Fraxetin is a plant-derived O-methylcoumarin [1]. Fraxetin exerts anti-inflammatory effects by directly scavenging reactive oxygen free radicals and activating antioxidant defenses, and intervening in inflammatory signals [2]. Fraxetin has anti-tumor, anti-inflammatory, and neuroprotective effects [3-4].
In MCF-7 cells, Fraxetin (10-60µM; 24h, 48h) significantly inhibited cell proliferation in a concentration and time-dependent manner [5]. In SKOV3 and SW626 cells, Fraxetin (80µM; 12h) suppresses the proliferation, migration, and invasion of ovarian cancer cells by inhibiting the TLR4/STAT3 signaling pathway [6]. In T98G and LN-229 cells, Fraxetin (5-50µM; 48h) inhibited cell viability in a concentration-dependent manner [7].
In C57BL/6J mice, Selenium-dependent glutathione reductase activity is significantly increased in the liver of Fraxetin (25mg/kg; po; 30d) treated mice [8]. In Dextran sulphate sodium (DSS)-induce a mouse model of colitis, Fraxetin (10mg/kg, 30mg/kg, 60mg/kg; po; 8d) alleviates DSS-induced colitis by modulating the inflammatory response, enhancing epithelial barrier integrity and regulating the gut microbiota [9].
References:
[1]. Wang H, Zou DA, Xie K, et al. Antibacterial mechanism of fraxetin against Staphylococcus aureus. Molecular Medicine Reports. 2014 Nov 1; 10(5): 2341-2345.
[2]. Balaha M, Ahmed N, Geddawy A, et al. Fraxetin prevented sodium fluoride-induced chronic pancreatitis in rats: Role of anti-inflammatory, antioxidant, antifibrotic and anti-apoptotic activities. International immunopharmacology. 2021 Apr 1; 93: 107372.
[3]. Ha NM, Son NT. Health benefits of fraxetin: from chemistry to medicine. Archiv der Pharmazie. 2024 Jul; 357(7): 2400092.
[4]. Fang T, Liu L, Liu W. Exploring the mechanism of fraxetin against acute myeloid leukemia through cell experiments and network pharmacology. BMC Complementary Medicine and Therapies. 2024 Jun 10; 24(1): 226.
[5]. Liu G, Liu Z, Yan Y, et al. Effect of fraxetin on proliferation and apoptosis in breast cancer cells. Oncology Letters. 2017 Dec 1; 14(6): 7374-7378.
[6]. Xu R, Ruan Y, Zhang L, et al. Fraxetin suppresses the proliferation, migration, and invasion of ovarian cancer cells by inhibiting the TLR4/STAT3 signaling pathway. Immunopharmacology and Immunotoxicology. 2023 May 4; 45(3): 287-294.
[7]. Yao H, Li X, Pan X, et al. Fraxetin exerts anticancer effect in glioma by suppressing MiR‐21‐3p. Drug Development Research. 2022 Apr; 83(2): 501-511.
[8]. MARTÍN‐ARAGÓN SA, Benedí JM, Villar AM. Modifications on antioxidant capacity and lipid peroxidation in mice under fraxetin treatment. Journal of pharmacy and pharmacology. 1997 Jan; 49(1): 49-52.
[9]. Sun X, Jin X, Wang L, et al. Fraxetin ameliorates symptoms of dextran sulphate sodium-induced colitis in mice. Heliyon. 2024 Jan 15; 10(1).
Fraxetin是一种植物来源的O-甲基香豆素 [1]。Fraxetin通过直接清除活性氧自由基、激活抗氧化防御机制以及干预炎症信号发挥抗炎作用 [2]。Fraxetin具有抗肿瘤、抗炎和神经保护作用 [3-4]。
在MCF-7细胞中，Fraxetin（10-60µM；24h、48h）以浓度和时间依赖性方式显著抑制细胞增殖 [5]。在SKOV3和SW626细胞中，Fraxetin（80µM；12h）通过抑制TLR4/STAT3信号通路抑制卵巢癌细胞的增殖、迁移和侵袭 [6]。在T98G和LN-229细胞中，Fraxetin（5-50µM；48h）以浓度依赖性方式抑制细胞活力 [7]。
在C57BL/6J小鼠中，Fraxetin（25mg/kg；po；30d）治疗组小鼠肝脏中硒依赖性谷胱甘肽还原酶活性显著升高 [8]。在葡聚糖硫酸钠（DSS）诱发的小鼠结肠炎模型中，Fraxetin（10mg/kg，30mg/kg，60mg/kg；po；8d）通过调节炎症反应、增强上皮屏障完整性和调节肠道菌群，减轻了DSS诱发的结肠炎 [9]。