远志属三种云南特产植物的化学成分及生物活性研究

Gout is a common disease caused by a disorder of purine metabolism resulting in hyperuricemia,and has been enlisted by the United Nations as one of the 20 stubborn diseases in the 21st century. Earlier research found that xanthone compounds had significant inhibitory activities on xanthine oxidase. This research, based on the previous work, deals with the chemical studies on three Yunnan local Polygala medicinal plants: Polygala sibirica var. megalopha, P. crotalarioides and P. lijiangensis, which are rich for xanthone compounds. The xanthine oxidase inhibitory activities and structure-activity relationships of xanthone compounds will also be studied to find the natural leading compounds which can inhibit xanthine oxidase. Finally, this research will determine the most active leading compounds as index componenst, and establish the determination method for the original plant.This subject has a significant meaning on the study of gout medicines, development of ethnic medical resources, and the further use of Polygala medicinal plants.

痛风症是一种因嘌呤代谢紊乱导致尿酸生成异常的常见病，已被联合国列为21世纪20大顽症之一。 前期研究工作发现xanthone类化合物对黄嘌呤氧化酶具有显著的抑制活性。本研究拟在已有工作基础上，对富含xanthone类化合物的云南特产远志属三种药用植物小远志、西南远志和丽江远志进行化学成分研究，开展 xanthone类化合物黄嘌呤氧化酶抑制活性筛选与构效关系研究，发现抑制黄嘌呤氧化酶的天然先导化合物。确定活性最好的先导化合物为指标性成分，建立原植物中的含量测定方法。本课题对痛风治疗药物的研制、民族药的资源开发以及远志属植物的进一步利用具有重要意义。

本项目系统研究了远志属三种云南特有植物的化学成分和黄嘌呤氧化酶抑制活性研究。从三种植物中共分离鉴定了80个化合物，其中新化合物21个，发现了两个新颖的黄酮骨架6位为羟甲基取代基的黄酮醇苷类化合物。 发现部分 xanthone 、黄酮醇苷具有显著的黄嘌呤氧化酶抑制活性，并进行了初步的构效关系研究。确定活性较好的两个共有先导化合物为指标性成分，建立了原植物中的含量测定方法。该项目正式发表研究论文8篇，其中SCI论文2篇（molecules, Phychemistry letter）。本研究为痛风治疗药物的研制和远志属植物的资源开发奠定了重要基础。