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

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

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蒿甲醚对小鼠日本血吸虫磷酸化酶、乳酸脱氢酶、腺苷三磷酸酶和葡萄糖磷酸脱氢酶的影响。
目的:研究蒿甲醚(Art)对日本血吸虫(S japonicum)磷酸化酶(PP)、乳酸脱氢酶(LDH)、葡萄糖-6-磷酸脱氢酶(G-6-PDH)和腺苷三磷酸酶(ATPase)的影响。方法:小鼠感染日本血吸虫尾蚴32 ~ 38 d, ig Art 100 ~ 300 mg。Kg-1,处理后24-72 h杀灭收集血吸虫。通过NADH和NADPH的形成测定PP、LDH和G-6-PDH的活性。37℃时ATP释放无机磷酸盐(Pi)的速率测定ATP酶活性。结果:感染小鼠ig Art 300 mg。kg-1处理24 ~ 48 h,雄虫和雌虫总PP和总PPa(活性形式)活性均显著升高,而PPb(非活性形式)活性无升高或仅略有升高。24-72 h ig Art 100-300 mg。kg-1, LDH和G-6-PDH的抑制率分别为9% ~ 59%(男性)和41% ~ 75%(女性),22% ~ 42%(男性)和74% ~ 89%(女性)。当艺术300毫克。kg-1给予感染小鼠24 h,只有Mg(2+)- atp酶活性在雌雄蠕虫中均有明显抑制。48 h时,Ca(2+)-ATPase、Mg(2+)-ATPase和Na(+)-K(+)-ATPase均被抑制,抑制率分别为17%(雄)和19%(雌),32%(雄)和48%(雌),29%(雄)和44%(雌)。结论:在血吸虫中,Art诱导的amp非依赖性PPa活性升高可促进糖原分解,Art抑制LDH可减少乳酸的形成。此外,Art对雌性刺参G-6-PDH活性有较强的抑制作用。
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