Please use this identifier to cite or link to this item: https://repositorio.unifesp.br/handle/11600/58533
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dc.contributor.authorMaluf, Sarah El Chamy [UNIFESP]
dc.contributor.authorMelo, Pollyana Maria Saud [UNIFESP]
dc.contributor.authorVarotti, Fernando de Pilla
dc.contributor.authorGazarini, Marcos Leoni [UNIFESP]
dc.contributor.authorCunha, Rodrigo Luiz Oliveira Rodrigues
dc.contributor.authorCarmona, Adriana Karaoglanovic [UNIFESP]
dc.date.accessioned2020-10-30T18:46:37Z
dc.date.available2020-10-30T18:46:37Z
dc.date.issued2016
dc.identifierhttps://doi.org/10.1016/j.parint.2015.09.006
dc.identifier.citationParasitology International. Clare, v. 65, n. 1, p. 20-22, 2016.
dc.identifier.issn1383-5769
dc.identifier.urihttps://repositorio.unifesp.br/handle/11600/58533
dc.description.abstractHypervalent organotellurium compounds (organotelluranes) have shown several promising applications, including their use as potent and selective cysteine protease inhibitors and antiprotozoal agents. Here, we report the antimalarial activities of three organotellurane derivatives (RF05, RF07 and RF19) in two Plasmodium falciparum strains (CQ(s) 3D7 and CQ(R) W2), which demonstrated significant decreases in parasitemia in vitro. The inhibition of intracellular P. falciparum proteases by RF05, RF07 and RF19 was determined and the IC50 values were 3.7 +/- 1.0 mu M, 1.1 +/- 02 mu M and 02 +/- 0.01 mu M, respectively. Using an assay performed in the presence of the ER Ca2+-ATPase inhibitor we showed that the main enzymatic targets were cysteine proteases stimulated by calcium (calpains). None of the compounds tested caused haemolysis or a significant decrease in endothelial cell viability in the concentration range used for the inhibition assay. Taken together, the results suggest promising compounds for the development of antimalarial drugs. (C) 2015 Elsevier Ireland Ltd. All rights reserved.en
dc.format.extent20-22
dc.language.isoeng
dc.publisherElsevier Ireland Ltd
dc.relation.ispartofParasitology International
dc.rightsAcesso restrito
dc.subjectPlasmodiumen
dc.subjectMalariaen
dc.subjectCalpainen
dc.subjectTellurium compoundsen
dc.titleHypervalent organotellurium compounds as inhibitors of P. falciparum calcium-dependent cysteine proteasesen
dc.typeArtigo
dc.description.affiliationUniv Fed Sao Paulo, Dept Biofis, BR-04039032 Sao Paulo, SP, Brazil
dc.description.affiliationUniv Fed Sao Joao Del Rei, Ctr Ciencias Saude, Nucleo Pesquisa Quim Biol, Divinopolis, MG, Brazil
dc.description.affiliationUniv Fed Sao Paulo, Dept Biociencias, Santos, SP, Brazil
dc.description.affiliationUniv Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP, Brazil
dc.description.affiliationUnifespUniv Fed Sao Paulo, Dept Biofis, BR-04039032 Sao Paulo, SP, Brazil
dc.description.affiliationUnifespUniv Fed Sao Paulo, Dept Biociencias, Santos, SP, Brazil
dc.identifier.doi10.1016/j.parint.2015.09.006
dc.description.sourceWeb of Science
dc.identifier.wosWOS:000366228500004
dc.coverageClare
dc.citation.volume65
dc.citation.issue1
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Artigo

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