Nakamura M, Hayashi Y, Nogami S, Shibuya T, Tanaka H
Jpn J Exp Med. 1986 Jun;56(3):107-12.
The filaricidal effect of milbemycin D, a compound closely related to ivermectin, was studied in vivo and in vitro using Litomosoides carinii. Microfilaria (mf) densities in the peripheral blood of cotton rats, Sigmodon hispidus, were reduced to less than 3% of initial densities within 24 hours after treating either subcutaneously or orally at doses of 0.05 to 50 mg/kg body weight. In cotton rats treated with diethylcarbamazine at a single dose of 200 mg/kg, mf densities were reduced transiently but recovered to initial levels within 2 weeks, whereas they remained at less than 20% of the initial levels in rats treated with milbemycin D even with a single dose of 0.05 mg/kg. No microfilaricidal effect was observed in cotton rats treated with milbemycin D at a dose of 50 mg/kg for 5 consecutive days. The microfilaricidal effect of milbemycin D was also shown in vitro in RPMI 1640 medium. The minimal effective dose of this compound was estimated to be between 1 and 10 micrograms/ml of medium.
使用卡里尼丝虫(Litomosoides carinii)在体内和体外研究了与伊维菌素密切相关的化合物米尔倍霉素D的杀丝虫作用。以0.05至50mg/kg体重的剂量皮下或口服给药后,棉鼠(Sigmodon hispidus)外周血中的微丝蚴(mf)密度在24小时内降至初始密度的3%以下。以200mg/kg的单剂量给予乙胺嗪治疗的棉鼠,mf密度短暂降低,但在2周内恢复到初始水平,而在用米尔倍霉素D治疗的大鼠中,即使单剂量为0.05mg/kg,mf密度仍保持在初始水平的20%以下。连续5天以50mg/kg的剂量用米尔倍霉素D治疗的棉鼠未观察到杀微丝蚴作用。米尔倍霉素D的杀微丝蚴作用在体外的RPMI 1640培养基中也得到了证实。该化合物的最小有效剂量估计在每毫升培养基1至10微克之间。