龙胆苦苷（Gentiopicroside, GPS）是从龙胆科植物中提取的主要活性成分，具有抗炎、抗氧化、镇痛、抗纤维化、抑制肿瘤细胞增殖以及改善糖脂代谢等多种药理作用，在治疗糖尿病、肝脏疾病、骨与关节疾病等多种疾病方面展现出广泛的应用前景。本文阐述龙胆苦苷的药代动力学研究现状，包括其在不同动物模型中药代动力学特性，以及在治疗糖尿病及其并发症、肝损伤、骨与关节疾病等疾病中的作用机制和作用靶点。研究表明，龙胆苦苷通过调节多种信号通路，如PI3K/AKT、FOXO1、PPAR-γ、NF-κB等，发挥其治疗作用。尽管目前的研究已取得一定进展，但仍存在局限性，如大多数研究集中于动物模型和体外实验，缺乏高质量的临床循证试验支持。未来的研究应进一步探索龙胆苦苷的新作用靶点和信号转导通路，提高其生物利用度，并加强中药复方的研究，以充分发挥其中医整体论治的优势。

Gentiopicroside (GPS) is the main active ingredient extracted from Gentiaceae. It has anti-inflammatory, antioxidant, analgesic, anti-fibrosis, inhibition of tumor cell proliferation and improvement of glucose and lipid metabolism. In the treatment of diabetes, liver diseases, bone and joint diseases and other diseases show a wide range of application prospects. This paper reviews the pharmacokinetics of gentiopicrin, including its pharmacokinetic properties in different animal models, and its mechanism and targets in the treatment of diabetes mellitus and its complications, liver injury, bone and joint diseases. Studies have shown that gentiopictin exerts its therapeutic effects by regulating various signaling pathways, such as PI3K/AKT, FOXO1, PPAR-γ, NF-κB, etc. Although the current research has made some progress, there are still limitations, such as most studies focused on animal models and in vitro experiments, lack of high-quality clinical evidence-based trials support. Future studies should further explore the new targets and signal transduction pathways of gentiopicroside, improve its bioavailability, and strengthen the research of traditional Chinese medicine compounds, so as to give full play to the advantages of holistic treatment of traditional Chinese medicine.

中医药防治糖尿病及其并发症学科创新引智基地（编号：B20055）国家重点研发计划：南非传统草药治疗糖尿病研究”（2021YFE0106300）