| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1494 | |
| Phytochemical name or plant extracts | Ellipticine | |
| PMID | 15078993 | |
| Literature evidence | Furthermore, 6-PA-ELL was found to induce splicing of the mRNA encoding the XBP1 transcription factor, characteristic of endoplasmic reticulum stress, and to induce activation of the endoplasmic reticulum-specific caspase-12 in mouse colon cancer cells. | |
| IUPAC name | 5,11-dimethyl-6H-pyrido[4,3-b]carbazole | |
| Phytochemicals’ class or type of plant extracts | Alkaloid | |
| Source of phytochemicals or plant Extracts | Berrywood tree, Asparagus cochinchinensis | |
| Geographical availability | Asparagus cochinchinensis - Cambodia, China North-Central, China South-Central, China Southeast, Hainan, Japan, Korea, Laos, Nansei-shoto, Philippines, Taiwan, Tibet, Vietnam | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Ovarian cancer | |
| Target gene or protein | ALDH1A1, Bax, Bcl-2, XIAP, cyt-c, Caspase 3, Caspase 9, p53, KIP1/p27 | |
| Gene or Protein evidence | At 3 mM concentration, ellipticine decreased the expression of ALDH1A1-positive BCSCs by 62% (p = 0.073) in the MCF7 cell line and by 53% (p = 0.024) in the SUM159 cell line compared to vehicle-treated cultures. Ellipticine increased the expression of Bax, but decreased the level of Bcl-2, Bcl-XL and X-linked inhibitor of apoptosis protein (XIAP), and subsequently triggered the mitochondrial apoptotic pathway (release of cytochrome c, and activation of caspase-9 and -3). Taken together, we have concluded that the molecular mechanisms during ellipticine-mediated growth inhibition and induction of apoptosis in MCF-7 cells were due to (1) cell cycle arrest and induction of apoptosis, (2) induction of p53 and KIP1/p27 expression, (3) triggering of Fas/Fas ligand pathway, (4) disruption of mitochondrial function, and (5) the apoptotic signaling was amplified by cross-talk between Fas death receptor and mitochondrial apoptotic pathway. | |
| Target pathways | Mitochondrial apoptotic pathway Fas/Fas ligand pathway | |
| IC50 | 1.25 ± 0.13 µM against MCF-7 | |
| Potency | The alkyloid compound ellipticine derived from the berrywood tree is a topoisomerase II poison that is used in ovarian and breast cancer treatment. | |
| Cell line/ mice model | MCF-7, MDA-MB-231/ HCT116 xenograft mouse tumor | |
| Additional information | In addition, ellipticine also induced apoptosis in MDA-MB-231 cells, as determined by using both DNA fragmentation and Annexin-V staining assay. In addition, pre-treatment of cells with caspase-9 inhibitor inhibited ellipticine-induced cell proliferation and apoptosis, indicating that caspase-9 activation was involved in MDA-MB-231 cell apoptosis induced by ellipticine. The fluorescence spectrum of ellipticine bound to mitochondria was insensitive to valinomycin, whereas it was markedly shifted toward the protonated form after carbonyl cyanide p-trifluoromethoxy-phenylhydrazone or nigericin addition. | |
| PubChem ID | 3213 | |
| Additional PMIDs | 15078993 23982874 23697684 16027529 15896464 2265453 16508181 21118972 20576524 24147360 8298010 26124567 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:531041-1 | |
| Safety | NA |