medicine extracts that have been anticipated for their cancer prevention effects [1]. In this chapter, we will introduce the anticancer activities of polysaccharides as well as the cancer prevention activities of sterols and triterpenes. 2. Mushroom-derived anticancer polysaccharides Research on mushroom-derived β-glucans began when Chihara, Hamuro, and others at the National Cancer Center Research Institute in Japan isolated and purified lentinan, a β-1,3glucan with branched chains formed by β-1,6-glycosidic bonds, from L. edodes in 1968 [2, 3]. Subsequently, many efficacy studies on lentinan, primarily concerning its antitumor activities, have been reported [4-6]. Ikekawa et al. intraperitoneally administered aqueous extracts of six types of edible mushrooms, and demonstrated their antitumor effects on cancer cell line sarcoma S-180 [7]. Upon such discoveries, polysaccharides lentinan and schizophyllan, glycoprotein krestin, and P. linteus mycelia extract meshima have been utilized as anticancer drugs.