From ancient times medicine and natural products have been closely linked through the use of traditional medicines and natural toxins. Macrofungi have an established history of use especially in traditional oriental medicine. Nowadays, mushrooms comprise a vast and yet largely untapped source of powerful new pharmaceutical products. In particular, and most importantly for modern medicine, they are an unlimited source of compounds that exhibit multidirectional activity: antioxidant, immuno-enhancing, immunostimulatory, antibacterial, antiviral, anti- inflammatory, antidiabetic, antiallergenic and anticarcinogenic [1, 2, 5-8]. In the presented work, a substances with biological activity from mainly Basidiomycota were reviewed, including low-molecular-weight (terpenoids, polyphenols steroids, quinones, amines, cerebrosides) (Tab.1) and high-molecular- weight compounds (homo and heteroglucans, glycans, glycoproteins, glycopeptides, peptides, proteins) (Tab. 2). Selected species of toxic and hallucinogenic mushrooms were also included in the review. At present, mushrooms are considered to be functional food. Beneficial health effects may be achieved through the direct consumption of fruiting bodies or the use of dietary supplements in the form of ready-to-use preparations containing mushroom extracts. The last years is also a period of a flourishing new field of medicine - mycopharmacology. The scientific approach to compounds contained in mushrooms allowed the isolation and identification of many valuable active substances which are used in the prevention and treatment of lifestyle diseases.
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