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

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

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Abstract 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 lycogel 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 quadruple topical ointment for dogs 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.