小檗碱是一种从黄连、黄柏等传统药用植物中提取的异喹啉类生物碱，拥有悠久的临床应用历史。近年来研究证实，小檗碱在降血糖、调血脂、抗肿瘤、心血管保护、抗炎及神经保护等方面展现出多种药理活性，但现有研究成果较为分散，缺乏系统性整合。系统综述小檗碱的主要药理作用及其相关分子机制，旨在阐明其多效性背后的共同调控网络，为其临床转化与创新药物研发提供重要理论支撑。小檗碱的药理作用主要通过三大关键通路协同实现：抑制核因子-κB（nuclear factor-κB，NF-κB）和丝裂原活化蛋白激酶（mitogen activated protein kinase，MAPK）信号通路以阻断炎症级联反应；激活核因子E2相关因子2/抗氧化反应元件（nuclear factor erythroid 2-related factor 2/antioxidant response element，Nrf2/ARE）途径以增强抗氧化防御；抑制NOD样受体热蛋白结构域相关蛋白3（NOD-like receptor family pyrin domain containing protein 3，NLRP3）炎症小体组装从而减少细胞焦亡。不仅为深入理解小檗碱的药理作用机制绘制了清晰的分子图谱，也为炎症、氧化应激及细胞程序性死亡相关疾病的药物靶点开发与多通路协同治疗策略设计奠定了科学基础，具有重要的理论价值与转化前景。

Berberine (BBR) is an isoquinoline alkaloid extracted from traditional medicinal plants such as Coptis chinensis and Phellodendron amurense, with a long history of clinical application. Recent studies have demonstrated that BBR exhibits multifaceted pharmacological activities, including blood glucose lowering, lipid regulation, anti-tumor effects, cardiovascular protection, anti-inflammation, and neuroprotection. However, existing research findings are relatively scattered and lack systematic integration. This article aims to systematically review the main pharmacological effects of BBR and its related molecular mechanisms, intending to elucidate the common regulatory network underlying its multifaceted effects and provide important theoretical support for its clinical translation and the development of innovative drugs. The results indicated that the multifaceted pharmacological effects of BBR are mainly achieved through the coordination of three key pathways: inhibiting the nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways to block inflammatory cascade reactions; activating the nuclear factor erythroid 2-related factor 2/antioxidant response element (Nrf2/ARE) pathway to enhance antioxidant defenses; and suppressing the assembly of the NOD-like receptor family, pyrin domain containing protein 3 (NLRP3) inflammasome to reduce cell pyroptosis. This study not only provides a clear molecular map for an in-depth understanding of the systemic pharmacological mechanisms of BBR, but also lays a scientific foundation for the development of drug targets and multi-pathway synergistic treatment strategies for diseases related to inflammation, oxidative stress, and programmed cell death, possessing significant theoretical value and translational prospects.

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中央高校基础研究业务费专项——北京中医药大学基础研究基金（揭榜挂帅）项目（2024-JYB-JBZD-051）