药物（PZQ）压力下日本血吸虫的耐药性诱导及抗血吸虫新药的筛选
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摘要
目的:
1日本血吸虫吡喹酮耐药虫体的筛选及其超微结构的观察
2体外实验观察地西泮类衍生物(B3, B30, B3-O2, B3-2O2)和五羟色胺/多巴胺受体拮抗剂(利培酮,奥氮平,喹硫平)的抗血吸虫效应。
方法:
(1)动物模型建立:按常规逸尾蚴方法获得日本血吸虫尾蚴,每只小鼠经腹部皮肤感染单只阳性钉螺逸出的日本血吸虫尾蚴(单性)60±2条。
(2)血吸虫成虫的获得:颈椎脱臼处死小鼠,肝门静脉灌注法收集成虫,将采集的活的雄性成虫置于DMEM培养液中,每皿6条,放入37℃、5% CO2培养箱中。
(3)体外培养的血吸虫活力评分标准:3分:虫体活跃、体态柔和、颜色呈透明状;2分:活动度略差,虫体稍僵硬、颜色呈半透明状;1分:虫体仅头端或尾端活动轻微,虫体僵硬呈白色;0分:完全死亡。
(4)应用本课题组测定的PZQ ED50(20.89㎎/㎏/只)作为亚治疗剂量,以七种不同诱导时间[ 5 d、10 d、20 d、30 d、60 d、90 d(1次/ d)和10 d (1次/2 d)]对成虫期日本血吸虫虫体进行药物压力下的耐药性筛选。
(5)应用PZQ ED50对感染日本血吸虫尾蚴3 w和6 w后小鼠喂饲连续给药30 d,肝门静脉灌注法收集雄性成虫,加入不同浓度PZQ连续培养5 d,观察虫体活力变化。
(6)成虫期虫体诱导30 d后再经治疗剂量PZQ连续喂饲给药5 d,体外培养观察虫体对药物的敏感性变化。
(7)收集日本血吸虫雄性成虫,加入不同浓度地西泮类衍生物(B3, B30, B3-O2, B3-2O2)和五羟色胺/多巴胺受体拮抗剂(利培酮、奥氮平、富马酸喹硫平)连续培养5 d,观察虫体活力并影像记录。
(8)扫描电镜观察虫体超微结构的变化:收集培养48 h后的日本血吸虫,用生理盐水(PH 7.4)冲洗3遍,放入4%戊二醛固定过夜, 0.1 M的磷酸盐缓冲液冲洗两次,每次10 min;1%的锇酸固定1 h;30%、50%、70%、80%、90%叔丁醇依次脱水,每次10 min,100%叔丁醇脱水三次,放入-20℃过夜;IB-5真空离子溅射镀膜机镀金,送入S570扫描电镜(日本EDAX公司)观察。
结果:
(1)成虫期日本血吸虫虫体经PZQ ED50以不同诱导时间作用后,随着用药时间的延长,所筛选到的虫体对药物的敏感性呈现下降趋势,连续用药30 d后的虫体对PZQ的敏感性降低最显著,表明30d是适宜的诱导时间。
(2)感染6 w的成虫期和感染3 w的童虫期虫体经PZQ ED50连续诱导30 d后,体外培养,虫体对PZQ的敏感性均显著下降,童虫期虫体经诱导后对PZQ的敏感性下降更显著。扫描电镜观察诱导后虫体的体表、抱雌沟与正常未诱导虫体相比损伤轻微,特别是童虫期诱导后虫体超微结构损伤程度更小。
(3)日本血吸虫成虫经药物筛选后再用治疗剂量(200㎎/㎏) PZQ连续给药5 d后,体外培养观察显示,虫体在不同浓度PZQ作用下存活率仍达100%,扫描电镜显示体表、抱雌沟损害比单纯用药30 d的虫体轻。
(4)地西泮类衍生物B3和B30在药物浓度为50μmol/L时,在体外可以导致日本血吸虫完全死亡;五羟色胺/多巴胺受体拮抗剂利培酮对日本血吸虫有一定的杀虫效应。
结论:
(1)在持续药物压力下,感染宿主体内不同发育阶段日本血吸虫可能对吡喹酮产生一定的耐受性,可筛选出耐药虫体,特别是在感染早期(3 w)的童虫阶段,在药物压力下更易于产生耐受性,为临床用药提供实验依据。
(2)地西泮衍生物B3、B30在体外抗血吸虫作用非常显著,而五羟色胺/多巴胺受体拮抗剂利培酮对日本血吸虫有一定的杀虫效应,具有潜在应用价值,值得进一步深入研究。
Objective:
(1) To selecte S .japonicum of decreased PZQ sensitivity and observe ultrastructural alterations of worms under drug pressure.
