【作者】 张坤；

【导师】 周应军；

【作者基本信息】 中南大学 ， 药物化学， 2011， 硕士

【摘要】 目的：明确抱茎苦荬菜抗脑缺血有效部位的主要化学成分,建立合理的质量控制体系,优化制备工艺使有效部位达到中药注射剂的质量要求,研究有效部位及代表性成分透过SD大鼠血脑屏障的能力。方法：1.在指纹图谱的指导下分离得到其中的主要有效成分并进行结构鉴定；2.通过测定相对校正因子实现以一种对照品测定多指标成分的含量,并与外标法比较；3.从提取、醇沉和柱层析三个方面对制备工艺进行优化；4.SD大鼠腹腔注射给药有效部位及主要单体成分,采集脑脊液进行HPLC对比研究。结果：1.从抱茎苦荬菜的有效部位中分离得到五个主要化合物,分别为咖啡酸(Is-1)、菊苣酸(Is-2)、木犀草素-7-0-β-D-葡萄糖苷-(1→6)-β-D-葡萄糖苷(工s-3)、木犀草素-7-0-β-D-葡萄糖醛酸苷(Is-4)、芹菜素-7-0-β-D-葡萄糖醛酸苷(Is-5)；2.咖啡酸、菊苣酸、木犀草素-7-0-β-D-葡萄糖苷-(1→6)-β-D-葡萄糖苷、芹菜素-7-0-β-D-葡萄糖醛酸苷和木犀草素-7-0-β-D-葡萄糖醛酸苷的校正因子分别是1.129、0.8733、1.320、1.129,与外标法测定含量无明显差异；3,工艺经过优化最终得到了含上述五种成分65%,大类成分含量84%的有效部位；4.五种成分的原型不能透过透过血脑屏障,Is-2组的脑脊液中有代谢产物检测出。结论：明确了抗脑缺血部位的物质基础,建立了合理的质量控制体系,优化了制备工艺得到了符合中药注射剂要求的有效部位,透过血脑屏障的研究为后期的抗脑缺血作用机制奠定了基础。更多还原

【Abstract】 Objective to confirm the chemical constituents in anti-cerebral ischemia fraction from Ixeris sonchifolia(Bge.) Hance,establish a reasonable quality control system,optimize the preparation process of the effective fraction and study their capacity of passing the blood brain barrier of SD rats.Methods 1.With the fingerprints of effective fraction,we isolated the major chemical constituents and identified their chemical structures.2.By measuring RCF,we established a method,which the content of all five compounds could be determined with one reference substance3.From extraction, alcohol precipitation and column chromatography, three aspects of preparation process was optimized.4.SD rats received intraperitoneal injection of the effective fraction and the major constituents.The different HPLC of cerebrospinal fluid was compared.Results l.Got five major constituents from the effective fraction:caffeic acid(Is-1),cichoric acid(Is-2),luteolin-7-0-β-D-glucopyranoside(1→6)-β-D-glucopyranoside(Is-3), luteolin-7-O-β-D-glucuronopyranoside(Is-4),apigenin-7-O-β-D-glucuronopyranoside (Is-5).the content of five components was around 96% in fingerprints.2.The relative correction factors of caffeic acid, cichoric acid,luteolin-7-O-β-D-glucopyranoside(1→6)-β-D-glucopyranoside, apigenin-7-O-β-D-glucuronopyranoside were identified as 1.129、0.8733、1.320、1.1293.This method was almost no different with external standard method.4.The total content of all the five major constituents in the effective fraction was around 65% and the content of major categories was around 84%.4.No parent drug was found in the cerebrospinal fluid, but some metabolin were found in CSF in Is-2 group.Conclusions Confirmed the chemical constituents in effective fraction,established a reasonable quality control system,got effective fraction which met the requirement of TCMI,study on passing BBB laid a foundation for further study on mechanism of anti-cerebral ischemia.更多还原