Fisetin is a natural flavonol found in many fruits and vegetables with multiple biological activities[1]. Fisetin is a strong antioxidant and can be used as an effective anti-aging agent[2]. Fisetin can be used as a chemotherapeutic agent for various cancers and as a neuroprotectant[3].
In vitro, treatment of human retinoblastoma Y79 cell line with Fisetin (25, 50, 100µM) for 24-72h inhibited cell viability and proliferation, cell invasion and migration, and intracellular vascular endothelial growth factor receptor (VEGFR) expression in a time- and dose-dependent manner[4]. Treatment of glioma cells (T98G and BEAS-2B cells) with Fisetin (1-500μM) for 24h and 48h inhibited cell proliferation and induced cell apoptosis and necrosis in a time- and dose-dependent manner[5]. Fisetin (0-40μM) treated A549 cells for 24-72h, inhibited cell proliferation in a time- and dose-dependent manner, led to cell cycle arrest, and inhibited cell adhesion, invasion, and migration[6].
In vivo, Fisetin (10, 20mg/kg) was orally treated for 10 days in mice with acute otitis media, significantly downregulated the mRNA levels of IL-1β, TNF-α, IL-6, and VEGF in mouse serum and middle ear tissue in a dose-dependent manner, upregulated the protein levels of SOD1, SOD2, HO-1, and Nrf2, and improved the inflammatory damage of the middle ear in mice[7]. Fisetin (223mg/kg) was treated with 4T1 breast tumor model mice by intraperitoneal injection for 3 weeks, inhibited the growth of 4T1 cell-derived in situ breast tumors, and promoted tumor cell apoptosis[8].
References:
[1] Antika L D, Dewi R M. Pharmacological aspects of fisetin[J]. Asian Pacific Journal of Tropical Biomedicine, 2021, 11(1): 1-9.
[2] Yousefzadeh M J, Zhu Y I, McGowan S J, et al. Fisetin is a senotherapeutic that extends health and lifespan[J]. EBioMedicine, 2018, 36: 18-28.
[3] Khan N, Syed D N, Ahmad N, et al. Fisetin: a dietary antioxidant for health promotion[J]. Antioxidants & redox signaling, 2013, 19(2): 151-162.
[4] Wang L, Chen N, Cheng H. Fisetin inhibits vascular endothelial growth factor induced angiogenesis in retinoblastoma cells[J]. Oncology Letters, 2020, 20(2): 1239-1244.
[5] Pak F, Oztopcu-Vatan P. Fisetin effects on cell proliferation and apoptosis in glioma cells[J]. Zeitschrift für Naturforschung C, 2019, 74(11-12): 295-302.
[6] Wang J, Huang S. Fisetin inhibits the growth and migration in the A549 human lung cancer cell line via the ERK1/2 pathway[J]. Experimental and Therapeutic Medicine, 2018, 15(3): 2667-2673.
[7] Li P, Chen D, Huang Y. Fisetin administration improves LPS-induced acute otitis media in mouse in vivo[J]. International journal of molecular medicine, 2018, 42(1): 237-247.
[8] Sun X, Ma X, Li Q, et al. Anti cancer effects of fisetin on mammary carcinoma cells via regulation of the PI3K/Akt/mTOR pathway: In vitro and in vivo studies[J]. International Journal of Molecular Medicine, 2018, 42(2): 811-820.
Fisetin是一种天然黄酮醇，存在于许多水果和蔬菜中，具有多种生物活性[1]。Fisetin是一种强抗氧化剂，能够作为有效的抗衰老剂[2]。Fisetin可作为多种癌症的化疗剂，也可作为神经保护剂[3]。
在体外，Fisetin（25, 50, 100µM）处理人视网膜母细胞瘤Y79细胞系24-72h，以时间和剂量依赖性方式抑制了细胞活力和增殖，抑制了细胞侵袭和迁移，抑制了细胞内血管内皮生长因子受体（VEGFR）的表达[4]。Fisetin（1-500μM）处理胶质瘤细胞（T98G和BEAS-2B细胞）细胞24h和48h，均以时间和剂量依赖性方式抑制了细胞增殖，诱导了细胞凋亡和坏死[5]。Fisetin（0-40μM）处理A549 细胞24-72h，以时间和剂量依赖性方式抑制了细胞增殖，导致了细胞周期停滞，抑制了细胞粘附、侵袭和迁移[6]。
在体内，Fisetin（10、20mg/kg）通过口服治疗急性中耳炎小鼠10天，以剂量依赖性方式显著下调了小鼠血清和中耳组织中IL-1β、TNF-α、IL-6和VEGF的mRNA水平，上调了SOD1、SOD2、HO-1和Nrf2的蛋白质水平，改善了小鼠的中耳炎症损伤[7]。Fisetin（223mg/kg）通过腹腔注射治疗4T1乳腺肿瘤模型小鼠3周，抑制了4T1细胞来源的原位乳腺肿瘤的生长，促进了肿瘤细胞凋亡[8]。