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:	SUWALSKY,MARIO, MUÑOZ,MAURICIO, MENNICKENT,SIGRID, SOTOMAYOR,CARLOS P, BOLOGNIN,SILVIA, ZATTA,PAOLO
Lenguaje:	English
Publicado:	Sociedad Chilena de Química 2010
Acceso en línea:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072010000100002
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spelling	oai:scielo:S0717-970720100001000022010-04-29STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELSSUWALSKY,MARIOMUÑOZ,MAURICIOMENNICKENT,SIGRIDSOTOMAYOR,CARLOS PBOLOGNIN,SILVIAZATTA,PAOLOVerapamil 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.info:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.55 n.1 20102010-01-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072010000100002en10.4067/S0717-97072010000100002
institution	Scielo Chile
collection	Scielo Chile
language	English
description	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.
author	SUWALSKY,MARIO MUÑOZ,MAURICIO MENNICKENT,SIGRID SOTOMAYOR,CARLOS P BOLOGNIN,SILVIA ZATTA,PAOLO
spellingShingle	SUWALSKY,MARIO MUÑOZ,MAURICIO MENNICKENT,SIGRID SOTOMAYOR,CARLOS P BOLOGNIN,SILVIA ZATTA,PAOLO STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
author_facet	SUWALSKY,MARIO MUÑOZ,MAURICIO MENNICKENT,SIGRID SOTOMAYOR,CARLOS P BOLOGNIN,SILVIA ZATTA,PAOLO
author_sort	SUWALSKY,MARIO
title	STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
title_short	STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
title_full	STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
title_fullStr	STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
title_full_unstemmed	STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS
title_sort	structural effects of verapamil on cell membranes and molecular models
publisher	Sociedad Chilena de Química
publishDate	2010
url	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072010000100002
work_keys_str_mv	AT suwalskymario structuraleffectsofverapamiloncellmembranesandmolecularmodels AT munozmauricio structuraleffectsofverapamiloncellmembranesandmolecularmodels AT mennickentsigrid structuraleffectsofverapamiloncellmembranesandmolecularmodels AT sotomayorcarlosp structuraleffectsofverapamiloncellmembranesandmolecularmodels AT bologninsilvia structuraleffectsofverapamiloncellmembranesandmolecularmodels AT zattapaolo structuraleffectsofverapamiloncellmembranesandmolecularmodels
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STRUCTURAL EFFECTS OF VERAPAMIL ON CELL MEMBRANES AND MOLECULAR MODELS

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