Rheumatoid arthritis (RA) is an autoimmune disease characterized by chronic synovitis and progressive joint destruction. Current clinical therapy drugs are limited by significant adverse effects and the development of drug resistance. Qinjiao (Gentianae Macrophyllae Radix), a well-known herb for dispelling wind-dampness in traditional Chinese medicine, has been historically used to treat RA with confirmed efficacy. Phytochemical studies have identified iridoids, triterpenoids, and flavonoids as the primary anti-RA constituents, with gentiopicroside, swertiamarin, ursolic acid, and kaempferol serving as key active monomers. These compounds exert multifaceted pharmacological effects through modulation of core signaling pathways including nuclear factor--κB (NF-κB), Janus kinase (JAK)/signal transducer and activator of transcription (STAT), and nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1), leading to anti-inflammatory activity, immune regulation, inhibition of fibroblast-like synoviocyte (FLS) proliferation and invasion, antioxidant effects, suppression of angiogenesis, and protection against bone destruction and cartilage damage. In clinical practice, Qinjiao is commonly combined with other botanicals such as Fangji (Stephaniae Tetrandrae Radix), Sangjisheng (Taxilli Herba), and Duhuo (Angelicae Pubescentis Radix) in composite formulas (e.g., Juanbi Tang and Compound Qixiong Granules), achieving synergistic multi-component and multi-target effects tailored to different TCM syndromes of RA. This review summarizes the comprehensive regulatory mechanisms through which Qinjiao intervenes in RA pathogenesis via multiple pathways, highlighting its promising therapeutic potential and providing a theoretical basis for further investigation of its pharmacodynamic material basis and clinical development.

Gentianae Macrophyllae Radix  /  rheumatoid arthritis  /  gentiopicroside  /  swertiamarin  /  ursolic acid  /  kaempferol  /  synovial fibroblasts