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Parasitology Research

, 105:275 | Cite as

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

  • Matheus Santos de Sá
  • José Fernando Oliveira Costa
  • Antoniana Ursine Krettli
  • Mariano Gustavo Zalis
  • Gabriela Lemos de Azevedo Maia
  • Ivana Maria Fechine Sette
  • Celso de Amorim Câmara
  • José Maria Barbosa Filho
  • Ana Maria Giulietti-Harley
  • Ricardo Ribeiro dos Santos
  • Milena Botelho Pereira SoaresEmail author
Original Paper

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 IC50 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.

Keywords

Malaria Chloroquine Mefloquine Antimalarial Activity Betulinic Acid 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgments

The authors wish to thank Fabrício Souza Silva for technical assistance. The experiments made in this study comply with the current laws of the Brazil. The approval for this work was obtained from the Ethics Committee on the Use of Laboratorial Animals (reference number 004/2002). This work received financial support from FIOCRUZ, RENORBIO, CNPq, FINEP, MCT, and INSEAR.

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Copyright information

© Springer-Verlag 2009

Authors and Affiliations

  • Matheus Santos de Sá
    • 1
  • José Fernando Oliveira Costa
    • 1
  • Antoniana Ursine Krettli
    • 2
  • Mariano Gustavo Zalis
    • 3
  • Gabriela Lemos de Azevedo Maia
    • 4
  • Ivana Maria Fechine Sette
    • 5
  • Celso de Amorim Câmara
    • 6
  • José Maria Barbosa Filho
    • 4
  • Ana Maria Giulietti-Harley
    • 7
  • Ricardo Ribeiro dos Santos
    • 1
  • Milena Botelho Pereira Soares
    • 1
    • 8
    Email author
  1. 1.Centro de Pesquisas Gonçalo MonizFundação Oswaldo CruzSalvadorBrazil
  2. 2.Centro de Pesquisas René RachouFundação Oswaldo CruzBelo HorizonteBrazil
  3. 3.Hospital Universitário Clementino Fraga FilhoUniversidade Federal do Rio de JaneiroRio de JaneiroBrazil
  4. 4.Universidade Federal da ParaíbaJoão PessoaBrazil
  5. 5.Universidade Estadual da ParaíbaCampina GrandeBrazil
  6. 6.Universidade Federal Rural de PernambucoRecifeBrazil
  7. 7.Universidade Estadual de Feira de SantanaFeira de SantanaBrazil
  8. 8.Laboratório de Engenharia Tecidual e Imunofarmacologia, Centro de Pesquisas Gonçalo MonizFundação Oswaldo CruzSalvadorBrazil

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