AbMole小讲堂丨Luteolin（木犀草素）：一种具有抗炎、抗氧化、抗肿瘤活性的天然产物及其科研应用
Luteolin（木犀草素，AbMole，M4589）是一种广泛存在于植物中的黄酮类化合物，具有多种生物活性，包括抑制炎症、抗氧化、抑制肿瘤生长以及抗菌等作用。在细胞实验中，Luteolin在20-40 µM浓度范围内显著抑制肺癌A549细胞的迁移、侵袭以及伪足形成，且对非癌性MRC-5细胞无毒性作用[1]。此外，Luteolin（CAS No.：491-70-3）在40 µM浓度下可显著减少HT29细胞的存活率，并通过增加活性氧（ROS）水平诱导细胞凋亡[2]。Luteolin在黑色素瘤研究中，体外细胞模型和体内小鼠模型均表现出抑制肿瘤生长的效果，其作用机制涉及基因组水平的调控[3]。Luteolin在肺癌小鼠模型中，通过增强T细胞介导的杀伤途径促进肿瘤细胞凋亡，显著抑制肿瘤生长[4]。Luteolin在抗菌研究中，对金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌MRSA）表现出抑制作用[5, 6]。在神经保护研究中，Luteolin可显著预防β-淀粉样蛋白（Aβ）诱导的PC-12细胞凋亡，并抑制细胞活力下降[7]。此外，Luteolin在α-葡萄糖苷酶抑制实验中表现出非竞争性抑制机制，其IC50值约为32 µM，显著低于阿卡波糖（815 µM）[8]。Luteolin在昆虫研究中，在0.1 mg/mL浓度下可显著缩短成虫寿命并降低繁殖力[9]。这些研究结果表明，Luteolin（木犀草素，AbMole，M4589）在多种细胞（如A549、HT29、PC-12）和动物模型（如小鼠）中具有广泛的科研应用潜力，其作用机制涉及多种信号通路和分子靶点。
参考文献及鸣谢
[1] Masraksa, W.; Tanasawet, S.; Hutamekalin, P.; et al. Luteolin attenuates migration and invasion of lung cancer cells via suppressing focal adhesion kinase and non-receptor tyrosine kinase signaling pathway.Nutrition research and practice2020,14(2), 127-133.
[2] Yang, H.; Liu, B. F.; Xie, F. J.; et al. Luteolin induces mitochondrial apoptosis in HT29 cells by inhibiting the Nrf2/ARE signaling pathway.Experimental and therapeutic medicine2020,19(3), 2179-2187.
[3] Schomberg, J.; Wang, Z.; Farhat, A.; et al. Luteolin inhibits melanoma growth in vitro and in vivo via regulating ECM and oncogenic pathways but not ROS.Biochemical pharmacology2020,177, 114025.
[4] Li, X.; Bai, Y.; Zhou, J.; et al. Luteolin targets peroxiredoxin 2 to augment T-cell-mediated cytotoxicity and suppress lung adenocarcinoma progression.European journal of pharmacology2025,1004, 177984.
[5] Sun, Y.; Sun, F.; Feng, W.; et al. Luteolin Inhibits the Biofilm Formation and Cytotoxicity of Methicillin-Resistant Staphylococcus aureus via Decreasing Bacterial Toxin Synthesis.Evidence-based complementary and alternative medicine : eCAM2022,2022, 4476339.
[6] Zhang, D.; Gao, X.; Song, X.; et al. Luteolin Showed a Resistance Elimination Effect on Gentamicin by Decreasing MATE mRNA Expression in Trueperella pyogenes.Microbial drug resistance (Larchmont, N.Y.)2019,25(4), 619-626.
[7] Wang, H. R.; Pei, S. Y.; Fan, D. X.; et al. Luteolin Protects Pheochromocytoma (PC-12) Cells against Abeta (25-35)-Induced Cell Apoptosis through the ER/ERK/MAPK Signalling Pathway.Evidence-based complementary and alternative medicine : eCAM2020,2020, 2861978.
[8] Djeujo, F. M.; Ragazzi, E.; Urettini, M.; et al. Magnolol and Luteolin Inhibition of alpha-Glucosidase Activity: Kinetics and Type of Interaction Detected by In Vitro and In Silico Studies.Pharmaceuticals (Basel, Switzerland)2022,15(2).
[9] Ren, X.; Li, M.; Zheng, L.; et al. Luteolin Effects on Mortality, Development and Population Parameters of Frankliniella occidentalis (Pergande).Insects2025,16(12).