硫氧还蛋白还原酶（TrxR）是抗肿瘤新颖的药物靶点，寻找新型TrxR抑制剂已经成为发现抗肿瘤药物的有效途径和研究热点。前期研究发现：麻疯树属植物含有罕见的天然非芳香型二萜类TrxR抑制剂，采用先化学分离再筛选活性的常规方法，需要对该属植物化学成分系统分离，周期漫长且微量活性成分易丢失。薄层色谱生物自显影技术可快速识别目标分子，并能定向指导分离过程，其联合紫外分光光度法可兼具定量分析的能力，具有高通量发现的优势。据此，本项目拟进行如下研究：①以TrxR为靶标，基于薄层色谱生物自显影技术建立快速识别并定向分离TrxR抑制剂的新方法；②采用本项目建立的方法辅以紫外分光光度法对我国麻疯树属5种植物新型TrxR抑制剂进行高通量筛选。该研究预期为高通量筛选TrxR抑制剂提供有效手段，为抗肿瘤药物的研发提供先导物；该项目是快速发现药物先导化合物的新策略，可为其它类酶抑制剂的快速发现提供借鉴。

Thioredoxin reductase (TrxR) is a promising drug target for cancer therapy. The screening of natural TrxR inhibitor as a potent strategy for the discovery of new anti-tumor agents, have attracted considerable attention.. Previous investigations have revealed that the genus Jatropha (Euphorbiaceae) was a source of the active diterpenoids represented the rare examples of non-aromatic TrxR inhibitors which were usually obtained by the determination of activity after separation, and showed the obvious disadvantages, such as long study period and poor-pertinence. Moreover, it was easy to lost for traces of active ingredients in the course of separation owing to lack of activity-guided isolation. TLC bioautography, a high-throughput screening (HTS) approaches, can recognize active compounds fast and guide the separation accurately, and further realized quantitative analysis by combining with ultraviolet spectrophotometry. Therefore, a new method targeting TrxR will be established to rapidly obtain TrxR inhibitors based on TLC bioautography. Additionally, HTS will be carried out for exploring the new types of TrxR inhibitors from the genus Jatropha in China by using the developed TLC-bioautography in combination with ultraviolet spectrophotometry.. Our project will be helpful to provide the new strategy for the discovery of leading compound, makes it possible to search for natural TrxR inhibitors extensively and rapaidly, provide leading compounds for the treatment of tumor, and give reference for exploring the other types of enzyme inhibitors.