Drimanes from Drimys brasiliensis with leishmanicidal and antimalarial activity

Vanessa Duarte Claudino,Rosendo Augusto Yunes,Alberto Giménez,Angela Malheiros,David Gutierrez-Yapu,Efrain Salamanca,Valdir Cechinel Filho,Franco Delle Monache,Kesia Caroline Da Silva

doi:10.1590/0074-0276108022013002

Abstract

This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50 ) values ranging from 39-100 µg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 µg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 µM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 µM. The CHCl3 extract demonstrated activity (IC50 of 3.0 µg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 µM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.

Highlights

Neglected tropical diseases, including leishmaniasis, are among the most common causes of illness among the poorest populations living in developing countries
Leishimanicidal activity of extracts and compounds isolated from stem bark of Drimys brasilensis in vitro on promastigote forms of Leishmania amazonensis and Leishmania brasiliensis
Based on the results presented above, D. brasiliensis can be considered a source of compounds with leishmanicidal activity

Summary

Introduction

Neglected tropical diseases, including leishmaniasis, are among the most common causes of illness among the poorest populations living in developing countries. The World Health Organization (WHO) considers leishmaniasis to be one of six major infectious diseases, with a high detection rate and the capacity to produce deformities It is a disease with a variety of agents, hosts, vectors and transmission patterns, but limited knowledge about some aspects of the disease makes it difficult to control (WHO 2010). It has recently been demonstrated that a hexane extract of the stem bark of Drimys brasiliensis and polygodial, a drimane, exhibit activity against Leishmania spp and Trypanosoma cruzi (Corrêa et al 2011) This information contributes to the further study of this plant species, with the aim of obtaining new drugs to treat the neglected diseases

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Conclusion