| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1137 | |
| Phytochemical name or plant extracts | Hirsutine | |
| PMID | 25672479 | |
| Literature evidence | Furthermore, hirsutine induced the DNA damage response in the MDA-MB-453 cells, but not in the MCF-7 cells, as highlighted by the upregulation of γH2AX expression. | |
| IUPAC name | methyl (E)-2-[(2S,3R,12bR)-3-ethyl-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl]-3-methoxyprop-2-enoate | |
| Phytochemicals’ class or type of plant extracts | Alkaloid | |
| Source of phytochemicals or plant Extracts | Uncaria tomentosa | |
| Geographical availability | Belize, Bolivia, Brazil North, Colombia, Costa Rica, Ecuador, French Guiana, Guatemala, Guyana, Honduras, Nicaragua, Panamá, Peru, Suriname, Trinidad-Tobago, Venezuela | |
| Plant parts | NA | |
| Other cancers | Breast cancer | |
| Target gene or protein | γH2AX, Caspase 3, Caspase 7 | |
| Gene or Protein evidence | Furthermore, hirsutine induced the DNA damage response in the MDA-MB-453 cells, but not in the MCF-7 cells, as highlighted by the upregulation of γH2AX expression. Such induction of apoptosis by hirsutine was related to the activation of caspases, as noted in the elevated caspase-3/7 activity in the MDA-MB-453 cells, but not in the MCF-7 cells, 3 h after treatment with hirsutine | |
| Target pathways | HER2, NF-κB and Akt pathways p38 MAPK pathway | |
| IC50 | NA | |
| Potency | Considering that there was no difference between MDA-MB-453 and MCF-7 cells in regards to irinotecan‑induced DNA damage response, our present results indicate the selective anticancer activity of hirsutine in HER2-positive breast cancer by inducing a DNA damage response. | |
| Cell line/ mice model | MCF-7, MDA-MB-231, MDA-MB-468, MDA-MB-453, ZR-75-1, BT-474 | |
| Additional information | Among six distinct human breast cancer cell lines, hirsutine showed strong cytotoxicity against HER2-positive/p53-mutated MDA-MB‑453 and BT474 cell lines. Conversely, HER2-negative/p53 wild‑type MCF-7 and ZR-75-1 cell lines showed resistance against hirsutine-induced cytotoxicity. Hirsutine induced apoptotic cell death in the MDA-MB-453 cells, but not in the MCF-7 cells, through activation of caspases. | |
| PubChem ID | 3037884 | |
| Additional PMIDs | NA | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:768322-1 | |
| Safety | NA |