Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas - Avenida Brasil 4365, CEP 21040-900, Manguinhos, Rio de Janeiro, RJ, Brazil.
Centro de Desenvolvimento Tecnológico em Saúde, Fundação Oswaldo Cruz - Avenida Brasil, 4365, CEP 21040-900, Manguinhos, Rio de Janeiro, RJ, Brazil; Universidade Iguaçu - Avenida Abílio Augusto Távora 2134, CEP 26260-045, Dom Rodrigo, Nova Iguaçu, RJ, Brazil.
Int J Parasitol Drugs Drug Resist. 2024 Apr;24:100525. doi: 10.1016/j.ijpddr.2024.100525. Epub 2024 Feb 9.
Leishmaniasis is a disease caused by Leishmania spp., affecting millions of people around the world. For decades, its treatment has been based on pentavalent antimonials, which notoriously cause toxic side effects in patients. In this study, epoxy-α-lapachone incorporated into an oil-in-water-type microemulsion (ELAP-ME) and meglumine antimoniate (MA) were assayed in monotherapy and in combination (ELAP-ME/MA) in BALB/c mice infected with Leishmania (Leishmania) amazonensis. In general, there was a reduction in paw lesion size (up to 37% reduction) and decreases of parasite loads in the footpad (∼40%) and lymph nodes (∼31%) of animals treated with ELAP-ME/MA, when compared to the non-treated control groups. Analyses of serum biochemical parameters revealed that the ELAP-ME/MA showed lower renal and hepatic toxicity when compared to MA 2-doses/week monotherapy. These findings indicate that the ELAP-ME/MA combination may be a promising approach for the treatment of cutaneous leishmaniasis.
利什曼病是由利什曼原虫引起的一种疾病，影响着全球数百万人。几十年来，其治疗一直基于五价锑，而五价锑在患者中会引起明显的毒性副作用。在这项研究中，环氧-α-拉帕酮被纳入油包水型微乳（ELAP-ME）中，并与葡甲胺锑（MA）在 BALB/c 感染了莱什曼（Leishmania）亚马逊ensis 的小鼠中进行了单药和联合治疗（ELAP-ME/MA）。一般来说，与未治疗的对照组相比，用 ELAP-ME/MA 治疗的动物的足垫病变大小（最大减少 37%）和足垫（约 40%）和淋巴结（约 31%）中的寄生虫负荷均有所降低。对血清生化参数的分析表明，与 MA 每周 2 剂量的单药治疗相比，ELAP-ME/MA 显示出较低的肾毒性和肝毒性。这些发现表明，ELAP-ME/MA 联合治疗可能是治疗皮肤利什曼病的一种有前途的方法。
