Ibarra O F, Jenkins D C
J Helminthol. 1984 Jun;58(2):107-12. doi: 10.1017/s0022149x00028583.
The response of the free-living stages of Nippostrongylus brasiliensis, Nematospiroides dubius, Haemonchus contortus, Trichostrongylus colubriformis and Ostertagia ostertagi to a wide variety of antiparasitic agents in vitro was investigated. All the major broad spectrum veterinary anthelmintics showed good activity against each of these worms with EC50 values varying from about 0.0002 mg/l for certain benzimidazoles and ivermectin to about 6.5 mg/l for febantel. Of 22 known narrow spectrum anthelmintics useful only against H. contortus and/or helminths other than trichostrongyles, only 10% showed good activity at concentrations equal to or less than 10.0 mg/l. Further, only one of 15 antiprotozoal agents showed good activity in these tests at the 10.0 mg/l level. The screening test employing free-living Nippostrongylus brasiliensis was selected for an extended trial where the evaluation of 1400 miscellaneous organic chemicals was undertaken. Approximately 10% of these showed activity at concentrations equal to or less than 10.0 mg/l. It is concluded that in vitro screening tests employing the free-living stages of these five genera of nematodes afford simple yet effective means for selecting relevant compounds for further evaluation as possible leads to new broad spectrum anthelmintics for use in ruminants. However, tests using the free-living stages of these worms, including H. contortus, are unsuitable for detecting narrow spectrum 'specifics', e.g., for the treatment of haemonchiasis.
研究了巴西日圆线虫、可疑螺旋线虫、捻转血矛线虫、蛇形毛圆线虫和奥斯特他线虫自由生活阶段对多种抗寄生虫药物的体外反应。所有主要的广谱兽用驱虫药对这些蠕虫均显示出良好的活性,其半数有效浓度(EC50)值有所不同,某些苯并咪唑和伊维菌素约为0.0002毫克/升,非班太尔约为6.5毫克/升。在22种已知的仅对捻转血矛线虫和/或毛圆科以外的蠕虫有效的窄谱驱虫药中,只有10%在浓度等于或低于10.0毫克/升时显示出良好活性。此外,在这些试验中,15种抗原虫药物中只有一种在10.0毫克/升水平显示出良好活性。采用自由生活的巴西日圆线虫进行的筛选试验被选作一项扩展试验,对1400种有机化学品进行了评估。其中约10%在浓度等于或低于10.0毫克/升时显示出活性。结论是,利用这五个属线虫的自由生活阶段进行体外筛选试验,为选择相关化合物进行进一步评估提供了简单而有效的手段,这些化合物有可能成为反刍动物用新型广谱驱虫药的先导物。然而,使用这些蠕虫(包括捻转血矛线虫)的自由生活阶段进行的试验不适合检测窄谱“特效药”,例如用于治疗血矛线虫病。