吡喹酮衍生物抗日本血吸虫生物学效应研究  

Biological effects research of praziquantel derivatives anti-Schistosoma japonicum

作　　者：孙缓[1] 董兰兰[1] 赵波[1] 仇思婕[1] 孙德群[2] 夏超明[1] 

机构地区：[1]苏州大学基础医学与生物科学学院病原生物学系,苏州215123 [2]山东大学威海分校海洋学院,威海264209

出　　处：《中国人兽共患病学报》2014年第6期556-562,共7页Chinese Journal of Zoonoses

基　　金：国家863项目(No.2012AA0203006)~~

摘　　要：目的观察32种YCH-II-P系列PZQ衍生物对体外培养的日本血吸虫成虫和童虫活性的影响。方法 ICR小鼠感染日本血吸虫尾蚴后第17d及第6周肝门静脉灌注法收集童虫与成虫,分别加不同浓度的化合物于培养液,过夜后(16h)无菌生理盐水洗涤虫体3次,换新鲜培养液继续培养虫体72h,每天置体视显微镜下观察其死亡率及活力降低情况,收集第72h虫体作扫描电镜观察。结果 32种YCH-II-P系列PZQ衍生物筛选出P96、P125、P126、P64种有效化合物。其中P96作用浓度为50μmol/L时虫体完全死亡,体外抗日本血吸虫成虫及童虫临界致死浓度均为25μmol/L,SEM显示虫体皮层及抱雌沟内壁损伤严重。结论 YCH-II-P系列PZQ衍生物中P96体外具有显著的杀日本血吸虫成虫和童虫作用效应。To observe the effects of 32 kinds of YCH-II-P series PZQ derivatives on juvenile and adult worms of Schistosoma japonicum （S. japonicum） in vitro, ICR mice were infected with S. japonicum cercariae. Mice were sacrificed on 6th week or 17 days after infection, and then the juvenile and adult schistosoma were collected by perfusion with ice-cold Hanks＇ balanced salt solution （HBSS, pH 7.2） from portal vein of liver. Worms were placed in DMEM medium containing different concentrations of drugs for 16 hours. The parasites were washed 3 times and soaked in drug-free medium for another 72 hours, observing under stereo-microscopy each day and by scanning electron microscope （SEM）. Four kinds of YCH-II-P series effective compounds were P96, P125, P126, and P6 in vitro, and the parasites completely died in the concentration of 50μmol/L. P96 and the critical lethal concentration against both adult and juvenile worms was 25μmol/L. SEM showed the parasites cortex and gynecophoral ditch with seriously injures. These findings demonstrated that the P96 is effective PZQ derivatives on both juvenile and adult S. japonicum in vitro.

关 键 词：日本血吸虫 PZQ衍生物 体外培养 

分 类 号：R383.24[医药卫生—医学寄生虫学]