Aim of the studyTo evaluate the anti-leishmanial activity and cytotoxicity of aqueous and organic extracts of ten plants used in Mexican traditional medicine as anti-parasitics.Materials and methodsFor the organic extracts, plant material was macerated in dichloromethane (CH2Cl2) and dichloromethane/methanol (CH2Cl2/MeOH) (1:1) during two weeks; the aqueous extracts were prepared by infusion. The extracts were tested against promastigotes and intracellular amastigotes of Leishmania amazonensis. The cytotoxicity was assayed in parallel on peritoneal macrophages of BALB/c mice.ResultsFour of the thirty extracts tested were active and selective against L. amazonensis promastigotes: Schinus molle (CH2Cl2 and CH2Cl2/MeOH), Lantana camara (CH2Cl2) and Prosopis laevigata (aqueous). These extracts had a median inhibitory concentration (IC50) against intracellular amastigotes under 50 μg/mL and a selectivity index (SI) higher than 5, which indicates that they constitute valuable candidates to obtain secondary metabolites with leishmanicidal activity.ConclusionsThe results derived from this study indicate that L. camara, P. laevigata, and S. molle might provide interesting new leads for the development of antileishmanial drugs.

Lantana camara (L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from L. camara were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican L. camara in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FI–FXVIII) were evaluated in vitro against Leishmania mexicana and L. amazonensis. FII, FX, FXI, FXV, and FXVI showed significant activity against both Leishmania strains, the most potent of which was FXV. Eicosane (1), squalene (2), β-ionone (3), caryophyllene oxide (4), β-caryophyllene (5), hexanoic acid (6), tiglic acid (7), a mixture of lantanilic (8) and camaric (9) acids, and lantadene B (10) were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic (8) and camaric (9) acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC50) = 12.02 ± 0.36 μM). This study indicates that this cultivar of L. camara has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.

No abstract

No abstract