Antiparasitic activity and effect of casearins isolated from Casearia sylvestris on Leishmania and Trypanosoma cruzi plasma membrane

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dc.contributor.authorBou, Diego Dinis [UNIFESP]
dc.contributor.authorTemporre, Andre G.
dc.contributor.authorPinto, Erika G.
dc.contributor.authorLagoa, Joao Henrique G. [UNIFESP]
dc.contributor.authorSartorellia, Patricia [UNIFESP]
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionAdolfo Lutz Inst
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.date.accessioned2016-01-24T14:37:07Z
dc.date.available2016-01-24T14:37:07Z
dc.date.issued2014-04-15
dc.description.abstractLeishmaniasis and Chagas disease are infectious diseases caused by parasite Leishmania sp. and Trypanosoma cruzi, respectively, and are included among the most neglected diseases in several underdeveloped and developing countries, with an urgent demand for new drugs. Considering the antiparasitic potential of MeOH extract from leaves of Casearia sylvestris Sw. (Salicaceae), a bioguided fractionation was conducted and afforded four active clerodane diterpenes (casearins A, B, G, and J). the obtained results indicated a superior efficacy of tested casearins against trypomastigotes of T. cruzi, with IC50 values ranging from 0.53 to 2.77 mu g/ml. Leishmania infantum promastigotes were also susceptible to casearins, with IC50 values in a range between 4.45 and 9.48 mu g/ml. These substances were also evaluated for mammalian cytotoxicity against NOV cells resulting in 50% cytotoxic concentrations (CC50) ranging from 1.46 to 13.76 mu g/ml. Additionally, the action of casearins on parasite membranes was investigated using the fluorescent probe SYTOX Green. the obtained results demonstrated a strong interaction of casearins A and B to the plasma membrane of T. cruzi parasites, corroborating their higher efficacy against these parasites. in contrast, the tested casearins induced no alteration in the permeability of plasma membrane of Leishmania parasites, suggesting that biochemical differences between Leishmania and T. cruzi plasma membrane might have contributed to the target effect of casearins on trypomastigotes. Thus, considering the importance of studying novel and selective drug candidates against protozoans, casearins A, B, G, and J could be used as tools to future drug design studies. (c) 2014 Elsevier GmbH. All rights reserved.en
dc.description.affiliationUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Diadema, SP, Brazil
dc.description.affiliationAdolfo Lutz Inst, Dept Parasitol, BR-01246000 São Paulo, SP, Brazil
dc.description.affiliationUniv São Paulo, Inst Med Trop São Paulo, BR-05403000 Silo Paulo, SP, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Diadema, SP, Brazil
dc.description.sourceWeb of Science
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipIDFAPESP: 2011/51739-0
dc.description.sponsorshipIDFAPESP: 2013/16320-4
dc.description.sponsorshipIDCNPq: 470853/2012-3
dc.format.extent676-681
dc.identifierhttp://dx.doi.org/10.1016/j.phymed.2014.01.004
dc.identifier.citationPhytomedicine. Jena: Elsevier Gmbh, Urban & Fischer Verlag, v. 21, n. 5, p. 676-681, 2014.
dc.identifier.doi10.1016/j.phymed.2014.01.004
dc.identifier.issn0944-7113
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/37667
dc.identifier.wosWOS:000334726800014
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofPhytomedicine
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rights.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.subjectCasearia sylvestrisen
dc.subjectSalicaceaeen
dc.subjectClerodane diterpenesen
dc.subjectLeishmaniaen
dc.subjectTrypanosoma cruzien
dc.subjectCasearinsen
dc.titleAntiparasitic activity and effect of casearins isolated from Casearia sylvestris on Leishmania and Trypanosoma cruzi plasma membraneen
dc.typeinfo:eu-repo/semantics/article
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