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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 LD_(50)×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 LD_(50)×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.
In this paper, we investigated the effect of F-30066, an anti-schistosome, and β- (5-nitro-2-furanyl) isopropylamine in vitro.It has been shown by experiments that F-30066 has a direct killing effect on Schistosoma japonicum.In vitro, In 4-10 μg / ml Tyrode solution mixed with sheep serum (2: 1), the parasites showed decreased activity, atrophy, bowel distortion, reproductive organ degeneration and reduction of intrauterine egg number and eventually paralysis. F-30066 role 1-4 hours of the parasites in the drug-free culture medium, the vitality can be significantly restored by the drug 8-16 hours is poor, to the role of 24 hours after the parasites Vitality can not be restored in the observation of the influence of the drug on the viability of the parasites in the host body, it was found that after oral administration of F-300661/2 LD_ (50) for 4-5 days, the viability of the parasites in the body can not be Fully recovered, the living time of the parasites was only about half that of the control group.The animals treated with toad tartar survived in the culture medium rapidly after they administered 1/2 LD_ (50) x 5 days Recovery, worms life time and the control group similar to F-30066 in vitro insecticidal effect can be antagonized by cysteine and glutathione, and When acid, di Dimercaptosuccinic sodium, lipoic acid and vitamin C class does not have this effect. Rabbit oral F-30066 to half an hour in serum 8 hours after the culturing schistosome parasite life time is significantly shortened.