Formononetin is a potent FGFR2 inhibitor with an IC50 of 4.3μM. Formononetin potently inhibits angiogenesis and tumor growth[1].
Formononetin (10, 80μM; 3d) inhibit Ishikawa, HEC-1A, and HEC-251 cells proliferation in a dose-dependent manner[2]. Formononetin (10, 25μM; 24h) is a potent protectant against cisplatin-induced cell death through inhibiting intracellular ROS accumulation in pig kidney epithelial LLC-PK1 cells[3]. Formononetin (0.1, 0.3, 1μM; 30-60min) increased CNE2 cell estrogen receptor-α (ERα) and bcl-2, but decreased protein-phosphatase and tensin homologue (PTEN) protein expression[4].
In mice hyperoxic acute lung injury, Formononetin (10, 100 mg/kg; ip; 72h) significantly attenuated hyperoxia-induced elevated lung water content, up-regulation of pro-inflammatory cytokine levels, and increased lung neutrophil infiltration[5]. In mice acute ischaemic injury model, formononetin (20mg/kg; po; 28d) promoted the expression of ER β and p53 in a dose-dependent manner[6].
References:
[1] Wu X Y, Xu H, Wu Z F, et al. Formononetin, a novel FGFR2 inhibitor, potently inhibits angiogenesis and tumor growth in preclinical models[J]. Oncotarget, 2015, 6(42): 44563.
[2]. Zhang Q, Huang X. The modulatory properties of Astragalus membranaceus treatment on endometrial cancer: an integrated pharmacological method[J]. PeerJ, 2021, 9: e11995.
[3] Lee H, Lee D, Kang K S, et al. Inhibition of intracellular ROS accumulation by Formononetin attenuates cisplatin-mediated apoptosis in LLC-PK1 cells[J]. International journal of molecular sciences, 2018, 19(3): 813.
[4] Guo Y H, Tang F Y, Wang Y, et al. Low concentration of Formononetin promotes proliferation of estrogen receptor-positive cells through an ERα-miR-375-PTEN-ERK1/2-bcl-2 pathway[J]. Oncotarget, 2017, 8(59): 100045.
[5]Chen Y, Wei D, Zhao J, et al. Reduction of hyperoxic acute lung injury in mice by Formononetin[J]. PloS one, 2021, 16(1): e0245050.
[6] Zhao L, Han J, Liu J, et al. A novel Formononetin derivative promotes anti-ischemic effects on acute ischemic injury in mice[J]. Frontiers in Microbiology, 2021, 12: 786464.
Formononetin是一种强效的FGFR2抑制剂，其IC50值约为4.31μM。Formononetin能有效抑制血管生成和肿瘤生长[1]。
Formononetin（10、80μM；3d）以剂量依赖的方式抑制Ishikawa，HEC-1A和HEC-251细胞的增殖[2]。Formononetin（10、25μM；24h）通过抑制猪肾上皮LLC-PK1细胞中细胞内ROS的积累，对顺铂诱导的细胞死亡具有有效的保护作用[3]。Formononetin（0.1、0.3、1μM；30-60min）可增加CNE2细胞中雌激素受体-α（ERα）和bcl-2的表达，但会降低蛋白磷酸酶和天丝同源物（PTEN）蛋白的表达[4]。
在小鼠高氧性急性肺损伤中，Formononetin（10、100mg/kg；ip；72h）显著减轻了高氧引起的肺水含量升高、促炎细胞因子水平上调和肺中性粒细胞浸润增加[5]。在小鼠急性缺血性损伤模型中，Formononetin（20mg/kg；po；28d）能以剂量依赖的方式促进ERβ和p53的表达[6]。