Considering the lack of effective and safe therapy for the treatment of Chagas disease, the antihypertensive drug manidipine (MDP) was in vitro evaluated against Trypanosoma cruzi. The bioenergetics of trypomastigotes was studied in the presence of the drug using fluorimetric and luminescent assays. Manidipine showed a potent antiparasitic activity, with IC₅₀ values of 0.1 μM (intracellular amastigotes) and 3 μM (trypomastigotes), resulting in a promising selectivity index against the amastigotes (>1459). Using fluorimetric analysis, the drug showed depolarisation of the electric potential of the plasma membrane with no alteration of the permeability. A decrease in ATP levels suggested a bioenergetic alteration of the mitochondria, which was confirmed by the depolarisation of the mitochondrial membrane potential and a slight increase of the ROS levels. This is the first study to show the promising in vitro effectiveness of the antihypertensive MDP against T. cruzi, which may represent a candidate for future investigations in animal models.

考虑到缺乏有效和安全的治疗南美锥虫病的方法，对降压药马尼地平（MDP）进行了体外克氏锥虫评估。在药物存在下，使用荧光测定法和发光测定法研究了锥虫的生物能。马尼地平显示出有效的抗寄生虫活性，IC ₅₀值分别为0.1μM（胞内变形虫）和3μM（锥虫），导致针对变形虫的选择性指数（> 1459）。使用荧光分析法，该药物显示质膜电位去极化，而渗透率没有变化。ATP含量的降低表明线粒体发生了生物能改变，这可以通过线粒体膜电位的去极化和ROS含量的轻微增加来证实。这是第一项显示抗高血压MDP对抗克氏锥虫（T. cruzi）的有前景的体外研究，它可能代表动物模型的未来研究对象。