Document Detail


Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice.
MedLine Citation:
PMID:  19367418     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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 Soares
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-04-15
Journal Detail:
Title:  Parasitology research     Volume:  105     ISSN:  1432-1955     ISO Abbreviation:  Parasitol. Res.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-05-22     Completed Date:  2009-07-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8703571     Medline TA:  Parasitol Res     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  275-9     Citation Subset:  IM    
Affiliation:
Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, Salvador, Bahia, Brazil.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antimalarials / pharmacology*,  therapeutic use*
Dose-Response Relationship, Drug
Humans
Inhibitory Concentration 50
Malaria / drug therapy*
Mice
Mice, Inbred BALB C
Parasitemia / drug therapy
Plasmodium berghei / drug effects*
Plasmodium falciparum / drug effects*
Survival Analysis
Triterpenes / pharmacology*,  therapeutic use*
Chemical
Reg. No./Substance:
0/Antimalarials; 0/Triterpenes; 472-15-1/betulinic acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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