on the human erythrocyte membrane and molecular models have been investigated and reported. This report presents the following evidence that diclofenac interacts with red cell membranes: a) X-ray diffraction and fluorescence spectroscopy of phospholipid bilayers showed that diclofenac interacted with a class of lipids found in the outer moiety of the erythrocyte membrane; b) in isolated unsealed human erythrocyte membranes (IUM) the drug induced a disordering effect on the acyl chains of the membrane lipid bilayer; c) in scanning electron microscopy (SEM) studies on human erythrocytes it was observed that the drug induced changes different from the normal biconcave morphology of most red blood cells. This is the first time in which structural effects of diclofenac on the human erythrocyte membrane have been described. |
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Keywords: | NSAIDs, nonsteroidal anti-inflammatory drugs DMPC, dimyristoylphosphatidylcholine DMPE, dimyristoylphosphatidylethanolamine SEM, scanning electron microscopy LUV, large unilamellar vesicles r, fluorescence anisotropy GP, generalized polarization DPH, 1,6-diphenyl-1,3,5-hexatriene laurdan, 6-dodecanoyl-2-dimethylaminonaphtalene IUM, isolated unsealed human erythrocyte membrane RBCS, red blood cells suspension |
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