几种苯并咪唑和微管蛋白抑制剂对贾第虫属的体外活性。
Activities of several benzimidazoles and tubulin inhibitors against Giardia spp. in vitro.
作者信息
Morgan U M, Reynoldson J A, Thompson R C
机构信息
Institute for Molecular Genetics and Animal Disease, School of Veterinary Studies, Murdoch University, Western Australia.
出版信息
Antimicrob Agents Chemother. 1993 Feb;37(2):328-31. doi: 10.1128/AAC.37.2.328.
Abstract
Previous studies in our laboratory have shown that albendazole is effective against Giardia spp. in vitro and in vivo, prompting an investigation of the effects of several related benzimidazoles (BZs) on the viability of this protozoan parasite. A range of BZs was tested, and their effects were compared with those of a number of microtubule inhibitors. The effects produced by the two types of drugs were markedly similar, namely, trophozoite detachment and distortion of morphology and general structure, indicating a potential antimicrotubule mode of action for BZs. Mebendazole, albendazole, and fenbendazole proved to be among the most effective BZs tested, exhibiting apparent irreversibility. Nocodazole, oxfendazole, and albendazole sulfoxide, among others, produced transient inhibitions only. Further studies are required to evaluate all available BZs and other antigiardial agents to ensure the development of the most effective and safest antigiardial agent possible.
摘要
我们实验室之前的研究表明，阿苯达唑在体外和体内对贾第虫属均有效，这促使人们对几种相关苯并咪唑（BZs）对这种原生动物寄生虫活力的影响展开研究。测试了一系列苯并咪唑，并将它们的效果与多种微管抑制剂的效果进行比较。这两类药物产生的效果明显相似，即滋养体脱离以及形态和总体结构的畸变，这表明苯并咪唑可能具有抗微管作用模式。甲苯达唑、阿苯达唑和芬苯达唑被证明是所测试的最有效的苯并咪唑，表现出明显的不可逆性。诺考达唑、奥芬达唑和阿苯达唑亚砜等仅产生短暂抑制作用。需要进一步研究以评估所有可用的苯并咪唑和其他抗贾第虫药物，以确保开发出可能最有效且最安全的抗贾第虫药物。
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