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蒿甲醚对小鼠体内日本血吸虫磷酸化酶、乳酸脱氢酶、三磷酸腺苷酶及葡萄糖磷酸脱氢酶的影响。

Effect of artemether on phosphorylase, lactate dehydrogenase, adenosine triphosphatase, and glucosephosphate dehydrogenase of Schistosoma japonicum harbored in mice.

作者信息

Xiao S H, You J Q, Guo H F, Mei J Y, Jiao P Y, Yao M Y, Zhuang Z N, Feng Z

机构信息

Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, WHO Collaborating Center for Malaria, Schistosomiasis and Filariasis, Shanghai, China.

出版信息

Zhongguo Yao Li Xue Bao. 1999 Aug;20(8):750-4.

Abstract

AIM

To study the effect of artemether (Art) on phosphorylase (PP), lactate dehydrogenase (LDH), glucose-6-phosphate dehydrogenase (G-6-PDH), and adenosine triphosphatase (ATPase) of S japonicum.

METHODS

Mice infected with S. japonicum cercariae for 32-38 d were treated i.g. with Art 100-300 mg.kg-1 and killed 24-72 h after treatment for collection of schistosomes. The activities of PP, LDH, and G-6-PDH were measured by the formation of NADH or NADPH. The activity of ATPase was measured by the rate of release of inorganic phosphate (Pi) from ATP at 37 degrees C.

RESULTS

After infected mice were treated i.g. with Art 300 mg.kg-1 for 24-48 h, the activities of total PP and PPa (active form) increased markedly in both male and female worms, while PPb (inactive form) showed no or only a slight increase. At 24-72 h after the above-mentioned mice were treated i.g. with Art 100-300 mg.kg-1, the inhibitory rates of LDH and G-6-PDH were 9%-59% (male) and 41%-75% (female) as well as 22%-42% (male) and 74%-89% (female), respectively. When Art 300 mg.kg-1 was given to infected mice for 24 h, only the activity of Mg(2+)-ATPase showed marked inhibition in both male and female worms. At 48 h, the Ca(2+)-ATPase, Mg(2+)-ATPase, and Na(+)-K(+)-ATPase were all inhibited, the inhibitory rates of 17% (male) and 19% (female), 32% (male) and 48% (female) as well as 29% (male) and 44% (female), respectively.

CONCLUSION

In schistosomes, the increase in the activity of AMP-independent PPa induced by Art may enhance the decomposition of glycogen and the inhibition of LDH by Art could reduce the formation of lactate. Moreover, Art exerts a potent inhibition on the G-6-PDH activity of the female S japonicum.

摘要

目的

研究蒿甲醚(Art)对日本血吸虫磷酸化酶(PP)、乳酸脱氢酶(LDH)、葡萄糖-6-磷酸脱氢酶(G-6-PDH)和三磷酸腺苷酶(ATPase)的影响。

方法

用100 - 300mg·kg-1的蒿甲醚灌胃感染日本血吸虫尾蚴32 - 38天的小鼠,给药后24 - 72小时处死小鼠收集血吸虫。通过NADH或NADPH的生成来测定PP、LDH和G-6-PDH的活性。通过在37℃下ATP释放无机磷酸(Pi)的速率来测定ATPase的活性。

结果

感染小鼠用300mg·kg-1的蒿甲醚灌胃24 - 48小时后,雄虫和雌虫中总PP和PPa(活性形式)的活性均显著增加,而PPb(无活性形式)无增加或仅略有增加。上述小鼠用100 - 300mg·kg-1的蒿甲醚灌胃后24 - 72小时,LDH和G-6-PDH的抑制率分别为9% - 59%(雄虫)和41% - 75%(雌虫)以及22% - 42%(雄虫)和74% - 89%(雌虫)。当给感染小鼠300mg·kg-1的蒿甲醚24小时时,仅雄虫和雌虫中的Mg(2+)-ATPase活性有显著抑制。48小时时,Ca(2+)-ATPase、Mg(2+)-ATPase和Na(+)-K(+)-ATPase均受到抑制,抑制率分别为17%(雄虫)和19%(雌虫)、32%(雄虫)和48%(雌虫)以及29%(雄虫)和44%(雌虫)。

结论

在血吸虫中,蒿甲醚诱导的不依赖AMP的PPa活性增加可能增强糖原分解,蒿甲醚对LDH的抑制可减少乳酸生成。此外,蒿甲醚对日本血吸虫雌虫的G-6-PDH活性有强力抑制作用。

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