| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-644 | |
| Phytochemical name or plant extracts | Coumestrol | |
| PMID | 23768371 | |
| Literature evidence | Coumestrol inhibited the phosphotransferase activity of CKII toward β-casein, with an IC50 of about 5 μM. | |
| IUPAC name | 3,9-dihydroxy-[1]benzofuro[3,2-c]chromen-6-one | |
| Phytochemicals’ class or type of plant extracts | Delta-lactone | |
| Source of phytochemicals or plant Extracts | Glycine max | |
| Geographical availability | Amur, China North-Central, China South-Central, China Southeast, Hainan, Inner Mongolia, Japan, Khabarovsk, Korea, Laos, Manchuria, Nansei-shoto, Primorye, Qinghai, Taiwan, Thailand, Tibet, Vietnam, Xinjiang | |
| Plant parts | Leaves | |
| Other cancers | Breast cancer, Colorectal cancer | |
| Target gene or protein | BCRP, Aromatase, ER | |
| Gene or Protein evidence | Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC(50)=63 nM). The flavonoids, coumestrol, luteolin and kaempferol also decreased aromatase enzyme activity, with Ki values of 1.3, 4.8 and 27.2 microM, respectively. A pure plant fluorescent estrogen, coumestrol, has Ka of 6 X 10(8) M-1 for the ER and is a single component as determined by HPLC. | |
| Target pathways | p53-p21(Cip1/WAF1) pathway | |
| IC50 | NA | |
| Potency | Coumestrol inhibits CKII activity and proliferation in breast cancer and colon cancer cells. The phytoestrogens genistein, daidzein, biochanin A, and coumestrol were tested and found to inhibit serum-stimulated growth in both T-47D and MCF-7 breast cancer cells at 10-100 microM. Oral administration of coumestrol did not appear to support the growth of DMBA-induced rat mammary tumors, nor did coumestrol act as an antiestrogen when administered orally in combination with 17 beta-estradiol. Coumestrol administered sc might, however, be able to support the growth of these tumors. At low concentrations, genistein and coumestrol significantly enhanced E2-induced and tyrosine kinase-mediated DNA synthesis; at high concentrations, inhibition was observed. | |
| Cell line/ mice model | MCF-7, HCT116, T47D, MDA-MB-231 | |
| Additional information | coumestrol is a novel dietary compound with potential application in preventing and improving UVB-associated skin aging. E(2) increased cell growth significantly, coumestrol increased cell growth moderately, and resveratrol and glycitein reduced cell growth. he content of ER protein in the breast cancer cells was strongly decreased by Gen, only a faint reduction could be observed following administration of Cou, whereas administration of Dai slightly increases ER protein levels. Genistein, glycitein, daidzein, equol, O-Desmethylangolensin (O-Dma) and coumestrol exerted a potent inhibitory effect on cell invasion (e.g. inhibition of 41.7+/-15% (P = 0.007) coumestrol (10 microM)). | |
| PubChem ID | 5281707 | |
| Additional PMIDs | 16506217 6685018 31881661 7892295 20043267 16118406 20460823 25531867 10523716 15971118 18647433 19167446 18424605 19800779 27010988 9679118 9681530 11509969 15105043 23768371 9343831 6766510 12477484 9770719 30612080 7440959 8049151 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:60450240-2 | |
| Safety | NA |