【作者】 程明；

【导师】 韩崇选； 张宏利；

【作者基本信息】 西北农林科技大学 ， 森林保护， 2007， 硕士

【摘要】 本论文对曼陀罗中的杀鼠活性成分进行系统的研究,主要得出以下结果:1.化学成分系统预试结果表明,曼陀罗中含有生物碱、鞣质类、甾体、萜类、黄酮、蒽醌及其甙类、香豆素及其甙类、皂甙类、挥发油、油脂类、氨基酸、多糖等化学成分。2.杀鼠活性测定结果表明,曼陀罗不同生育期的杀鼠活性明显不同,样品含量为15%时,8、9、10月份样品的毒杀率分别为20%、60%、30%;样品含量为20%时,毒杀率分别为50%、90%、70%,即曼陀罗9月份的样品杀鼠活性最强。同时还可以看出,曼陀罗对毒杀试鼠的性别具有一定的选择性。毒性测定结果表明,试鼠对曼陀罗的耐受量范围为4～16 g·kg-1,致死中量LD50=7.04 g·kg-1。3.滴定法以甲基红—溴甲酚绿为指示剂测得曼陀罗8、9、10月份样品的总碱含量分别为0.60 mg·g-1、3.26 mg·g-1、1.22 mg·g-1,比中国药典(2005)中采用甲基红为指示剂所测得的总碱含量高(分别为0.35 mg·g-1、3.01 mg·g-1和1.02 mg·g-1);紫外分光光度法测得曼陀罗8、9、10月份样品的总碱含量分别为0.78 mg·g-1、3.44 mg·g-1、1.50 mg·g-1。结果表明,两种不同的测定方法对曼陀罗总碱含量的测定结果无显著影响(P>0.05),但不同采样时期的样品中总碱含量差异极显著(P<0.01),即曼陀罗不同生育期的总碱含量:9月>10月>8月。4.采用酸性乙醇渗漉提取曼陀罗中的生物碱,优选的最佳提取工艺为:采用pH=3的80%酸性乙醇溶液提取3次(料液比为15∶1),可以较大限度的提取出曼陀罗中的总生物碱。5.采用活性跟踪和柱层析分离相结合的方法从曼陀罗氯仿萃取物中分离得到3个单体化合物,经鉴定,为东莨菪碱、R2和R3。6.东莨菪碱、R2和R3对小鼠的毒性测定结果表明,试鼠对东莨菪碱的耐受量范围为25～200 mg·kg-1,致死中量LD50=60.89 g·kg-1;试鼠对R2的耐受量范围为50～200 mg·kg-1,致死中量LD50=113.47 g·kg-1;R3对试鼠不具有明显的急性毒性,未能测出LD50数值。通过毒性反应症状,判断东莨菪碱和R2属于神经毒剂。7.通过亚急性毒性试验过程中多个指标的观察与测定,确定了东莨菪碱活性作用的靶器官是肝脏和肾脏,同时对脾脏和肠道也产生了一定程度的影响。更多还原

【Abstract】 The killing active ingredients of Datura stramonium for rat were systemic researched in this paper. Results are as below:1. The chemical ingredients of Datura stramonium were pretested. The results showed that there were many chemical ingredients in Datura stramonium,including alkaloid,tannin,steroid,terpene,flavone,anthraquinone and glycosides,coumarins and glycosides,saponins,essential oil,fat,amino acid and polysaccharide and others.2. The rat killing activity was determined. The results indicated that Datura stramonium in different phage had different rat killing activity. When sample content was 15%,the rat killing from August,September and October were seperately 20%,60% and 30%.,while the sample content was 20%,the rat killing from August,September and October were seperately 50%,90% and 70%. So the rat killing of Datura stramonium from September is the strongest. At the same time,The sex effected the rat killing poison of Datura stramonium. The rat killing toxicity was determinated by infusion. The tolerated dose of rat to Datura stramonium was 4～16 g·kg-1,LD50=7.04 g·kg-1.3. In titrimetric method,methyl red-bromocresol green was elected as indicator which help to get high content of total alkaloids in Datura stramonium comparing to the methyl red indicator in Chinese Pharmacopoeia(2005); In Ultraviolet spectrophtonetric method,obtain the content of total alkaloids of the sample from August,September and October were seperately 0.78 mg·g-1、3.44 mg·g-1、1.50 mg·g-1. The results showed that there was no significant difference(P>0.05)between two methods to determine the content of total alkaloids in Datura stramonium,while there was significant difference(P<0.01)in content of total alkaloids in Datura stramonium sample from different phage,that is,the sample content from September > the one from October > the one from August.4. Alkaloids in Datura stramonium were extracted by infiltration with acid ethanol. The optimized extract craft was:the total alkaloids in Datura stramonium was extracted mostly by extracting three times with 80% acid ethanol,pH=3(the rate of material to liquid 15∶1).5. The rat killing active ingredients of Datura stramonium were identified by activity track and column Chromatography. After identifying,they were scopolamine,R2 and R3. 6. The toxicity of scopolamine,R2 and R3 to rat were determined. The results showed that the tolerated dose range of rat to scopolamine was 25～200 mg·kg-1,LD50=60.89 g·kg-1; the tolerated dose range of rat to R2 was 50～200 mg·kg-1,LD50=113.47 g·kg-1; There was no significant acute toxicity of R3 to rat,which LD50 was not identified. Scopolamine and R2 belongs to nerve agents.7. After observation and determination indicators in subacute toxicity test,the target organ on which scopolamine acted was liver and kidney,and scopolamine affected the spleen and intestinal tract in some degree.更多还原