| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1309 | |
| Phytochemical name or plant extracts | Baicalein | |
| PMID | 26578185 | |
| Literature evidence | Most free flavones (26-28 and 30) showed significant cytotoxic activities at 10 μM (up to 61.2% inhibition rate). | |
| IUPAC name | (2S,3S,4S,5R,6S)-6-(5,6-dihydroxy-4-oxo-2-phenylchromen-7-yl)oxy-3,4,5-trihydroxyoxane-2-carboxylic acid | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Scutelleria baicalensis | |
| Geographical availability | Amur, Buryatiya, China North-Central, China South-Central, Chita, Inner Mongolia, Irkutsk, Khabarovsk, Korea, Manchuria, Mongolia, Primorye, Vietnam, Yakutskiya | |
| Plant parts | Root | |
| Other cancers | Breast cancer, Colon cancer, Liver cancer | |
| Target gene or protein | PTEN, STAT-3, CYP1A1 , CDKN1A, CXCL9, CXCL10, FKBP5, ZBTB4, GILZ, EMT | |
| Gene or Protein evidence | Baicalein, propofol, and curcumin can induce PTEN upregulation by affecting miRNAs in suppressing breast and lung cancer progression, PAX8-AS1-N bound to miR-17-5p, and up-regulated miR-17-5p targets, such as PTEN, CDKN1A, and ZBTB4, baicalein as an attractive phytochemical compound for reducing metastatic potential of breast cancer cells by regulating STAT3 activity, the expression of pro-inflammatory factors associated with M1 macrophages, including TNF-α, IL-1β, CXCL9 and CXCL10, were increased after baicalein treatment, baicalein was a GR agonist via an HRE/Luc assay and induced GR target genes, FKBP5 and GILZ. Taken together, these results suggest that baicalin and baicalein of Scutellaria baicalensis Georgi may suppress the EMT of breast epithelial cells and the tumorigenic activity of breast cancer cells. | |
| Target pathways | Inhibits E2-induced migration, adhesion and invasion through interfering with GPR30 signaling pathway activation Down-regulates the expression of MMP-2/9 involved mitogen-activated protein kinases (MAPK) signaling pathway (MDA-MB-231) Triggers the mitochondrial-dependent apoptotic pathway by enhancing the level of intracellular ROS, disrupting the mitochondrial membrane potential, downregulating anti-apoptotic protein Bcl-2, upregulating pro-apoptotic protein Bax, releasingcytochrome C and activating caspase-9 and caspase-3 in MCF-7 cells. Potentiates the M1 macrophage polarization via the NF-kappaB/TNF-? signaling pathway - induces the production of TNF-? and the activation of NF-kappaB | |
| IC50 | 68.3 µM against MCF-7 | |
| Potency | This study demonstrated that free flavones showed potent anti-influenza, anti-cancer and anti-oxidative activities. | |
| Cell line/ mice model | HT-29, Caco-2, HepG2, SW480, MCF-7, MDA-MB-231, MCF10A., SKBR-3, MDA-MB-468 , MMTV-PyMT | |
| Additional information | Induces apoptosis in HT-29 and Caco-2 cells Reduces the TGF-?1-mediated EMT, anchorage-independent growth and cell migration of MDA-MB-231 cells, reduces Slug via the NF-?B pathway in MCF10A cells Strongly suppresses STAT3 activity, the production of interleukin (IL)-6 and the metastatic potential of breast cancer cells both in vitro and in vivo Mediate the cell-cycle arrest principally in G0/G1-phase (MCF-7) Prevents upregulation of CYR61 and CTGF mRNA levels induced by G1, a specific GPR 30 agonist, Suppresses the expression of GPR30 target genes, cysteine-rich 61 (CYR61) and connective tissue growth factor (CTGF) induced by E2 and causes a decrease in tyrosine phosphorylation of epidermal growth factor receptor (EGFR) as well as phosphorylation of extracellular signal-regulated kinase (ERK) and serine/threonine kinase Akt Inhibits the expression and secretion of matrix metalloproteinases 2/9 (MMP-2/9) in MDA-MB-231 cells Has PR antagonist and GR agonist activity in vitro and demonstrates GR agonist activity in the uterus in vivo Activates PAX8-AS1-N which in turn up-regulates miR-17-5p targets, such as PTEN, CDKN1A, and ZBTB4 Inhibits FN-induced EMT by inhibiting calpain-2 - reduces the expression of FN, calpain-2, and vimentin, but increased E-cadherin expression Supresses FN-induced downregulation of the epithelial markers E-cadherin and ZO-1 and upregulation of the mesenchymal markers N-cadherin, vimentin, and Snail (MCF-10A) Prevents the E2-induced ERa-mediated activation of nuclear transcriptional signaling, thereby decreasing the mRNA levels of ERa target genes, Inhibits E2-induced GPR30-mediated signal transduction, as well as the transcription of GPR30-regulated genes Inhibits HIF stabilization and also reduces its transcription activity, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells | |
| PubChem ID | 64982 | |
| Additional PMIDs | 25686495 33268707 25130856 25672442 20580866 31849483 33670518 29693272 14644660 34512367 19666078 32146686 31000696 28060756 34195430 26756423 28789417 30306879 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:458155-1 | |
| Safety | Further analysis revealed that baicalin and baicalein, the major flavones of these butanol extracts, inhibited TGF-β1-mediated EMT by reducing the expression level of the EMT-related transcription factor, Slug via the NF-κB pathway, and subsequently increased migration in MCF10A cells. |