【作者】 刘丹华；

【导师】 李继平；

【作者基本信息】 辽宁师范大学 ， 物理化学， 2007， 硕士

【摘要】 本文首先以水飞蓟素为原料,对水飞蓟宾的精制与纯化方法进行研究。应用超声波辅助手段对传统的重结晶方法进行了改进,并与柱层析精制水飞蓟宾的方法进行比较,考虑到产率、毒性、价格和实验条件等因素,最终确定精制水飞蓟宾的最佳方法为超声波辅助重结晶法。改进后精制水飞蓟宾的方法为:先用乙醇作溶剂,使用超声波超声,超声条件为时间45min,温度60℃,功率100%,再放置两天,然后乙醇重结晶,产率由原工艺的18.0%提高到为21.8%。其次,为了探讨水飞蓟宾(L-1)及其衍生物的防醉酒作用,以水飞蓟宾为先导化合物,采用在弱碱性条件下,用缩合的方法合成了2种7位水飞蓟宾衍生物。分别为N-苯基乙酰胺水飞蓟宾(L-2)、N、N-二甲基乙酰胺水飞蓟宾(L-3),并通过熔点测定、红外光谱、核磁共振波谱对其结构进行了表征。对N-苯基乙酰胺水飞蓟宾的合成进行了改进,产率由原工艺的3.0%提高到13.8%,降低了分离的难度。最后,建立了急性酒精中毒动物模型,对小鼠进行醉酒的实验。结果表明,在给酒前先给予水飞蓟宾及其衍生物,可以降低醉酒小鼠的数目。给药组小鼠醒酒时间比对照组要短,其中高剂量组对小鼠醒酒时间影响不大,低剂量组和中剂量组明显缩短小鼠的睡眠时间,中剂量组(8mg/20g)是解酒的最合适剂量。经过计算表明,该结果有统计学意义。通过小白鼠实验证明,水飞蓟宾及其衍生物具有解酒防醉的功效,为今后医疗事业提供了实验依据。更多还原

【Abstract】 At first, Silybum marianum(L.) were used as original material to research the method of refining and purifying silybin. Ultrasonic waves was used to improve the recrystallization experiment, compared it with column chromatography. In view of productivity, toxicity, cost, experiment conditions and so on, recrystallization along with ultrasonic waves was selected as the best method to refine silybin. The improved refining method conditions are as follows: ethanol was used as solvent firstly and ultrasonic wave was used to vibrate. Ultrasonic conditions are: time: 45min, temperature: 60℃, power: 100%. Laying up two days, the product was used to recrystallize with ethanol, The productivity was improved from 18.0 % to 21.8 %.Secondly, in order to probe the effect of silybin(L-1) and its derivatives on antitemulence, two kind of seven-location silybin derivatives were synthesized by means of condensation reaction at weak alkaline condition. They are N-phenylacetamide-silybin(L-2), 2-(dimethylamino)ethyl-silybin(L-3), and were characterized with measurements of their melting points、IR and NMR. The synthetic method of N- benzene-acetamide-silybin was improved, productivity is raised from 3.0 % to 13.8 %, and reducing the difficulty of separation.Finally, A model of animal acute alcoholism was established. Some drunk experiments to rats was accomplished. These experiment results indicate that giving silybin and its derivatives before giving alcohol to the rats, the amount of the drunk rats can reduced. The group of rats having been given the product had a less time to sober up than the comparison group. The high dosage has less effect to the time of sober up, the less and intermediate dosage can reduce the sleeping time obviously. Intermediate dosage(8mg/20g) is the most appropriate to sober up. Calculation indicate that it has statistic means. Rat experiments indicate that silybin and its derivatires have sobering up and alleviating effect, it provide experiment basis to medical treatment in the future .更多还原