代谢激活是药物性肝损伤和上市药物被撤销的主要原因。代谢激活过程中产生的具有亲电活性的代谢中间体，一方面能够和细胞内的生物大分子，如蛋白质或核酸，发生共价结合而诱发肝毒性、肾毒性及致 癌性等毒性作用；另一方面还会共价修饰药物代谢酶，使其产生不可逆性抑制，从而诱发严重的药物-药物相互 作用。中药成分的代谢激活已经成为了国内外中草药毒性研究领域的热点。本文针对易被细胞色素P450酶 代谢激活的不同结构与关键基团，如芳香胺、芳香硝基物、含氮杂环化合物、对苯二酚、亚甲二氧基苯、呋喃等,各类型的代表性中药成分，以及所涉及的P450亚型酶与相关毒性进行了综述，并对该领域进行了研究展望。

Metabolic activation is the main cause of drug- induced liver injury and the withdrawal of listed drugs. Metabolic intermediates that are produced during metabolic activation can induce toxicity, such as hepatotoxicity, nephrotoxicity and carcinogenicity, etc., by combining covalent bonding with biological macromolecules in cells, such as proteins or nucleic acids. On the other hand, the drug- metabolizing enzyme can be covalently modified to produce irreversible inhibition, which can induce serious drug-drug interactions. The metabolic activation of herbal ingredients has become a hot topic in the research field of Chinese herbal medicine. In this paper, we reviewed the typical herbal ingredients classified by the their structures and key groups, such as aromatic amines, nitroarenes, azaheterocycles, hydroquinones, methylenedioxyphenyl and furans, etc., that can be activated by cytochrome P450 enzyme metabolism, the involved P450 isoforms and related toxicity, as well as the prospect of research on this field.

国家科技部“中医药现代化研究”重点专项（2017YFC1702000）：基于器官芯片技术的中药安全性有效性评价体系，负责人：杨凌；上海市科学技术委员会上海市优秀学术带头人计划（18XD1403600）：代谢酶介导的中药不良反应早期评价及预警体系的构建，负责人：葛广波；大连市科 学技术局大连市支持高层次人才创新创业项目（2016RQ025）：羧酸酯酶1检测试剂盒的研发及其生物医学应用，负责人：葛广波。