Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice
Autor: | Matheus Santos de Sá, Milena Botelho Pereira Soares, Ricardo Ribeiro dos Santos, Mariano G. Zalis, Gabriela Lemos de Azevedo Maia, Ivana Maria Fechine Sette, José Fernando Oliveira Costa, Celso A. Câmara, Antoniana U. Krettli, Ana Maria Giulietti-Harley, José Maria Barbosa Filho |
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Rok vydání: | 2008 |
Předmět: |
Plasmodium berghei
Plasmodium falciparum Drug resistance Parasitemia Pharmacology chemistry.chemical_compound Antimalarials Inhibitory Concentration 50 Mice In vivo Chloroquine Betulinic acid parasitic diseases medicine Animals Humans Betulinic Acid Mice Inbred BALB C General Veterinary biology Dose-Response Relationship Drug General Medicine biology.organism_classification medicine.disease Survival Analysis Triterpenes Malaria Infectious Diseases chemistry Insect Science Parasitology Pentacyclic Triterpenes medicine.drug |
Zdroj: | Parasitology research. 105(1) |
ISSN: | 1432-1955 |
Popis: | 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 microM, 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. |
Databáze: | OpenAIRE |
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