Strote G
Department of Helminthology, Bernhard Nocht Institute, Hamburg, FRG.
Trop Med Parasitol. 1987 Sep;38(3):211-3.
The effect of two new filaricidal compounds, CGP 6140 and CGP 20376, on the microfilariae of O. volvulus was tested in vitro. Culture medium consisted of a 1:1 mixture of IMDM/NCTC 135 supplemented with 20% heat-inactivated foetal calf serum and gentamycin. For pulse experiments the microfilariae were exposed to the drugs for one or three hours in medium without serum and then replaced to serum supplemented medium. In the continuous cultures the microfilariae were exposed to the drugs fur up to 72 hours without a change of medium. The effect of the drugs was assessed by their ability to reduce the larval motility. A reduction of motility of 98-100% after 24 hours of exposure occurred at levels of 1 micron/ml CGP 20376 or 10 mu mg/ml CGP 6140. After exposure for one hour CGP 20376 immobilized 100% of the microfilariae irreversibly at a drug level of 1 microgram/ml. Whereas no significant immobilization was seen with CGP 6140 after one hour. After exposure for three hours CGP 6140 immobilized up to 100% of the microfilariae at drug levels of 10 and 5 micrograms/ml.
在体外测试了两种新型杀丝虫化合物CGP 6140和CGP 20376对盘尾丝虫微丝蚴的作用。培养基由IMDM/NCTC 135的1:1混合物组成，并添加20%热灭活胎牛血清和庆大霉素。在脉冲实验中，微丝蚴在无血清培养基中暴露于药物1或3小时，然后更换为补充血清的培养基。在连续培养中，微丝蚴暴露于药物长达72小时，培养基不更换。通过药物降低幼虫活力的能力来评估药物的效果。在暴露24小时后，当CGP 20376的浓度为1微克/毫升或CGP 6140的浓度为10微克/毫升时，幼虫活力降低了98 - 100%。暴露1小时后，CGP 20376在药物浓度为1微克/毫升时使100%的微丝蚴不可逆地固定。而CGP 6140在暴露1小时后未见明显固定作用。暴露3小时后，CGP 6140在药物浓度为10和5微克/毫升时使高达100%的微丝蚴固定。
