| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1038 | |
| Phytochemical name or plant extracts | Luteolin | |
| PMID | 29097115 | |
| Literature evidence | The present study aimed to characterize the metabolism and further antiproliferative activity of the hydroxylated flavonoids apigenin, luteolin, scutellarein, kaempferol and quercetin in CYP1 recombinant enzymes and in the CYP1 expressing cell lines MCF7 and MDA-MB-468, respectively. | |
| IUPAC name | 2-[3,4-dihydroxyphenyl]-5,7-dihydroxy-4-chromenone | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Avicennia marina | |
| Geographical availability | Aldabra, Andaman Is., Bangladesh, Bismarck Archipelago, Borneo, Cape Provinces, China Southeast, Christmas I., Cocos (Keeling) Is., Comoros, Djibouti, Egypt, Eritrea, Gulf States, Hainan, India, Iran, Jawa, Kenya, KwaZulu-Natal, Lesser Sunda Is., Madagascar, Malaya, Maluku, Mozambique, Mozambique Channel Is., Myanmar, Nansei-shoto, New Caledonia, New Guinea, New South Wales, New Zealand North, Nicobar Is., Norfolk Is., Northern Territory, Oman, Pakistan, Philippines, Queensland, Saudi Arabia, Seychelles, Sinai, Socotra, Solomon Is., Somalia, South Australia, Sri Lanka, Sudan, Sulawesi, Sumatera, Taiwan, Tanzania, Thailand, Vanuatu, Victoria, Vietnam, Western Australia, Yemen | |
| Plant parts | Leaves | |
| Other cancers | Breast cancer, Colon cancer, Lung cancer, Liver cancer | |
| Target gene or protein | Cyclin E2, Bcl-2, Caspase 3, Bax, VEGF, YAP/TAZ, ABCG2, CD44, EMT, VEGF, MPA, Aromatase, CYP1A1, CYP1B1 | |
| Gene or Protein evidence | Luteolin sensitises drug-resistant human breast cancer cells to tamoxifen via the inhibition of cyclin E2 expression. Luteolin remarkably declined MDA-MB-453 and MCF-7 cells viability and accelerated apoptosis which accompanied by Bax up-regulation, Bcl-2 down-regulation and Caspase-3 cleavage. LU treatment also decreased xenograft tumor VEGF expression and blood-vessel density. Luteolin suppresses epithelial-mesenchymal transition and migration of triple-negative breast cancer cells by inhibiting YAP/TAZ activity. Herein, luteolin, a flavonoid found in Taraxacum officinale extract, was determined to inhibit the expressions of stemness-related transcriptional factors, the ATP-binding cassette transporter G2 (ABCG2), CD44, aldehyde dehydrogenase 1 activity as well as the sphere formation properties of breast CSCs. Our goal is to identify potential YAP/TAZ inhibitors from naturally derivative molecules and further study its effects on inhibiting EMT and metastasis of TNBC. Luteolin treatment reduced breast cancer cell viability, progestin-dependent VEGF secretion from breast cancer cells, and growth of MPA-dependent human breast cancer cell xenograft tumors in nude mice. The flavonoids, coumestrol, luteolin and kaempferol also decreased aromatase enzyme activity, with Ki values of 1.3, 4.8 and 27.2 microM, respectively. Taken collectively, the data demonstrate that the metabolism of hydroxylated flavonoids by cytochrome P450 CYP1 enzymes, notably CYP1A1 and CYP1B1, can enhance their antiproliferative activity in breast cancer cells. | |
| Target pathways | Luteolin exerted its anti-tumour effects possibly involved the elevated expression of miR-203 and the inhibited Ras/Raf/MEK/ERK signalling. Luteolin suppresses the metastasis of triple-negative breast cancer by reversing epithelial-to-mesenchymal transition via downregulation of beta-catenin expression . MLL3 Induced by Luteolin Causes Apoptosis in Tamoxifen-Resistant Breast Cancer Cells through H3K4 Monomethylation and Suppression of the PI3K/AKT/mTOR Pathway. Luteolin Regulation of Estrogen Signaling and Cell Cycle Pathway Genes in MCF-7 Human Breast Cancer Cells. Luteolin Inhibits Breast Cancer Stemness and Enhances Chemosensitivity through the Nrf2-Mediated Pathway. CONCLUSION: The results suggested that Luteolin isolated from Avicennia marina could probably induce apoptosis on breast cancer cell line by the regulation of p53 and Bcl-2 pathways. | |
| IC50 | 0.41 μM against MDA-MB-231 2 ± 0.3 μM against MDA-MB-468 | |
| Potency | Luteolin, a widely distributed flavone, has shown in vitro growth inhibitory effect against MCF-7. Flavone, apigenin and luteolin showed potent inhibitory effects on the proliferation of Hs578T, MDA-MB-231 and MCF-7 breast cancer cells in a concentration and time-dependent manner. Luteolin exerts anti-tumor activity through the suppression of epidermal growth factor receptor-mediated pathway in MDA-MB-231 ER-negative breast cancer cells. Luteolin inhibits cell cycle progression and induces apoptosis of breast cancer cells through downregulation of human telomerase reverse transcriptase. Luteolin also acts as an antiproliferative by suppressing receptor tyrosine-kinase activity and apoptosis, both of which could prevent incipient colonization of breast cancer. | |
| Cell line/ mice model | MDA-MB-468, MCF-7, MDA-MB-453, MDA-MB-231, Hs578T, Progestin-dependent xenograft, LNM35, HT29, HepG2 | |
| Additional information | Luteolin (Lu) is one of the flavonoids with anticancer activity, but its poor water solubility limits its use clinically. Luteolin improved the TAM-induced cognitive impairment and hepatic steatosis in rats by alleviating inflammation and modulating hepatic beta-catenin levels. Luteolin also causes cell cycle arrest at the G2/M phase and decreases mitochondrial membrane potential. Luteolin and galangin exhibited prooxidative properties 24h after the treatment in HCT-116 cells, while myricetin induced prooxidative effects in MDA-MB-231 cells. Luteolin and quercetin were the strongest inhibitors with IC(50) values of 0.8 and 1.3microM, respectively. | |
| PubChem ID | 5280445 | |
| Additional PMIDs | 20403331 23790951 27234523 28096694 29593542 33000272 34131251 27034599 22838964 24494074 25560707 28552787 34770867 14644660 33925607 21074525 30306879 32668964 33654432 29375370 15041478 22926442 29579978 25272060 26312209 29928143 25947916 32768952 29277460 21731475 23990719 25984842 26828287 27959422 29097115 31611756 30930986 31368817 32526242 33950812 34265292 34452179 18446505 8049151 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:861130-1 | |
| Safety | NA |