| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-689 | |
| Phytochemical name or plant extracts | Piperlongumine | |
| PMID | 25813625 | |
| Literature evidence | However, knockdown of HO-1 expression and pharmacological inhibition of its activity abolished the ability of piperlongumine to induce apoptosis in MCF-7 cells, whereas those promoted apoptosis in MCF-10A cells, indicating that HO-1 has anti-tumor functions in cancer cells but cytoprotective functions in normal cells. | |
| IUPAC name | 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one | |
| Phytochemicals’ class or type of plant extracts | Alkaloid | |
| Source of phytochemicals or plant Extracts | Piper longum | |
| Geographical availability | Assam, Bangladesh, Cambodia, China South-Central, East Himalaya, Laos, Myanmar, Nicobar Is., Thailand, Vietnam | |
| Plant parts | Fruits | |
| Other cancers | Breast cancer, Lung cancer, Kidney cancer | |
| Target gene or protein | SETDB1, EGFR, STAT-3, ZBTB4, Sp1, Sp3, Sp4, Cyclin D1, Survivin, cMyc, EGFR | |
| Gene or Protein evidence | 1) PL downregulates SETDB1 expression, and decreased SETDB1 expression enhanced caspase 9 dependent-PARP cleavage during PL-induced cell death. 2)Piperlongumine also downregulated expression of Sp1, Sp3, Sp4, and several pro-oncogenic Sp-regulated genes, including cyclin D1, survivin, cMyc, EGFR and hepatocyte growth factor receptor (cMet), and these responses were also attenuated after cotreatment with glutathione. 3) Drug-repositioning screening identified piperlongumine as a direct STAT3 inhibitor with potent activity against breast cancer. 4)Mechanistic studies in Panc1 cells showed that piperlongumine-induced ROS decreased expression of cMyc via an epigenetic pathway, and this resulted in downregulation of cMyc-regulated miRNAs miR-27a, miR-20a, and miR-17 and induction of the transcriptional repressors ZBTB10 and ZBTB4. | |
| Target pathways | Mechanistic studies in Panc1 cells showed that piperlongumine-induced ROS decreased expression of cMyc via an epigenetic pathway, and this resulted in downregulation of cMyc-regulated miRNAs miR-27a, miR-20a, and miR-17 and induction of the transcriptional repressors ZBTB10 and ZBTB4. | |
| IC50 | NA | |
| Potency | Thus, PL represents a promising new agent for rapid entry into the clinic for use in treating breast cancer, as well as other cancers in which Stat3 has a role. | |
| Cell line/ mice model | A549, 786-O, SKBR-3, Female athymic nu/nu mice | |
| Additional information | Piperlongumine, an alkaloid causes inhibition of PI3Â K/Akt/mTOR signaling axis to induce caspase-dependent apoptosis in human triple-negative breast cancer cells. | |
| PubChem ID | 637858 | |
| Additional PMIDs | 31735020 28673967 24681959 25984950 24729100 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:682031-1 | |
| Safety | NA |