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dc.contributor.authorBastos, Tanira Matutino
dc.contributor.authorRusso, Helena Mannochio
dc.contributor.authorMoretti, Nilmar Silvio [UNIFESP]
dc.contributor.authorSchenkman, Sergio [UNIFESP]
dc.contributor.authorMarcourt, Laurence
dc.contributor.authorGupta, Mahabir Prashad
dc.contributor.authorWolfender, Jean-Luc
dc.contributor.authorQueiroz, Emerson Ferreira
dc.contributor.authorSoares, Milena Botelho Pereira
dc.date.accessioned2021-11-26T21:36:40Z
dc.date.available2021-11-26T21:36:40Z
dc.date.issued2019
dc.identifier.urihttps://repositorio.unifesp.br/xmlui/handle/11600/62313
dc.description.abstractBenznidazole and nifurtimox, the only drugs available for the treatment of Chagas disease, have limited efficacy and have been associated with severe adverse side effects. Thus, there is an urgent need to find new biotargets for the identification of novel bioactive compounds against the parasite and with low toxicity. Silent information regulator 2 (Sir2) enzymes, or sirtuins, have emerged as attractive targets for the development of novel antitrypanosomatid agents. In the present work, we evaluated the inhibitory effect of natural compounds isolated from cashew nut (Anacardium occidentale, L. Anacardiaceae) against the target enzymes TcSir2rp1 and TcSir2rp3 as well as the parasite. Two derivates of cardol (1, 2), cardanol (3, 4), and anacardic acid (5, 6) were investigated. The two anacardic acids (5, 6) inhibited both TcSir2rp1 and TcSir2rp3, while the cardol compound (2) inhibited only TcSir2rp1. The most potent sirtuin inhibitor active against the parasite was the cardol compound (2), with an EC50 value of 12.25 μM, similar to that of benznidazole. Additionally, compounds (1, 4), which were inactive against the sirtuin targets, presented anti-T. cruzi effects. In conclusion, our results showed the potential of Anacardium occidentale compounds for the development of potential sirtuin inhibitors and anti-Trypanosoma cruzi agents.pt_BR
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)pt_BR
dc.languageengpt_BR
dc.publisherMDPIpt_BR
dc.relation.ispartofMoleculespt_BR
dc.rightsAcesso abertopt_BR
dc.subjectTrypanosoma cruzipt_BR
dc.subjectSirtuinspt_BR
dc.subjectAnacardium occidentalept_BR
dc.subjectDrug discoverypt_BR
dc.titleChemical constituents of Anacardium occidentale as inhibitors of Trypanosoma cruzi Sirtuinspt_BR
dc.typeArtigopt_BR
dc.description.sponsorshipIDFAPESP: 2018/09948-0pt_BR
dc.identifier.doidoi:10.3390/molecules24071299pt_BR
unifesp.campusEscola Paulista de Medicina (EPM)pt_BR
unifesp.graduateProgramMicrobiologia e Imunologiapt_BR
unifesp.knowledgeAreaOutrapt_BR
dc.contributor.authorLatteshttp://lattes.cnpq.br/2131472726202687pt_BR
unifesp.departamentoMicrobiologia, Imunologia e Parasitologiapt_BR


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