Treatment against visceral leishmaniasis (VL) is mainly hampered by drug toxicity, long treatment regimens and/or high costs. Thus, the identification of novel and low-cost antileishmanial agents is urgent. Acarbose (ACA) is a specific inhibitor of glucosidase-like proteins, which has been used for treating diabetes. In the present study, we show that this molecule also presents in vitro and in vivo specific antileishmanial activity against Leishmania infantum. Results showed an in vitro direct action against L. infantum promastigotes and amastigotes, and low toxicity to mammalian cells. In addition, in vivo experiments performed using free ACA or incorporated in a Pluronic^® F127-based polymeric micelle system called ACA/Mic proved effective for the treatment of L. infantum-infected BALB/c mice. Treated animals presented significant reductions in the parasite load in their spleens, livers, bone marrows and draining lymph nodes when compared to the controls, as well as the development of antileishmanial Th1-type humoral and cellular responses based on high levels of IFN-γ, IL-12, TNF-α, GM-CSF, nitrite and IgG2a isotype antibodies. In addition, ACA or ACA-treated animals suffered from low organ toxicity. Treatment with ACA/Mic outperformed treatments using either Miltefosine or free ACA based on parasitological and immunological evaluations performed one and 15 days post-therapy. In conclusion, data suggest that the ACA/Mic is a potential therapeutic agent against L. infantum and merits further consideration for VL treatment.

内脏利什曼病 (VL) 的治疗主要受到药物毒性、长期治疗方案和/或高成本的阻碍。因此，迫切需要鉴定新型和低成本的杀虫剂。阿卡波糖 (ACA) 是一种葡萄糖苷酶样蛋白的特异性抑制剂，已用于治疗糖尿病。在本研究中，我们表明该分子还具有针对婴儿利什曼原虫的体外和体内特异性抗利什曼原虫活性。结果显示在体外对L. infantum 前鞭毛体和无鞭毛体有直接作用，对哺乳动物细胞毒性低。此外，使用游离 ACA 或并入 Pluronic ^{®进行的体内实验}被称为 ACA/Mic 的基于 F127 的聚合物胶束系统证明对治疗婴儿乳杆菌感染的 BALB/c 小鼠有效。与对照组相比，接受治疗的动物的脾脏、肝脏、骨髓和引流淋巴结中的寄生虫负荷显着降低，并且基于高水平的 IFN-γ 的抗寄生虫 Th1 型体液和细胞反应的发展， IL-12、TNF-α、GM-CSF、亚硝酸盐和 IgG2a 同种型抗体。此外，ACA 或 ACA 治疗的动物器官毒性较低。根据在治疗后 1 天和 15 天进行的寄生虫学和免疫学评估，使用 ACA/Mic 的治疗优于使用米替福新或免费 ACA 的治疗。总之，数据表明 ACA/Mic 是一种潜在的治疗剂L. infantum值得进一步考虑进行 VL 治疗。