Compounds 1 and 2 (selenocyanate and diselenide derivatives, respectively) were evaluated for their potential use in vivo against visceral leishmaniasis (VL). Both entities showed low cytoxicity in vitro in Vero and Caco-2 cell lines. However, the compounds were not suitable for their oral administration, since they exhibited poor values of intestinal permeability in vitro. Microsomal stability assays did not show any metabolite for compound 1 after 120 min, whereas 2 was highly metabolized by the enzyme CYP450. Thus, the in vivo efficacy of compound 1 was assessed in a murine model of L. infantum VL. The daily i.v. administration of 1 mg/kg of compound 1 during 5 consecutive days reduced parasite load in liver, spleen and bone marrow (99.2%, 91.7% and 61.4%, respectively) compared to non-treated mice. To the best of our knowledge, this is the first time that a selenium compound has been tested in vivo against VL. Thus, this work evidences the possible usefulness of selenocyanate derivatives for the treatment of this disease.

评估了化合物1和2（分别为硒氰酸酯和二硒化物衍生物）在体内对抗内脏利什曼病（VL）的潜在用途。两个实体显示出低细胞毒性在体外在Vero和Caco-2细胞系。但是，这些化合物不适合口服，因为它们在体外的肠通透性差。微粒体稳定性试验未显示120分钟后化合物1的任何代谢产物，而2被CYP450酶高度代谢。因此，在小鼠的模型中评估了化合物1的体内功效。婴儿乳杆菌VL。与未治疗的小鼠相比，连续5天每天静脉注射1 mg / kg的化合物1减少了肝脏，脾脏和骨髓中的寄生虫负荷（分别为99.2％，91.7％和61.4％）。据我们所知，这是硒化合物首次在体内针对VL进行测试。因此，这项工作证明了硒氰酸酯衍生物可能用于治疗该疾病。