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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

Anti-Trypanosoma cruzi Activity in vitro of Phases and Isolated Compounds from Excoecaria lucida Leaves

Author(s): Cristiane F. da Silva*, Ania O. Pacheco, Rayane N. Alves, Josean F. Tavares, Marcelo S. da Silva and Julio C.E. Arranz

Volume 14, Issue 6, 2018

Page: [556 - 562] Pages: 7

DOI: 10.2174/1573406414666180112112154

Price: $65

Abstract

Background: Chagas disease is caused by the protozoan parasite Trypanosoma cruzi. This illness is found mainly in 21 Latin American countries and an estimated 8 million people are infected worldwide. The unsatisfactory chemotherapy provokes severe toxicity and resistant strains. Medicinal plants constitute a promising source of new drugs and remedies against all kinds of disorders, mainly infectious diseases arousing interest worldwide.

Objective: The aim of this study is the isolation, structural identification and evaluation of the trypanocidal activity of samples present in the Excoecaria lucida Sw. leaves.

Methods: Total extract (TE) of E. lucidaSw. leaves was obtained by ethanol extract therefore fractionated sequentially with hexane, ethyl acetate and n-butanol, to obtain three phases: Hex, EA and But, respectively. Ellagic acid (EL1) was purified from both EA and But phases, while EL2; a 1:1 stigmasterol-3-O-β-D-glucopyranoside plus sitosterol-3-O-β-D-glucopyranoside mixture was obtained from the Hex phase. Activity assays were performed using bloodstream and intracellular forms of T. cruzi and cytotoxicity assays using L929 fibroblasts.

Results: The EL1 and EL2 samples were more active against bloodstream trypomastigote forms with EC50 of 53.0±3.6 and 58.2±29.0 µg/mL, respectively; at 100 µg/mL. These samples also showed 70% of inhibition of L929 cells infection. Toxicity assays demonstrated that after 96 h of treatment only the fractions Hex and EA presented detectable cytotoxicity.

Conclusion: Ellagic acid, stigmasterol-3-O-β-D-glucopyranoside and sitosterol-3-O-β-Dglucopyranoside are reported for the first time in E. lucida Sw. leaves as well as their biological activity studies supporting further investigations for Chagas disease treatment.

Keywords: Excoecaria lucida Sw., Chagas disease, Trypanosoma cruzi, in vitro studies, natural products, ellagic acid.

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