Luteolin

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.