Echinatin
(Synonyms: 刺甘草查尔酮) 目录号 : GC38226
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。
Cas No.:34221-41-5
Sample solution is provided at 25 µL, 10mM.
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]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in DMEM medium containing 10% fetal bovine serum (FBS) and placed in an incubator at 37℃ with 5% CO2 saturation. 2.5×103 HepG2 cells were seeded in 96-well plates and allowed to adhere completely before subsequent operations. Cells were treated with Echinatin (0, 10, 15, 20, and 25μM) in different concentration gradients. After waiting for 24 hours, 10μl of predissolved MTT solution (5mg/ml) was added to the wells and the incubation was continued for another 4 hours. Subsequently, 100μl of DMSO solution was added after the liquid in the wells was completely aspirated. Finally, the absorbance value at the wavelength of 492nm was recorded. |
Reaction Conditions | 0, 10, 15, 20, and 25μM; 24h |
Applications | Echinatin treatment significantly inhibited the cell viability of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | BALB/c nude mice (female, 4 weeks of age) were maintained under SPF grade conditions. After acclimatization to the experimental environment for 1 week, the mice were subcutaneously injected with 80µl sterile PBS solution containing 143B osteosarcoma cells suspension (cell density of 2×106 cells/mL). Ten mice were randomly divided into two groups (n=5 in each group) and treated with Echinatin (60mg/kg) or 0.5% carboxymethylcellulose sodium (CMC-Na) by gavage once every two days. Body weight and tumor volume were recorded, and after 2 weeks, all mice were sacrificed by cervical dislocation. Finally, tumor samples were collected for analysis. |
Dosage form | 60mg/kg; every two days for 2 weeks; p.o. |
Applications | Echinatin inhibited the growth of 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. |
References: | |
| Cas No. | 34221-41-5 | SDF | |
| 别名 | 刺甘草查尔酮 | ||
| Canonical SMILES | O=C(C1=CC=C(O)C=C1)/C=C/C2=CC=C(O)C=C2OC | ||
| 分子式 | C16H14O4 | 分子量 | 270.28 |
| 溶解度 | DMSO: 250 mg/mL (924.97 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6999 mL | 18.4993 mL | 36.9987 mL |
| 5 mM | 740 μL | 3.6999 mL | 7.3997 mL |
| 10 mM | 370 μL | 1.8499 mL | 3.6999 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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