Frontiers in Pharmacology · 4 authors, 3 centres
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This narrative review summarizes preclinical *in vitro* and *in vivo* evidence that scopoletin, a plant-derived coumarin, demonstrates a broad range of pharmacological activities including anticancer, anti-inflammatory, and neuroprotective effects. The central finding is that while scopoletin shows promise as a lead compound for drug development, its poor aqueous solubility and low oral bioavailability are significant limitations requiring future research to address.
This narrative review synthesizes preclinical research on the plant-derived coumarin scopoletin. The authors report that *in vitro* and *in vivo* experimental studies demonstrate scopoletin has antimicrobial, anticancer, anti-inflammatory, anti-angiogenic, antioxidant, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties, as well as immunomodulatory effects. It is also noted as an inhibitor of enzymes like acetylcholinesterase. However, pharmacokinetic studies indicate scopoletin has low bioavailability due to poor aqueous solubility, rapid absorption, and extensive metabolism. Toxicity research suggests it is non-toxic to most cell types tested. The review concludes that scopoletin is a suitable lead compound for developing new derivatives to treat conditions like cancer and neurodegenerative disease. Key limitations noted are the preclinical nature of all evidence and the need for future studies to improve bioavailability and verify safety in humans.