(2) Investigate four kinds of Diazepam derivatives(B3、B30、B3-O2 and B3-2O2) and three kinds of 5-HT receptor/ dopamine antagonists(risperidone、olanzapine、quetiapine fumarate) activity on anti-schistosoma.
Methods:
(1) Infection of experimental animals: S. japomicum cercariae released from laboratory infected snails, were kindly provided by Institute of Parasitic Diseases of Jiangsu province. Mice were infected with 60±2 S. japonicum cercariae each, through the shaved abdominal skin(single-sex infection).
(2) Collect adult worms: All groups of animals were sacrificed by cervical dislocation after the final treatment. In mice, worms were collected by the perfusion technique. Only male worms (usually 5-6) were distributed in duplicate tissue culture dishes (3.0 cm) in DMEM supplemented with 20% newborn calf serum. Dishes were kept at 37 ?C in an atmosphere of 5% CO2 in air.
(3) Motility criteria: Motility was scored using the following criteria: 3 (moving whole body); 2 (moving only parts of body); 1 (immobile but not dead, unstained with vital dye); and 0 (immobile, stained with vital dye).
(4) A batch of mice were infected with cercariae and six weeks later mice were randomly divided into seven groups (usually 10 mice per group) each of which was treated with subcurative doses of PZQ. Treatments were repeated for 5、10、20、30、60、90 days (1 time/per day)、10 days (1 time/2 days) and mice were perfused three weeks after the initial treatment.
(5) 3 weeks and 6 weeks after infection of S. japonicum, the mice were treated intragastrically with subcurative doses of PZQ for 30 consecutive days. The male adult worms were obtained by perfusion of mice three weeks after the initial treatment, then these worms were subjected in vitro in the medium with different PZQ concentrations. After incubation overnight (about 16 hours later), the worms were washed and resuspended in drug-free medium and observed for the subsequent 5 days.
(6) Mice, 6 weeks after infection with S. japonicum, was induced with subcurative doses of PZQ for 30 consecutive days. The selected-worms were treated with 200 mg/kg PZQ repeatedly for 5 consecutive days. The survived worms were cultured in the medium with different PZQ concentrations and were observed for the subsequent 5 days.
(7) In vitro test, adult male worms kept in medium were exposed overnight to four kinds of Diazepam derivatives(B3、B30、B3-O2 and B3-2O2) and 5-HT receptor/ dopamine antagonist(risperidone、olanzapine、quetiapine fumarate) with different concentrations. After that, worms were washed and resuspended in drug-free medium, then were observed during the following 5 days.
(8) Preparation of specimen for scanning electron microscopy analysis: Worms were rinsed 3 times with physiological saline and fixed in 2.5% glutaraldehyde(pH 7.4) at 4°C for 24 hours, then worms were washed with phosphate( 0.2 mol/L, pH 7.4) two times and post-fixed in 1% osmium tetroxide for 1 hour. After that, the worms were dehydrated through a graded series of tert-butyl alcohol and stored at -20°C overnight. After drying, the worms were mounted on aluminium stubs and coated with platinum and paladium in an ion-sputtering apparatus, IB-5 (EIKO) for 10min. Then the worms were examined and photographed in a Hitachi scanning electron microscope S-570 (EDAX Japan).
