Objective To evaluate the in-vivo efficacy of three artemisinin derivatives artemether, artesunate and dihydroartemisinin against schistosomulum of praziquantel-resistant Schistosoma japonicum,. Methods The S. japonicum subjected to subcurative dose of praziquantel for 11 rounds was served as a praziquantel-resistant strain, while the field-derived strain without exposure to praziquantel was served as a praziquantel-susceptible strain. The mice infected with the two strains of cercaria were treated with artemether, artesunate and dihydroartemisinin at a single dose of 300 mg/kg by gavage in days 7 and 8 post-infection, respectively. All mice were dissected 45 days post-infection, and the adult worms were collected to estimate worm and female worm burden reductions caused by drug treatment. Results Administration of artemether, artesunate and dihydroartemisinin at a single dose of 300 mg/kg given on days 7 and 8 post-infection achieved total worm burden reductions of 69.8%-71.0%and female worm burden reductions of 75.4%-79.8%in mice infected with praziquantel-susceptible strain, whereas the same treatments reduced total worm burdens of 64.6%-66.1% and female worm burdens of 69.3%-71.1% in mice infected with praziquantel-resistant strain. There were no significant differences between the two strains. Conclusion Praziquantel-resistant S. japonicum remains sensitive to the three major artemisinin derivatives artemether, artesunate and dihydroartemisinin, and no cross-resistance is observed between praziquantel and artemisinin in S. japonicum.%目的:观察3种青蒿素衍生物双氢青蒿素、青蒿琥酯和蒿甲醚对日本血吸虫吡喹酮抗性株童虫的体内作用效果。方法以经11轮亚治疗剂量吡喹酮筛选的日本血吸虫为吡喹酮抗性株,以未暴露于吡喹酮的日本血吸虫作为吡喹酮敏感株,收集2虫株尾蚴感染小鼠,以300 mg/kg双氢青蒿素、青蒿琥酯和蒿甲醚对感染后7~8 d童虫分别进行2次灌服用药(总剂量600 mg/kg),所有小鼠于感染后45 d解剖,收集小鼠体内成虫并计数,计算减虫率和减雌率。结果300 mg/kg双氢青蒿素、蒿甲醚和青蒿琥酯2日疗法(总剂量600 mg/kg)对日本血吸虫吡喹酮敏感株7~8 d童虫的减虫率为69.8%~71.0%,减雌率为75.4%~79.8%;对日本血吸虫吡喹酮抗性株7~8 d童虫的减虫率为64.6%~66.1%,减雌率为69.3%~71.1%,差异均无统计学意义(均P>0.05)。结论日本血吸虫吡喹酮抗性株对青蒿素类衍生物双氢青蒿素、青蒿琥酯和蒿甲醚依然敏感,青蒿素衍生物与吡喹酮在日本血吸虫中不存在交叉抗药性。
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