Medicinal properties of mushrooms are known in many regions of the world since ancient times. The results of actually professional studies proved in fruiting bodies of mushrooms the presence of bioiologically active metabolites. This studies are main connected with species of mushrooms from Basidiomycota taxon (earlier Basidiomycetes), often species of popular edible mushrooms, too. The article presents review of the main groups biologically active compounds in fuitbodies of mushrooms: proteins, free aminoacids, biogenic amins, carbohydrates, indole compounds, fatty acids, sterols, sphingolipids, terpenoids, benzoquinons, statins, vitamins, enzymes. The review pays attention to the numerous bioelements, too. The article underlines the significance of mushrooms metabolites in the therapy such serious diseases as: cardiovascular diseases, hypercholesterolemia, cancer, diabetes and obesity. Some of metabolites posses other medicinal properties – namely: antiviral, antibacterial and antiparasitic activity, too.