Results:
(1) Seven groups of mice were treated intragastrically 6 weeks after infected with S. japonicum by the subcurative doses of PZQ in different days. After selecting for 30 consecutive days, the surviving worms’sensitivity to PZQ was significantly decreased. These findings showed that the treatment with subcurative doses for 30 consecutive days was the suitable time to select worms of sensitivity decreased.
(2) The mice infected with S. japonicum 3 weeks and 6 weeks later were treated intragastrically with subcurative doses of PZQ for 30 consecutive days. Both of the surviving worms had the lower sensitivity to PZQ than the original unselected worms, the parasite sensitivity decreased more obvious when mice were treated in 3 weeks after infection. The damages of ultrastructure in the tegument and gynecophoral canal in the selected-worms were slighter compared with the worms from untreated mice by SEM.
(3) While the selected-worms were repeatedly treated with 200 mg/kg PZQ for 5 consecutive days, the survived worms cultured in the medium with different PZQ concentrations were still alive completely. The damages of ultrastructure in the tegument and gynecophoral canal in the repeated treatment selected-worms were slighter compared with the worms from the mice after incubating to drug pressure for 30 days.
(4) In vitro test, adult worms incubated in DMEM medium containing B3、B30 at concentrations of 50μmol/L were all killed; Worms cultured in risperidone have low survival rates.
Conclusion:
(1) After exposure to subcurative doses of PZQ for 30 consecutive days, the sensitivity of the survived worms in different stages to PZQ decreased, especially 3-week-old worms were strikingly refractory to the drug, which provide a foundation for designing respective clinical trials in humans.
(2) Diazepam derivatives, B3 and B30 on S. Japonicum have showed its effect of killing worm; while 5-HT / dopamine receptor antagonist risperidone has a little effect on worms. These results would be helpful for further development of new broad-spectrum anthelminthics.
1日本血吸虫吡喹酮耐药虫体的筛选及其超微结构的观察
2体外实验观察地西泮类衍生物(B3, B30, B3-O2, B3-2O2)和五羟色胺/多巴胺受体拮抗剂(利培酮,奥氮平,喹硫平)的抗血吸虫效应。
方法:
(1)动物模型建立:按常规逸尾蚴方法获得日本血吸虫尾蚴,每只小鼠经腹部皮肤感染单只阳性钉螺逸出的日本血吸虫尾蚴(单性)60±2条。
(2)血吸虫成虫的获得:颈椎脱臼处死小鼠,肝门静脉灌注法收集成虫,将采集的活的雄性成虫置于DMEM培养液中,每皿6条,放入37℃、5% CO2培养箱中。
(3)体外培养的血吸虫活力评分标准:3分:虫体活跃、体态柔和、颜色呈透明状;2分:活动度略差,虫体稍僵硬、颜色呈半透明状;1分:虫体仅头端或尾端活动轻微,虫体僵硬呈白色;0分:完全死亡。
