Xiao S, You J, Guo H, Jiao P, Mei J, Yao M, Feng Z
Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, WHO Collaborating Center of Malaria, Schistosomiasis and Filariasis, Shanghai 200025.
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1998;16(1):25-8.
To study the effect of artemether (Art) on hexokinase (HK), glucose phosphate isomerase (GPI) and phosphofructokinase (PFK) of Schistosoma japonicum.
Mice infected with schistosome cercariae for 4-5 wk were treated ig with Art 100 or 300 mg.kg-1 and killed 24 h or 48 h after medication for collection of schistosomes. The activities of HK, GPI and PFK of the worms were determined by measuring the formation of NADPH or consumption of NADH.
Worms from the infected mice treated ig with Art at a single dose of 300 mg.kg-1 the inhibition rates of HK activity of female and male worms were 33.7% and 13.7%, respectively 24 h after administration. Similar results were seen in GPI activity, but 48 h after medication, the inhibition rate of GPI increased to 46.2% (female) and 32.9% (male), respectively. Worms from mice treated with Art 100 or 300 mg.kg-1, the inhibitory effect on PFK in female worms was found much higher than that of male worms the inhibition rates of PFK were 64.9%-71.0% in female worms and 16.3%-54.2% in male worms, respectively at 24 h and 48 h after treatment.
The results suggest that in the glycolytic pathway of schistosome PFK might be one of the targets attacked by Art.
研究蒿甲醚（Art）对日本血吸虫己糖激酶（HK）、磷酸葡萄糖异构酶（GPI）和磷酸果糖激酶（PFK）的影响。
用日本血吸虫尾蚴感染小鼠4 - 5周后，分别以100或300 mg·kg-1的蒿甲醚灌胃给药，给药后24小时或48小时处死小鼠收集血吸虫。通过检测NADPH的生成或NADH的消耗来测定虫体中HK、GPI和PFK的活性。
单次灌胃给予300 mg·kg-1蒿甲醚的感染小鼠，给药24小时后，雌、雄虫体HK活性的抑制率分别为33.7%和13.7%。GPI活性也有类似结果，但给药48小时后，GPI的抑制率分别升至46.2%（雌性）和32.9%（雄性）。给予100或300 mg·kg-1蒿甲醚处理的小鼠虫体，对雌虫PFK的抑制作用明显高于雄虫，给药后24小时和48小时，雌虫PFK的抑制率分别为64.9% - 71.0%，雄虫为16.3% - 54.2%。
结果提示在血吸虫糖酵解途径中，PFK可能是蒿甲醚攻击的靶点之一。
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