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

Submitted by Martha Silveira Berbert ([email protected]) on 2011-04-13T03:09:38Z No. of bitstreams: 1 Antimalarial activity of betulinic acid and derivatives.pdf: 140654 bytes, checksum: 63efcdfed845e5e6dd5cd247c4090c8d (MD5)Made available in DSpace on 2011-04-13T03:09:38Z (GMT). No. of bitstreams: 1 Antimalarial activity of betulinic acid and derivatives.pdf: 140654 bytes, checksum: 63efcdfed845e5e6dd5cd247c4090c8d (MD5) Previous issue date: 2009-04-15Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, BrasilCentro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, BrasilCentro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, Minas Gerais, BrasilHospital Universitário Clementino Fraga Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, BrasilUniversidade Federal da Paraíba, João Pessoa, Paraíba, BrasilUniversidade Estadual da Paraíba, Campina Grande, Paraíba, BrasilUniversidade Federal Rural de Pernambuco, Recife, Pernambuco, BrasilUniversidade Federal da Paraíba, João Pessoa, Paraíba, BrasilUniversidade Estadual de Feira de Santana, Feira de Santana, Bahia, BrasilCentro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, BrasilLaboratório de Engenharia Tecidual e Imunofarmacologia. Centro de Pesquisas Gonçalo Moniz - FIOCRUZ, Bahia, BrasilMalaria 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