Recent advances in bioactive coumarin scoparone: A comprehensive review.

Scoparone (SP) is a naturally occurring coumarin widely distributed in various medicinal plants. Owing to immunosuppressive properties, SP has long been recognized as one of the principal bioactive compounds in traditional liver-protective preparations. For the first time, this study presents a systematic review of its phytochemical investigations, structural elucidation, biosynthesis, pharmacological values, synthetic advancements, pharmacokinetics, and metabolism. SP was identified as a major compound in several medicinal species, particularly the genera Artemisia and Citrus, and its biosynthesis involves enzymatic transformations of phenylpropanoid precursors. SP induces cell death programs against the growth of tumor cells, and inhibits inflammatory mediators in anti-inflammatory action. It also exhibited antidiarrheal, anti-allergic, antimicrobial, antiviral, antileishmanial, anti-insect, antiplatelet, and vasorelaxant activities. Notably, SP exerts protective actions on multiple organs, including the liver, heart, brain, bone, lungs, pancreas, stomach, skin, hair, and penile tissues. Multiple in vitro and in vivo studies have elucidated its molecular mechanisms of action, with the Toll-like receptor 4/nuclear factor kappa B (TLR4/NF-κB) signaling pathway being the most frequently proposed. Pharmacokinetic analyses indicate that SP is rapidly distributed and eliminated in the body through demethylation, hydroxylation, glucuronidation, and conjugation with other functional groups. Further preclinical and clinical studies are encouraged to validate its pharmacological potential. In addition, synthetic modification and formulation optimization aimed at improving its bioavailability and metabolic stability will be crucial for future drug development.