(4)应用本课题组测定的PZQ ED50(20.89㎎/㎏/只)作为亚治疗剂量,以七种不同诱导时间[ 5 d、10 d、20 d、30 d、60 d、90 d(1次/ d)和10 d (1次/2 d)]对成虫期日本血吸虫虫体进行药物压力下的耐药性筛选。
(5)应用PZQ ED50对感染日本血吸虫尾蚴3 w和6 w后小鼠喂饲连续给药30 d,肝门静脉灌注法收集雄性成虫,加入不同浓度PZQ连续培养5 d,观察虫体活力变化。
(6)成虫期虫体诱导30 d后再经治疗剂量PZQ连续喂饲给药5 d,体外培养观察虫体对药物的敏感性变化。
(7)收集日本血吸虫雄性成虫,加入不同浓度地西泮类衍生物(B3, B30, B3-O2, B3-2O2)和五羟色胺/多巴胺受体拮抗剂(利培酮、奥氮平、富马酸喹硫平)连续培养5 d,观察虫体活力并影像记录。
(8)扫描电镜观察虫体超微结构的变化:收集培养48 h后的日本血吸虫,用生理盐水(PH 7.4)冲洗3遍,放入4%戊二醛固定过夜, 0.1 M的磷酸盐缓冲液冲洗两次,每次10 min;1%的锇酸固定1 h;30%、50%、70%、80%、90%叔丁醇依次脱水,每次10 min,100%叔丁醇脱水三次,放入-20℃过夜;IB-5真空离子溅射镀膜机镀金,送入S570扫描电镜(日本EDAX公司)观察。
结果:
(1)成虫期日本血吸虫虫体经PZQ ED50以不同诱导时间作用后,随着用药时间的延长,所筛选到的虫体对药物的敏感性呈现下降趋势,连续用药30 d后的虫体对PZQ的敏感性降低最显著,表明30d是适宜的诱导时间。
(2)感染6 w的成虫期和感染3 w的童虫期虫体经PZQ ED50连续诱导30 d后,体外培养,虫体对PZQ的敏感性均显著下降,童虫期虫体经诱导后对PZQ的敏感性下降更显著。扫描电镜观察诱导后虫体的体表、抱雌沟与正常未诱导虫体相比损伤轻微,特别是童虫期诱导后虫体超微结构损伤程度更小。
(3)日本血吸虫成虫经药物筛选后再用治疗剂量(200㎎/㎏) PZQ连续给药5 d后,体外培养观察显示,虫体在不同浓度PZQ作用下存活率仍达100%,扫描电镜显示体表、抱雌沟损害比单纯用药30 d的虫体轻。
(4)地西泮类衍生物B3和B30在药物浓度为50μmol/L时,在体外可以导致日本血吸虫完全死亡;五羟色胺/多巴胺受体拮抗剂利培酮对日本血吸虫有一定的杀虫效应。
结论:
(1)在持续药物压力下,感染宿主体内不同发育阶段日本血吸虫可能对吡喹酮产生一定的耐受性,可筛选出耐药虫体,特别是在感染早期(3 w)的童虫阶段,在药物压力下更易于产生耐受性,为临床用药提供实验依据。
(2)地西泮衍生物B3、B30在体外抗血吸虫作用非常显著,而五羟色胺/多巴胺受体拮抗剂利培酮对日本血吸虫有一定的杀虫效应,具有潜在应用价值,值得进一步深入研究。
Objective:
(1) To selecte S .japonicum of decreased PZQ sensitivity and observe ultrastructural alterations of worms under drug pressure.
(2) Investigate four kinds of Diazepam derivatives(B3、B30、B3-O2 and B3-2O2) and three kinds of 5-HT receptor/ dopamine antagonists(risperidone、olanzapine、quetiapine fumarate) activity on anti-schistosoma.
Methods:
(1) Infection of experimental animals: S. japomicum cercariae released from laboratory infected snails, were kindly provided by Institute of Parasitic Diseases of Jiangsu province. Mice were infected with 60±2 S. japonicum cercariae each, through the shaved abdominal skin(single-sex infection).
(2) Collect adult worms: All groups of animals were sacrificed by cervical dislocation after the final treatment. In mice, worms were collected by the perfusion technique. Only male worms (usually 5-6) were distributed in duplicate tissue culture dishes (3.0 cm) in DMEM supplemented with 20% newborn calf serum. Dishes were kept at 37 ?C in an atmosphere of 5% CO2 in air.
(3) Motility criteria: Motility was scored using the following criteria: 3 (moving whole body); 2 (moving only parts of body); 1 (immobile but not dead, unstained with vital dye); and 0 (immobile, stained with vital dye).
