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

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-p...

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Published in:Parasitology research (1987) 2012-01, Vol.110 (1), p.95-101
Main Authors: Morais, Thiago R., Romoff, Paulete, Fávero, Oriana A., Reimão, Juliana Q., Lourenço, Walkyria C., Tempone, André G., Hristov, Angelica D., Di Santi, Silvia M., Lago, João Henrique G., Sartorelli, Patricia, Ferreira, Marcelo J. P.
Format: Article
Language:English
Subjects:
Animals
Antiprotozoal Agents - isolation & purification
Antiprotozoal Agents - pharmacology
Antiprotozoal Agents - toxicity
Asteraceae
Asteraceae - chemistry
Benzoquinones - isolation & purification
Benzoquinones - pharmacology
Benzoquinones - toxicity
Biological and medical sciences
Biomedical and Life Sciences
Biomedicine
Brazil
Cell Line
Cell Survival - drug effects
Chromatography
Fundamental and applied biological sciences. Psychology
General aspects
General aspects and techniques. Study of several systematic groups. Models
Immunology
Inhibitory Concentration 50
Invertebrates
Leishmania
Leishmania - drug effects
Macaca mulatta
Medical Microbiology
Microbiology
Original Paper
Plant Extracts - isolation & purification
Plant Extracts - pharmacology
Plant Extracts - toxicity
Plant Leaves - chemistry
Plasmodium falciparum
Plasmodium falciparum - drug effects
Spectrum Analysis
Trypanosoma cruzi
Trypanosoma cruzi - drug effects
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Summary: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 CH 2 C l2 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 fractionation of the CH 2 Cl 2 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 IC 50 of 17.22, 12.93, and 11.86 μg/mL, respectively. Jacaranone was also tested in vitro against the Trypanosoma cruzi trypomastigotes and Plasmodium falciparum chloroquine-resistant parasites (K1 strain) showing an IC 50 of 13 and 7.82 μg/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 μg/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.
ISSN:0932-0113
1432-1955
DOI:10.1007/s00436-011-2454-9