一种抗肿瘤验方化学成分及抗肿瘤活性的研究（Ⅰ）

【作者】 蒋永福；

【导师】 张焜；

【作者基本信息】 广东工业大学 ， 应用化学， 2003， 硕士

【摘要】 中药复方作为中华民族的智慧结晶，对治疗疾病有着极大的优势。中药复方的抗肿瘤活性已得到国际公认。发挥我国药用植物资源丰富的优势，从中药复方中寻找抗肿瘤新药是一条重要途径。 肿瘤的形成和生长依靠人体中的新生微血管提供营养。只要控制了肿瘤周围的新生微血管的形成和生长，就可以控制肿瘤的生长，直至其消失。而新生微血管的形成依赖于称之为甲硫氨酸氨肽酶Ⅱ(Methionine aminopeptidaseⅡ，简称MetAP2)的物质，因此如果能够有效地控制MetAP2，就可以有效控制肿瘤的生长，能控制MetAP2的物质就可能成为新型抗肿瘤药物。 本论文主要以MetAP2为标靶研究一种抗肿瘤复方中的黄药子的新型抗肿瘤活性组分。黄药子是常用的抗肿瘤中药，己在长期使用过程中被证明是有显著疗效的。 本论文采取先对黄药子的乙醇浸提物进行柱层析粗分，然后分别对个粗分组分再进一步在离心薄层层析仪上细分，以MetAP2为标靶对各分离组分进行了活性测试。通过对组分Ⅱ的研究，在黄药子中首次找到了对MetAP2具有强活性的成分，对其进行了GC-MS分析后，证实它们分别是一些脂肪酸。阐明了其抗肿瘤作用机理，并指出三种酸的抗肿瘤作用是协同的，在组分Ⅲ中发现了四种甾醇，它们分别为胆甾醇、豆甾醇、γ-麦角甾烯醇和β-谷甾醇，其中胆甾醇和γ-麦角甾烯醇是第一次从黄药子中发现。 这些研究成果为新型抗肿瘤药物的开发和黄药子的进一步推广应用提供了强有力的理论依据。更多还原

【Abstract】 As a crystallization of wisdom of the Chinese Nation, Chinese Traditional Medicine Compound have an advantage in treatment of disease. Their anti-tumor activity is recognized by many people in the world. Finding new type anti-tumor drug from compound is an important way to exploit dominance of rich drug plant resource of china..Formation and growth of tumor depend on nourishment which supplied by angiogenesis. If the formation and growth of angiogenesis around tumor is controlled, the tumor growth can be controlled until its disappear. It was proved that the growth of angiogenesis is dependent on Methionine aminopetidase n, one kind of enzyme, which is shorted by MetAP2.If MetAP2 is controlled effectively, the growth of tumor then can be controlled. The Matter that can control MetAP2 will probably be a new type drug of anti-tumor.In this essay, a new type anti-tumor activity component of Dioscorea bulbifura L was studied and MetAP2 was made as a target to determinate anti-tumor activity. Dioscorea bulbifera L is one kind of anti-tumor Chinese Traditional Medicine in common use and it was proved to be of high curative effect during the long run.The ethanol extraction of Dioscorea bulbifera L is crudely separated by column chromatography and then the crude separation component was subdivided by centrifugal thin layer chromatography. All components are carried through activity assay according to MetAP2.Some components with high anti-tumor activity are found out from Dioscorea bulbifera L. Their structure are analyzed by GC-MS. They are Hexadecanoic acid, Octadecanoic acid and 9,12-Octadecadienoic acid. This fraction’s activity is dependent on cooperation of components. On the other way, two kind of cholesterol are found out in the first time. They are Cholest-5-en-3-ol and Gama-ergostenol.These achievements offer strong theoretical foundation for development of new type anti-tumor drugs and popularization application of Dioscorea bulbifera L.更多还原