Based on the analysis of more than 270 patents and scientific articles, this state-of-the-art review presents Ganoderma lucidum, a medicinal basidiomycete mushroom with immunomodulatory and anti-cancer effects. Cultivation methods for the commercial production of G. lucidum fruit bodies and mycelia are summarized, with main active compounds of triterpenoids, polysaccharides, and proteins, often found in forms of proteoglycans or glycopeptides. Pharmacological effects with emphasis on anti-cancer and immunomodulatory functions are presented, separately for spores and dry mycelia, and for the groups of triterpenoids, polysaccharides, proteins and glycoproteins. Patents disclosing preparation methods of extracts and purified pharmaceutical isolates are reviewed, and examples of anti-cancer formulations, used as pharmaceuticals or nutraceuticals, are given. The review suggests that according to the present understanding, the anti-cancer activity of G. lucidum may be attributed to at least five groups of mechanisms: (1) activation/modulation of the immune response of the host, (2) direct cytotoxicity to cancer cells, (3) inhibition of tumor-induced angiogenesis, (4) inhibition of cancer cells proliferation and invasive metastasis behaviour, and (5) carcinogens deactivation with protection of cells. Although, the data from recent in vitro and in vivo studies demonstrate promising anti-cancer effects, a need is identified for further (1) isolation and purification of compounds, with deeper understanding of their individual and synergistic pharmacological effects, (2) molecular level studies of the antitumor and immuno-supportive mechanisms, (3) well designed in vivo tests and controlled clinical studies, and (4) standardisation and quality control for G. lucidum strains, cultivation processes, extracts and commercial formulations.
