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

LAURELLA L; CERNY N; KAREN VARGAS GOMEZ; BIVONA A; ANDRES SANCHEZ ALBERTI; MALCHIODI E; CAZORLA S; SULSEN V

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

Universidad Ncional de Cordoba Y Rosario

American trypanosomiasis or Chagas disease is caused by the protozoan Trypanosoma cruziand affect 6-7 million people worldwide. Drugs available for its treatment have limited efficacyand are associated with serious adverse effects. Therefore, there is an urgent need to find newsafer and more effective drugs for its treatment. Natural compounds have been considered asan important strategy for finding new drugs with antiparasitic activity. Thus, the aim of thiswork was to isolate compounds with anti-T. cruzi activity from the active dichloromethaneextract of Mikania periplocifolia (Asteraceae). The fractionation and purification of the extract,performed by chromatographic methods, alllowed the isolation of a pure compound (A) thatwas tested on T. cruzi. The isolated compound was a terpenoid with a ɣ-lactone moiety. Thiscompound showed moderate active against trypomastigotes with a 50% inhibitoryconcentration (IC50) of 57.8 µg/ml. On amastigotes, this compound presented an IC50=7.7µg/ml. The cytotoxicity was evaluated on mammalian cells (CC50=37.9 µg/ml). These resultsdemonstrate 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 ofthe in vivo activity of compound A will also be considered.