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Background  To 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.    Methods  Crude 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.    Results  At 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.    Conclusions  The 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.

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