Department of Medical Parasitology, Faculty of Medicine, Alexandria University, Alexandria, Egypt.
Parasit Vectors. 2011 May 11;4:73. doi: 10.1186/1756-3305-4-73.
Miltefosine, which is the first oral drug licensed for the treatment of leishmaniasis, was recently reported to be a promising lead compound for the synthesis of novel antischistosomal derivatives with potent activity in vivo against different developmental stages of Schistosoma mansoni. In this paper an in vitro study was carried out to investigate whether it has a biocidal activity against the aquatic stages of Schistosoma mansoni and its snail intermediate host, Biomphalaria alexandrina , thus being also a molluscicide. Additionally, to see whether miltefosine can have a broad spectrum antischistosomal activity, a similar in vitro study was carried out on the adult stage of Schistosoma haematobium, the second major human species, its larval stages and snail intermediate host, Bulinus truncutes. This was checked by scanning electron microscopy.
Miltefosine proved to have in vitro ovicidal, schistolarvicidal and lethal activity on adult worms of both Schistosoma species and has considerable molluscicidal activity on their snail hosts. Scanning electron microscopy revealed several morphological changes on the different stages of the parasite and on the soft body of the snail, which further strengthens the current evidence of miltefosine's activity. This is the first report of mollusicidal activity of miltefosine and its in vitro schistosomicidal activity against S.haematobium.
This study highlights miltefosine not only as a potential promising lead compound for the synthesis of novel broad spectrum schistosomicidal derivatives, but also for molluscicidals.
米替福新是第一种被批准用于治疗利什曼病的口服药物,最近有报道称,它是一种很有前途的先导化合物,可用于合成新型抗血吸虫衍生物,对曼氏血吸虫的不同发育阶段具有强大的体内活性。本文进行了一项体外研究,以调查米替福新是否对曼氏血吸虫的水生阶段及其蜗牛中间宿主埃及血吸虫具有杀菌活性,因此也是一种杀螺剂。此外,为了观察米替福新是否具有广谱抗血吸虫活性,我们对第二种主要人类血吸虫——埃及血吸虫的成虫阶段及其幼虫阶段和蜗牛中间宿主——斑氏小腆螺,也进行了类似的体外研究。这是通过扫描电子显微镜检查来检查的。
米替福新被证明对两种血吸虫的成虫具有体外杀卵、杀幼虫和致死活性,并对其蜗牛宿主具有相当大的杀螺活性。扫描电子显微镜显示,寄生虫的不同阶段和蜗牛的软体组织都发生了几种形态变化,这进一步加强了米替福新活性的现有证据。这是米替福新具有杀螺活性及其对埃及血吸虫的体外杀血吸虫活性的首次报道。
这项研究不仅强调了米替福新作为合成新型广谱杀血吸虫衍生物的潜在有前途的先导化合物的潜力,还强调了它作为杀螺剂的潜力。