In vitro and in vivo assessment of the anti-malarial activity of Caesalpinia pluviosa

Malaria Journal

Research

Fernanda G Bueno¹  João Carlos P Mello¹  Wanessa C Souza-Neiras²  Ana Carolina AV Kayano²  Fabio TM Costa²  Stefanie CP Lopes²  Lucy M Yamauchi³  Mary A Foglio⁴  Elaine C Cabral⁵  Marcos N Eberlin⁵ 

[1] Departamento de Farmácia Universidade Estadual de Maringá, Maringá, PR, Brazil;Departamento de Genética, Evolução e Bioagentes, Instituto de Biologia, Universidade de Campinas (UNICAMP), Campinas, SP, Brazil;Departamento de Microbiologia, Centro de Ciências Biológicas, Universidade Estadual de Londrina, Londrina, PR, Brazil;Divisão de Fotoquímica, Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), UNICAMP, Campinas, SP, Brazil;Thomson Mass Spectrometry Laboratory, Instituto de Química, UNICAMP, Campinas, SP, Brazil;

关键词: Malaria;    Quercetin;    Crude Extract;    Artesunate;    Parasite Growth;   

DOI  :  10.1186/1475-2875-10-112

 received in 2011-02-08, accepted in 2011-05-02,  发布年份 2011

来源: Springer

【 摘 要 】

BackgroundTo overcome the problem of increasing drug resistance, traditional medicines are an important source for potential new anti-malarials. Caesalpinia pluviosa, commonly named "sibipiruna", originates from Brazil and possess multiple therapeutic properties, including anti-malarial activity.MethodsCrude extract (CE) was obtained from stem bark by purification using different solvents, resulting in seven fractions. An MTT assay was performed to evaluate cytotoxicity in MCF-7 cells. The CE and its fractions were tested in vitro against chloroquine-sensitive (3D7) and -resistant (S20) strains of Plasmodium falciparum and in vivo in Plasmodium chabaudi-infected mice. In vitro interaction with artesunate and the active C. pluviosa fractions was assessed, and mass spectrometry analyses were conducted.ResultsAt non-toxic concentrations, the 100% ethanolic (F4) and 50% methanolic (F5) fractions possessed significant anti-malarial activity against both 3D7 and S20 strains. Drug interaction assays with artesunate showed a synergistic interaction with the F4. Four days of treatment with this fraction significantly inhibited parasitaemia in mice in a dose-dependent manner. Mass spectrometry analyses revealed the presence of an ion corresponding to m/z 303.0450, suggesting the presence of quercetin. However, a second set of analyses, with a quercetin standard, showed distinct ions of m/z 137 and 153.ConclusionsThe findings show that the F4 fraction of C. pluviosa exhibits anti-malarial activity in vitro at non-toxic concentrations, which was potentiated in the presence of artesunate. Moreover, this anti-malarial activity was also sustained in vivo after treatment of infected mice. Finally, mass spectrometry analyses suggest that a new compound, most likely an isomer of quercetin, is responsible for the anti-malarial activity of the F4.

【 授权许可】

Unknown   
© Kayano et al; licensee BioMed Central Ltd. 2011. This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.