抗癌散抗肿瘤活性物质的基础研究

【作者】 楼一层；

【导师】 刘焱文；

【作者基本信息】 湖北中医学院 ， 中医基础理论， 2006， 博士

【摘要】 抗癌散是中药传统的经验方，通过临床应用具有很好的抗肿瘤作用，临床常用于治疗肺癌、肝癌、脑癌，疗效确切。该方所用药材均为常用无毒的天然植物，其中水红花子为抗癌散的君药，是蓼科植物红蓼Polygonum orientale L．的成熟果实，具有散血消瘀、消积止痛、健脾利湿之功效，临床上多用于治疗癌症。本论文对抗癌散的物质基础进行了相关研究。 本论文采用现代药理学方法，结合多年临床疗效观察，对抗癌散复方中药味配伍进行了筛选研究，确定处方为：水红花子、白花蛇舌草、七叶一支花(蚤休)、三七、西洋参、柴胡等六种中药组成。从而为提高该中药方剂临床疗效和降低服用剂量提供了依据，也为深入研究该复方奠定了良好的基础。 本论文在中医药理论指导下，通过中药化学、药理学、分子生物学等多学科交叉的研究方法，将复方抗癌散视为整体，用溶剂法将其分成不同的极性部位。药理研究表明，抗肿瘤作用的主要有效部位为乙酸乙酯提取物和正丁醇提取物。采用色谱法，从正丁醇提取物中分离和鉴定出了4个单体化合物。其中正丁基-β-D-吡喃果糖苷具有较好的抗肿瘤活性，该化合物为首次在该方剂各单味药中发现，这对探讨抗癌散的物质基础具有重要意义。 对水红花子的化学成分进行了研究，采用硅胶、Sephadex LH-20等柱色谱法分离和鉴定出了7个化合物，分别为二氢槲皮素(dihydroquercetin)，3，5，7-三羟基色原酮(3，5，7-trihydroxylchromone)，山萘酚(kaempferol)，3，5，7-三羟基二氢黄酮醇(3，5，7-trihydroxy flavonol)，槲皮素(dihydroflavonol)，阿魏酸-对羟基苯乙醇酯(P-hydroxyphenylethanol ferulate)和对香豆酸-对羟基苯乙醇酯(P-hydroxyphenylethanol P-coumarate)。这对于进一步阐述抗癌散的中医方剂的物质基础具有一定的意义。 为了探讨中药复方各单味药化学成分在提取过程中的互相影响，本研究采用HPLC法和紫外分光光度法，对本方及配方中的多味药的提取物中薯蓣更多还原

【Abstract】 Kangaisan, which is mixed by Oldenlandia diffusa Roxh, fruit of Polygonum orientate L. and so on, is the compound of traditional Chinese medicine (TCM). Clinical research results indicated that Kangaisan had obvious anti-tumor effects to a series of cancers. The fruit of Polygonum orientale L. is the basis of kangaisan. In the traditional Chinese medical experience, it is widely used for its excellent curative effects. Recently, some research had showed that the fruit of Polygonum orientate L. had notable anti-tumor effect.On the base of decades of curative effect observation in clinical, we had screened out the effective prescription under the condition of modern pharmacological techniques. It provided guidance for curative effect improvement and dosage decrease; on the other hand, it established upstanding basis for the deeply research.For the sake of complexity, it is singularly of the research on phytochemistry of compounds. In this paper, the effective chemical compound group of kangaisan had been systematically researched with the guidance of Chinese medical theory. The research method of subject-across such as plant chemistry, pharmacology and molecular biology, was utilized to expose the anti-tumor mechanism and substantial basis of kangaisan. Pharmacological research indicated that the extraction parts of n-Butanol and ethyl acetate. We had separated 4 chemical compounds; and the chemical compound Ⅱ(n-butyl-β-D-fructopyranoside) was the firstly found in the prescription. At the same time, it has effective anti-tumor effect. In proceed, the substantial base research is legible for the sake of tracing inspection of MTT colorimetry.On the other hand, The compounds were separated by repeated silica gel and Sephadex LH-20 chromatographies.The structures of compounds isolated were identified by analysis of their spectral data and chemical reactions.Results Seven compounds were isolated and their structures were identified , such as更多还原