Abstract:Ganoderma lucidum (Leyss. ex Fr.) Karst., a medicinal fungus called “Lingzhi” in China, has been used in traditional Chinese medicine in China for the prevention and treatment of various types of diseases, such as cancer, hepatopathy, arthritis, hypertension, neurasthenia, and chronic hepatitis. It is clear that the anticancer activity of G. lucidum is mainly due to polysaccharides and/or triterpenoids of the fungus. However, until now, the mechanism of the anticancer action of G. lucidum has not been well understood and, previously, the activation of the immune response of the host was widely considered to be the only mechanism by which G. lucidum prevented and/or treated cancer. However, recent studies reviewed in the present paper have shown that the potential mechanisms of anticancer action include not only the activation of the immune response of the host, but also the induction of cell differentiation, the induction of Phase II metabolizing enzymes, the inhibition of angiogenesis, and the inhibition of the expression of the urokinase-type plasminogen activator (uPA) and the uPA receptor in cancer cells. To further elucidate the mechanisms of action of G. lucidum, more in vivo tests and randomized controlled clinical trials should be carried out, and the molecular mechanisms should be studied intensively. Additionally, whether the anticancer compounds in G. lucidum act synergistically or independently should be further studied.