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用于杀丝虫剂筛选的胸腔内注射方法的评估

Evaluation of the intrathoracic injection method for screening of filaricides.

作者信息

Shibuya T, Tanaka H, Nogami S, Oikawa Y, Saito M

出版信息

Jpn J Exp Med. 1978 Oct;48(5):411-8.

PMID:748620
Abstract

Intrathoracic injection technique was utilized to examine its value in screening of antifilaria drugs in Litomosoides carinii in the cotton rat, Sigmodon hispidus, using existing filaricides such as diethylcarbamazine, Mel W. metrifonate, suramin, arsenics and antimonials. Diethylcarbamazine at a dose of 100 mg/kg for 5 days given intrathoracically caused marked decrease of more than 95% of the microfilaria count in the blood 1 week after the initial injection which is the same effect as was observed by intraperitoneal injection. Whereas adult worms in the pleural cavity were not affected. Mel W at a dose of 10 mg/kg for 5 days killed all adults but had no effect on microfilaria density in the blood. When it was given intraperitoneally, even a larger dose of 50 mg/kg did not affect adults in the pleural cavity. In cotton rats tolerating suramin at 80 and 40 mg/kg for 5 days, adult worms were intact. However, a reduced dose of 20 mg/kg and 10 mg/kg given weekly for 6 weeks showed remarkable macrofilaricidal activity. Thus the slow action of suramin was reproduced by this method. There was no significant change in the microfilaria density in the blood. Aresenics such as Mapharsemin and Neo Neo Arsemin, and antimonials such as stibophen and tartar emetic were shown to have macrofilaricidal activity by intrathoracic injection with no effect on microfilaria density in the blood within a week. Effect of existing filaricides by this method showed remarkable coincidence with their action Wuchereria bancrofti.

摘要

采用胸腔注射技术,利用现有杀丝虫剂如乙胺嗪、美拉胂醇、苏拉明、砷剂和锑剂,检测其在棉鼠体内对卡氏罗阿丝虫抗丝虫药物筛选中的价值。胸腔内注射剂量为100mg/kg的乙胺嗪,连续5天,首次注射1周后,血液中微丝蚴计数显著下降超过95%,这与腹腔注射观察到的效果相同。而胸腔内的成虫未受影响。剂量为10mg/kg的美拉胂醇连续5天可杀死所有成虫,但对血液中微丝蚴密度无影响。腹腔注射时,即使剂量高达50mg/kg也不影响胸腔内的成虫。在耐受剂量为80mg/kg和40mg/kg的苏拉明连续5天的棉鼠中,成虫完好无损。然而,每周给予20mg/kg和10mg/kg的降低剂量,连续6周,显示出显著的杀大丝虫活性。因此,通过这种方法再现了苏拉明的缓慢作用。血液中微丝蚴密度无显著变化。胸腔注射砷剂如马法胂明和新胂凡纳明,以及锑剂如梯波芬和吐酒石,显示具有杀大丝虫活性,且在1周内对血液中微丝蚴密度无影响。通过这种方法检测现有杀丝虫剂的效果与它们对班氏吴策线虫的作用显示出显著的一致性。

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