三七是一种著名的多年生草本植物，广泛用作医药和保健食品的原料。由于其多种治疗作用，近年来对三七的研究工作迅速增加，迫切需要对这种重要药用植物的研究进展进行全面综述。在此，我们总结了三七代表性生物活性成分及其心血管保护、抗肿瘤、免疫调节等多种药理作用的最新研究。更重要的是，我们强调人参皂苷的生物合成和调控，人参皂苷是三七的主要生物活性成分。综述了人参皂苷生物合成中涉及的关键酶和转录因子 (TF)，包括多种 CYP450、UGT、bHLH 和 ERF TF。我们还基于多组学数据构建了一个转录调控网络，并预测了介导人参皂苷生物合成的候选转录因子。最后，重点介绍了目前人参皂苷生产的三种主要生物技术方法。本综述涵盖了过去几十年的进展，为三七资源的质量评价和合理利用和开发提供了见解。现代组学技术有利于探索人参皂苷生物合成的分子机制，这对于三七新品种的选育至关重要。鉴定生物合成人参皂苷的功能酶将有助于制定高效、大规模生产特定人参皂苷的潜在策略。© 作者 2024。由牛津大学出版社代表南京农业大学出版。

Panax notoginseng is a famous perennial herb widely used as material for medicine and health-care food. Due to its various therapeutic effects, research work on P. notoginseng has rapidly increased in recent years, urging a comprehensive review of research progress on this important medicinal plant. Here, we summarize the latest studies on the representative bioactive constituents of P. notoginseng and their multiple pharmacological effects, like cardiovascular protection, anti-tumor, and immunomodulatory activities. More importantly, we emphasize the biosynthesis and regulation of ginsenosides, which are the main bioactive ingredients of P. notoginseng. Key enzymes and transcription factors (TFs) involved in the biosynthesis of ginsenosides are reviewed, including diverse CYP450s, UGTs, bHLH, and ERF TFs. We also construct a transcriptional regulatory network based on multi-omics data and predicted candidate TFs mediating the biosynthesis of ginsenosides. Finally, the current three major biotechnological approaches for ginsenoside production are highlighted. This review covers advances in the past decades, providing insights into quality evaluation and perspectives for the rational utilization and development of P. notoginseng resources. Modern omics technologies facilitate the exploration of the molecular mechanisms of ginsenoside biosynthesis, which is crucial to the breeding of novel P. notoginseng varieties. The identification of functional enzymes for biosynthesizing ginsenosides will lead to the formulation of potential strategies for the efficient and large-scale production of specific ginsenosides.© The Author(s) 2024. Published by Oxford University Press on behalf of Nanjing Agricultural University.