Nature has always proved to be a significant reservoir of bioactive scaffolds which have been used for the
discovery of drugs since times. Medicinal plants continue to be a solid niche for biologically active and therapeutically
effective chemical entities, opening up new avenues for the successful treatment of several human diseases. Contribution of
plant-derived compounds either in their original or semi-synthetic derivative forms extends far back in time in drug
discovery. This review aims to focus on the sources, biological, and pharmacological profile of a pharmacologically active
plant-derived coumarin, osthole, which is an important component of numerous remedial plants such as Cnidium monnieri.
Several studies have revealed that osthole possess pharmacological properties such as anticancer, antioxidant, antihyperglycemic, neuroprotective, and antiplatelet. Osthole has been reported to regulate various signaling pathways which
in turn modulate several apoptosis related proteins, cell cycle regulators, protein kinases, transcriptional factors, cytokines,
and growth receptors affiliated with inflammation, proliferation and several other ailments. Osthole is known to halt
proliferation and metastasis of cancerous cells by arresting the cell cycle and inducing apoptosis. The data in this review
paper supports the pharmacological potential of osthole but further experimentation, biosafety profiling and synergistic
effects of this compound need to be focused by the researchers to understand the full spectrum of pharmacological potential
of this therapeutically potent compound.