Echinatin is the chalcone in the Chinese herbal medicine Gancao, with anti-inflammatory effects and antioxidant properties[1]. Echinatin binds to heat shock protein 90 (HSP90), inhibits the ATPase activity, and disrupts the interaction between cochaperone SGT1 and HSP90-NLRP3[2]. Echinatin has been widely used in animal models of ischemia/reperfusion to improve cardiac function[3].
In vitro, Echinatin treatment for 24 hours significantly inhibited the viability of HepG2 and Huh-7 cells with IC50 values of 23.48μM and 23.08μM, respectively[4]. Echinatin treatment at 20µM for 48 hours significantly promoted KYSE30 cell apoptosis and inhibited AKT/mTOR signaling pathway[5]. Echinatin treatment at 30µM for 24h inhibited lipopolysaccharide (LPS)-induced inflammatory response and downregulated the mRNA expression and release of IL-1β and IL-6 in RAW264.7 cells[6].
In vivo, Echinatin treatment (60mg/kg; every two days; p.o.) for 2 weeks inhibited the growth of 143B cell-xenograft tumors in mice, decreased the expression levels of PCNA, Bcl-2, vimentin, MMP2, Snail, and β-catenin, and increased the expression levels of p-p38 and GSK3β[7]. Oral Echinatin at a dose of 25mg/kg/day for 45 consecutive days improved lipid levels and alleviated pancreatic and renal impairment in a diabetic rat model[8].
References:
[1] Liang M, Li X, Ouyang X, et al. Antioxidant mechanisms of echinatin and licochalcone A[J]. Molecules, 2018, 24(1): 3.
[2] Xu G, Fu S, Zhan X, et al. Echinatin effectively protects against NLRP3 inflammasome–driven diseases by targeting HSP90[J]. JCI insight, 2021, 6(2): e134601.
[3] Tian X, Liu C, Jiang H L, et al. Cardioprotection provided by Echinatin against ischemia/reperfusion in isolated rat hearts[J]. BMC cardiovascular disorders, 2016, 16(1): 119.
[4] Wang J, Li Z, Han X, et al. Echinatin inhibits the growth and metastasis of human hepatocellular carcinoma cells through p38 and JNK signaling pathways[J]. Tissue and Cell, 2025, 95: 102907.
[5] Hong P, Liu Q W, Xie Y, et al. Echinatin suppresses esophageal cancer tumor growth and invasion through inducing AKT/mTOR-dependent autophagy and apoptosis[J]. Cell Death & Disease, 2020, 11(7): 524.
[6] Luo L, Wang H, Xiong J, et al. Echinatin attenuates acute lung injury and inflammatory responses via TAK1-MAPK/NF-κB and Keap1-Nrf2-HO-1 signaling pathways in macrophages[J]. Plos one, 2024, 19(5): e0303556.
[7] Lu Q, Huang H, Wang X, et al. Echinatin inhibits the growth and metastasis of human osteosarcoma cells through Wnt/β-catenin and p38 signaling pathways[J]. Pharmacological Research, 2023, 191: 106760.
[8] Li X, Lu P, Wan H, et al. Echinatin ameliorates hyperglycemia and associated pathogenesis, oxidative stress and inflammation in STZ-induced diabetes in rats[J]. Biochemical and Biophysical Research Communications, 2025: 152174.
Echinatin是中药甘草中的查尔酮类成分，具有抗炎作用与抗氧化特性[1]。Echinatin通过结合热休克蛋白90，抑制ATP酶活性，并破坏SGT1共伴侣蛋白与HSP90-NLRP3之间的相互作用[2]。Echinatin已广泛应用于缺血再灌注动物模型中以改善心脏功能[3]。
在体外，Echinatin处理24小时能显著抑制HepG2和Huh-7细胞活力，IC50值分别为23.48μM和23.08μM[4]。使用20µM的Echinatin处理KYSE30细胞48小时，可显著促进细胞凋亡并抑制AKT/mTOR信号通路[5]。以30µM的Echinatin处理RAW264.7细胞24小时，能抑制脂多糖(LPS)诱导的炎症反应，下调IL-1β和IL-6的mRNA表达及释放[6]。
在体内，每两日口服60mg/kg/day剂量的Echinatin连续2周，可抑制143B细胞移植瘤在小鼠体内的生长，降低PCNA、Bcl-2、波形蛋白、MMP2、Snail和β-catenin的表达水平，同时提高p-p38和GSK3β的表达[7]。连续45日每日口服25mg/kg/day剂量的Echinatin，能改善糖尿病大鼠模型的脂质水平，并减轻胰腺和肾脏损伤[8]。