Abstract: Kadsura coccinea is recognized for both medicinal and edible applications, with its rhizomes traditionally utilized in folk medicine for inflammation reduction and pain alleviation, while the fruits are characterized by juicy texture, sweet flavor, and high nutritional value. The pharmacological activities of Kadsura coccinea, specifically antibacterial, anti-inflammatory, hepatoprotective, and antitumor effects, are systematically validated through empirical research, as these therapeutic actions are pharmacologically correlated with its unique phytochemical composition comprising lignans, triterpenoids, volatile oils, and phenolic compounds. To further elucidate the anti-inflammatory and anticancer-active constituents along with the pharmacodynamic material basis of Kadsura coccinea, the aforementioned chemical components and their bioactivities in anti-inflammatory and anticancer contexts are comprehensively reviewed, with particular emphasis on their mechanisms of action involving inhibition of cell proliferation, induction of apoptosis, and immunoregulation. This review aims to provide novel perspectives for medicinal exploitation and resource utilization of natural botanical resources, expand the application domains of Kadsura coccinea, and promote the sustainable development of its industrial chain.