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St. John's wort (Hypericum perforatum) has been used as a medical herb for over 2000 years. Over the past two decades, its application as a standardized plant extract for treating depression has undergone rigorous scientific investigation, and its effectiveness has been shown in studies comparing it with other commonly used antidepressants and placebos. Safety and tolerability studies have revealed that Hypericum preparations have better safety and tolerability profiles than synthetic antidepressants. The indications for St. John's wort preparations are mild or moderate depression. The mechanism of the antidepressant action of Hypericum extract is not fully known. The view of the chemical composition and pharmaceutical a toxicological properties of biologically active substances of Hypericum perforatum is the main purpose of this paper.