Anti-Leishmania amazonensis activity of the terpenoid fraction from Eugenia pruniformis leaves.

Ricardo D.D.G Albuquerque,Marcelo G Santos,Ricardo S Esteves,Deivid C Soares,Veronica F Amaral,Gabrielle B Bezerra,Eliane Fialho,Christian Ferreira,André L.M Albert,Adriana P Oliveira,Leandro Rocha,Carlos L.A Passos

doi:10.1590/0001-3765202020201181

Abstract

Leishmaniasis is caused by protozoan parasites belonging to the genus Leishmania and includes cutaneous, mucocutaneous and visceral clinical forms. Drugs currently available for leishmaniasis treatment present high toxicity, and development of parasite resistance. Plants constitute an important source of compounds with leishmanicidal potential. This study aimed to evaluate the anti-Leishmania amazonensis activity of the terpenoid fraction of Eugenia pruniformis leaves (TF-EpL). TF-EpL was active against the promastigote and intracellular amastigote forms of L. amazonensis with IC50(24h) value of 43.60μg/mL and 44.77μg/mL, respectively. TF-EpL altered the cell cycle of the parasite, increasing 2.32-fold the cells in the Sub-G0/G1 phase. TF-EpL also changed the ΔΨm and increased ROS and the number of annexin-V-PI positive promastigotes, which suggests incidental death. β-sitosterol, ursolic acid, corosolic acid and asiatic acid were isolated from TF-EpL. The results showed the antileishmanial activity of E. pruniformis terpenoids and its potential for further studies as a source of new drugs for leishmaniasis.

Highlights

Leishmaniasis is a neglected tropical disease caused by unicellular protozoan parasites of the genus Leishmania, that affect 98 countries on 5 continents, with approximately 0.7 to 1 million cases of cutaneous leishmaniasis and 50.000 to 90.000 cases of visceral leishmaniasis occur every year
The n-hexane extract (20.0 g) was purified with acetone to afford the terpenoid fraction (TF-EpL), which was chromatographed on a Silica Gel 60 column eluted with n-hexane, ethyl acetate and methanol, using an increasing polarity gradient to yield 81 fractions (1-89) that were combined with the aid of Thin Layer Chromatography (TLC) analysis
Leishmaniasis is a neglected parasitic disease for which the current antileishmania therapies are complicated by drug toxicity, need for parenteral administration, high cost, increasing treatment failure rates, and emergence of drug resistance (Burza et al 2018)

Summary

Introduction

Leishmaniasis is a neglected tropical disease caused by unicellular protozoan parasites of the genus Leishmania, that affect 98 countries on 5 continents, with approximately 0.7 to 1 million cases of cutaneous leishmaniasis and 50.000 to 90.000 cases of visceral leishmaniasis occur every year. The pentavalent antimonials are the first-line drugs for leishmaniasis treatment, amphotericin B deoxycholate, liposomal amphotericin B and paromomycin, are secondary options for resistant cases (Burza et al 2018). All these compounds have limitations in their use because of side effects, high cost, induction of parasite resistance and in-patient administration (Andrews et al 2014).

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Results