Osthole is an O-methylated coumarin that inhibits Ca2+ channels. It exhibits anticancer, antioxidative, anti-inflammatory, and cardioprotective activities. In glioblastoma cells, osthole inhibits IGF-1-induced epithelial-to-mesenchymal transition (EMT), decreases phosphorylation of Akt and GSK-3β, inhibiting cell migration. Osthole also exhibits anti-metastatic potential in lung cancer cells, inhibiting migration and invasion by decreasing expression of matrix metalloproteinases 2 and 9 (MMP2/9). In animal models of ischemia/reperfusion, osthole decreases levels of ROS, malondialdehyde, IL-6, TNF-α, and myeloperoxidase, increases activity of superoxide dismutase, and improves lung injury pathology. Osthole also inhibits lung inflammation induced by administration of carrageenan in vivo. In animal models of cardiac ischemia/reperfusion, this compound inhibits lipid peroxidation and decreases expression of HMGB1 and NF-κB.