| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-628 | |
| Phytochemical name or plant extracts | 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (ON-III) | |
| PMID | 19242112 | |
| Literature evidence | These results suggest that ON-III is a potential novel anti-cancer agent for erbB-2-overexpressing cancer. | |
| IUPAC name | (E)-1-(2,4-dihydroxy-6-methoxy-3,5-dimethylphenyl)-3-phenylprop-2-en-1-one | |
| Phytochemicals’ class or type of plant extracts | Chalcone | |
| Source of phytochemicals or plant Extracts | Eugenia aquea | |
| Geographical availability | Borneo, Jawa, Lesser Sunda Is., Malaya, Maluku, New Guinea, Queensland, Sulawesi, Sumatera | |
| Plant parts | Leaves | |
| Other cancers | Breast cancer, Lung cancer | |
| Target gene or protein | Bim, erbB-2, MAPK, AKT, PARP, Caspase 3, KDR | |
| Gene or Protein evidence | Also, ON-III upregulated the expression of proapoptotic BH3-only Bcl-2 family member Bim. Bim siRNA could inhibit ON-III-mediated apoptosis in MDA-MB-453 cells. It concludes that ON-III inhibits erbB-2 tyrosine kinase phosphorylation, shuts down its downstream pathway and triggered apoptosis via induction of Bim. In this study, we reported that ON-III repressed tyrosine phosphorylation of erbB-2 without reduced erbB-2 receptor expression in MDA-MB-453 cells. Activation of mitogen-activated protein kinase (MAPK) and AKT, downstream molecules of erbB-2-mediated signal transduction pathway, was inhibited following exposure to ON-III. ON-III induced apoptosis in breast cancer cells as determined by caspase-3 and PARP cleavage. Our previous study showed that ON-III (2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone) extracted from Traditional Chinese Medicine Cleistocaly xoperculatus dry flower could inhibit KDR tyrosine kinase phosphorylation and tumor growth in vivo. | |
| Target pathways | erbB-2 tyrosine kinase receptor signal pathway | |
| IC50 | 24.5 μg/ml against MDA-MB-453 | |
| Potency | These results suggest that ON-III is a potential novel anti-cancer agent for erbB-2-overexpressing cancer. | |
| Cell line/ mice model | MDA-MB-453, A549 | |
| Additional information | The results revealed that ChalcEA inhibited proliferation of the A549 lung cancer cell lines in a time- and dose-dependent manner with IC50 values of 25.36 and 19.60 µM for 24 and 48 h treatments, respectively. Western blot analysis indicated that ChalcEA exerted its anti-proliferative effects by promoting apoptosis via the activation of caspase-9 and caspase-3. Based on in silico results, ChalcEA with the binding energy of -6.53 kcal/mol could compete better than 4-methyl benzenesulfonamide (-6.43 kcal/mol) as an inhibitor of caspase-3 (PDB: 2XYG). ChalcEA has potential since it has three hydrophobic features. These results provided a basis for further study of ChalcEA as an active compound for anticancer therapeutics. | |
| PubChem ID | 10424762 | |
| Additional PMIDs | 32269629 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:593631-1 | |
| Safety | NA |