蕭樹華, 商韻徵. F-30066体外抗血吸虫作用的研究J. 药学学报, 1963, 10(12): 701-707.
引用本文: 蕭樹華, 商韻徵. F-30066体外抗血吸虫作用的研究J. 药学学报, 1963, 10(12): 701-707.
XIAO SHU-HUA AND SHANG YUN-CHENG, . STUDIES ON THE EFFECT OF F-30066 ON SCHISTOSOMA JAPONICUM IN VITROJ. Acta Pharmaceutica Sinica, 1963, 10(12): 701-707.
Citation: XIAO SHU-HUA AND SHANG YUN-CHENG, . STUDIES ON THE EFFECT OF F-30066 ON SCHISTOSOMA JAPONICUM IN VITROJ. Acta Pharmaceutica Sinica, 1963, 10(12): 701-707.

F-30066体外抗血吸虫作用的研究

STUDIES ON THE EFFECT OF F-30066 ON SCHISTOSOMA JAPONICUM IN VITRO

  • 摘要: 本文研究了F-30066,即β-(5-硝基-2-呋喃)丙烯酰异丙胺,体外抗血吸虫的作用.实验证明F-30066对体外血吸虫具有直接杀灭作用.在含F-30066 4-10微克/毫升的Tyrode液与绵羊血清混合液(2∶1)内,虫体表现为活动减弱、萎缩、肠管扭曲、生殖器官退化和子宫内虫卵数减少,终至麻痹死亡.经F-30066作用1—4小时的虫体移置于不含药物的培基中时,其活力可明显恢复,经药物作用8—16小时的则较差,至作用24小时后,虫体的活力不能恢复.在药物对宿主体内虫体生活力影响的观察中,发现小白鼠口服F-300661/2 LD50×4—5天后.其体内受作用的虫体活力在培基内不能完全恢复,虫体的生活时间仅及对照组的一半左右.用吐酒石治疗的动物,于投服1/2 LD50×5天后,其体内存活的虫体活力在培基内迅速恢复,虫体的生活时间与对照组的相似.F-30066的体外杀虫作用能被半胱氨酸与谷胱甘肽所拮抗,而胱氨酸、二巰基丁二酸钠、硫辛酸及维生素丙等则无此作用.用口服F-30066半小时到8小时后的家兔血清培养血吸虫时,虫体的生活时间显著缩短.

     

    Abstract: It was found that F-30066, a new furacin derivative, possessed a direct effect on schistosomes in vitro. Trials were made with sheep serum-Tyrode solution (1:2) containing 0.5% glucose. When parasites were kept in the medium containing 4— 10 μg/ml of F-30066, the motility of the worms decreased gradually and the shrinkage of the worm body followed. After 24 hours, only slow body movement in the female and slow sucker movement in the male were observed. At the same time the reproductive organs of the worms degenerated and the number of ova in the uteri was markedly reduced. Within 48 hours, both male and female worms were killed after a long period of paralysis. In order to explore the effect of F-30066 on the survival of worms in vivo, mice infected with schistosomes were treated with F-30066 or tartar emetic in the dosage of 1/2 LD50 per os for 5 days. Each day worms were removed from 2—3 mice and maintained in the medium. In case of tartar emetic, the motility of the worms recovered gradually and the worms survived as long as those from the control group. In case of F-30066, the worms became sluggish and could not recover completely. After the 4th and the 5th dose, the worms survived in the medium for only 4.2—7.0 days, while the survival time of the worms from control group was 12.4 days. The difference is statistically significant. When worms were placed in serum taken from rabbits 1/2 to 8 hours after a single oral dosage of 1.3gm/kg of F-30066, the survival time of the parasites was reduced from 12.2—12.8 days to 3.2—9.1 days. It was found furthermore that the antischistosomal activity of F-30066 in vitro could be antagonized by cysteine, but not by cystine, lipoic acid, sodium dimercaptosuccinate, or vitamine C.

     

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