【作者】 黄赵刚；

【导师】 李俊； 李绍平；

【作者基本信息】 安徽医科大学 ， 药理学， 2005， 硕士

【摘要】 三七为五加科(Araliaceae)植物三七Panax notoginseng (Burk.) F.H. Chen.的干燥根,是我国传统的名贵中药材,具有散瘀止血、消肿止痛的功效。三七总皂苷(total saponins of Panax notoginseng, PNS)在临床上被广泛用于治疗冠心病、心绞痛、中风、动脉粥样硬化等。这些作用都与抗血小板聚集功能有关,但由于PNS中含有多种皂苷成分,如三七皂苷R1、人参皂苷Rg1、Re、Rb1、Rc、Rd和Rf等,因此,其抗血小板聚集的活性成分并不清楚。现代药理研究表明:药物发挥作用的首要步骤是与细胞膜上的某些受体或通道结合。本研究运用血小板生物亲和吸附、HPLC分离分析筛选研究PNS活性成分,将活性成分筛选与分离分析相结合,排除了大量非活性成分的干扰,具有高选择性和高效率等特点。通过首先建立PNS的HPLC指纹图谱,然后将PNS在生理条件下与血小板相互作用,洗去非结合成分,改变洗脱液的pH值,破坏血小板结构,洗去结合成分,收集各洗脱液,将各洗脱液HPLC分析,其图谱与PNS标准图谱比较,找出结合成分(准活性成分),并进一步通过药理实验确证,最终发现皂苷B、A、C为PNS抗血小板聚集主要活性成分。这对于加强三七(总皂苷)的质量控制、三七的深层开发、以及作用于循环系统先导化合物的发现有积极意义,同时可进一步探索和改进生物膜色谱技术在中药活性成分筛选中的应用。更多还原

【Abstract】 Panax notoginseng is highly prized in China for its therapeutic abilities to stop haemorrhages, to influence blood circulation and to act as a tonic agent. Saponins (PNS), the major bioactive components in Panax notoginseg, are used to treat coronary heart disease, cardiac angina, apoplexy and atherosclerosis in clinic. These effects are correlated with their anti-platelet aggregation. However, PNS contain several kinds of active components such as notoginsenoside R1, ginsenoside Rg1, Rb1, Rc, Rd and Rf. It is still unknown that which saponin is mainly contribute to the therapeutic effects of PNS.Modern pharmacological studies have shown that combination with some receptors or channels on cell membrane is the first step of drug action. In this article, platelet bio-specific extraction coupled with high performance liquid chromatography (HPLC) was used to screen anti-platelet aggregation agents in PNS, which can eliminate the interference of lots of non-bioactive agents, and have the characteristic of high efficiency and high selectivity. In brief, first, HPLC fingerprint of PNS was developed. Secondly, PNS was added into platelet and interaction was performed at physiological conditions. Then, no combined components were removed by washing with phosphate buffered saline. Finally, changed the elution buffer pH to destroy the platelet, the bound components would be delivered. The eluent was collected for HPLC analysis. Comparing the HPLC profiles of eluent and PNS, we easily found the components which combined with platelets (potential anti-platelet aggregation agents). Furthermore, we confirmed their biological activity by using pharmacological assay. Based on the research above, we found that Saponin B, A and C are the main anti-platelet aggregation components in PNS.更多还原