| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-301 | |
| Phytochemical name or plant extracts | Rottlerin | |
| PMID | 24359639 | |
| Literature evidence | Although, autophagy inhibitors suppress the formation of cytoplasmic vacuolization and autophagy in breast CSCs, the potency of Rott to induce autophagy and apoptosis might be based on its capability to activate several pathways such as AMPK and proteasome inhibition. | |
| IUPAC name | (E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethylchromen-8-yl]-3-phenylprop-2-en-1-one | |
| Phytochemicals’ class or type of plant extracts | Chromenol | |
| Source of phytochemicals or plant Extracts | Mallotus philippinensis | |
| Geographical availability | Andaman Is., Assam, Bangladesh, Bismarck Archipelago, Borneo, Cambodia, China South-Central, China Southeast, East Himalaya, Hainan, India, Jawa, Laos, Lesser Sunda Is., Malaya, Maluku, Myanmar, Nansei-shoto, Nepal, New Guinea, New South Wales, Nicobar Is., Northern Territory, Pakistan, Philippines, Queensland, Solomon Is., Sri Lanka, Sulawesi, Sumatera, Taiwan, Thailand, Tibet, Vietnam, West Himalaya | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Prostate cancer | |
| Target gene or protein | Atg12, Beclin-1, Bcl-2, Bcl-xL, XIAP, cIAP-1, LRP6 | |
| Gene or Protein evidence | The levels of Atg12 and Beclin-1 expression were increased in a dose dependent manner following treatment with Rott. The cellular levels of Bcl-2, Bcl-xL, XIAP and cIAP-1 proteins were significantly decreased after the treatments with Rott for 48 h. Furthermore, the inhibitory effects of rottlerin on LRP6 expression/phosphorylation and Wnt/β-catenin signaling were confirmed in human prostate cancer PC-3 and DU145 cells and breast cancer MDA-MB-231 and T-47D cells. | |
| Target pathways | Akt/mTOR pathway AMPK pathway | |
| IC50 | NA | |
| Potency | Molecular docking results between C2-domain of protein kinase C-delta and Rott indicated that both hydrogen bonding and hydrophobic interactions contributed significantly for ligand binding with minimum binding affinity of ≈ 7.5 Kcal/mol. | |
| Cell line/ mice model | MDA-MB-231, T47D, PC-3, DU145, MCF-7 | |
| Additional information | Although, autophagy inhibitors suppress the formation of cytoplasmic vacuolization and autophagy in breast CSCs, the potency of Rott to induce autophagy and apoptosis might be based on its capability to activate several pathways such as AMPK and proteasome inhibition. | |
| PubChem ID | 5281847 | |
| Additional PMIDs | 24607787 18097625 18261747 25650742 25661734 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:351650-1 | |
| Safety | NA |