Departamento de Sanidad Animal, Facultad de Veterinaria, Universidad de León, Campus de Vegazana, León, Spain.
Instituto de Ganadería de Montaña (CSIC-Universidad de León), Grulleros, León, Spain.
PLoS Negl Trop Dis. 2024 Oct 7;18(10):e0012532. doi: 10.1371/journal.pntd.0012532. eCollection 2024 Oct.
Strongyloidiasis is a neglected tropical disease estimated to affect more than 600 million people worldwide. Recently, the World Health Organization road map on neglected tropical diseases 2021-2030 has put the focus on strongyloidiasis, including this disease within its mass drug administration campaigns. With the use of ivermectin in extensive treatment of all populations at-risk, identifying effective therapeutic alternatives is crucial in case ivermectin resistance arises. The objective of the present study was the development of a larval migration inhibition assay to evaluate the anthelmintic efficacy of commercial drugs and diamine and aminoalcohol derivatives against infective Strongyloides ratti third stage larvae. Through this technique, we successfully screened and estimated the in vitro anthelmintic efficacy of six commercial drugs, seven diamine derivatives and eight aminoalcohol derivatives. Unexpectedly, the half-maximal effective concentration of ivermectin and moxidectin (2.21 and 2.34 μM, respectively) were observed as the highest value obtained among all commercial drugs tested by this in vitro technique. Moreover, some diamine and aminoalcohol derivatives showed superior efficacy inhibiting S. ratti motility compared to ivermectin, with five compounds (AA23, AA34, AO2 AO7 and AO14b) also displaying selectivity indexes on HepG2 and Caco2 higher than 1. These findings underscore the potential of these derivatives as promising alternatives for strongyloidiasis treatment, warranting further investigation and in vivo efficacy assessment.
钩虫病是一种被忽视的热带病,估计影响全球超过 6 亿人。最近,世界卫生组织 2021-2030 年被忽视热带病路线图将重点放在钩虫病上,包括将该疾病纳入大规模药物治疗运动中。随着伊维菌素在广泛治疗所有高危人群中的应用,如果出现伊维菌素耐药性,确定有效的治疗替代方法至关重要。本研究的目的是开发幼虫迁移抑制试验,以评估商业药物和二胺及氨基醇衍生物对感染性大鼠钩虫第三期幼虫的驱虫效果。通过该技术,我们成功筛选并评估了六种商业药物、七种二胺衍生物和八种氨基醇衍生物的体外驱虫效果。出乎意料的是,伊维菌素和莫昔克丁的半数有效浓度(分别为 2.21 和 2.34 μM)是通过该体外技术测试的所有商业药物中获得的最高值。此外,一些二胺和氨基醇衍生物在抑制大鼠钩虫运动方面显示出优于伊维菌素的效果,其中五种化合物(AA23、AA34、AO2、AO7 和 AO14b)对 HepG2 和 Caco2 的选择性指数也高于 1。这些发现强调了这些衍生物作为钩虫病治疗有前途的替代方法的潜力,值得进一步研究和体内疗效评估。