STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
Verapamil is one of the frequently prescribed calcium channel blockers used in the treatment of hypertension and angina pectoris. Results of evaluations of the therapy have led to reports of toxic effects. This study presents several evidences that verapamil affects human cells. Scanning electrón mi...
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| Autores principales: | , , , , , |
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| Lenguaje: | English |
| Publicado: |
Sociedad Chilena de Química
2010
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| Acceso en línea: | http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072010000100002 |
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| Sumario: | Verapamil is one of the frequently prescribed calcium channel blockers used in the treatment of hypertension and angina pectoris. Results of evaluations of the therapy have led to reports of toxic effects. This study presents several evidences that verapamil affects human cells. Scanning electrón microscopy observations of intact human erythrocytes indicated that they underwent morphological alterations as increasing verapamil concentrations starting from 5 µM changed their discoid normal shape, and finally to hemolysis. Fluorescence spectroscopy on isolated unsealed human erythrocyte membranes confirmed these outcomes. In fact, the assays showed that verapamil induced a significant increase of the anisotropy parameters and a modérate one of the generalized polarization, indicative of enhanced order at the acyl chain and polar head regions of the erythrocyte membrane lipid bilayer. X-ray diffraction experiments on dimyristoylphosphatidylcholine and dimyristoylphosphatidylethanolamine bilayers, classes of the major phospholipids present in both outer and inner sides of the erythrocyte membrane, respectively showed that verapamil perturbed the polar head and acyl chain regions of both lipid bilayers. These interactions were found to be stronger with DMPC bilayers. On the other hand, human SH-SY5Y neuroblastoma cells incubated with verapamil suffered a sharp decrease of cell viability. |
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