云南抗血吸虫抗疟活性植物与有效成分基础研究

项目名称： 云南抗血吸虫抗疟活性植物与有效成分基础研究

项目编号： No.81460532

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： 姜北

作者单位： 大理大学

项目金额： 46万元

中文摘要： 血吸虫病、疟疾等是严重危害人类健康的疾病，目前全球虽有吡喹酮、青蒿素等少数几个药物可以控制，但这些药物结构单一、副作用明显，同时有因虫体耐药性增加而集体失效的风险，因此寻找替代性药物、加快新一代抗血吸虫抗疟药物研究、确保寄生虫病防治药物战略安全，意义重大。根据药物研发规律，由天然产物中寻找活性成分或先导化合物是一个重要的发现新一代抗血吸虫、抗疟药物的手段。云南药用植物资源异常丰富，如能通过系统的整合筛选，很有可能从中发现具有研究、开发潜力的新一代抗血吸虫、抗疟药物。本项目拟先以体外活性筛查的方式，对400种以上产自云南不同生长环境、不同科属的植物样品进行抗血吸虫、抗疟活性初步测试，确定8-10种效果较好的植物样品，进行活性成分跟踪分离、结构鉴定；继而选取1-2种有潜力的成分以动物实验方式进行活性效果评价，并进行适当的结构改造，了解构效关系，为研发新一代抗血吸虫、抗疟药物提供基础性研究依据。

中文关键词： 抗血吸虫活性；抗疟活性；植物；活性成分；基础研究

英文摘要： Schistosomiasis and malaria are serious diseases seriously harmful to people's health. Although a few drugs like praziquantel and artemisinin can currently be used all over the world to control the diseases, however, these medicines have significant defects such as severe side effects and the molecular structural similarity which can lead to great risk that all the drugs may lose the anti-parasite effects together due to parasite drug-resistance increasing. Therefore, to develop new generation of anti-parasite drugs as the complementary and alternative drugs is of great significance for the strategic security to prevent and control the parasite diseases. According to the rules for drug development, it is definitively an important way to start researches from natural products. Yunnan is rich in medicinal plant resources. By systematical integration and screens, it is quite possible to find potential candidates or lead compounds for new generation of anti-parasite drugs from Yunnan plant resources. Based on such conception, this project plans to collect more than 400 different plant samples from most plant families distributed in Yunnan. By in vitro assays, anti-schistosomal and anti-malarial activities of the samples will be evaluated, and 8-10 plant samples which show strong bioactivities will be selected for further study to determine the major bioactive constituents. 1-2 compounds which have best activities in the in vitro assays and low cute toxicity will be subjected to animal study to evaluate the in vivo anti-schistosomal and anti-malarial activities. Moreover, the structure-active relationship will be studied as well by synthetic chemistry and in vitro bioactive assays. The purpose of this study is to lay research foundations for the development of new generation of anti-schistosomal and anti-malarial drug in the future.

英文关键词： anti-schistosomal activity;anti-malarial activity;plants;active constituents;basic research