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中药活性成分直接作用靶点发现的新技术及应用

New technology and application of direct action target discovery of Chinese medicine active ingredients
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摘要 中药作为传统医学的瑰宝,其活性成分的作用和机制复杂多样。为深入探究中药活性成分的直接作用靶点,推动中药药效机制的研究和新药开发,本文综述了当前在中药活性成分靶点发现领域中应用广泛或具有潜力的新技术,旨在为相关领域提供新的视角和思路。目前,中药活性成分靶点发现技术主要分为标记法和非标记法。标记法通过设计特定的分子探针来识别和捕获作用靶点,具有高灵敏度和特异性;非标记法则通过监测靶蛋白稳定性等生物物理性质的变化来识别靶点,简便准确且无需修饰药物。二者各有其独特优势,从不同角度揭示了中药活性成分与生物分子间的相互作用机制,为中药药效机制的研究和新药开发提供了科学依据和创新思路。本文综述了2006年2月~2025年1月以来,在中药活性成分靶点鉴定方面的活性成分靶点识别、天然产物研究、蛋白质组学技术应用等领域的研究成果与方法进展。本文将聚焦研究方法与应用维度进行综述,以期补充传统药物发现的方法,为该领域后续研究提供借鉴与参考。 Traditional Chinese medicine(TCM),as a treasure of traditional medicine,has complex and diverse active ingredients and mechanisms of action.For the purpose of thoroughly investigate the direct targets of active ingredients in traditional Chinese medicine,promote research into the efficacy mechanisms of TCM,and advance new drug development.This paper presents a review of new technologies that are widely used or have potential in the field of target discovery for active ingredients in TCM.It is intended to provide new perspectives and ideas for related fields.Currently,active ingredient target discovery technologies for TCM are mainly divided into labelling methods and non-labelling methods.Labelling methods identify and capture targets through the design of specific molecular probes,offering high sensitivity and specificity.The non-labelling method identifies targets by monitoring changes in biophysical properties such as target protein stability.It is simple,accurate,and does not require drug modification.Both approaches have their unique advantages,revealing the mechanisms of interaction between active components of traditional Chinese medicine and biomolecules from different perspectives.This provides scientific basis and innovative ideas for the study of the efficacy mechanisms of traditional Chinese medicine and the development of new drugs.This paper reviews the research achievements and methodological advances from February 2006 to January 2025,in the identification of active components in TCM,natural products research,and the application of proteomics technologies for target identification.The review focuses on research methodologies and application dimensions,aiming to supply traditional drug discovery approaches and provide insights for future studies in this field.
作者 贺晓琴 田居意 林琦越 罗飘 张倩 王继刚 HE Xiao-qin;TIAN Ju-yi;LIN Qi-yue;LUO Piao;ZHANG Qian;WANG Ji-gang(Guangdong Basic Research Center of Excellence for Integrated Traditional and Western Medicine for Qingzhi Diseases,Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics,School of Traditional Chinese Medicine,Southern Medical University,Guangzhou 510515,China;School of Pharmacy,Southern Medical University,Guangzhou 510515,China;Artemisinin Research Center,Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China)
出处 《药学学报》 北大核心 2026年第1期37-46,共10页 Acta Pharmaceutica Sinica
基金 国家自然科学基金资助项目(82305014,82304827)。
关键词 中药活性成分 直接作用靶点 新技术 标记法 非标记法 active ingredients of traditional Chinese medicine direct action target new technology labelling method non-labelling method
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