瑞卢,佐的衍生物,作为一种潜在的抗氨基菌剂,对抗Entamoeba histolytica
Maritza Velásquez-Torres1, José Guadalupe Trujillo-Ferrara2, Marycarmen Godínez-Victoria1
1Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de Mexico 11340, Mexico.
Pharmaceuticals (Basel, Switzerland)
|June 28, 2023
概括
利卢在体外和在体内显示出有前途的抗氨基酸活性对抗Entamoeba histolytica. 这项研究表明,利鲁可能是对虫病的潜在替代治疗方法,减少寄生虫的生存能力并影响关键酶.
科学领域:
- 传染性疾病 传染性疾病
- 寄生虫学的寄生虫学
- 药物发现 药物发现 药物发现
背景情况:
- 由Entamoeba histolytica引起的阿米病是全球性的健康问题,导致阿米结肠炎和肝脏.
- 目前的治疗方法,如美特罗尼达,由于副作用而存在局限性.
- 在之前的研究中,瑞卢已显示出潜在的抗寄生虫活性.
研究的目的:
- 为了研究里卢对Entamoeba histolytica的 in vitro 和 in silico 抗氨基酸活性.
- 探索瑞卢作为一种潜在的替代性治疗药物,用于阿米比亚症.
主要方法:
- 在体外测试评估Entamoeba histolytica trophozoite活力和riluzole治疗后的超结构变化.
- 对亡样细胞死亡,活性氧物种 (ROS) 和氧化生产的分析.
- 在基分子对接研究中,评估riluzole对关键的氨基酸抗氧化酶的亲和力.
主要成果:
- 瑞卢治疗 (IC50为319.5μM 5小时) 显著降低了Entamoeba histolytica的活力48.1%.
- 观察到的超结构性损伤包括血膜损失,核变化和溶解,这表明了类似于细胞亡的细胞死亡.
- 利卢触发了ROS和氧化的产生,并降低了抗氧化酶基因表达的调节.
- 对接研究显示,利鲁对Entamoeba histolytica抗氧化酶 (thioredoxin,thioredoxin减少酶,rubrerythrin,peroxiredoxin) 的亲和力比米特罗尼达更高.
结论:
- 利鲁在体外和体内表现出显著的抗氨基酸活性,对抗Entamoeba histolytica.
- 该药物通过诱导细胞死亡和向必需的抗氧化酶,显示出作为替代治疗的潜力.
- 进一步的体内研究是有必要的,以评估riluzole在治疗阿米巴肝的疗效.
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