Chemotherapeutic effect of CGI 18041 against subperiodic Brugia malayi infection in Presbytis cristata.

J W Mak, Z Ngah, M F Choong, V Navaratnam
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Abstract

CGI 18041, an adduct of benzothiazol isothiocyanate N-methyl piperazine, was evaluated for its antifilarial properties in subperiodic Brugia malayi infected Presbytis cristata. Animals experimentally infected with 200-400 subperiodic Brugia malayi infective larvae, were matched according to microfilaria density, infective dose, and duration of infection. They were then randomly assigned to various treatment and control groups. The compound was suspended in 1% Tween 20 in distilled water, sonicated, and then fed to monkeys using a stomach tube. Control animals received an equivalent volume of drug diluent. CGI 18041 at a single oral dose of 50 mg/kg had complete adulticidal and microfilaricidal activities against subperiodic B. malayi in P. cristata. It was also extremely effective at a single dose of 25 mg/kg, the final geometric mean microfilaria count being 1.6% of initial level, and only 1.0% of the infective dose was recovered as live adult worms at autopsy 6 weeks post-treatment. In control animals, these were 226.9% and 5.56% respectively.

CGI 18041治疗冠老年炎亚周期性马来布鲁氏菌感染的疗效观察。
研究了异硫氰酸苯并噻唑n -甲基哌嗪加合物CGI 18041对亚周期性马来布鲁吉亚感染的冠状老年炎的抗丝性能。实验动物感染200 ~ 400只马来布鲁氏虫亚周期性感染幼虫,根据微丝蚴密度、感染剂量和感染持续时间进行配对。然后他们被随机分配到不同的实验组和对照组。将这种化合物悬浮在1%吐温20蒸馏水中,对其进行超声波检测,然后用胃管喂给猴子。对照动物接受等量的药物稀释液。CGI 18041单次口服剂量为50 mg/kg时,对冠棘棘虫亚周期马来双歧杆菌具有完全的杀虫和杀微丝活性。单次剂量为25 mg/kg时也非常有效,最终几何平均微丝蚴数为初始水平的1.6%,并且在治疗后6周尸检时,只有1.0%的感染剂量被恢复为活的成虫。对照组分别为226.9%和5.56%。
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