萧樹华, 徐月琴. 六种抗血吸虫药物对血吸虫谷-丙转氨酶与谷-草转氨酶的影响J. 药学学报, 1965, 12(4): 242-248.
引用本文: 萧樹华, 徐月琴. 六种抗血吸虫药物对血吸虫谷-丙转氨酶与谷-草转氨酶的影响J. 药学学报, 1965, 12(4): 242-248.
SHIAO SHU-HWA AND HSU YUEH-CHIN, . STUDIES ON THE EFFECT OF SOME SCHISTOSOMACIDES ON GLUTAMIC-PYRUVIC TRANSAMINASE AND GLUTAMICOXALOACETIC TRANSAMINASE OF SCHISTOSOMA JAPONICUMJ. Acta Pharmaceutica Sinica, 1965, 12(4): 242-248.
Citation: SHIAO SHU-HWA AND HSU YUEH-CHIN, . STUDIES ON THE EFFECT OF SOME SCHISTOSOMACIDES ON GLUTAMIC-PYRUVIC TRANSAMINASE AND GLUTAMICOXALOACETIC TRANSAMINASE OF SCHISTOSOMA JAPONICUMJ. Acta Pharmaceutica Sinica, 1965, 12(4): 242-248.

六种抗血吸虫药物对血吸虫谷-丙转氨酶与谷-草转氨酶的影响

STUDIES ON THE EFFECT OF SOME SCHISTOSOMACIDES ON GLUTAMIC-PYRUVIC TRANSAMINASE AND GLUTAMICOXALOACETIC TRANSAMINASE OF SCHISTOSOMA JAPONICUM

  • 摘要: 本文初步探讨了6种抗血吸虫药物对血吸虫谷-丙转氨酶与谷-草转氨酶的影响,观察到将药物直接加至血吸虫匀浆中时,吐酒石2×10-4克分子及南瓜子氨酸5×10-2克分子的浓度皆能使谷-丙转氨酶的活力减低50%左右,后者尚可使谷-草转氨酶的活力增强24%.F30066的浓度为2×10-4克分子时,可抑制谷-草转氨酶的活力28%,对谷-丙转氨酶则无明显影响.萱草根素、甲基敌百虫及玫苯胺对血吸虫匀浆的两种转氨酶均无明显作用.在体外培养试验中,吐酒石使血吸虫谷-丙转氨酶活力减低一半所需的药物浓度为直接加至匀浆中的5倍.血吸虫在含F30066 2×10-4克分子的培基中培养4小时后,谷-丙转氨酶与谷-草转氨酶的活力分别下降25及14%.南瓜子氨酸、玫苯胺、甲基敌百虫及萱草根素对体外培养血吸虫的两种转氨酶活力均无明显影响.在体内试验中,除玫苯胺外,都能引起虫体明显退化,但两种转氨酶的活力似与对照组的相仿.根据试验结果,可以认为,有效药物的抗血吸虫作用可能不是在由转氨酶所促化的代谢环节上.

     

    Abstract: The present paper reports a series of experiments on the influence of tartar emetic, F30066, cucurbitine (a new amino acid isolated from Cucurbita moschata Duch. var. melonaeformis Mark), hemerocallin (an active principle of Hemerocalli thunbergii Baker), dipterex or rosaniline on glutamic-pyruvic transaminase(GPT) and glutamic- oxaloacetic transaminase(GOT) of schistosomes.It was found that when drugs were added to the homogenates of the worms, tartar emetic and cucurbitine had an inhibitory effect on GPT. When the final concentration of tartar emetic was 2×10-4M and that of cucurbitine was 5×10-2M, the extent of inhibition amounted to about 50%. Simul- taneously, cucurbitine showed a weak enhancing effect on GOT. On the contrary, F30066 exerted a weak inhibitory effect on GOT but no effect on GPT. Other compounds did not show any effect on either enzyme. In order to explore the effect of the schistosomacides on the GPT and GOT of the worms maintained in culture medium, the parasites were kept in Tyrode's solution con- taining the drugs. After 1 and 4 hours of incubation, the worms were removed from the medium and homogenized for the determination of its GPT and GOT. When the final concentration of tartar emetic in the medium reached 10-3M, the activity of GPT in Schistosoma japonicum was also decreased to about 50%.When schistosomes were placed in Tyrode's solution containing 2×10-4 M of F30066 for 4 hours, the activity of GPT was decreased to 25%, while no effect on GOT of the worms was observed. In order to investigate the in vivo effect of the drugs, infected mice were treated with the schistosomacides at the dosage of 1/2 LD50 for 5 days. The worms were re- moved each day from 3-5 mice and homogenized as quickly as possible for determining its activity of GPT and GOT. During the treatment, it was apparent that the worms decreased in size and their reproductive organs were degenerated, but no appreciable change in the activity of GPT or GOT was observed. It was concluded that the anti- schistosomal activity of the drugs tested had no effect on the metabolic sequences which were catalysed by GPT or GOT.

     

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