苯硫脲嗪对棉鼠丝虫和马来丝虫感染的治疗

新化合物苯硫脲嗪(4-硝基-4’-(1-甲基哌嗪-4-硫代甲酰氨基)二苯胺)具有抗丝虫作用。感染棉鼠丝虫的棉鼠或长爪沙鼠和感染马来丝虫的长爪沙鼠用苯硫脲嗪ig 200mg/(kg·d)×3d皆获治愈。苯硫脲嗪对微丝蚴亦有作用,给药开始后3d,受治棉鼠周围血中的微丝蚴即消失,而受治长爪沙鼠腹腔内的马来丝虫微丝蚴活动减弱、僵直或自溶。两种丝虫经苯硫脲嗪作用后,虫体被破坏、崩解,特别是马来丝虫,出现大量死虫肉芽肿,虫周细胞反应强烈。

Therapy of phenthiourezine on infections of Litomosoides carinii and Brugia malayi

A new compound, phen-thiourezine [(4-nitro-4′- 1 -methyl-piperaziny 1 -4-thioformylamino) di-phenylamine; code number(S80016)]was synthesized by our institute in 1980 and found to be effective in screening test against Litomosoides carinii harboured in cotton rat.In this paper, the results of experimental therapy of phenthioure-zine on filariasis were described. The oral curative dose of phenthio- urezine in the treatment of cotton rats and Mongolian jirds infected with L.carinii or Mongolian jirds infected with Brugia malayi was 200 mg/kg daily for 3 days. The LD50 in mice given orally with a single dose of phenthiourezine was 2.2 g/kg. The drug also exhibited a strong action on microfilariae. 3 days after the start of treatment, the microfilariae of L.carinii in peripheral blood disappeared, while those of B. malayi in peritoneal cavity of Mongolian jirds decreased in their motoractivity,immobilized and even lysed. Histopathological observations showed that after treatment with phenthiourezine, the tissues of both species of adult worms were damaged and collapsed, especially in the case of B.malayi, numerous dead worm granulomas were formed and a strong cellular reaction around the worm could be seen.