| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-439 | |
| Phytochemical name or plant extracts | Isoliquiritigenin | |
| PMID | 12589938 | |
| Literature evidence | The chalcone isoliquiritigenin (ISL) is a component of licorice extract exhibiting either antitumorigenic activity or estrogen receptor (ER) alpha-dependent growth promoting effects on breast cancer cells. | |
| IUPAC name | (E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one | |
| Phytochemicals’ class or type of plant extracts | Chalcone | |
| Source of phytochemicals or plant Extracts | Glycyrrhiza glabra | |
| Geographical availability | Afghanistan, Albania, Bulgaria, Central European Rus, China North-Central, Cyprus, East Aegean Is., East European Russia, Greece, Iran, Iraq, Italy, Kazakhstan, Kirgizstan, Krym, Lebanon-Syria, Mongolia, North Caucasus, Pakistan, Palestine, Romania, Sardegna, Saudi Arabia, Sicilia, South European Russi, Tadzhikistan, Transcaucasus, Turkey, Turkmenistan, Ukraine, Uzbekistan, West Siberia, Xinjiang, Yugoslavia | |
| Plant parts | Rhizome | |
| Other cancers | Breast cancer, Cervical cancer | |
| Target gene or protein | Arg-1, HO-1, iNOS, microRNA 155, SHIP1, STAT-3, STAT6, PLA2, COX-2, CYP4A, PGE2, COX-1, FLAP, 5-LOX, LTB4, HIF-1α, VEGF, MMP2, MM9, Aromatase | |
| Gene or Protein evidence | TFGR and ISL inhibited gene and protein expression of Arg-1, up-regulated gene of HO-1 and protein expression of iNOS, enhanced the expression of microRNA 155 and its target gene SHIP1, meanwhile down-regulated the phosphorylation of STAT3 and STAT6. Furthermore, isoliquiritigenin inhibited mRNA expression of multiple forms of AA-metabolizing enzymes, including phospholipase A2 (PLA2), cyclooxygenases (COX)-2 and cytochrome P450 (CYP) 4A, and decreased secretion of their products, including prostaglandin E2 (PGE2) and 20-hydroxyeicosatetraenoic acid (20-HETE), without affecting COX-1, 5-lipoxygenase (5-LOX), 5-lipoxygenase activating protein (FLAP), and leukotriene B4 (LTB4). With regard to anticancer property, ISL was able to suppress HIF-1α level, VEGF expression and secretion, cell migration and to decrease the expression and secretion of MMP-9/-2. In this brief review, we summarize the studies on phytochemicals such as biochanin A, genistein, quercetin, isoliquiritigenin, resveratrol, and grape seed extracts related to their effect on the activation of breast cancer-associated aromatase promoters and discuss their aromatase inhibitory potential to be used as safer chemotherapeutic agents for specific hormone-dependent breast cancer. | |
| Target pathways | VEGF/VEGFR-2 signaling pathway ERK-1/2 signaling p38, PI3K/Akt and NF-κB signaling pathways Upstream signaling pathways, including the expression of phosphatidylinositol-3 kinase (PI3K), the phosphorylation of p38 and Akt kinase and NF-κB DNA binding activity, were suppressed by ISL | |
| IC50 | 22.96 to 74.92 μmol/L against MDA-MB-231 | |
| Potency | Thus, low concentration of ISL may have therapeutic potential in the treatment of aggressive breast carcinoma and other neoplasms. These findings suggest that ISL suppresses the migration of MDA-MB-231 cells by inhibiting the upstream signaling pathways. Transfection experiments reveal that ISL is able to transactivate the endogenous ER alpha in MCF7 cells and this is supported by the capability to induce down-regulation of ER alpha protein levels and up-regulation of pS2 mRNA. | |
| Cell line/ mice model | MCF-7, A-549, BGC-823, MDA-MB-231, HepG2 | |
| Additional information | NA | |
| PubChem ID | 638278 | |
| Additional PMIDs | 20033868 23425066 30417769 23327692 23874474 23861918 28615942 23747687 21693041 25365296 12589938 23401151 26651537 34963387 27609747 27097427 11911276 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:496941-1 | |
| Safety | NA |