广东紫珠促凝血活性成分及其作用机制研究

项目名称： 广东紫珠促凝血活性成分及其作用机制研究

项目编号： No.81460589

项目类型： 地区科学基金项目

立项/批准年度： 2015

项目学科： 医药、卫生

项目作者： 付辉政

作者单位： 江西省药品检验检测研究院

项目金额： 47万元

中文摘要： 出血是临床上常见的多发病症，严重者可危及生命。西药止血存在较为严重的不良反应，因此天然止血药物的研发具有重要意义。在前期研究中，采用活性追踪方法，从具有显著促ADP诱导血小板聚集活性的广东紫珠70%乙醇提取物其中2个活性组分中得到了28个化合物，其中新化合物8个。对28个化合物进行了促ADP诱导血小板聚集活性筛选，4个化合物(2个苯乙醇苷类和2个梓醇类)显示较强的促ADP诱导血小板聚集活性。已有的药理试验表明还存在其它高活性组分，活性组分中还存在苯乙醇苷类和梓醇类，为明确广东紫珠促凝血活性的物质基础、活性成分和作用机制。为此，本课题拟在药物化学和药理学的密切配合下，对广东紫珠展开系统深入研究，得到活性成分，探讨其构效关系，并对活性强的成分进行作用机制研究。为寻找促凝血先导化合物以及研究和开发具有自主知识产权的创新促凝血中药提供科学依据。

中文关键词： 广东紫珠；促凝血作用；活性成分；构效关系；作用机制

英文摘要： Haemorrhage is a common clinical multiple symptoms, severe cases can be life-threatening. Hemostatic drugs had widespread adverse reactions. Therefore it is of great significance to research natural hemostatic drugs. In our prophase research, we found 70% ethanol extraction of Callicarpa kwangtungensis Chun could promote ADP induced platelet aggregation. According to the screening results of its activity tracking, 28 compounds were isolated from 2 compositions of the extraction, among which 8 were new. 4 compounds (2 phenylethanoid glycosides and 2 catalpols ) showed strong promoting activity on ADP-induced platelet aggregation. Pharmacological tests have shown there are other active components, in which there are phenylethanoid glycosides or catalpols. In order to clarify the procoagulant substances in Callicarpa kwangtungensis Chun, reveal the active ingredients and their mechanism. So, Callicarpa kwangtungensis Chun will be systematic study in this subject, to get active ingredients, to investigate their structure-activity relationships. Further to study on the mechanism of strong components. Finally, we can provide scientific basis for finding procoagulant lead compounds and for development of novel procoagulant TCM possessing independent.

英文关键词： Callicarpa kwangtungensis Chun;Procoagulant activities;Active ingredients;Structure-Activity Relationship(SAP);Mechanisms