Nowak M, Hutchinson G W, Copeman D B
Trop Med Parasitol. 1987 Jun;38(2):128-30.
A primary in vitro screen was developed to screen for drug activity against isolated Onchocerca gibsoni. The assay estimates variation in motility through the use of a motility meter. Of the seven compounds tested in the screen; ivermectin, CGP 6140, CGP20376, Mel W and furapyrimidone gave MI50 concentrations (the concentration at which the motility was reduced to 50% of the control value at 72 hours) below 10(-4) M, whereas suramin gave variable results depending on the varying susceptibility of individual worms and levamisole at 10(-4) M had no significant effect on the worms. The effects of these drugs were not reversible as removal of the worms into drug-free medium caused no increase in motility. Thus the reduction in motility is regarded as indicating significant metabolic damage. The results compared favourably with reported in vivo tertiary screens for activity against Onchocerca species. This is a quantitative, inexpensive and reproducible method for assessing the effectiveness of drugs against Onchocerca and could be included into the primary screens for activity against filarial worms.
开发了一种体外初步筛选方法，用于筛选针对分离出的吉氏盘尾丝虫的药物活性。该检测方法通过使用运动计来估计运动性的变化。在筛选中测试的七种化合物中，伊维菌素、CGP 6140、CGP20376、Mel W和呋喃嘧酮的半数抑制浓度（即72小时时运动性降低至对照值50%的浓度）低于10^(-4) M，而苏拉明的结果因个体蠕虫的敏感性不同而有所变化，10^(-4) M的左旋咪唑对蠕虫没有显著影响。这些药物的作用是不可逆的，因为将蠕虫转移到无药物培养基中不会导致运动性增加。因此，运动性的降低被认为表明存在显著的代谢损伤。该结果与报道的针对盘尾丝虫属物种的体内三级筛选结果相比具有优势。这是一种定量、廉价且可重复的方法，用于评估药物对盘尾丝虫的有效性，可纳入针对丝虫的初步筛选中。
