More than 500 species of Hypericum are located throughout Europe, North America, North Africa, and Asia. These plants have a long history of employment in folk medicine as anti-inflammatory, antibacterial, and antiviral medicines, as well as for the treatment of burns, gastrointestinal problems, and depression. The most significant species of this genus are Hypericum perforatum L. and Hypericum triquetrifolium Turra because of their pharmacological activities. Hypericum perforatum L. and Hypericum triquetrifolium are widely known for their efficacy in reducing inflammation and improving wound healing. The main reason these plants have been used for treatment of mild to moderate depression. Nevertheless, some similar species are also utilized in conventional medicine and have been previously analyzed for their biological activity and phytochemical composition. The main classes of active substances are found in Hypericum species, including naphthodianthrones (such as hypericin and pseudohyperricin), phloroglucinols (such as hyperforin), flavonoids (such as rutin, hyperoside, isoquercitrin, quercitrin, and amentoflavone), and phenylpropanoids (chlorogenic acid). This review's objective is to provide a summary of the most recent research on potential medicinal uses for Hypericum perforatum L., and Hypericum triquetrifolium Turra.