Dehydrocostus lactone (DHL) is a sesquiterpene lactone originally found in species of Saussurea lappa C.B. Clarke (Compositae). DHL exhibits antibiotic, antioxidative, anti-angiogenic, anticancer chemotherapeutic, and chemopreventive activities. DHL inhibited cancer cell lines throughout PI3K/Akt Signaling Pathway, through inhibiting Wnt/β-catenin pathway. One of the latest investigation showed, that DHL inhibited the activity of cytosolic thioredoxin reductase (TrxR1) in HeLa cells, which elicited an accumulation of reactive oxygen species (ROS) in cells and a collapse of the intracellular redox equilibrium and eventually induced apoptosis of HeLa cells.