Hypericum ascyron L. (H. ascyron) is a significant medicinal plant traditionally used for various conditions like hematemesis, hemoptysis, injuries from falls, irregular menses, dysmenorrhea, and liver fire-induced headaches. A comprehensive literature search was conducted using databases like SciFinder and Web of Science to explore its traditional uses, geographical distribution, botanical description, phytochemistry, and pharmacology. The objective of this review is to lay groundwork and suggest fresh avenues of investigation into the possible uses of the plant. Currently, two hundred and seventy compounds have been isolated and identified from H. ascyron, including phloroglucinols, xanthones, flavonoids, phenolics, steroids and triterpenoids, volatile components, and other compounds. Notably, phloroglucinols, xanthones, and flavonoids have exhibited remarkable pharmacological effects like antioxidant, antidiabetic, anti-inflammatory, antidepressant, cytotoxic, and antimicrobial activities. Despite extensive research, further studies are needed to understand new components and mechanisms of action, requiring more detailed investigations. This thorough exploration could facilitate the advancement and utilization of H. ascyron.