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Title: | Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice |
Authors: | Sá, Matheus Santos de Costa, José Fernando Gustavo Krettli, Antoniana Ursini Zalis, Mariano Gustavo Maia, Gabriela Lemos de Azevedo Sette, Ivana Maria Fechine Câmara, Celso de Amorim Barbosa Filho, José Maria Harley, Ana Maria Giulietti Santos, Ricardo Ribeiro dos Soares, Milena Botelho Pereira |
Affilliation: | Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, Brasil Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, Brasil Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, Minas Gerais, Brasil Hospital Universitário Clementino Fraga Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brasil Universidade Federal da Paraíba, João Pessoa, Paraíba, Brasil Universidade Estadual da Paraíba, Campina Grande, Paraíba, Brasil Universidade Federal Rural de Pernambuco, Recife, Pernambuco, Brasil Universidade Federal da Paraíba, João Pessoa, Paraíba, Brasil Universidade Estadual de Feira de Santana, Feira de Santana, Bahia, Brasil Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, Brasil Laboratório de Engenharia Tecidual e Imunofarmacologia. Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, Brasil |
Abstract: | 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. |
DeCS: | Malária Plasmodium berghei Antimaláricos Plasmodium falciparum Triterpenos Relação Dose-Resposta a Droga |
Issue Date: | 2009 |
Citation: | SÁ, M. S. et al. Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice. Parasitol Research, v. 105, n.1, p.275-279, 2009. |
DOI: | 10.1007/s00436-009-1394-0 |
ISSN: | 0932-0113 |
Copyright: | open access |
Appears in Collections: | BA - IGM - Artigos de Periódicos |
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