Hypericum perforatum is known as St. John's Wort. H. perforatum extracts and essential oil are important in drug development with numerous pharmacological activities around the world, including Iran. For a long time, H. perforatum has been used in traditional medicines for healing skin wounds, eczema, burns, diseases of the alimentary tract, and psychological disorders especially depression. H. perforatum has recently been shown to have antioxidant, anticonvulsant, analgesic, anti-inflammatory, cytotoxic and antidiabetic activities. Hypericin, pseudohypericin, hyperoside, rutin, quercetin and hyperforin are the main compounds which are reported in this plant. a-Pinene, caryophyllene, caryophyllene oxide, germacrene D and 2-methyloctane were identified as the major constituents for H. perforatum essential oil collected from different parts of the world. Due to the easy collection of the plant, its widespread and also remarkable biological activities, this plant has become a medicine worldwide. This review presents comprehensive analyzed information on the botanical, chemical and pharmacological aspects of H. perforatum at preclinical and clinical levels.