Zanthoxylum rhoifolium Lam. (Rutaceae) has been traditionally used in the treatment of microbial infections and parasitic diseases. In the present study, the antileishmanial effect induced by the ethanol extract of stem barks from Z. rhoifolium (ZR-EEtOH) and its n-hexane fraction (ZR-FHEX) on infection and infectivity of murine macrophages by promastigote forms of Leishmania amazonensis were investigated. In different set of experiments, macrophages or promastigotes were pretreated with ZR-EEtOH or ZR-FHEX at non-lethal concentrations for 24 hours, and then macrophages were submitted to infection by promastigotes. Moreover, their effects on activation of macrophages, as well as on the DNA content, size and number of promastigotes by flow cytometry were also evaluated. The infection rate and the number of internalized amastigote forms were markedly decreased after pretreatment of macrophages or promastigotes when compared with nontreated cells. The increase in phagocytic capability and nitrite content was also observed. Furthermore, the decrease of DNA content, size and number of promastigotes was also observed. In conclusion, ZREEtOH and ZR-FHEX promoted a markedly significant antileishmanial effect and reduction of infection of macrophages, probably underlying defense mechanisms activation in macrophages. These findings reinforce the potential application of Z. rhoifolium in the treatment of leishmaniasis.
Background: imosa caesalpiniifolia Benth. (Mimosaceae) is a native plant from Brazilian Caatinga/Cerrado used in traditional medicine. The aim of this work was to investigate the chemical composition and the antileishmanial activity of the inflorescences from M. caesalpiniifolia. Method: The ethanolic extract from M. caesalpiniifolia inflorescences was submitted to fractionation in silica gel chromatography column, and the known structures were elucidated using spectroscopic methods. The antileishmanial activity of the EtOH extract and pure compounds was evaluated against the promastigote forms of Leishmania amazonensis. Results: In this study, the EtOH extract from M. caesalpiniifolia inflorescences (IC50 = 74.52 µg mL-1) and lupeol (IC50 = 15.40 µg mL-1) demonstrated significant inhibition of the growth at 48 h for promastigote forms of L. amazonensis when compared with Glucantime® (IC50 = 1190.21 µg mL-1), a reference drug. Moreover, the cytotoxicity evaluation of EtOH extract of M. caesalpiniifolia inflorescences against murine peritoneal macrophages was also determined. Then, the selectivity index shows that the EtOH extract of M. caesalpiniifolia inflorescences is more toxic to the parasite than mammalian host cells. The chemical characterization of the ethanolic extract from M. caesalpiniifolia inflorescences resulted in the identification of fatty acids and isoprenoids as lupeol acetate, lupeol, β-amyrin, a mixture of steroids and a mixture of fatty acid triterpenyl esters. 3-O-Acyl triterpenoids are being reported for the first time in M. caesalpiniifolia. Conclusion: The EtOH extract of M. caesalpiniifolia inflorescences is a rich source of triterpenoids and a promising natural product against leishmaniasis.
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