Chemical Constituents of Anacardium occidentale as Inhibitors of Trypanosoma cruzi Sirtuins

dc.creatorBastos, Tanira Matutino
dc.creatorRusso, Helena Mannochio
dc.creatorMoretti, Nilmar Silvio
dc.creatorSchenkman, Sergio
dc.creatorMarcourt, Laurence
dc.creatorGupta, Mahabir Prashad
dc.creatorWolfender, Jean-Luc
dc.creatorQueiroz, Emerson Ferreira
dc.creatorSoares, Milena Botelho Pereira
dc.date2019-08-06T17:59:50Z
dc.date2019-08-06T17:59:50Z
dc.date2019
dc.date.accessioned2023-09-26T20:12:29Z
dc.date.available2023-09-26T20:12:29Z
dc.identifierBASTOS,Tanira Matutino et al. Chemical Constituents of Anacardium occidentale as Inhibitors of Trypanosoma cruzi Sirtuins. Molecules, v. 24, p. 1-13, 2019.
dc.identifier1420-3049
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/34633
dc.identifier10.3390/molecules24071299
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8851389
dc.descriptionFundação de Amparo à Pesquisa do Estado da Bahia (FAPESB); Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, Grant 015/22031-0 to S.S. and N.M., Grant 2018/09948-0 to N.M.); and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). SS and M.S are the recipients of a fellowship from Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).
dc.descriptionBenznidazole 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.
dc.formatapplication/pdf
dc.languageeng
dc.publisherMDPI
dc.rightsopen access
dc.subjectTrypanosoma cruzi
dc.subjectSirtuins
dc.subjectAnacardium occidentale
dc.subjectDescoberta de drogas
dc.subjectTrypanosoma cruzi
dc.subjectSirtuins
dc.subjectAnacardium occidentale
dc.subjectDrug discovery
dc.titleChemical Constituents of Anacardium occidentale as Inhibitors of Trypanosoma cruzi Sirtuins
dc.typeArticle


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