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青蒿素衍生物8—2A为对乙酰氨基苯磺酸酯,系我所研制的有效抗疟青蒿素衍生物。对PlasmodiumbergheiNstrain的ED_(50),PO:64.27,ip:38.11,im:26.36(mg/kg),急性毒性试验,LD_(50),po:3143.90,ip:1507.05,im:2280.37(mg/kg)。与A—A比较,对鼠疟有更好的疗效及较高的治疗指数和安全系数。长期毒性试验,分别以54,108,216(mg/kg/d×14d,im),大白鼠的体重较对照组为低,外周血内出现有核红细胞0~1/1视野及心肌损伤或供血不足。病理形态学检查:中剂量组出现肝、肾轻微炎症反应,大剂量组出现肝、肾可逆性变性。豚鼠过敏反应阴性。小鼠致畸试验:每840mg/kg共10日,出现死胎1只。
Artemisinin derivative 8-2A is acetaminosulphonate, which is an effective anti-malaria artemisinin derivative that I developed. ED_(50) for Plasmodiumberghei Nstrain, PO: 64.27, ip: 38.11, im: 26.36 (mg/kg), acute toxicity test, LD_(50), po: 3143.90, ip: 1507. 05, im: 2280.37 (mg/kg). Compared with A-A, there is a better efficacy and a higher therapeutic index and safety factor for mouse malaria. The long-term toxicity test was 54.108.216 (mg/kg/d.times.14d, im). The weight of the rats was lower than that of the control group. There were nucleated red blood cells in the peripheral blood and 0 to 1/1 visual field and myocardial injury. Insufficient blood supply. Histopathological examination showed mild liver and kidney inflammatory reactions in the middle-dose group and reversible degeneration of the liver and kidney in the high-dose group. Allergic reactions in guinea pigs were negative. Teratogenicity test in mice: A total of 1 dead fetus appeared every 10 days for 840 mg/kg.