Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships

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dc.contributor.authorMorais, Thiago R. [UNIFESP]
dc.contributor.authorCosta-Silva, Thais A. da
dc.contributor.authorTempone, Andre G.
dc.contributor.authorBorborema, Samanta Etel T.
dc.contributor.authorScotti, Marcus T.
dc.contributor.authorSousa, Raquel Maria F. de
dc.contributor.authorAraujo, Ana Carolina C.
dc.contributor.authorOliveira, Alberto de
dc.contributor.authorMorais, Sergio Antonio L. de
dc.contributor.authorSartorelli, Patricia [UNIFESP]
dc.contributor.authorLago, Joao Henrique G. [UNIFESP]
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionAdolfo Lutz Inst
dc.contributor.institutionUniv Fed Paraiba
dc.contributor.institutionUniversidade Federal de Uberlândia (UFU)
dc.date.accessioned2016-01-24T14:37:11Z
dc.date.available2016-01-24T14:37:11Z
dc.date.issued2014-05-01
dc.description.abstractLeishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. in this work, the in vitro antiparasitic activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal activity with IC50 values in the range between 15 and 58 mu g/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 mu g/mL. the complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-activity relationships were performed using Decision Trees.en
dc.description.affiliationUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Diadema, SP, Brazil
dc.description.affiliationAdolfo Lutz Inst, Ctr Parasitol, BR-01246902 São Paulo, Brazil
dc.description.affiliationUniv Fed Paraiba, Ctr Ciencias Aplicadas & Educ, BR-58297000 Rio Tinto, Brazil
dc.description.affiliationUniv Fed Uberlandia, Inst Quim, BR-38400902 Uberlandia, MG, 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.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG)
dc.description.sponsorshipIDCNPq: 300546/2012-2
dc.description.sponsorshipIDCNPq: 471458/2012-0
dc.description.sponsorshipIDFAPESP: 2011/51739-0
dc.description.sponsorshipIDFAPESP: 2012/18756-1
dc.description.sponsorshipIDFAPESP: 2013/16320-4
dc.format.extent5761-5776
dc.identifierhttp://dx.doi.org/10.3390/molecules19055761
dc.identifier.citationMolecules. Basel: Mdpi Ag, v. 19, n. 5, p. 5761-5776, 2014.
dc.identifier.doi10.3390/molecules19055761
dc.identifier.fileWOS000337113000020.pdf
dc.identifier.issn1420-3049
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/37702
dc.identifier.wosWOS:000337113000020
dc.language.isoeng
dc.publisherMdpi Ag
dc.relation.ispartofMolecules
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectSchinus terebinthifoliusen
dc.subjectleavesen
dc.subjecttirucallane triterpenoidsen
dc.subjectLeishmania (L.) infantumen
dc.subjectTrypanosoma cruzien
dc.subjectstructure-activityen
dc.titleAntiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationshipsen
dc.typeinfo:eu-repo/semantics/article
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