Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice

Malaria is one of the most important tropical diseases and mainly affects populations living in developing countries. Reduced sensitivity of Plasmodium sp. to formerly recommended antimalarial drugs places an increasing burden on malaria control programs as well as on national health systems in ende...

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Published in:Parasitology research (1987) 2009-07, Vol.105 (1), p.275-279
Main Authors: de Sá, Matheus Santos, Costa, José Fernando Oliveira, Krettli, Antoniana Ursine, Zalis, Mariano Gustavo, Maia, Gabriela Lemos de Azevedo, Sette, Ivana Maria Fechine, Câmara, Celso de Amorim, Filho, José Maria Barbosa, Giulietti-Harley, Ana Maria, Ribeiro dos Santos, Ricardo, Soares, Milena Botelho Pereira
Format: Article
Language:English
Subjects:
Animals
Antimalarials - pharmacology
Antimalarials - therapeutic use
Biological and medical sciences
Biomedical and Life Sciences
Biomedicine
Dose-Response Relationship, Drug
Fundamental and applied biological sciences. Psychology
General aspects
General aspects and techniques. Study of several systematic groups. Models
Humans
Immunology
Inhibitory Concentration 50
Invertebrates
Malaria - drug therapy
Medical Microbiology
Mice
Mice, Inbred BALB C
Microbiology
Original Paper
Parasitemia - drug therapy
Plasmodium berghei - drug effects
Plasmodium falciparum - drug effects
Survival Analysis
Triterpenes - pharmacology
Triterpenes - therapeutic use
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Summary:Malaria is one of the most important tropical diseases and mainly affects populations living in developing countries. Reduced sensitivity of Plasmodium sp. to formerly recommended antimalarial drugs places an increasing burden on malaria control programs as well as on national health systems in endemic countries. The present study aims to evaluate the antimalarial activity of betulinic acid and its derivative compounds, betulonic acid, betulinic acid acetate, betulinic acid methyl ester, and betulinic acid methyl ester acetate. These substances showed antiplasmodial activity against chloroquine-resistant Plasmodium falciparum parasites in vitro, with IC 50 values of 9.89, 10.01, 5.99, 51.58, and 45.79 μM, respectively. Mice infected with Plasmodium berghei and treated with betulinic acid acetate had a dose-dependent reduction of parasitemia. Our results indicate that betulinic acid and its derivative compounds are candidates for the development of new antimalarial drugs.
ISSN:0932-0113
1432-1955
DOI:10.1007/s00436-009-1394-0