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Título : Plasmodium berghei: In vitro and in vivo activity of dequalinium
Autor : Rodrigues, Juan R.
Gamboa, Neira
Palabras clave : Hematinines
Bisquinolines
CQ
chloroquine
DQ
dequalinium
Globin
Heme
LEP
eupeptin
Malaria
P. berghei
Plasmodium berghei
DMSO
dimethyl sulfoxide
Globin
GSH
glutathione
Heme
PEP
pepstatin
PBS
RBC
phosphate-buVered saline
red blood cells
SDS–PAGE
sodium dodecyl sulfate
polyacrylamide gel electrophoresis
Fecha de publicación : 14-Jan-2013
Resumen : Bisquinoline compounds have exhibited remarkable activity in vitro and in vivo against Plasmodium parasites by inhibition of heme detoxiWcation. We have tested the ability of dequalinium 1,1 -(1,10 decanediyl)bis(4-amino-2-methylquinoline), a known antimicrobial agent, to inhibit -hematin synthesis using a non-emzymatic colorimetric assay and globin proteolysis by electrophoretic analysis (SDS– PAGE-15%). Dequalinium was able to inhibit both processes in vitro with close correlation to a murine malaria model, reducing parasitemia levels, prolonging the survival time post-infection and curing 40% of infected mice using a combination therapy with a loading dose of chloroquine. These results conWrm that dequalinium is a promising lead for antimalarial drug development. © 2006 Elsevier Inc. All rights reserved.
URI : http://saber.ucv.ve/jspui/handle/123456789/2366
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