Giardia lamblia, the causative agent of giardiasis, is an intestinal infection with worldwide distribution and high rates of prevalence. Increased resistance of the parasite and the side effects of the reference drugs employed in the treatment of giardiasis make it necessary to seek new therapeutic agents. Therefore,the aim of this study was to examine the activity of hexadecylphosphocholine (miltefosine), a membrane active alkylphospholipid, that is licensed as an antileishmanial agent against giardiasis. The efficacy of miltefosine was evaluated both in vitro and in vivo in Swiss albino mice. Results of the in vitro testing revealed susceptibility of G. lamblia trophozoites to miltefosine with the following effective concentrations:EC50s of between 20 and 40 lM, and EC90s of between 20 and 80 lM. Immediate total lysis of the organisms was achieved by 100 lM. In vivo testing showed that oral administration of miltefosine,in a daily dose regimen course of 20 mg/kg for three successive days, to infected mice resulted in total elimination of the parasite from the intestine and amelioration of intestinal pathology. Scanning and transmission electron microscopy studies revealed that miltefosine induced severe morphological alterations to G. lamblia trophozoites, mainly at the level of cell membrane and adhesive disc. In conclusion,we believe that this is the first study highlighting G. lamblia as a possible new target for miltefosine.

中文翻译：

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贾第鞭毛虫：miltefosine的新目标。

贾第鞭毛虫病的病原体贾第鞭毛虫是一种肠道感染，在世界范围内分布且患病率很高。寄生虫的抗药性增加以及用于贾第鞭毛虫病的参考药物的副作用使得有必要寻找新的治疗剂。因此，本研究的目的是研究十六烷基磷酸胆碱（miltefosine）的活性，后者是一种具有膜活性的烷基磷脂，被许可用作抗贾第鞭毛虫病的抗疟剂。在瑞士的白化病小鼠体内和体外评估了米替福星的疗效。体外测试结果显示，兰伯氏菌滋养体对米替磷碱的敏感度为以下有效浓度：EC50为20至40 lM，EC90为20至80 lM。生物体立即完全溶解达到100 lM。体内试验表明，对受感染的小鼠连续三天以20 mg / kg的日剂量疗程口服米替福星，可以彻底清除肠道中的寄生虫，并改善肠道病理。扫描和透射电镜研究表明，米线磷碱可导致严重的形态变化，主要发生在细胞膜和粘膜圆盘上。总而言之，我们相信这是首次强调兰氏乳杆菌作为米替福辛可能的新靶标的研究。感染的小鼠的肠道感染完全消除了肠道中的寄生虫，并改善了肠道病理。扫描和透射电镜研究表明，米线磷碱可引起严重的形态变化，主要发生在细胞膜和粘膜圆盘上。总而言之，我们相信这是首次强调兰氏乳杆菌作为米替福辛可能的新靶标的研究。感染的小鼠的肠道感染完全消除了肠道中的寄生虫，并改善了肠道病理。扫描和透射电镜研究表明，米线磷碱可引起严重的形态变化，主要发生在细胞膜和粘膜圆盘上。总而言之，我们相信这是首次强调兰氏乳杆菌作为米替福辛可能的新靶标的研究。