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本实验以不同方法从九里香Murraya paniculata(L.)Jacks皮分离9种抗生育有效物质,并比较其效价和毒性。其中以Sephadex G_(100)柱层析-CTAB络合物(V)和不络合物(Ⅶ)、磷酸氢钙吸附酸溶-CTAB络合物(Ⅶ)、Sephadex G_(100)柱层析-磷酸氢钙吸附酸溶-CTAB不络合物(Ⅷ)及Sephadex G_(100)柱层析-磷酸氢钙吸附酸溶-Sephadex G_(200)柱层析物(Ⅸ)等5种分离物的抗生育效果显著,小鼠腹腔注射有效剂量分别为1.0,1.0,0.5,0.2和0.06mg/30g;小鼠腹腔注射给药LD_(50)分别为21,56,31,24和9.3mg/20g。狗的亚急性毒性试验,尿常规、血象、肝功能和肾功能均正常,重要脏器的病理学检查,均未发现有与药物有关的病变。豚鼠抗原性试验也未见有过敏症状发生。但家兔热源试验阳性。化合物Ⅵ初步用于临床中期妊娠引产,8例中7例有效,但也有发热发冷副反应。
In this experiment, nine anti-fertility-effective substances were isolated from Murraya paniculata (L.) Jacks skin by different methods, and their potency and toxicity were compared. Sephadex G_ (100) column chromatography-CTAB complex (V) and non-complex (VII), calcium phosphate dibasic adsorbed acid-CTAB complex - Five kinds of isolates such as calcium phosphate dibasic adsorbed acid-soluble-CTAB non-complex (Ⅷ), Sephadex G-100 column adsorbed acid-Sephadex G 200 column Ⅸ The effective dose of intraperitoneal injection was 1.0,1.0,0.5,0.2 and 0.06mg / 30g, respectively. The LD 50 of mice injected intraperitoneally were 21, 56, 31, 24 and 9.3 mg / 20g. Subacute toxicity test dogs, urine, blood, liver function and renal function were normal, pathological examination of vital organs, and no drug-related lesions were found. Guinea pig antigenicity test also showed no allergic symptoms occurred. But the rabbit heat test was positive. Compound Ⅵ preliminary clinical midterm pregnancy induced abortion, 7 cases were effective in 8 cases, but there are also side effects of fever and chills.