Membrane effects of trifluoperazine, dibucaine and praziquantel on human erythrocytes

dc.creatorMalheiros, SVP
dc.creatorBrito, MA
dc.creatorBrites, D
dc.creatorMeirelles, NC
dc.date2000
dc.dateMAY 1
dc.date2014-12-02T16:29:57Z
dc.date2015-11-26T17:38:27Z
dc.date2014-12-02T16:29:57Z
dc.date2015-11-26T17:38:27Z
dc.date.accessioned2018-03-29T00:20:05Z
dc.date.available2018-03-29T00:20:05Z
dc.identifierChemico-biological Interactions. Elsevier Sci Ireland Ltd, v. 126, n. 2, n. 79, n. 95, 2000.
dc.identifier0009-2797
dc.identifierWOS:000087275300001
dc.identifier10.1016/S0009-2797(00)00150-2
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/53580
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/53580
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/53580
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1286213
dc.descriptionTrifluoperazine (TFP) is a potent antipsychotic agent, dibucaine (DBC) is a local anaesthetic and praziquantel (PZQ) is a highly effective agent against schistosomiasis. The present work was conducted to (i) investigate the cytotoxic effects of TFP, DEC and PZQ on human erythrocyte membranes; and (ii) compare the alterations induced by the cationic drugs (TFP and DEC) with those induced by the uncharged compound (PZQ), in an attempt to have a better insight on the pathways of each drug-membrane interaction. The erythrocyte morphological alterations induced by sublytic concentrations of TFP, DEC and PZQ were evaluated by scanning electron microscopy and expressed quantitatively by the morphological index. Haemolysis and release of membrane lipids (phospholipids and cholesterol) produced by selected concentrations of TFP, DEC and PZQ, were compared with those resulting from the corresponding triple concentrations of each drug. Our results showed that the uncharged molecule of PZQ induces the same morphological alterations (stomatocytosis) as the cationic drugs TFP and DEC. Haemolysis was shown to vary with the drug used and to be concentration-dependent, with values similar to 10-fold more elevated for TFP and DEC than for PZQ, which revealed st maximum of 6% haemolysis for the highest concentration tested. Different concentration-response curves were obtained for lipid elution, although the profiles of cholesterol and phospholipids released were similar for all drugs. Nevertheless, at a fixed rate of 50% haemolysis, TFP induced a similar to 2-fold increment in the elution of cholesterol when compared with that produced by DEC (P < 0.05). The different effects induced by TFP, DEC and PZQ on erythrocyte morphology, haemolysis and lipid exfoliation are related to the physical and chemical characteristics of each compound. These results suggest that distinct cell membrane interaction pathways lead to drug-specific mechanisms of cytotoxicity. (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.
dc.description126
dc.description2
dc.description79
dc.description95
dc.languageen
dc.publisherElsevier Sci Ireland Ltd
dc.publisherClare
dc.publisherIrlanda
dc.relationChemico-biological Interactions
dc.relationChem.-Biol. Interact.
dc.rightsfechado
dc.rightshttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.sourceWeb of Science
dc.subjectdibucaine
dc.subjecterythrocyte morphology
dc.subjecthaemolysis
dc.subjectlipids
dc.subjectpraziquantel
dc.subjecttrifluoperazine
dc.subjectLocal-anesthetic Dibucaine
dc.subjectBiological-membranes
dc.subjectSchistosoma-mansoni
dc.subjectShape Changes
dc.subjectHemolysis
dc.subjectPhenothiazines
dc.subjectPhospholipids
dc.subjectMechanisms
dc.subjectDrugs
dc.titleMembrane effects of trifluoperazine, dibucaine and praziquantel on human erythrocytes
dc.typeArtículos de revistas


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