【作者】 宁哲；

【导师】 韩梅；

【作者基本信息】 吉林农业大学 ， 野生动植物保护与利用， 2008， 硕士

【摘要】 蒺藜（Tribulus terrestris L.）,为蒺藜科（Zygophylaceae）蒺藜属（Trihulus）植物,始载于《神农本草经》,为历版药典所收载。味辛、苦,性微温,有小毒,具有平肝解郁、活血祛风、明目、止痒的功效,用于头痛眩晕,胸胁胀痛,乳闭乳痈,风疹瘙痒,其中皂苷类成分是蒺藜的有效部位之一。现代药理研究证明,蒺藜的皂苷类成分在治疗与预防心脑血管疾病及抗衰老、增强性功能、抑制迟发性变态反应等方面具有良好的效果。国外已开发出增强性功能以及软化血管的药物,我国市场上也已经出现以茎叶中蒺藜总皂为主要药效成分的中药“心脑舒通胶囊”、“心脑舒通片”。但有关蒺藜在抗肿瘤方面的单体活性成分研究报道较少。本研究在综述国内外对蒺藜的化学成分和药理研究进展的基础上,利用各种色谱手段,包括硅胶,凝胶等常压柱色谱和高速逆流色谱等从中药蒺藜全草中分离得到了化合物Ⅰ,Ⅱ,Ⅲ,其中化合物Ⅲ为消旋体化合物。进一步使用HSCCC色谱技术从消旋体化合物中拆分出化合物Ⅳ。并且通过波谱分析(IR,¹HNMR,¹³CNMR,ESI/MS,¹H-¹HCOSY,HMBC,NOESY HSQC等)和化学方法鉴定了以上化合物的结构分别是:（Ⅰ）β-谷甾醇,（Ⅱ）β-谷甾醇-β-D-葡萄吡喃糖苷,（Ⅲ）（R,S）海柯皂苷元-3-O-β-D-吡喃葡萄糖基（1-2）-[β-D-吡喃木糖（1-3）]-β-D-吡喃葡萄糖基(1-4-β-D-吡喃半乳糖苷,（Ⅳ）海柯皂苷元-3-O-β-D-吡喃葡萄糖基（1-2）-[β-D-吡喃木糖（1-3）]-β-D-吡喃葡萄糖基（1-4）-β-D-吡喃半乳糖苷。本研究对化合物Ⅰ、Ⅱ、Ⅲ、Ⅳ进行了药理实验,结果表明:只有化合物Ⅳ对Wish细胞的生长具有选择性抑制。并且对几种癌细胞显示出相当大的细胞毒性（MCF7（乳腺癌）、Bel7402（肝癌）、BGC823（胃癌）、Caco-2（结肠癌））。化合物Ⅳ与其对应异构体组成的混合物以及其它二个化合物没有明显的活性。本论文分析了该现象产生的原因,若要揭示其化学结构与药理活性之间的深层次关系,还有待于更深一步的科学研究。本课题为蒺藜皂苷类化合物抗癌活性作用机理的研究及蒺藜药物开发提供了科学的理论支撑。更多还原

【Abstract】 The plant Tribulus terrestris L.（Zygophyliaceae） is used in folk medicine.The steroidal saponins is active part of T.terrestris Lin..The application of reactive component like saponin in T.terrestris included the pharmacdogical action on cardiac and cerebral vessels,inhibition senility and sexual behavior increasing.The preparation for increasing sexual behavior and softening blood vessel had been researched in the Overseas.In our country market had already appeared the preparation of Xinnaoshutong which active part was steroidal saponins extracted form total grass of T.terrestris.It is necessary to research the chemical compounds to form the active compound.To established the method of content determination of crude drugs of T. terrestris.Report related to monomer active component of Tribulus terrestris L.utilized in anti-oncoma was extremely little.Based on chemical composition of the entire plants of T.terrestris L.and advancement of pharmacological research,CompoundⅠ,Ⅱ,Ⅲ,Ⅳwere isolated from it by using open column （SiO_z,Sephadex LH-20）,preparative HSCCC methods et al..And compoundⅢwas racemic compound.Furthermore,CompoundⅣwas isolated from racemic compound with the technology of chromatographic technique HSCCC.And according to spectroscopic analysis, including IR,¹H-NMR,¹³C-NMR,ESI/MS,H-¹H COSY,HMBC,NOESY,HSQC and chemical methods,the structure of Compounds were identified as:（Ⅰ）β-sitosterol,（Ⅱ）13-sito sterol-β-D-glucopyranosyl,（Ⅲ）（R,S）Hecogen in-3-O-β-D-glucopyranosyl（1-2）-[β-D-xylopy ranosyl（1-3）]-β-D-glucopyranosyl（1-4）-β-D-galactopyranoside,（Ⅳ） Hecogen in-3-O-β-D-gluco pyranosyl（1-2）-[β-D-xylopyranosyl（1-3）]-β-D-glucopyranosyl（1-4）-β-D-galactopyranosideAccording to pharmaco-experiment of CompoundⅠ,Ⅱ,ⅢandⅣ,the result showed: only CompoundⅣrestrained selectively the growth of Wish cell.Furthermore,it poisoned dramatically to MCF7,Be17402,BGC823 and Caco-2.There was not evident activity for CompoundⅣand its compound constructed with itself’ isomeride.The reasons of phenomenon was analyzed,however,if its relationship between chemical constitution and pharmacological activity was revealed,the further research would be engaged.The science theory was provided for the puncturevine pharmacodynamics function and the action mechanism research of T.terrestris and the puncturevine innovation medicine development.更多还原