Lecová L, Stuchlíková L, Prchal L, Skálová L
Department of biochemical sciences, Faculty of Pharmacy,Charles University in Prague,Heyrovského 1203, 500 05, Hradec Králové,Czech Republic.
Parasitology. 2014 Nov;141(13):1686-98. doi: 10.1017/S0031182014001401. Epub 2014 Sep 9.
Monepantel (MOP), a new anthelmintic drug from a group of amino-acetonitrile derivatives, has been intensively studied during last years. Many authors examined this new drug from different perspectives, e.g. efficacy against different species and stages of parasites, mode of action, metabolism, pharmacokinetics, toxicity, resistance, ecotoxicity, etc. MOP is an anthelmintic for livestock (currently only sheep and goats), with molecular mode of action which is different to all other anthelmintics. MOP has a broad-spectrum of activity against gastrointestinal nematodes of sheep, including adults and L4 larvae of the most important species. The key feature of MOP is its full effectiveness against strains of nematodes resistant to benzimidazoles, levamisole, macrocyclic lactones and closantel. After oral administration, MOP is quickly absorbed into the bloodstream and quickly metabolized to MOP sulfone that has a similar efficacy as the parent molecule. Several other MOP metabolites formed in ovine hepatocytes were described. MOP and its metabolites are considered to be non-toxic to environment and its components, such as soil microflora, aquatic organisms, dung organisms, vegetation, etc. The aim of the presented review was not to collect all reported data but to bring an overview of various approaches in the study of MOP and to evaluate their principal results.
莫能菌素(MOP)是一种新型驱虫药,属于氨基乙腈衍生物类,在过去几年中受到了深入研究。许多作者从不同角度对这种新药进行了研究,例如对不同种类和阶段寄生虫的疗效、作用方式、代谢、药代动力学、毒性、耐药性、生态毒性等。MOP是一种用于家畜(目前仅用于绵羊和山羊)的驱虫药,其分子作用方式与所有其他驱虫药不同。MOP对绵羊的胃肠道线虫具有广谱活性,包括最重要种类的成虫和L4幼虫。MOP的关键特性是其对耐苯并咪唑、左旋咪唑、大环内酯类和氯氰碘柳胺的线虫菌株具有完全有效性。口服给药后,MOP迅速吸收进入血液并迅速代谢为莫能菌素砜,其疗效与母体分子相似。还描述了在绵羊肝细胞中形成的其他几种MOP代谢产物。MOP及其代谢产物被认为对环境及其成分,如土壤微生物、水生生物、粪便生物、植被等无毒。本综述的目的不是收集所有已报道的数据,而是对MOP研究中的各种方法进行概述并评估其主要结果。