基于目标成分敲除/敲入技术辨识中药药效物质基础研究进展

中药具有多成分、多靶点、多途径的特色和复杂性,药效物质基础的研究是中药研究必经之路,是阐释中药整体功效及作用本质的核心环节,明确的药效物质基础将有助于中药走向国际。现阶段的中药物质基础研究方法各有优劣,目标成分敲除/敲入模式自被提出以来因其独特的优势而备受关注,该模式利用准确高效的提取分离技术从方药全提取物中无损失、无破坏的分离出目标成分,通过对比目标成分敲除/敲入前后方药提取物药效的变化,进而研究目标成分对中药整体药效的贡献。整个研究过程始终将方药提取物看作一个整体,能较好的体现中药多成分、多靶点整合调节的特点。该模式的运用,不仅有助于中药药效物质基础的研究,还将对制定中药质量控制标准及临床合理用药提供帮助,但因目标成分分离技术的局限而使该模式的应用受到制约。作者通过查阅近年来文献,对该模式的研究流程及应用方法进行归纳总结,以期为本模式的应用提供参考。

Research progress on identification of pharmacodynamic substance basis of traditional Chinese medicine based on target constituent knock-out/knock-in technology

The effective material basis of traditional Chinese medicine(TCM)is an indispensable part of studies on TCM,and each technology has its advantages and disadvantages.The target constituent knock-out/knock-in technology has attracted much attention since it was proposed because of its unique advantages of regarding the extract of the formula as a whole,which can better reflect the characteristics of multi-component and multi-target integration and regulation of TCM.This method investigated the contribution of target constituent to the overall efficacy of a TCM by analyzing the changes in efficacy of the remaining formula before and after knock-out/knock-in of the target constitution.The application of this model not only facilitates studies of the effective constituents of TCM,but also help to develop the quality control standard of TCM.However,the application of this model is restricted due to the limitation of target constituent separation technology.By reviewing the literatures in recent years,this study summarized the research process and application of this method for a reference.