Evaluation of the in vitro trypanocidal activity of triterpenes uvaol, betulinic acid and its semi-synthetic derivatives against the Y strain of Trypanosoma cruzi / Avaliação da atividade tripanocida in vitro dos triterpenos uvaol, ácido betulínico e seus derivados semissintéticos contra a cepa Y de Trypanosoma cruzi

• Autor(a) principal: Júnior, Moisés Soares Moreira
• Data de Publicação: 2021
• Outros Autores: Flauzino, Lúzio Gabriel Bocalon, Marçal, Maria Gabriela, Ferreira, Daniele da Silva, Pauletti, Patrícia Mendonça, Januário, Ana Helena, e Silva, Márcio Luís Andrade, Magalhães, Lizandra Guidi Magalhães, Cunha, Wilson Roberto
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Revista Veras
• Texto Completo: https://ojs.brazilianjournals.com.br/ojs/index.php/BRJD/article/view/36073
• topic: betulinic acid; neglected tropical diseases; Trypanosoma cruzi; uvaol

Chagas disease is a neglected tropical disease that affects millions of people worldwide. Trypanosoma cruzi (T. cruzi) is the causative agent of Chagas disease and its transmission occurs through blood meal by triatomine bugs, being oral transmission the most common form. More than 100 years after the disease´s discovery, benzonidazole is the only efficient drug against T. cruzi; however, this drug has numerous serious side effects and is only efficient in the acute phase of the disease. Natural products, such as triterpenes, have been an important source of new substances to combat human parasitology. In this study, two triterpenes, uvaol and betulinic acid, were tested against the parasite T. cruzi. The best results of in vitro tests were observed for uvaol with an IC50 value of 70.3 µM against the trypomastigost forms and an IC50 value of 90.6 µM against the amastigost forms. Three semi-synthetic derivatives of betulinic acid were obtained; the acetylated derivative showed excellent results against trypomastigotes forms (IC50 = 15.67 µM), but was not active against the amastigotes forms. The cytotoxic MTT test was also performed on LLCMK2 cells (Macaca mullata kidney epithelial cells) and betulinic acid showed the highest selectivity index (SI) with a value of 1.3.