Termitomyces is a genus of edible mushrooms commonly consumed in Africa and Asia among the mushrooms collected from the wild. Termitomyces mushrooms grow as symbionts in the termite nests, where they produce various enzymes to help termites digest lignocellulosic substrates. Many species of Termitomyces are used by different ethnic groups with ethnomedicinal knowledge. Bioactive components that Termitomyces mushrooms contain have potential uses as antioxidants, immunomodulators, antitumors, and antimicrobials. Termitomyces also has a potential for treating neurodegenerative disorders. Here, we review the bioactive compounds from Termitomyces species that have been isolated and assayed in vitro and/or in vivo for their medicinal properties.