In vivo activities of the new anthelmintic depsipeptide PF 1022A
In vivo activities of the new anthelmintic depsipeptide PF 1022A
复制标题
DOI：
10.1007/s004360050031
复制
发表时间：
2000-03-01
影响因子：
2
通讯作者：
Mencke, N
中科院分区：
文献类型：
--
作者：
von Samson-Himmelstjerna, G;Harder, A;Mencke, N
pf1022a是一类新的具有抗寄生虫活性的环状沉积肽的成员。在体外和实验室动物研究之后，对其在伴侣动物和家畜身上的驱虫功效进行了测试，以对抗多种肠道线虫和肺蠕虫。研究在老鼠，狗，马身上进行。羊和牛。动物要么是自然感染，要么是实验感染。研究了pf1022a对鼠强线虫和巴西尼波圆线虫的防治作用。犬有棘球绦虫，马有小圆管绦虫。绵羊中有强色毛虫和弯曲血螨，牛中有胎生双孔虫。伴侣动物和家畜口服、皮下或静脉注射的剂量为每公斤体重1至10毫克。在上述所有的检查中都发现了很高的疗效。无临床不耐受症状。（1995）描述了其口服后对弯血螨、色毛毛虱和八角鱼的杀灭作用。相比之下，他们发现PF 1022A在亲本施用后对黄斑绦虫和ostertagi的活性显著降低。几项体外研究表明，PF 1022A在1 μ g/ml （Martin等人，1996年）和0.1 μ g/ml （Conder等人，1995年）剂量下对旋毛虫和巴西强nippolyus有很强的活性。为了进一步了解PF 1022A的驱虫能力，我们在大鼠、狗、马、羊和牛中通过不同的施用途径研究了其对几种重要线虫的活性。
PF 1022A is a member of a new class of cyclic depsipeptides with antiparasitic activity. Following in vitro and laboratory animal studies it was tested for its anthelmintic efficacy in companion and livestock animals against a wide spectrum of intestinal nematodes and lungworms. Studies were carried out in rats, dogs, horses. sheep, and cattle. Animals were either naturally or experimentally infested. The efficacy of PF 1022A was investigated against the following parasite species: Stronglyoides ratti and Nippostrongylus brasiliensis rats. Ancylostoma caininum in dogs, small strongyles (cyathostomes) in horses. Trichostronglyus colubriformis and Haemonchus contortus in sheep, and Dictyocaulus viviparus in cattle. Doses varied from 1 to 10 mg/kg body weight for oral, subcutaneous or intravenous application in companion and livestock animals. High degrees of efficacy were found in all the above-cited examinations. and no clinical signs of intolerability were observed. (1995) described its activity in the jird against Haemonchus contortus, Trichostronglyus colubriformis, and Ostertagia ostertagi after oral application. By contrast, they found a significant decrease in the activity of PF 1022A against T. colubriformis and O. ostertagi after parental application. Several in vitro studies revealed that PF 1022A was very active against Trichinella spiralis and Nippostronglyus brasiliensis when it was given at 1 mu g/ml (Martin ct al. 1996) and at 0.1 mu M against H. contortus (Conder et al, 1995). To provide further insight into the anthelmintic capacity of PF 1022A we investigated its activity against several important nematodes using different routes of application in rats, dogs, horses, sheep, and cattle.