Leishmanicidal activity of onopordopicrin isolated from the leaves of Brachylaena discolor

Julião A. Monjane1*, Diandra Capusiri2, Alberto Giménez2, Olov Sterner3
1Chemistry Department, Eduardo Mondlane University, P.O. Box 257, Maputo, Mozambique.
2Instituto de Investigaciones Fármaco Bioquímicos, San Andrés University, La Paz, Bolivia.
3Centre for Analysis and Synthesis, Lund University, P.O. Box 22100, Lund, Sweden.

Corresponding Author: juliao.monjane@uem.mz; Tel: +258 82 867 6497
Recieved Date: May 09, 2018; Accepted Date: July 05, 2018; Published Date: 08 July 2018
Citation: Monjane JA, Capusiri D, Giménez A, Sterner O. Leishmanicidal activity of onopordopicrin isolated from the leaves of Brachylaena discolor. Trop J Nat Prod Res. 2018; 2(7):328-331.  https://doi.org//10.26538/tjnpr/v2i7.5
Copyright: © 2018 Monjane et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Brachylaena discolor (Asteraceae) is a medicinal plant used in Mozambique to treat stomachache, tuberculosis, and diabetes. To discover new lead compounds with leishmanicidal activity, a methanolic extract of the leaves of this plant was investigated. Through fractionation, employing several chromatographic methods, two sesquiterpene lactones onopordopicrin (1) and its germacronolide epoxide derivative (2), together with other ten know phenolic compounds derivatives (3-12) were isolated. The structures of the isolated compounds were determined by spectroscopic methods, mainly 1D and 2D NMR experiments, as well as by comparing their spectroscopic data as reported in the literature. Compounds 1 and 2 were evaluated for their leishmanicidal activity using the Colorimetric method-XXT. Compound 1 showed a significant leishmanicidal activity against Leishmania amazonensis and L. braziliensis (IC50 values 39.6 and 27.9 ?M, respectively) as compared to miltefosine (12.5 and 12.0 ?M, respectively), a currently used agent to treat leishmaniosis. While compound 2 was inactive against both stains tested with IC50 values >50?M compared with the same agent. Compounds 3-12 were not assayed for leishmanicidal activity. This is the first study reporting the above-mentioned activity of onopordopicrin (1). The results could suggest that compound 1 is a promising lead structure to treat leishmaniosis.

Keywords: Asteraceae, Brachylaena discolor, Onopordopicrin, Germanocronolides, Antileishmanial activity.
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