Antiproliferative effect and ultrastructural alterations induced by 5- O -methylembelin on Trypanosoma cruzi

SPINA R; LOZANO E; BARRERA P; AGUERO MA; TAPIA A; FERESIN G; SOSA MA

PHYTOMEDICINE

ELSEVIER GMBH

Año: 2018 vol. 46 p. 111 - 118

0944-7113

ackground: Embelin (EMB), obtained from Oxalis erythrorhiza Gillies ex Hooker et Arnott (Oxalidaceae), wasreported against Trypanosoma cruzi and Leishmania spp. Additionally, antiprotozoan activity against Plasmodiumfalciparum was reported for its methylated derivative (ME).Purpose: To evaluate the potential anti-Trypanosoma cruzi activity of EMB, ME and 2,5-di-O-methylembelin(DME) and analyze the possible mechanism of action.Study design/Methods: EMB was isolated by a chromatographic method from the air-dried ground whole plant.To evaluate the effects of methylation, ME and DME were synthesized and tested against T. cruzi epimastigotesand trypomastigotes. The most active compound ME was evaluated against amastigotes. Ultrastructural alterations,ROS generation and the effect on mitochondrial activity of ME were measured.Results: Compounds inhibited the proliferation of epimastigotes. ME was also active against intracellularamastigotes. Mitochondrial alterations were observed by TEM. Additionally, ME modified the mitochondrialactivity, and induced an increase in ROS levels. These evidences postulate the mitochondrion as a possible targetof ME.