(4) A batch of mice were infected with cercariae and six weeks later mice were randomly divided into seven groups (usually 10 mice per group) each of which was treated with subcurative doses of PZQ. Treatments were repeated for 5、10、20、30、60、90 days (1 time/per day)、10 days (1 time/2 days) and mice were perfused three weeks after the initial treatment.
(5) 3 weeks and 6 weeks after infection of S. japonicum, the mice were treated intragastrically with subcurative doses of PZQ for 30 consecutive days. The male adult worms were obtained by perfusion of mice three weeks after the initial treatment, then these worms were subjected in vitro in the medium with different PZQ concentrations. After incubation overnight (about 16 hours later), the worms were washed and resuspended in drug-free medium and observed for the subsequent 5 days.
(6) Mice, 6 weeks after infection with S. japonicum, was induced with subcurative doses of PZQ for 30 consecutive days. The selected-worms were treated with 200 mg/kg PZQ repeatedly for 5 consecutive days. The survived worms were cultured in the medium with different PZQ concentrations and were observed for the subsequent 5 days.
(7) In vitro test, adult male worms kept in medium were exposed overnight to four kinds of Diazepam derivatives(B3、B30、B3-O2 and B3-2O2) and 5-HT receptor/ dopamine antagonist(risperidone、olanzapine、quetiapine fumarate) with different concentrations. After that, worms were washed and resuspended in drug-free medium, then were observed during the following 5 days.
(8) Preparation of specimen for scanning electron microscopy analysis: Worms were rinsed 3 times with physiological saline and fixed in 2.5% glutaraldehyde(pH 7.4) at 4°C for 24 hours, then worms were washed with phosphate( 0.2 mol/L, pH 7.4) two times and post-fixed in 1% osmium tetroxide for 1 hour. After that, the worms were dehydrated through a graded series of tert-butyl alcohol and stored at -20°C overnight. After drying, the worms were mounted on aluminium stubs and coated with platinum and paladium in an ion-sputtering apparatus, IB-5 (EIKO) for 10min. Then the worms were examined and photographed in a Hitachi scanning electron microscope S-570 (EDAX Japan).
Results:
(1) Seven groups of mice were treated intragastrically 6 weeks after infected with S. japonicum by the subcurative doses of PZQ in different days. After selecting for 30 consecutive days, the surviving worms’sensitivity to PZQ was significantly decreased. These findings showed that the treatment with subcurative doses for 30 consecutive days was the suitable time to select worms of sensitivity decreased.
(2) The mice infected with S. japonicum 3 weeks and 6 weeks later were treated intragastrically with subcurative doses of PZQ for 30 consecutive days. Both of the surviving worms had the lower sensitivity to PZQ than the original unselected worms, the parasite sensitivity decreased more obvious when mice were treated in 3 weeks after infection. The damages of ultrastructure in the tegument and gynecophoral canal in the selected-worms were slighter compared with the worms from untreated mice by SEM.
(3) While the selected-worms were repeatedly treated with 200 mg/kg PZQ for 5 consecutive days, the survived worms cultured in the medium with different PZQ concentrations were still alive completely. The damages of ultrastructure in the tegument and gynecophoral canal in the repeated treatment selected-worms were slighter compared with the worms from the mice after incubating to drug pressure for 30 days.
(4) In vitro test, adult worms incubated in DMEM medium containing B3、B30 at concentrations of 50μmol/L were all killed; Worms cultured in risperidone have low survival rates.
Conclusion:
(1) After exposure to subcurative doses of PZQ for 30 consecutive days, the sensitivity of the survived worms in different stages to PZQ decreased, especially 3-week-old worms were strikingly refractory to the drug, which provide a foundation for designing respective clinical trials in humans.
(2) Diazepam derivatives, B3 and B30 on S. Japonicum have showed its effect of killing worm; while 5-HT / dopamine receptor antagonist risperidone has a little effect on worms. These results would be helpful for further development of new broad-spectrum anthelminthics.
引文
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