RG-II型植物果胶的结构与保护心血管作用的关系研究

Rhamnogalacturonan II (RG-II) has complex and relatively conserved structure. The preparation of RG-II type pectin is difficult due to its low content. Therefore, there is little report on the relationship between the structure and pharmaceutical activity of RG-II. In this project, the structure of RG-II type pectin from grape, panax ginseng, panax quinquefolium, panax notoginseng and Apocynum venetum and their protective effects on cardiovascular disease will be deeply studied. We will search for the stable and efficient preparation method of RG-II type pectin from plant, and prepare multigram-scale of RG-II; the fine structures of different RG-II would be studied in detail by acid hydrolysis, enzymatic hydrolysis, NMR and MS, and the structure of RG-II would be modified to prepare structural units; the inhibitory effects of RG-II with different structures on arrhythmia, hyperlipoidemia and hypertension would be analyzed, and the relationship between the structures of RG-II and their cardiovascular protective activity would be discussed. This project will provide new ideas for studying the relationship of structure-activity in pectin, and provide theoretical basis for the pharmacological application of RG-II type pectin.

II型果胶（RG-II）结构复杂，相对保守，具有保护心血管功能。由于在植物中含量较低，样品制备困难，鲜有研究RG-II型果胶结构与活性关系的报道。本项目拟研究葡萄、人参、西洋参、三七和罗布麻中RG-II型果胶的结构与保护心血管活性的关系。研究内容包括：探索稳定高效制备RG-II型果胶的方法和路线，能够以克级规模制备RG-II型果胶样品；利用多种方法如酸水解、酶水解、核磁共振、飞行质谱等，分析RG-II型果胶结构，同时对其结构进行修饰以及制备分子中的结构单元；利用大鼠心律失常、高血脂和高血压三种模型研究不同结构的RG-II及结构单元对心血管的保护作用，探讨RG-II的结构与保护心血管作用的构效关系。本项目的研究成果为RG-II型果胶的应用以及开发保护心血管药物提供了理论基础，也为果胶结构与功能关系提供了新的信息。

RG-II型果胶是一类结构复杂的果胶类型，具有潜在的保护心血管的功能。由于样品制备困难，限制了RG-II型果胶的药理活性研究。本项目以人参等5种植物为原料，探索出稳定制备RG-II型果胶的方法。利用碱皂化与果胶酶降解结合的方式实现了克级制备不同来源RG-II结构域的目标。利用两步酸水解能够定向制备不同来源RG-II的主链、侧链A和侧链B。利用ESI-MS/MS及NMR等仪器手段详细解析了不同来源RG-II的结构特征。建立了大鼠心律失常、高血脂和高血压三种模型，通过分析RG-II果胶对心律失常、高血脂和高血压的调节作用，发现RG-II果胶结构域具有一定的心血管保护作用，并且不同植物来源的RG-II活性作用相似，推测与RG-II保守的结构有关。本项目的研究结果为RG-II型果胶的制备及药理活性提供了方法学参考，对多糖的理论研究和实际应用都具有重要的意义。项目执行期间发表SCI论文4篇，参加国内会议6次，获得国内发明专利授权1项。