Ticona Juan C, Bilbao-Ramos Pablo, Flores Ninoska, Dea-Ayuela M Auxiliadora, Bolás-Fernández Francisco, Jiménez Ignacio A, Bazzocchi Isabel L
Instituto Universitario de Bio-Orgánica Antonio González and Departamento de Química Orgánica, Universidad de La Laguna, Avenida Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain.
Instituto de Investigaciones Fármaco Bioquímicas, Facultad de Ciencias Farmacéuticas y Bioquímicas, Universidad Mayor de San Andrés, Avenida Saavedra 2224, Miraflores, La Paz, Bolivia.
Foods. 2020 Sep 7;9(9):1250. doi: 10.3390/foods9091250.
The current therapies of leishmaniasis, the second most widespread neglected tropical disease, have limited effectiveness and toxic side effects. In this regard, natural products play an important role in overcoming the current need for new leishmanicidal agents. The present study reports a bioassay-guided fractionation of the ethanolic extract of leaves of against four species of spp. promastigote forms, which afforded six known alkamides (-). Their structures were established on the basis of spectroscopic and spectrometric analysis. Compounds and were identified as the most promising ones, displaying higher potency against spp. promastigotes (IC values ranging from 1.6 to 3.8 µM) and amastigotes of (IC values ranging from 8.2 to 9.1 µM) than the reference drug, miltefosine. The efficacy of ()-piplartine () against infection in an in vivo model for cutaneous leishmaniasis was evidenced by a significant reduction of the lesion size footpad and spleen parasite burden, similar to those of glucantime used as the reference drug. This study reinforces the therapeutic potential of ()-piplartine as a promising lead compound against neglected infectious diseases caused by parasites.
利什曼病是第二大广泛流行的被忽视热带病，其现有治疗方法效果有限且存在毒副作用。在这方面，天然产物在满足当前对新型杀利什曼原虫药物的需求中发挥着重要作用。本研究报告了对 叶乙醇提取物针对四种 属前鞭毛体形式进行生物测定导向的分级分离，得到了六种已知的链状酰胺（-）。它们的结构通过光谱和波谱分析得以确定。化合物 和 被确定为最有前景的化合物，对 属前鞭毛体（IC值范围为1.6至3.8 μM）和 的无鞭毛体（IC值范围为8.2至9.1 μM）显示出比参考药物米替福新更高的效力。在皮肤利什曼病的体内模型中，（）-哌普拉丁（）对 感染的疗效通过足垫病变大小和脾脏寄生虫负荷的显著降低得以证明，与用作参考药物的葡糖胺类似。本研究强化了（）-哌普拉丁作为针对由 寄生虫引起的被忽视传染病的有前景先导化合物的治疗潜力。
