Piplartine (
piperlongumine, 5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1H)-pyridinone) is a biologically active
alkaloid/
amide from peppers, as from long pepper (Piper longum L. - Piperaceae). Long pepper is one of the most widely used in
Ayurvedic medicine, which is used to treat many diseases, including
tumors. The purpose of the current paper is to address to the chemical structure establishment and to systematically survey the published articles and highlight recent advances in the knowledge of the therapeutic potential of
piplartine, establishing new goals for future research. The reported pharmacological activities of
piplartine include cytotoxic, genotoxic, antitumor, antiangiogenic, antimetastatic, antiplatelet aggregation, antinociceptive,
anxiolytic,
antidepressant, anti-atherosclerotic,
antidiabetic, antibacterial, antifungal, leishmanicidal, trypanocidal, and schistosomicidal activities. Among the multiple pharmacological effects of
piplartine, its anticancer property is the most promising. Therefore, the preclinical anticancer potential of
piplartine has been extensively investigated, which recently resulted in one patent. This compound is selectively cytotoxic against
cancer cells by induction of oxidative stress, induces genotoxicity, as an alternative strategy to killing
tumor cells, has excellent oral bioavailability in mice, inhibits
tumor growth in mice, and presents only weak systemic toxicity. In summary, we conclude that
piplartine is effective for use in
cancer therapy and its safety using chronic toxicological studies should be addressed to support the viability of clinical trials.