Piperlongumine is primarily studied for its anticancer properties. It selectively kills cancer cells by increasing reactive oxygen species (ROS) levels within tumor cells, leading to apoptosis. This compound shows activity against a range of cancers including breast, prostate, lung, and colon cancers. It also enhances the effectiveness of conventional chemotherapy drugs and may help overcome drug resistance. In addition to its anticancer effects, piperlongumine exhibits anti-inflammatory and antioxidant activities. It has been investigated for use in managing chronic inflammatory conditions and neurodegenerative diseases due to its ability to modulate key signaling pathways such as NF-κB and MAPK. Recent research explores its potential in metabolic disorders, where it may improve insulin sensitivity and reduce obesity-related inflammation. Its ability to cross the blood-brain barrier makes it a candidate for treating central nervous system disorders. Most applications remain in preclinical stages, but piperlongumine is a promising lead compound for developing new therapeutic agents.