Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells[1][2][3].
IC50 & Target
Human Endogenous Metabolite
体外研究 (In Vitro)
Luteolin (0-160 µM; 24 hours; NCI-H460 cells) treatment inhibits the viability of NCI-H460 cells in a concentration-dependent manner[1]. Luteolin (20-80 µM; 24 hours; NCI-H460 cells) treatment causes an accumulation of cells in the S phase[1]. Luteolin (320-580 µM; 48 hours; NCI-H460 cells) treatment induces apoptosis[1]. Luteolin (20-80 µM; 24 hours; NCI-H460 cells) treatment increases the protein expression levels of apoptotic regulatory proteins, including the Bax/Bcl-2 ratio, in a concentration-dependent manner, however, only 80 µM Luteolin inhibits the expression of Bad. Luteolin also decreases the expression of Sirt1 in the NCI-H460 cell line in a concentration-dependent manner[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
NCI-H460 cells
Concentration:
0 µM, 20 µM, 40 µM, 80 µM and 160 µM
Incubation Time:
24 hours
Result:
Inhibited the viability of NCI-H460 cells in a concentration-dependent manner.
Cell Cycle Analysis[1]
Cell Line:
NCI-H460 cells
Concentration:
20 µM, 40 µM, 80 µM
Incubation Time:
24 hours
Result:
Induced cell cycle arrest in the S phase.
Apoptosis Analysis[1]
Cell Line:
NCI-H460 cells
Concentration:
320 µM, 440 µM, 580 µM
Incubation Time:
48 hours
Result:
Apoptotic fraction was markedly increased.
Western Blot Analysis[1]
Cell Line:
NCI-H460 cells
Concentration:
20 µM, 40 µM, 80 µM
Incubation Time:
24 hours
Result:
Increased the protein expression levels of apoptotic regulatory proteins and decreased the expression of Sirt1 in the NCI-H460 cell line in a concentration-dependent manner.
体内研究 (In Vivo)
Luteolin (10-100 mg/kg; oral gavage; daily; for 12 weeks; adult male Wistar rats) has an antioxidant effect and can also protect against non-alcoholic steatohepatitis through targeting the pro-inflammatory IL-1 and Il-18 pathways in rats with a high carbohydrate/high fat diet[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Adult male Wistar rats (200-220 g)[2]
Dosage:
10 mg/kg, 25 mg/kg, 50 mg/kg or 100 mg/kg
Administration:
Oral gavage; daily; for 12 weeks
Result:
Significantly reduced ALT and AST activity and reduced levels of bilirubin, hyaluronic acid and malondialdehyde. Shows an antioxidant activity such as a significant increase in reduced glutathione. IFN-γ, TNF-α, IL-1α and IL-18 levels decreased significantly.
Clinical Trial
分子量
286.24
Formula
C15H10O6
CAS 号
491-70-3
中文名称
木犀草素；檞片素；木樨草素
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Ma L, et al. Luteolin exerts an anticancer effect on NCI-H460 human non-small cell lung cancer cells through the induction of Sirt1-mediated apoptosis. Mol Med Rep. 2015 Sep;12(3):4196-4202.
[2]. Abu-Elsaad N, et al. Protection against nonalcoholic steatohepatitis through targeting IL-18 and IL-1alpha by luteolin. Pharmacol Rep. 2019 Aug;71(4):688-694.
[3]. Xiuwen Tang, et al. Luteolin inhibits Nrf2 leading to negative regulation of the Nrf2/ARE pathway and sensitization of human lung carcinoma A549 cells to therapeutic drugs. Free Radic Biol Med. 2011 Jun 1;50(11):1599-609.
