Scopoletin is a coumarin compound found in various medicinal and edible plants, known for its diverse pharmacological activities. This review summarizes its pharmacology, pharmacokinetics, and toxicity. Scopoletin exhibits antimicrobial, anticancer, anti-inflammatory, anti-angiogenic, antioxidant, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties. It also acts as an inhibitor of enzymes such as choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies show that scopoletin has low bioavailability, rapid absorption, and extensive metabolism, which may be related to its poor solubility in aqueous media. Toxicity studies indicate that scopoletin is non-toxic to most cell types tested, suggesting it does not cause treatment-associated mortality or abnormal performance at the test dose. Scopoletin has potential as a drug candidate for treating cancer, liver disease, diabetes, neurodegenerative diseases, and mental disorders. It is a suitable lead compound for developing new, efficient, and low-toxicity derivatives. Further studies are needed to explore its molecular mechanisms, verify its toxicity, and improve its oral bioavailability. Scopoletin is found in various plant sources, including medicinal and edible plants, and has been analyzed in several species. It has shown anti-microbial, anti-bacterial, anti-parasitic, anti-viral, anti-cancer, anti-inflammatory, and other activities. Scopoletin also has effects on liver diseases, the cardiovascular system, diabetes, neurodegenerative disorders, and mental disorders. It has anti-oxidant, anti-gout, anti-allergic, anti-vitiligo, anti-aging, immunomodulatory, anti-nociceptive, anti-spinal cord injury, and other properties. Pharmacokinetic studies show that scopoletin is absorbed, metabolized, and excreted in the body, with low bioavailability and extensive metabolism. Scopoletin is a promising compound with potential therapeutic applications in various diseases.Scopoletin is a coumarin compound found in various medicinal and edible plants, known for its diverse pharmacological activities. This review summarizes its pharmacology, pharmacokinetics, and toxicity. Scopoletin exhibits antimicrobial, anticancer, anti-inflammatory, anti-angiogenic, antioxidant, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties. It also acts as an inhibitor of enzymes such as choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies show that scopoletin has low bioavailability, rapid absorption, and extensive metabolism, which may be related to its poor solubility in aqueous media. Toxicity studies indicate that scopoletin is non-toxic to most cell types tested, suggesting it does not cause treatment-associated mortality or abnormal performance at the test dose. Scopoletin has potential as a drug candidate for treating cancer, liver disease, diabetes, neurodegenerative diseases, and mental disorders. It is a suitable lead compound for developing new, efficient, and low-toxicity derivatives. Further studies are needed to explore its molecular mechanisms, verify its toxicity, and improve its oral bioavailability. Scopoletin is found in various plant sources, including medicinal and edible plants, and has been analyzed in several species. It has shown anti-microbial, anti-bacterial, anti-parasitic, anti-viral, anti-cancer, anti-inflammatory, and other activities. Scopoletin also has effects on liver diseases, the cardiovascular system, diabetes, neurodegenerative disorders, and mental disorders. It has anti-oxidant, anti-gout, anti-allergic, anti-vitiligo, anti-aging, immunomodulatory, anti-nociceptive, anti-spinal cord injury, and other properties. Pharmacokinetic studies show that scopoletin is absorbed, metabolized, and excreted in the body, with low bioavailability and extensive metabolism. Scopoletin is a promising compound with potential therapeutic applications in various diseases.