EMBELIN AND ITS METHYLATED DERIVATIVE ARE ACTIVE AGAINST Trypanosoma cruzi

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

Congreso; XXXIII Reunión Anual de la Sociedad de Biología de Cuyo; 2016

Sociedad de Biología de Cuyo

Trypanosoma cruzi is a parasite responsible of Chagas disease, an endemic pathology that affects millions people in LatinAmerica. On the other hand, the benzoquinone embelin, a natural compound from Oxalis erythrorhiza, was studied due to itsbiological properties (antiinflamatory affects, antioxidant and antitumour activity, among other). The aim was evaluate the effectof embelin (1) and its methylated derivative (2) on different stages of the parasite. The compound (1) and (2) were tested ongrowth and viability of Dm28c strain epimastigotes. Viability was determined by the eosin exclusion method and proliferation bycounting the parasites in a Neubauer hemocytometer. The effects on epimastigote ultrastructure were observed by TEM. Toevaluate the effect of the compounds on intracellular amastigotes, infected and non infected Vero cells were cultured in DMEM.The number of intracellular parasites was counting after staining the cells with Giemsa. Compounds (1) and (2) showed to beactive on proliferation of epimastigotes without affecting the viability. The IC50 value of (2) on epimastigotes was similar tobenznidazole (control) whereas, the IC50 value for (1) was higher. Methylated embelin (2) induced ultrastructural alterations, suchas mitochondrial swelling and cytoplasmic vacuolization. Citotoxicity on Vero cells was similar to that of benznidazole.Proliferating amastigotes were also affected by the methylated embelin, as well as the release of parasites. The results indicate thatembelin (1) and its derivative (2) exhibit cytostatic activity on epimastigotes of Trypanosoma cruzi. The effects on mitochondriacould be related to embelin inducing ROS generation. The results in amastigotes suggest that methylated embelin could affect theproliferation of amastigotes and/or the release from cells. Further studies will be needed to identify the molecular targets on thisparasite. (CICITCA UNSJ PIO-SECITI150 2015-0100022)).