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新型化合物在感染捻转血矛线虫的沙鼠和绵羊体内显示出驱虫活性。

Novel compound shows in vivo anthelmintic activity in gerbils and sheep infected by Haemonchus contortus.

机构信息

Instituto de Ganadería de Montaña, CSIC-Universidad de León, 24346, Grulleros, León, Spain.

Departamento de Ciencias Biomédicas, Facultad de Veterinaria, Universidad de León, 24071, León, Spain.

出版信息

Sci Rep. 2022 Jul 29;12(1):13004. doi: 10.1038/s41598-022-17112-3.

Abstract

The control of gastrointestinal nematodes in livestock is becoming increasingly difficult due to the limited number of available drugs and the rapid development of anthelmintic resistance. Therefore, it is imperative to develop new anthelmintics that are effective against nematodes. Under this context, we tested the potential toxicity of three compounds in mice and their potential anthelmintic efficacy in Mongolian gerbils infected with Haemonchus contortus. The compounds were selected from previous in vitro experiments: two diamine (AAD-1 and AAD-2) and one benzimidazole (2aBZ) derivatives. 2aBZ was also selected to test its efficacy in sheep. In Mongolian gerbils, the benzimidazole reduced the percentage of pre-adults present in the stomach of gerbils by 95% at a dose of 200 mg/kg. In sheep, there was a 99% reduction in the number of eggs shed in faeces after 7 days at a dose of 120 mg/kg and a 95% reduction in the number of worm adults present in the abomasum. In conclusion, 2aBZ could be considered a promising candidate for the treatment of helminth infections in small ruminants.

摘要

由于可用药物数量有限且驱虫剂耐药性迅速发展,控制家畜胃肠道线虫变得越来越困难。因此,开发针对线虫有效的新型驱虫剂势在必行。在这种情况下,我们在小鼠中测试了三种化合物的潜在毒性及其对感染捻转血矛线虫的蒙古沙鼠的潜在驱虫效果。这些化合物是从以前的体外实验中选择的:两种二胺(AAD-1 和 AAD-2)和一种苯并咪唑(2aBZ)衍生物。选择 2aBZ 来测试其在绵羊中的疗效。在蒙古沙鼠中,苯并咪唑在 200mg/kg 的剂量下将胃中前幼虫的存在百分比降低了 95%。在绵羊中,在 120mg/kg 的剂量下,粪便中脱落的卵数量减少了 99%,在皱胃中存在的成虫数量减少了 95%。总之,2aBZ 可以被认为是治疗小反刍动物寄生虫感染的有前途的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3333/9338094/8675ab55195e/41598_2022_17112_Fig1_HTML.jpg

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