From ancient times onward, mushrooms have been an indispensable component for both culinary and medicinal purposes. Finding such substances that might alter the human body’s immune systems is the focus of current research on mushrooms with improved therapeutic qualities. Over the course of the last decade, the medicinal properties of mushrooms have garnered considerable attention from the scientific community in the West. Research has demonstrated that mushrooms have anticancer, antiproliferative, antioxidant, immunomodulatory, and antidiabetic characteristics. One of the key elements that make up the mushroom’s cell walls is β-glucans, which are among the other polysaccharides that are vital to the organisms biological functions. Xerocomus, Lactarius, Albatrellus, Flammulina, Suillus, Inonotus, Inocybe, Funlia, Russula, Pleurotus, Cordyceps, Agaricus, Ganoderma, Clitocybe, Antrodia, Trametes, Ganoderma, and Fomes are the genera of mushrooms that have been linked to effective therapies against cancer. Similar to how Inonotus obliquus fruiting bodies have been used in eastern European folk medicine since the sixteenth century, Piptoporus betulinus was used in traditional Czech Republican medicine to treat colorectal cancer. Mitotic kinase inhibitor, antimitotic, reactive oxygen species inducer, angiogenesis inhibitor, and topoisomerase inhibitor are important roles played by anticancer drugs. These actions finally cause apoptosis and stop the spread of cancer. Given the growing interest in mycotherapy, the scientific community has to commit to expanding clinical trials and recommending safe-originated, genetically pure supplements. In the present article, a succinct report on the method used to extract the active components from mushroom that has certain medicinal uses is briefly described. We have discussed in brief several edible mushrooms that contain anti-tumorigenic substances and how they affect cancer cells in different ways.