中药活性成分靶点确定及作用机制研究方法进展  

Progress of target determination and mechanism of bioactive components of traditional Chinese medicine

作　　者：吴雪芬 卫晓红 武玉卓 夏桂阳 夏欢 王玲燕 商洪才[1] 林生 WU Xue-fen;WEI Xiao-hong;WU Yu-zhuo;XIA Gui-yang;XIA Huan;WANG Ling-yan;SHANG Hong-cai;LIN Sheng(Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing,Dongzhimen Hospital,Beijing University of Chinese Medicine,Bejing 100700,China)

机构地区：[1]北京中医药大学东直门医院中医内科学教育部和北京市重点实验室,北京100700

出　　处：《中国中药杂志》2022年第17期4565-4573,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(82073978,81522050,82104441);北京市自然科学基金杰出青年基金项目(JQ18026)。

摘　　要：中药活性成分是中药发挥药效作用的物质基础,靶点是中药活性成分发挥疗效的生物学基础。确定中药活性成分的靶点是中药药效物质研究的重要内容,对于中药分子机制研究和新药开发具有积极的意义。蛋白质是最主要的一类药物靶点,研究中药活性成分与蛋白质的相互作用是确定中药活性成分靶点的主要手段。目前,检测活性成分与蛋白质相互作用的技术主要包括表面等离子共振技术、荧光共振能量转移技术、生物膜干涉技术、分子对接技术、蛋白组芯片技术、分子靶点“钩钓”技术、定点突变技术及靶蛋白共结晶技术等。该综述对近十年生物靶点检测技术的原理及其在寻找中药活性成分靶点中的应用进行归纳总结,以期为阐明中药药理机制提供研究思路。The pharmacodynamic substances of traditional Chinese medicine(TCM) are the basis for the research of TCM and the development of innovative drugs. However, the lack of clarity of targets and molecular mechanisms is the bottleneck problem that restricts the research of pharmacodynamic substances of TCM. Bioactive components are the material basis of the efficacy of TCM, which exert activity by regulating the corresponding targets. Therefore, it is very important to identify the targets of the bioactive components to elucidate the pharmacological mechanism of TCM. Proteins are the most important drug targets, and study of the interaction between the proteins and bioactive components of TCM plays a key role in the development of pharmacological mechanism of TCM. In recent years, the main techniques for detecting the interaction between the bioactive components and proteins include surface plasmon resonance, fluorescence resonance energy transfer, bio-layer interference, molecular docking, proteome chip, target fishing, target mutant, and protein crystallization techniques, etc. This review summarized the biological target detection techniques and their applications in locating the targets of the bioactive components in TCM in the last decade, and this paper will provide useful strategies to elucidate the pharmacological mechanisms of TCM.

关 键 词：中药活性成分 表面等离子共振技术 荧光共振能量转移技术 生物膜干涉技术 分子对接技术 蛋白组芯片技术 分子靶点“钩钓”技术 定点突变技术 靶蛋白共结晶技术 

分 类 号：R284[医药卫生—中药学]