Codonopsis pilosula (Franch.) Nannf. (Dangshen), a vital medicinal herb in Traditional Chinese Medicine (TCM), is renowned for its adaptogenic, immunomodulatory, and multi-pharmacological properties. This review comprehensively examines the phytochemical composition and diverse biological activities of C. pilosula, highlighting its therapeutic potential in modern medicine. The plant contains bioactive compounds, including polysaccharides, alkaloids, triterpenes, polyacetylenes, and phenolic acids, which contribute to its broad-spectrum effects. Pharmacological studies reveal its antioxidant, anticancer, immunomodulatory, antidiabetic, antimicrobial, neuroprotective, hepatoprotective, cardioprotective, and antiviral activities. Key mechanisms include ROS scavenging, Nrf2/Keap1 pathway activation, apoptosis induction via signalling pathway, α-glucosidase inhibition, and immune regulation through MAPK/NF-κB signaling. Notably, C. pilosula polysaccharides (CPPs) demonstrate neuroprotection against Aβ-induced toxicity and enhance cognitive function in Alzheimer’s models, while lobetyolin exhibits selective anticancer effects by disrupting glutamine metabolism. Additionally, C. pilosula shows promise in metabolic disorders, sepsis management, and myocardial repair. It is noted that C. pilosula compounds exhibited multiple therapeutic effects at low concentrations (IC50 10-50 μg/mL). Despite its therapeutic potential, challenges in sustainable cultivation and quality control necessitate further research. This review underscores C. pilosula’s role as a multi-target herbal medicine, bridging traditional use and scientific validation for future drug development and functional food applications.

Keywords:Codonopsis pilosula; Dangshen; Polysaccharides; Immunomodulation; Neuroprotection; Anticancer; Antioxidant; Traditional Chinese Medicine