The higher fungi are a rich source of chemical compounds with multi-directional therapeutic and pro-health effects. This review summarizes the results of the most important chemical and biological studies of the fruiting bodies and the mycelial cultures of Laetiporus sulphureus. Numerous studies have demonstrated the antimicrobial, anticancer, cytotoxic, hypoglycemic anti-inflammatory and antioxidant activity of the extracts. Currently, only a few wood-decay fungi have practical use in medicine. Therefore it seems important to continue research on the effectiveness and safety of extracts and compounds of natural origin, including fungi, whose potential is not still used.