| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1022 | |
| Phytochemical name or plant extracts | Formononetin | |
| PMID | 29277346 | |
| Literature evidence | Considering specific foods, an increased the risk of developing breast cancer was seen with a moderate intake of formononetin, but no significant associations were found between breast cancer risk and other isoflavone-rich diets. | |
| IUPAC name | 7-hydroxy-3-(4-methoxyphenyl)chromen-4-one | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Astragalus membranaceus | |
| Geographical availability | Altay, Amur, Buryatiya, China North-Central, China South-Central, Chita, Inner Mongolia, Irkutsk, Kazakhstan, Khabarovsk, Krasnoyarsk, Manchuria, Mongolia, Primorye, Qinghai, Sakhalin, Tibet, Tuva, West Siberia, Xinjiang, Yakutskiya | |
| Plant parts | Root | |
| Other cancers | Breast cancer, Colorectal cancer | |
| Target gene or protein | hTERT,c-MYC,Bcl-2, Ha-ras, QR, C3, COX7RP, SULT1A3, ERα, miR-375, AKT, Bcl-2, MMP2, MMP9, TIMP-1, TIMP-2, TNF-α, IL-6 and IL-1β, nitrite, PGE2, iNOS, COX-2 | |
| Gene or Protein evidence | SULT1A3 was of great significance in determining sulfonation of formononetin, A collection of primary estrogen receptor (ER)-regulated genes by estradiol (E2), including hTERT, c-MYC, BCL2 and Ha-ras (oncogenic) and quinone reductase (QR), human complement 3 (C3) and COX7RP (non-oncogenic) were selected as marker genes for a MCF-7 cell-based endogenous gene expression assay. After treatment with formononetin, ERα, miR-375, p-Akt, and Bcl-2 expression was significantly upregulated. Collectively, these results suggest that formononetin inhibited breast cancer cell migration and invasion by reducing the expression of MMP-2 and MMP-9 through the PI3K/AKT signaling pathway. In vitro, formononetin reduced the expression of matrix metalloproteinase-2 (MMP-2), MMP-9 and increased the expression of tissue inhibitor of metalloproteinase-1 (TIMP-1) and TIMP-2. Results showed that formononetin significantly reduced the production of TNF-α, IL-6 and IL-1β, nitrite and PGE2, as well as protein levels of iNOS and COX-2. | |
| Target pathways | ERK1/2 signaling pathway Nrf2-mediated signaling pathway PI3K/AKT signaling pathway PI3K/AKT/mTOR signaling pathway ERK1/2 MAPK-Bax pathway Extracellular signal-regulated kinase1/2 (ERK1/2) mitogen-activated protein kinase (MAPK) signaling pathway Insulin-like growth factor 1(IGF1)/IGF1R-phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) pathway Ras-p38MAPK pathway | |
| IC50 | NA | |
| Potency | These findings demonstrate a potentially new therapeutic strategy of formononetin as anti-invasive agent for breast cancer. | |
| Cell line/ mice model | MCF-7, MDA-MB-231, 4T1, ER-positive MCF-7, T47D, Caco-2, SKBR-3, HUVEC, LNCaP, PC-3 | |
| Additional information | Exhibits the anti-estrogenic effects on E2-induced transcriptions of marker genes including hTERT, c-MYC, BCL2 and Ha-ras (oncogenic) and quinone reductase (QR), human complement 3 (C3) and COX7RP (non-oncogenic) Modulates ERβ and increases luciferase activity in MCF7 breast cancer cells with limited proliferative effect Enhances the antiproliferative effects of epirubicin in MDA-MB-231 cell line Enhances the effect of epirubicin in multidrug resistance protein (MRP)-expressing human breast cancer cell line MDA-MB-231 | |
| PubChem ID | 5280378 | |
| Additional PMIDs | 15069695 15876415 19928832 22828872 29913427 9704568 22328166 24488720 9631496 16773531 24056502 28105248 29523109 33424409 19847742 24508860 24067281 23286459 29277346 23982890 26059153 21943063 24977660 25613180 25663261 30243825 33510641 15796199 30551465 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:478611-1 | |
| Safety | MTT assay and MAP2 immunoreactivity experiments showed that formononetin produced significant neuroprotective activity by preventing BV2 microglia conditioned media-induced toxicity to HT22 neurons. |