Blood shizonticidal activities of phenazines and naphthoquinoidal compounds against Plasmodium falciparum in vitro and in mice malaria studies

dc.creatorSouza, Nicolli Bellotti de
dc.creatorAndrade, Isabel Mayer de
dc.creatorCarneiro, Paula Fernandes
dc.creatorJardim, Guilherme AM
dc.creatorMelo, Isadora MM de
dc.creatorSilva Júnior, Eufrânio N da
dc.creatorKrettli, Antoniana Ursine
dc.date2015-03-06T17:49:56Z
dc.date2015-03-06T17:49:56Z
dc.date2014
dc.date.accessioned2023-09-26T22:27:27Z
dc.date.available2023-09-26T22:27:27Z
dc.identifierSOUZA, Nicolli Bellotti de et al. Blood shizonticidal activities of phenazines and naphthoquinoidal compounds against Plasmodium falciparum in vitro and in mice malaria studies. Mem Inst Oswaldo Cruz, v. 109, n. 5, p. 254-552, 2014
dc.identifier1678-8060
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/9649
dc.identifier10.1590/0074-0276130603
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8879469
dc.descriptionDue to the recent advances of atovaquone, a naphthoquinone, through clinical trials as treatment for malarial infection, 19 quinone derivatives with previously reported structures were also evaluated for blood schizonticide activity against the malaria parasite Plasmodium falciparum. These compounds include 2-hydroxy-3-methylamino naphthoquinones (2-9), lapachol (10), nor-lapachol (11), iso-lapachol (12), phthiocol (13) and phenazines (12-20). Their cytotoxicities were also evaluated against human hepatoma and normal monkey kidney cell lines. Compounds 2 and 5 showed the highest activity against P. falciparum chloroquine-resistant blood-stage parasites (clone W2), indicated by their low inhibitory concentration for 50% (IC50) of parasite growth. The therapeutic potential of the active compounds was evaluated according to the selectivity index, which is a ratio of the cytotoxicity minimum lethal dose which eliminates 50% of cells and the in vitro IC50. Naphthoquinones 2 and 5, with activities similar to the reference antimalarial chloroquine, were also active against malaria in mice and suppressed parasitaemia by more than 60% in contrast to compound 11 which was inactive. Based on their in vitro and in vivo activities, compounds 2 and 5 are considered promising molecules for antimalarial treatment and warrant further study.
dc.formatapplication/pdf
dc.languageeng
dc.publisherFundação Oswaldo Cruz
dc.rightsopen access
dc.subjectPlasmodium falciparum
dc.subjectPlasmodium berghei
dc.subjectantimalarials
dc.subjectlapachol
dc.subjectquinones
dc.subjectphenazines
dc.titleBlood shizonticidal activities of phenazines and naphthoquinoidal compounds against Plasmodium falciparum in vitro and in mice malaria studies
dc.typeArticle


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