| 郭奕泽.基于CYP450酶介导代谢的中药与化学药相互作用研究进展[J].安徽医药,待发表. |
| 基于CYP450酶介导代谢的中药与化学药相互作用研究进展 |
|
| 投稿时间：2026-08-28 录用日期：2026-10-22 |
| DOI： |
| 中文关键词: 细胞色素P450 中药 化学药 药物相互作用 药代动力学 |
| 英文关键词: |
| 基金项目: |
|
| 摘要点击次数: 34 |
| 全文下载次数: 0 |
| 中文摘要: |
| 中药与化学药联合应用在慢性病、器官移植、肿瘤及心脑血管疾病等治疗场景中较为常见，细胞色素P450（cytochrome P450，CYP450）酶介导的代谢性相互作用是联合用药安全评价的重要内容。中药及其活性成分可通过可逆性抑制、时间依赖性抑制或核受体介导的酶诱导改变CYP450活性，进而影响化学药的体内暴露、疗效及不良反应风险。本文围绕CYP3A4/5、CYP2C9、CYP2C19、CYP2D6和CYP1A2等主要亚型，综述五味子制剂、黄连及小檗碱、丹参、人参、银杏、甘草等中药及成分与化学药相互作用的研究证据，并比较体外酶学、临床探针药“鸡尾酒”试验、治疗药物监测、药物基因组学、生理药代动力学及群体药代动力学模型等研究方法。现有证据表明，不同中药或制剂的体外CYP作用向人体效应的外推一致性差异较大；五酯胶囊与他克莫司、小檗碱与部分CYP底物之间已有较明确的人体药代学或血药浓度证据，而人参、银杏和甘草等的临床效应多表现为较弱或制剂依赖。评价中药与化学药相互作用应综合制剂质量、实际暴露、底物治疗窗、遗传多态性及转运体等因素。未来需加强标准化制剂的人体研究和模型外部验证，为中西药联合用药风险识别及个体化管理提供依据。 |
| 英文摘要: |
| The concomitant use of traditional Chinese medicines (TCMs) and conventional chemical drugs is common in chronic disease management, organ transplantation, oncology, and cardiovascular or cerebrovascular care. Cytochrome P450 (CYP450)-mediated metabolic interactions are therefore an important component of medication-safety assessment. Herbal preparations and their constituents may alter CYP activity through reversible inhibition, time-dependent inhibition, or nuclear receptor-mediated induction, thereby changing systemic drug exposure, efficacy, and toxicity. This review summarizes evidence on interactions involving major CYP isoforms, including CYP3A4/5, CYP2C9, CYP2C19, CYP2D6, and CYP1A2, with emphasis on Schisandra preparations, Coptis/berberine, Salvia miltiorrhiza, ginseng, Ginkgo biloba, and licorice. In vitro enzyme assays, clinical cocktail probe studies, therapeutic drug monitoring, pharmacogenetics, physiologically based pharmacokinetic modeling, and population pharmacokinetic approaches are also compared. Current evidence shows substantial variation in the translation of in vitro CYP effects to human outcomes. Relatively clear human pharmacokinetic or concentration-monitoring evidence is available for Wuzhi Capsule–tacrolimus and for repeated berberine administration with selected CYP substrates, whereas the clinical effects of ginseng, Ginkgo biloba, and licorice are generally modest or formulation-dependent. Evaluation of herb–drug interactions should therefore integrate product quality, actual exposure, therapeutic index of the victim drug, genetic polymorphisms, and transporter involvement. Further studies using standardized herbal products and externally validated quantitative models are needed to support risk identification and individualized management of combined traditional Chinese and conventional drug therapy. |
|
查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|
