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紫锥菊中菊苣酸和单咖啡酰酒石酸纯化工艺及菊苣酸性质研究

Study on Purification Process of Cichoric Acid and Caftaric Acid in Echinacea Purpurea and Property of Cichoric Acid

【作者】 郭建伟

【导师】 陈波;

【作者基本信息】 湖南师范大学 , 药物分析, 2009, 硕士

【摘要】 紫锥菊(Echinacea purpurea)是原产美洲的一类菊科植物,因其具有显著的免疫调节功效,是目前国际上普遍关注的一种免疫促进剂和免疫调节剂。目前药理研究表明,其中有免疫活性的物质是:咖啡酸衍生物、多糖、烷基酰胺类物质。菊苣酸为咖啡酸衍生物,是紫锥菊中最重要的免疫活性成分之一。目前研究制备的菊苣酸含量还只能用来制作标准品,这严重限制了菊苣酸在药理药效等方面的研究。为此,本论文研究了较大规模纯化菊苣酸的方法,并在此基础上初步对菊苣酸在模拟胃肠道环境中的稳定性进行了研究,同时建立了一种在线抗氧化活性筛选的方法,本文做了如下工作:1.建立了大孔吸附树脂pH梯度洗脱同时分离纯化单咖啡酰酒石酸和菊苣酸的方法。该方法有如下优点:1)样品前处理简单;2)洗脱剂为含少量酸的水溶液,绿色环保;3)所用试剂能够回收利用,有效的节约生产成本。2.研究了紫锥菊提取物中菊苣酸及菊苣酸单体在模拟胃肠道环境下的稳定性。本实验利用高效液相色谱研究菊苣酸在人工胃液、人工肠液环境中的稳定性,为菊苣酸的体内代谢过程提供基础性研究。结果表明,菊苣酸在模拟胃肠道环境下性质稳定,从稳定性角度考虑,菊苣酸适合开发为口服制剂。3.建立了HPLC-DPPH在线研究紫锥菊提取物抗氧化活性筛选的方法。本方法具体过程如下:用高效液相色谱将紫锥菊提取物的组分进行分离,然后通过柱后衍生的方法,泵入DPPH溶液,在517 nm处检测,如分离出来的成分有DPPH自由基清除作用,就会产生负峰,从而可以说明该成分具有抗氧化活性。该方法能够快速筛选天然产物中具有活性的成分。

【Abstract】 Echinace purpurea is a native north American perennial medicinal herb that has been used for many years as an agent to enhance immune system function.It is composed of four major groups of compounds:the caffeic acid derivatives(caftaric acid,cichoric acid and echinacoside), alkamides,glycoproteins,and polysaccharides.Cichoric acid is one of the most important immune active component.So far,the cichoric aicd of high purity is difficult to prepared in large quantity,so that is restricted in Pharmacology research.In the thesis,a large scale preparation of cichoric acid was studied.Meanwhile,we have studied the stability of cichoric acid in the artificial gastric juices and artificial intestinal juice by high performance liquid chromatography to examine the stability in the environment of simulation stomach and intestines way.A rapid on-line method for screening of Echinace purpurea extract for radical scavenging components was developed.We has mainly finished the following work:1.A purified process was developed for the simultaneous purification of cichoric acid and caftaric acid in Echinacea Purpurea by pH gradient Elution.This method has the following advantages: 1)Sample Pretreatment is simple;2)It is green environmental protection due to the products were purified by macroporous resin column Chromatography with water containing acid as eluent;3)it can save production cost because Recycling Utilization of reagent is achieved.2.The stability of Echinecea purpurea preparation and cichoric acid in simulated gastrointestinal tract was studied.A HPLC method was developed to determine the stability of cichoric acid in the Artificial Gastric Juices and Artificial Intestinal Juice.The research can provide the basic support for the metabolite in body for cichoric acid.The result demonstrated that cichoric acid is stable in the Artificial Gastric Juices and Artificial Intestinal Juice.And can be made into oral preparation.3.A rapid on-line screening for antioxidant activity in extract of echinecea purpurea was developed.The extract of Echinecea purpurea was separated by HPLC,and HPLC-separated analytes react postcolumn with the DPPH solution,and the induced bleaching is detected as a negative peak by an absorbance detector at 517 nm.There was the negative peak if the compound in Echinecea purpurea showing the antioxidant activity.The method can be applied to screen the active component from natural product quickly.

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