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.

berberine  /  organ injury  /  metabolic diseases  /  inflammation  /  hypoglycemic effect  /  lipid-regulating effect  /  antitumor  /  cardiovascular protection  /  anti-inflammatory  /  neuroprotective