【作者】 雷萌；

【导师】 刘宏民；

【作者基本信息】 郑州大学 ， 有机化学， 2004， 硕士

【摘要】 本论文进一步研究了唇形科香茶属植物冬凌草的活性成分，并以其具有抗癌活性的贝壳杉烯型二萜为先导化合物进行了衍生物的研究。另外，为了进一步开发应用Acetvlkamebakaurinin，我们探讨了将其制成β-环糊精包合物的方法。具体工作如下： 一、对冬凌草的提取工艺进行了更进一步的研究，发现了不同产地或是相同产地、不同采摘时期的冬凌草的主要成分差别很大；确定了冬凌草浸泡的最佳时间；研究了浸泡乙醇浓度对冬凌草提取效率的影响。这对今后的研究工作意义重大。 二、对冬凌草中的化学成分进行了研究，共从冬凌草干叶的乙醇提取物中分离出十一个化合物，其中四种为首次从冬凌草中分离，分别为Acetvlkamebakaurinin(1)、Kamebakaurinin(2)、豆甾醇(4)、3’，4’，5-trihydroxy-6，7-dimethoxyflavone(3)，对于化合物(1)，我们首次得到了它的单晶结构。另外七个为己知化合物，分别是β —谷甾醇(5)、冬凌草甲素(6)、冬凌草乙素(7)、pedalidin(9)、lasiodonin(8)、乌苏酸(10)和2α-羟基乌苏酸(11)。我们还对部分样品进行了活性测试。 三、以提取的具有抗癌活性的贝壳杉烯型二萜化合物为先导化合物设计合成了冬凌草甲素7，14-缩醛酮类衍生物、Acetylkamebakaurinin的丙叉基保护衍生物、冬凌草甲素葡萄糖苷衍生物，并对其中部分样品进行了活性测试。所有化合物均通过元素分析、红外和核磁谱进行了结构验证。 四、通过研磨的方法将Acetylkamebakaurinin制成了包合物，从而大大改善了其溶解 郑州大学2004届硕士学位论文度，这对进一步开发应用Acetylkamebakaurinin有重要意义。 /:l、为本课题新药研究项目的顺利进行，提取分离了充足的冬凌草甲素和冬凌草乙素。 本论文对冬凌草活性成分的提取工艺、分离、衍生物的合成和Acetylkamebakaurinin包合物的制备进行了一系列的研究，并对部分提取成分和衍生物进行了活性测试。更多还原

【Abstract】 In this thesis, the chemical constituents of Rubdosia rubescens (Ldbiatase) Hara have been investigated further and the derivatives of ent-kaurene diterpene, which have a-methylene cyclopentanone function group in their molecule and show the antitumor activity, have been designed and prepared. In addition, for the better application of Acetylkamebakaurinin, we studied the preparation method of the inclusion complex of Acetylkamebakaurinin- 3 -cyclodexitrin. The detailed contents are shown as followings:1 By investigating different processes for the extraction of Rabdosia rubescens Hemsl, we found that the main constituents of Rabdosia rubescens Hemsl harvested in different areas or in same area but differ period manifested great difference. What’s more, by doing that, we confirmed the best extraction time and we studied the affection of alcohol’s concentration on the extraction efficiency of Rabdosia rubescens Hemsl.2, We studied the chemical constituents of Rabdosia rubescens Hemsl and isolated eleven compounds from the alcohol extraction of the dry leaves of Rabdosia rubescens Hemsl. Of which there are four compounds Acetylkamebakaurinin , Kamebakaurinin. sigmasterol and 3’,4’,5-trihydroxy-6,7-dimemoxyflavone which have been isolated from this plant for the first time. For compound (1), we first get it’s crystal structure. The other seven compounds are known before. They are 3 -sitosterol, oridonin, ponicidin, pedalidin, lasiodonin, ursolic acid and 2 ,3 -dihydroxy-urs-12-ene-28-oic acid respectively.3m 7, 14-acetal derivatives of oridonin and Acetylkamebakaurinin were designed and synthesized and oridonin -6-O- -D-glucopyranoside were prepared via four steps. All the structures were characterized by elemental analysis, IR, and NMR spectra.4, We obtained the inclusion complex of Acetylkamebakaurinin- -cyclodexitrin via abrasive method, which improved the solubility in water.5, In order to make our project go well, we isolated and purified enough amounts of oridonin and ponicidin .In a word, in this thesis, the process for the extraction of Rabdosia rubescens Hemsl, the isolation , the synthesis of it’s derivatives and the preparation of the inclusion complex of Acetylkamebakaurinin- -cyclodexitrin were studied. And partial of the chemical constituents and derivatives were tested for antitumer activities.更多还原