Abstract

The objective of this study was to carry out phytochemical analysis of the bark extract of Casearia javitensis and to evaluate its antipromastigote activity against Leishmania amazonensis. The ethanol extract (EE) was fractionated in open-column chromatography to obtain the hexane (FrHex), dichloromethane (FrDcm), ethyl acetate (FrAcOET) and methanol (FrMeOH) fractions. The EE and its fractions were analyzed by thin layer chromatography (TLC). FrDcm was analyzed in high performance liquid chromatography with diode array detection (HPLC-DAD). The antipromastigote assay of Leishmania amazonensis and the cytotoxicity test against the acute monocytic leukemia cell line (THP-1) were performed by the MTT colorimetric assay. The phytochemical profile in TLC detected terpenes in all samples. However, in the ultraviolet spectrum (HPLC-DAD) for FrDcm suggested the presence of a phenolic compound. FrHex and FrDcm showed antipromastigote activity (IC50 = 116.6 ± 0.9 and 59.4 ± 1.1 μg mL-1, respectively) and low cytotoxicity (CC50 = 333.4 ± 3.2 and 241.2 ± 1.9 μg mL-1, respectively). The selectivity index for FrDcm was 4.1. We conclude that the FrDcm of C. javitensis has potantial as a leishmanicide, and this activity may be related to the presence of phenolic compound.

Highlights

  • The leishmaniases are a group of infectious disease, non-contagious, caused by protozoan parasites of the genus Leishmania, which affects skin and mucous membranes, transmitted to humans by the bite of infected female phlebotomine sandflies[1]

  • Endemic in 97 countries, an estimated 1 billion people live in an area at risk for the disease worldwide and there are no optimistic forecasts for its control for the few years[1,2]

  • Sesquiterpenes and monoterpenes, phenylpropanoids, steroids, phenolic glycosides, alkaloids and flavonoids have been isolated[13,23]. Several of these chemical compounds, isolated from plant extracts, have been reported leishmanicidal activity[24], especially the terpene compounds obtained from Casearia Sylvestris[20] and flavonic compounds obtained from C. arborea[21] present in the genus Casearia

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Summary

Introduction

The leishmaniases are a group of infectious disease, non-contagious, caused by protozoan parasites of the genus Leishmania, which affects skin and mucous membranes, transmitted to humans by the bite of infected female phlebotomine sandflies[1]. Species of the Casearia genus present in the literature a study with antiparasitic activity, with activity between trypomastigotes of Trypanosoma cruzi (IC50 ranging from 0.53 to 2.77 μg mL-1) for clerodane diterpenes (casearins A, B, G, and J) and for Leishmania infantum promastigotes were susceptible to casearins obtained from Casearia sylvestris, with IC50 values ranging from 4.45 to 9.48 μg mL-1[20], and the tricine compound, a flavone, obtained from of C. arborea demonstrated activity against the intracellular amastigotes of L. infantum, with an IC50 value of 56 μM[21].

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