Anti-malarial, anti-trypanosomal, and anti-leishmanial activities of jacaranone isolated from Pentacalia desiderabilis (Vell.) Cuatrec. (Asteraceae)

Anti-malarial, anti-trypanosomal, and anti-leishmanial activities of jacaranone isolated from Pentacalia desiderabilis (Vell.) Cuatrec. (Asteraceae)

Author Morais, Thiago R. Google Scholar
Romoff, Paulete Google Scholar
Favero, Oriana A. Google Scholar
Reimao, Juliana Q. Google Scholar
Lourenco, Walkyria C. Google Scholar
Tempone, Andre G. Google Scholar
Hristov, Angelica D. Google Scholar
Di Santi, Silvia M. Google Scholar
Lago, Joao Henrique G. Autor UNIFESP Google Scholar
Sartorelli, Patricia Autor UNIFESP Google Scholar
Ferreira, Marcelo J. P. Google Scholar
Institution Univ Presbiteriana Mackenzie
Inst Adolfo Lutz Registro
Nucl Estudos Malaria
Universidade Federal de São Paulo (UNIFESP)
Abstract Leishmaniasis, Chagas disease, and malaria affect the poorest population around the world, with an elevated mortality and morbidity. in addition, the therapeutic alternatives are usually toxic or ineffective drugs especially those against the trypanosomatids. in the course of selection of new anti-protozoal compounds from Brazilian flora, the CH2C12 phase from MeOH extract obtained from the leaves of Pentacalia desiderabilis (Vell.) Cuatrec. (Asteraceae) showed in vitro anti-leishmanial, anti-malarial, and anti-trypanosomal activities. the chromatographic fraction-ation of the CH2C12 phase led to the isolation of the bioactive compound, which was characterized as jacaranone [ methyl (1-hydroxy-4-oxo-2,5-cyclohexandienyl) acetate], by spectroscopic methods. This compound showed activity against promastigotes of Leishmania (L.) chagasi, Leishmania (V.) braziliensis, and Leishmania (L.). amazonensis showing an IC50 of 17.22, 12.93, and 11.86 mu g/mL, respectively. Jacaranone was also tested in vitro against the Trypanosoma cruzi trypomastigotes and Plasmodium falciparum chloroquine-resistant parasites (K1 strain) showing an IC50 of 13 and 7.82 mu g/mL, respectively, and was 3.5-fold more effective than benznidazole in anti-Trypanosoma cruzi assay. However, despite of the potential against promatigotes forms, this compound was not effective against amastigotes of L. (L.) chagasi and T. cruzi. the cytotoxicity study using Kidney Rhesus monkey cells, demonstrated that jacaranone showed selectivity against P. falciparum (21.75 mu g/mL) and a selectivity index of 3. the obtained results suggested that jacaranone, as other similar secondary metabolites or synthetic analogs, might be useful tolls for drug design for in vivo studies against protozoan diseases.
Language English
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Grant number CNPq: 473405/2008-3
CNPq: 477422/2009-8
FAPESP: 06/57626-5
FAPESP: 08/11496-9
Date 2012-01-01
Published in Parasitology Research. New York: Springer, v. 110, n. 1, p. 95-101, 2012.
ISSN 0932-0113 (Sherpa/Romeo, impact factor)
Publisher Springer
Extent 95-101
Access rights Closed access
Type Article
Web of Science ID WOS:000299521000009

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