有毒中药效-毒转换机制的研究一直是中药合理应用的难点，以蒽醌类、二苯乙烯苷类成分及含有该类成分的中药为研究对象，梳理了这2类效-毒同源物质及其体内代谢规律与产物，分析了效-毒同源物质原型及其代谢产物的构-效与构-毒关系，整合并总结了含蒽醌、二苯乙烯苷类有毒中药的药效与毒性作用机制及毒-效转换关系与规律。为进一步阐释中药效-毒转换机制的研究，基于蛋白组学技术、药物靶点及药物作用机制研究方法，提出了以蒽醌类、二苯乙烯苷类成分为例的中药效-毒转换靶点与机制研究的策略与展望，为中药效-毒转换机制与转换规律的探究提供思路与方法借鉴。

The study of the efficacy-toxicity conversion mechanism of toxic traditional Chinese medicine (TCM) has always been a difficult point in the rational application of Chinese herbal medicine. In this paper, we have taken the anthraquinones, stilbene glycosides and TCM containing these components as the research objects, sorted out these two types of efficacy-toxicity homologous substances and their metabolism patterns and products in vivo, analyzed the efficacy-toxicity of prototypes of these homologous substances and structure-activity and structure-toxicity relationships of their metabolites, and integrated and summarized the mechanism of efficacy and toxicity, as well as the relationships and patterns of efficacy-toxicity conversion for toxic TCM containing anthraquinone and stilbene glycosides. To further elucidate the mechanism of the efficacy-toxicity conversion of TCM, we proposed strategies and prospects for the study of the targets and mechanism of efficacy-toxicity conversion of Chinese medicines based on proteomics technology, drug targets and drug mechanism of action by taking anthraquinones and stilbene glycosides as examples, in order to provide ideas and methodological reference for the investigation of the rules of efficacy-toxicity conversion of TCM.

R285

国家自然科学基金资助项目（82174090）；江苏省高校“青蓝工程”中青年学术带头人；江苏省高校333工程第三层次培养对象