申请人一直围绕着从中药和天然药物中寻找活性先导化合物，以及在此基础上的创新药物研究开展了比较系统的研究工作。先后从30余种中药及天然药物中分离鉴定了800余种天然产物，其中新化合物200余种(包括新骨架化合物20余类)，并从中发现了多个具抗肿瘤、治疗神经系统疾病等作用的活性先导物。近年来，已主持国家自然科学基金、教育部新世纪人才、广州市珠江科技新星等科研及人才基金多项；已在SCI杂志上发表研究论文88篇，其中以第一或通讯作者在Angew Chem Int Ed、Org Lett (6篇)、Chem Eur J等杂志上发表研究论文33篇；获授权发明专利7项。本项目拟在前期工作基础上，对桃金娘科植物中的间苯三酚-萜类加合物的抗菌、抗病毒活性成分开展进一步研究，为治疗感染性疾病的新药研发提供科学依据。

The applicant’s research focuses on the discovery of bioactive compounds from traditional Chinese medicines (TCM) and natural products, as well as the new drugs development based on the lead compounds from TCM and natural products. In recent years, the applicant has carried out systematical phytochemical investigations on over 30 herbal medicines, such as Flueggea suffruticosa. As a result, over 800 compounds were isolated and identified from those medicinal plants, including over 200 new ones, and more than 20 of which possessed novel carbon skeletons. Five compounds had been selected as Hot off the press by journal Nat Prod Rep. Among them, several compounds with significant activities on tumours and central nervous system diseases, etc, had been discovered. Over the last five years, the applicant has been awarded multiple research grants and talent programs, including NSFC project and the program for new century excellent talents of the Ministry of Education, etc. So far, the applicant has published 88 scientific papers in SCI journals, 33 of which are first or corresponding author papers including the articles published in Angew Chem Int Ed, Org Lett, Chem Eur J, etc. Seven patents had been authorized. Based on our earlier studies, we are planning to carry out further investigation on the phloroglucinol-terpene adducts of the plants of family Myrtaceae. Their antibacterial and antiviral activities, as well as their structure-activity relationship and mechanism of function will also be investigated. And the results could provide scientific basis for the new drug development on the treatment of infectious disease.

天然产物由于具有结构多样性和生物活性多样性的特点，是创新药物研究中发现先导分子的重要来源。本项目以天然产物基础和应用研究为研究目标，建立了结合天然产物化学、计算生物学、分子生物学、药理学多学科交叉研究团队、技术平台和人才队伍，围绕天然药物资源中新类型、新结构的天然产物的发现和活性研究，取得了以下成绩：（1）对马鞭草科、车前科、益母草属以及五味子科等10余种药用植物的化学成分进行了研究，分离得到了500余个天然产物，包括100余个新的结构；（2）通过活性筛选，发现了系列具有抗HIV、精神性疾病、肿瘤以及在抗炎免疫等方面的系列天然产物活性分子，结构类型涉及到二萜、三萜以及生物碱等类型，为进一步的新药研发提供科学依据和研究基础；（3）初步完成了抗HIV活性分子“二苯胺酯”成药性评价，研究表明该目标分子是很有开发前景的抗HIV候选药物，作用机理研究表明化合物“二苯胺酯”抑制病毒（＋）链DNA的合成，为新的作用机制，相关研究已经申请了专利进行保护，拥有自主知识产权；（4）共发表SCI论文16篇，其中13篇为通讯作者，2项专利获得授权。（5）培养博士生1名、硕士生3名，另外1名博士研究生和2名硕士研究生已经完成了研究工作，将于2018年夏季申请毕业答辩；项目五味子化学于2015年获得了云南省自然科学科学技术奖特等奖（排名第4）；项目负责人获得了中国科学院王宽诚西部学者突出贡献奖（2015年）、中国药学会赛诺菲生物药物奖（2015）以及入选了中国科学院首批青年创新促进会优秀会员等奖项和荣誉。