Isolation of a terpenoid compound from Mikania sp. with activity on Trypanosoma cruzi

KAREN VARGAS GOMEZ; EMILIO MALCHIOIDI; NATASH CERNY; ANDRES SANCHEZ ALBERTI; VALERIA P. SÜLSEN ; LAURA C. LAURELLA ; AUGUSTO BIVONA; SILVIA CAZORLA

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas. RICiFa 2020+1; 2021

American trypanosomiasis or Chagas disease is caused by the protozoan Trypanosoma cruzi and affect 6-7 million people worldwide. Drugs available for its treatment have limited efficacy and are associated with serious adverse effects. Therefore, there is an urgent need to find new safer and more effective drugs for its treatment. Natural compounds have been considered as an important strategy for finding new drugs with antiparasitic activity. Thus, the aim of this work was to isolate compounds with anti-T. cruzi activity from the active dichloromethane extract of Mikania periplocifolia (Asteraceae). The fractionation and purification of the extract, performed by chromatographic methods, alllowed the isolation of a pure compound (A) that was tested on T. cruzi. The isolated compound was a terpenoid with a ɣ-lactone moiety. This compound showed moderate active against trypomastigotes with a 50% inhibitory concentration (IC50) of 57.8 µg/ml. On amastigotes, this compound presented an IC50=7.7 µg/ml. The cytotoxicity was evaluated on mammalian cells (CC50=37.9 µg/ml). These results demonstrate that compound A was active an selective against the intracellular form of T. cruzi. Further analysis will be encouraged in order to complete its identification. The evaluation of the in vivo activity of compound A will also be considered.