中药药效物质基础的多元组分协同作用机制不清、有效形态难以捕获，是制约中药现代化研究的核心瓶颈。自组装技术作为一种新兴的纳米技术，凭借其独特的分子定向聚集能力，为深入解析中药药效物质基础提供了新的研究思路与手段。通过聚焦中药炮制、煎煮等过程中的自组装现象，以及解析这种自组装现象的分子机制及其与中药药效的相关性，阐释基于“成分-结构-药效”的药效物质基础学说。系统总结了多种中药自组装纳米结构的制备技术，包括冷冻干燥制备法、煎煮-分离制备法、中药碳点技术、中药囊泡技术及中药单体自组装法，这些技术不仅为阐明中药复杂体系的有效成分及其作用形式提供了关键解析工具，也为中药现代化研究开辟了新路径。

The complexity of the synergistic mechanisms among the multi-component active substances in traditional Chinese Medicine (TCM) and the difficulty in capturing their effective forms represent core bottlenecks hindering the modernization research of TCM. Self-assembly technology, as an emerging nanotechnology, that provides new research approaches and methods for in-depth analysis of the pharmacological basis of TCM with its unique molecular directional aggregation capability. This paper focuses on the self-assembly phenomena during the processes of TCM preparation and decoction, and elucidates the molecular mechanisms of these phenomena and their relevance to the efficacy of TCM. It explains the pharmacological substance basis theory based on “components-structure-efficacy”. The paper also systematically summarizes various preparation techniques for self-assembled nanostructures of TCM, including freeze-drying preparation method, decoction-separation preparation method, TCM carbon dot technology, TCM vesicle technology, and TCM monomer self-assembly method. These technologies not only provide key analytical tools for clarifying the effective components and their forms of action in the complex system of TCM but also open up new paths for the modernization research of TCM.

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河南省高等学校重点科研项目（25A360016）；河南中医药大学科研苗圃工程项目（MP2024-03）；河南省卫生健康委国家中医临床研究基地科研专项（2022JDZX109）；河南省卫生健康委河南省医学科技攻关计划项目（LHGJ20230685）；国家自然科学基金青年基金（82204736）