Abstract: As a classic traditional Chinese medicinal herb, Dipsaci Radix possesses a complex basis of bioactive substances and extensive pharmacological activities. Existing studies have confirmed that Dipsaci Radix demonstrates significant efficacy in preventing and treating osteoporosis and promoting fracture repair, and exhibits multidimensional therapeutic potential in chronic inflammatory and neurodegenerative diseases, such as intervening in rheumatoid arthritis, alleviating neuroinflammation, and improving cognitive impairment. The therapeutic effects of Dipsaci Radix fully reflect the synergistic characteristics of “multiple components” and “multiple targets” of traditional Chinese medicinal herbs. Its active components can improve local pathological conditions by targeting multiple key signaling pathways and can exert global immune and homeostatic regulation by reshaping the host gut microbiota and modulating related metabolic networks. This article systematically reviews the main chemical components of Dipsaci Radix and research progress on its pharmacological effects, deeply analyzes its bioactive substance basis and physiological regulatory networks, aiming to clarify the intervention mechanisms of Dipsaci Radix in complex diseases and provide a solid scientific basis for precise drug development and clinical translation.