Abstract / Summary
Abstract Ganoderma lucidum has attracted increasing attention in cancer research because of its diverse bioactive components and immunomodulatory properties. However, its antitumor effects are often discussed as broad “anticancer activity”, which may obscure the distinct roles of different components. This review summarizes the antitumor mechanisms of G. lucidum-derived components through mechanistic stratification while considering differences in material definition, structural characterization, and evidence strength. Fruiting body-derived polysaccharides have been more frequently investigated for immune microenvironment remodeling, macrophage regulation, lymphocyte responses and gut microbiota-associated systemic effects, although selected preparations also exert direct effects on tumor-cell proliferation, apoptosis, epithelial–mesenchymal transition and senescence. Triterpenoids, particularly chemically defined compounds, have more commonly been studied for tumor-cell-intrinsic processes such as oncogenic signaling, cell-cycle progression, programmed cell death, metabolic vulnerability and therapeutic resistance, while overlapping immunological and microenvironmental effects have also been reported. Spore-derived preparations, including sporoderm-broken spores and spore oil, should be regarded as complex bioactive systems rather than single active components, with combined effects on tumor cells, immune responses, lipid metabolism and host condition. Fungal immunomodulatory proteins, further show potential in regulating tumor stemness, migration and treatment sensitivity. In addition, G. lucidum-derived components may enhance immune checkpoint blockade, improve radio-chemotherapy responses and serve as functional materials in engineered delivery systems. Future studies should further clarify how specific components act on defined targets and mechanisms in particular cancer types and therapeutic settings, thereby supporting their development as mechanism-defined and quality-controllable adjunctive strategies for cancer therapy.