还原青蒿素合并呋喃双胺的遗传毒性研究

STUDIES ON THE HEREDOTOXICITY OF DIHYDROARTEMISININE-FURADI-AMINE

口服预防血吸虫病药物青蒿-双胺的遗传毒理研究证明,小鼠分别口服青蒿-双胺、还原青蒿素和呋喃双胺,剂量为各自的1/50～1/5LD_(50),其微核出现率均<3‰,与阴性对照组无差异(P>0.05)。Ames试验表明,青蒿-双胺和呋喃双胺测试浓度为0.1μg/皿以上时,对TA_(100)菌株出现阳性诱变性;而还原青蒿素没有发现阳性。致畸胎试验提示,药物有明显胚胎毒性。青蒿-双胺剂量为26.25～210mg/kg时,其死亡胚胎率为47.2—100％,但对存活胎鼠无致畸胎作用。

The heredotoxicity study of dihydroartemisinine-furadiamine showed that when 1/50-1/ 5 LD50 doses were administered to mice, the positive micronucleus test of dihy-droartemisinine-furadiamine, dihydroarternisinine and furadiamine was <3% for all, there was no statistical difference between these groups and the control group. The Ames test showed that the mutation of dihydroartemisine-furadiamine and furadiamine with TA100 were positive when the drug was 0. 5μg/dish and 0. I/dish respectively, but negative with dihy-droartemisinine. These results suggested that the mutation was due to furadiamine. The em-bryotoxicity of dihydroartemisinie-furadiamine was definite, when doses of 26. 25, 52. 5 and 210mg/kg were given to the pregnant wistar rats, the rate of embryo death was 47. 2, 82. 7 and 100% respectively, but there was no teratogenic change with survived rats embryo.