Luteolin is a flavonoid compound with multiple functions such as anti-inflammatory, antioxidant, and anti-cancer[1, 2]. Luteolin is an effective inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2)[3].
In vitro, Luteolin (0-160µM) treatment of NCI-H460 cells for 24h inhibited cell viability in a concentration-dependent manner, induced cell cycle arrest at the S phase, increased the protein expression level of apoptosis regulatory proteins, and also inhibited cell migration[4]. Luteolin (0.05, 0.1, 5μM) treatment of rat bone marrow mesenchymal stem cells (BMSC) for 24-72h activated the PI3K/Akt signaling pathway and promoted BMSC osteogenic differentiation[5].
In vivo, oral administration of Luteolin (10, 25, 50, 100 mg/kg/day) to treat rats with nonalcoholic steatohepatitis (NASH) significantly reduced the levels of serum liver function biomarkers (ALT, AST, total bilirubin), hyaluronic acid, and malondialdehyde, and also reduced the levels of proinflammatory factors IFN-γ, TNF-α, IL-1α, and IL-18[6]. Luteolin (50, 100 mg/kg/day) to treat rats with cognitive impairment induced by infusion of Aβ (1-40) peptide significantly improved Aβ-induced spatial learning and spatial working memory impairment and cognitive impairment, increased the levels of SOD and GSH-Px in hippocampal homogenate, and reduced the level of MDA[7].
References:
[1] Coleta M, Campos M G, Cotrim M D, et al. Assessment of luteolin (3′, 4′, 5, 7-tetrahydroxyflavone) neuropharmacological activity[J]. Behavioural brain research, 2008, 189(1): 75-82.
[2] Ziyan L, Yongmei Z, Nan Z, et al. Evaluation of the anti-inflammatory activity of luteolin in experimental animal models[J]. Planta medica, 2007, 73(03): 221-226.
[3] Tang X, Wang H, Fan L, 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[J]. Free Radical Biology and Medicine, 2011, 50(11): 1599-1609.
[4] Ma L, Peng H, Li K, et al. Luteolin exerts an anticancer effect on NCI-H460 human non-small cell lung cancer cells through the induction of Sirt1-mediated apoptosis[J]. Molecular medicine reports, 2015, 12(3): 4196-4202.
[5] Liang G, Zhao J, Dou Y, et al. Mechanism and experimental verification of luteolin for the treatment of osteoporosis based on network pharmacology[J]. Frontiers in Endocrinology, 2022, 13: 866641.
[6] Abu-Elsaad N, El-Karef A. Protection against nonalcoholic steatohepatitis through targeting IL-18 and IL-1alpha by luteolin[J]. Pharmacological Reports, 2019, 71: 688-694.
[7] Yu T X, Zhang P, Guan Y, et al. Protective effects of luteolin against cognitive impairment induced by infusion of Aβ peptide in rats[J]. International Journal of Clinical and Experimental Pathology, 2015, 8(6): 6740.
木犀草素（Luteolin）是一种黄酮类化合物，具有抗炎、抗氧化、抗癌等多种功能[1, 2]。Luteolin是一种有效的核因子红细胞2相关因子2（Nrf2）抑制剂[3]。
在体外，Luteolin（0-160µM）处理NCI-H460细胞24h，以浓度依赖性方式抑制了细胞活力，诱导了细胞周期停滞在S期，增加了凋亡调节蛋白的蛋白表达水平，还对细胞的迁移具有抑制作用[4]。Luteolin（0.05、0.1、5μM）处理大鼠骨髓间充质干细胞（BMSC）24-72h，激活了PI3K/Akt信号通路促进BMSC成骨分化[5]。
在体内，Luteolin（10、25、50、100 mg/kg/day）通过口服治疗非酒精性脂肪性肝炎（NASH）大鼠，可显著降低血清中肝功能的生物标志物（ALT、AST、总胆红素）、透明质酸和丙二醛的含量，还降低了促炎因子IFN-γ、TNF-α、IL-1α和IL-18水平[6]。Luteolin（50、100 、200mg/kg/day）通过口服治疗输注Aβ（1-40）肽引起的认知障碍模型大鼠，显著改善Aβ引起的空间学习和空间工作记忆损伤以及认知能力损伤，增加了海马体匀浆中SOD和GSH-Px的水平，同时降低了MDA的水平[7]。