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目的:测定消旋吡喹酮(Pra)、左旋吡喹酮(L-Pra)和右旋吡喹酮(D-Pra)对不同发育期日本血吸虫的作用。方法:用含20%小牛血清的PRMI1640培养不同发育期的血吸虫,测定上述三种药物的体外抗血吸虫作用。体内试验系于小鼠感染血吸虫尾蚴后不同时间灌服(ig)Pra、L-Pra或D-Pra,根据残留平均虫数评估药效。结果:依据药物引起虫的皮层损害程度,虫龄为28d(d28)和35d(d35)的成虫对L-Pra最敏感,而14d(d14)童虫则最不敏感。在药物浓度为0.1-1μg/ml时,L-Pra的抗血吸虫作用较Pra的为强,即使L-Pra的浓度减至Pra最低有效药浓度的1/2亦有效。在体外,上述浓度的D-Pra对不同发育期血吸虫无明显作用。感染小鼠ig单剂量的L-Pra,Pra或D-Pra300mg/kg或500mg/kg,仅前2种药物对3h(do)、21d(d21)童虫和d28及d35成虫有较明显的疗效,而对3d(d3)、7d(d7)和d14童虫的疗效甚差或无效。与L-Pra和Pra相比,D-Pra仅对d35成虫有较差的疗效。感染d35血吸虫成虫的小鼠用L-Pra150mg/kgig治疗,其疗效与用?
Objective: To determine the effect of praziquantel (Pra), L-Pra and D-Pra on Schistosoma japonicum at different developmental stages. Methods: Schistosoma japonicum was cultured in PRMI1640 containing 20% calf serum at different developmental stages to determine the in vitro anti-schistosome effect of these three drugs. In vivo tests were performed on mice infected with Schistosoma japonicum cercariae at different times (ig) Pra, L-Pra or D-Pra, according to the residual average number of insects to assess efficacy. Results: According to the degree of cortical damage caused by the drug, adult worms 28 d (d28) and 35 d (d35) were the most sensitive to L-Pra, while insects 14 d (d14) were the most insensitive. The anti-schistosome effect of L-Pra was stronger than that of Pra at the drug concentration of 0.1-1 μg / ml, which was effective even when the concentration of L-Pra was reduced to 1/2 of the minimum effective dose of Pra. In vitro, the above concentration of D-Pra had no significant effect on schistosomiasis in different developmental stages. Infection with single doses of L-Pra, Pra or D-Pra at 300 mg / kg or 500 mg / kg in mice ig, only the first two drugs have a significant effect on 3h (do), 21d (d21) and adult d28 and d35 , While the effects on 3d (d3), 7d (d7) and d14 squirrels were poor or ineffective. Compared to L-Pra and Pra, D-Pra has poorer efficacy on d35 adults only. Mice infected with d35 schistosome adult with L-Pra150mg / kgig treatment, its efficacy and use?