蒿甲醚对小鼠体内日本血吸虫磷酸化酶、乳酸脱氢酶、三磷酸腺苷酶和磷酸葡萄糖脱氢酶的影响<英文>  

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

作　　者：肖树华[1] 尤纪青[1] 郭惠芳[1] 梅静艳[1] 焦佩英[1] 姚民一[1] 庄兆农 冯正[1] 

机构地区：[1]中国预防医学科学院寄生虫病研究所世界卫生组织疟疾,血吸虫病和丝虫病合作中心,上海中国200025

出　　处：《中国药理学报》1999年第8期750-754,共5页Acta Pharmacologica Sinica

基　　金：Project supported by the National Natural Science Foundation of China (№ 39670662);in part by Tropical Medicine Research Center granted from NIH of USA (№ I P50AT39461-01).

摘　　要：目的:观察蒿甲醚(Art)对日本血吸虫磷酸化酶(PP)、乳酸脱氢酶(LDH)、6-磷酸葡萄糖脱氢酶(G-6-PDH)和三磷酸腺苷酶(ATPase)的影响。方法:感染32-38天的小鼠于灌服Art 100-300mg·kg^(-1)后24-72h剖杀,收集雌()、雄虫(),按NADH和NADPH的形成和无机磷的释放量测定虫的上述4种酶。结果:感染小鼠用Art 300mg·kg^(-1)治疗后24-48h,、虫的总PP和PPa(激活型)活力明显增加,而PPb则无或仅有轻度增加。上述小鼠用Art 100-300mg·kg^(-1)治疗后24-72h,LDH和G-6-PDH的抑制率分别为9％-59％()和41％-75％()及22％-42％()和74%-80%()。用300mg·kg^(-1)治疗后24h,仅虫的Mg^2-ATPase明显受抑制,48h后,Ca^(2+)-ATPase、Mg^(2+)-ATPase和Na^+-K^+-ATPase分别抑制17％()和19％(),32％()和48％(),及29％()和44％()。结论:Art引起血吸虫PPa活力的增加,使虫的糖原分解,并抑制LDH使虫糖酵解的终产物乳酸明显减少。此外,对血吸虫虫的G-6-PDH有明显的抑制作用。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 ig 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℃. RESULTS: After infected mice were treated ig 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 ig 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 Mg2+-ATPase showed marked inhibition in both male and female worms. At 48 h, the Ca2+-ATPase, Mg2+-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 formalin of lactate. Moreover, Art exerts a potent inhibition on the G-6-PDH activity of the female S japonicum.

关 键 词：日本血吸虫 蒿甲醚 磷酸化酶 药理 乳酸脱氢酶 

分 类 号：R978.61[医药卫生—药品]