Corilagin
(Synonyms: 柯里拉京) 目录号 : GN10346
Corilagin是一种天然植物多酚单宁酸，可作为SARS-CoV-2刺突蛋白RBD与宿主受体血管紧张素转换酶2（ACE2）结合的强效抑制剂，IC50值为5.5μM。
Cas No.:23094-69-1
Sample solution is provided at 25 µL, 10mM.
Corilagin, a natural plant polyphenol tannic acid, is a potent inhibitor of the binding of SARS CoV-2 spike protein RBD to host receptor angiotensin-converting enzyme 2 (ACE2), with an IC50 value of 5.5μM[1]. Corilagin, as a non-nucleoside inhibitor of SARS-CoV-2 RNA-dependent RNA polymerase (RdRp), directly binds to RdRp and effectively inhibits the SARS-CoV-2 replication, with an EC50 value of 0.13μM[2]. Corilagin possesses potential anti-inflammatory and anti-virus properties, and has been widely applied in various anti-cancer researches[3].
In vitro, Corilagin inhibited the viability of ovarian cancer cells and the IC50 values for 24 hours and 48 hours of treatment with Corilagin on A2780 cells were 61.32μM and 47.81μM, respectively[4]. Treatment of MCF-7 cells with 80μM Corilagin for 48 hours significantly inhibited cell growth and activated both intrinsic and extrinsic mitochondrial apoptotic pathways[5]. Corilagin treatment (40μM; 48h) induced cell cycle arrest in cholangiocarcinoma cells, suppressed cell proliferation and inhibited the expression of Notch1 protein[6].
In vivo, Corilagin treatment via intragastric administration (40mg/kg/day) for one month significantly reduced the levels of inflammatory factors in the plasma of rats with peripheral artery disease (PAD) model, and alleviated the severity of atherosclerotic lesions in the arteries[7]. In the rabbit atherosclerosis model induced by high-fat diet (HFD), after 4 weeks of intragastric administration with 4mg/kg/day dose of Corilagin, the levels of serum total cholesterol, triglyceride and low-density lipoprotein cholesterol were significantly reduced, the level of high-density lipoprotein cholesterol was increased, the intimal thickening of the thoracic aorta was reduced, and the formation of foam cells was decreased[8]. Intraperitoneal injection with 30mg/kg/day of Corilagin for one week disrupted the nuclear receptor coactivator 4 (NCOA4)-ferritin interaction and inhibited ferroptosis mediated by ferroprotein phagocytosis, thereby alleviating intestinal ischemia/reperfusion injury in mice[9].
References:
[1] Hanson Q M, Wilson K M, Shen M, et al. Targeting ACE2–RBD interaction as a platform for COVID-19 therapeutics: development and drug-repurposing screen of an AlphaLISA proximity assay[J]. ACS Pharmacology & Translational Science, 2020, 3(6): 1352-1360.
[2] Li Q, Yi D, Lei X, et al. Corilagin inhibits SARS-CoV-2 replication by targeting viral RNA-dependent RNA polymerase[J]. Acta Pharmaceutica Sinica B, 2021, 11(6): 1555-1567.
[3] Li X, Deng Y, Zheng Z, et al. Corilagin, a promising medicinal herbal agent[J]. Biomedicine & Pharmacotherapy, 2018, 99: 43-50.
[4] Xu Z, Jiang Y, Shan T, et al. Study on the Effects and Mechanism of Corilagin on A2780 Cell Apoptosis[J]. Current Issues in Molecular Biology, 2025, 47(2): 105.
[5] Tong Y, Zhang G, Li Y, et al. Corilagin inhibits breast cancer growth via reactive oxygen species‐dependent apoptosis and autophagy[J]. Journal of cellular and molecular medicine, 2018, 22(8): 3795-3807.
[6] Gu Y, Xiao L, Ming Y, et al. Corilagin suppresses cholangiocarcinoma progression through Notch signaling pathway in vitro and in vivo[J]. International Journal of Oncology, 2016, 48(5): 1868-1876.
[7] Li Y, Wang Y, Chen Y, et al. Corilagin ameliorates atherosclerosis in peripheral artery disease via the toll-like receptor-4 signaling pathway in vitro and in vivo[J]. Frontiers in immunology, 2020, 11: 1611.
[8] He B, Chen D, Zhang X, et al. Antiatherosclerotic effects of corilagin via suppression of the LOX-1/MyD88/NF-κB signaling pathway in vivo and in vitro[J]. Journal of Natural Medicines, 2022, 76(2): 389-401.
[9] Wang Y, Li B, Liu G, et al. Corilagin attenuates intestinal ischemia/reperfusion injury in mice by inhibiting ferritinophagy-mediated ferroptosis through disrupting NCOA4-ferritin interaction[J]. Life sciences, 2023, 334: 122176.
Corilagin是一种天然植物多酚单宁酸，可作为SARS-CoV-2刺突蛋白RBD与宿主受体血管紧张素转换酶2（ACE2）结合的强效抑制剂，IC50值为5.5μM[1]。Corilagin可作为SARS-CoV-2 RNA依赖性RNA聚合酶（RdRp）的非核苷类抑制剂，可直接结合RdRp并有效抑制病毒复制，EC50值为0.13μM[2]。Corilagin具有显著的抗炎和抗病毒特性，且被广泛应用于抗癌研究中[3]。
在体外，Corilagin可抑制卵巢癌细胞活性，处理A2780细胞24小时和48小时后的IC50值分别为61.32μM和47.81μM[4]。80μM浓度的Corilagin处理MCF-7细胞48小时可显著抑制细胞生长，并激活线粒体内源性和外源性凋亡途径[5]。40μM浓度的Corilagin处理胆管癌细胞48小时后可诱导细胞周期阻滞，抑制细胞增殖能力以及降低Notch1蛋白表达[6]。
在体内，每日灌胃40mg/kg剂量的Corilagin，连续一个月，可显著降低外周动脉疾病（PAD）大鼠模型的血浆炎症因子水平且减轻动脉粥样硬化病变程度[7]。在高脂饮食（HFD）诱导的兔动脉粥样硬化模型中，4mg/kg/day剂量的Corilagin经灌胃给药处理4周后，血清总胆固醇、甘油三酯及低密度脂蛋白胆固醇水平显著降低，同时胸主动脉内膜增厚减轻且泡沫细胞形成减少[8]。腹腔注射30mg/kg/day剂量的Corilagin一周可阻断核受体辅激活因子4（NCOA4）-铁蛋白相互作用并抑制铁死亡，从而缓解由缺血/再灌注引起的小鼠肠道损伤[9]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | The MCF-7 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and 100U/mL penicillin/streptomycin, under a 5% CO2 and 95% air environment at 37℃. The cells were seeded at a density of 5 × 103 cells per well in a 96-well plate, then treated with Corilagin (0, 20, 40, 60, 80, 100μM) for 48 hours, followed by the addition of 20μL MTT (5mg/mL) for 4 hours, and finally 150μL DMSO was added. The absorbance was measured at 490nm using an enzyme reader. The cell proliferation status was detected using the EdU cell proliferation detection kit, and the number of cells incorporating EdU was determined by fluorescence microscopy. |
Reaction Conditions | 0, 20, 40, 60, 80, 100μM; 48h |
Applications | Corilagin significantly inhibited MCF-7 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice |
Preparation Method | 200µL of 1 × 107 Hep-2 cells were injected subcutaneously into the right side of each 4-5-week-old athymic nude mouse to establish a laryngeal cancer transplantation model. When the tumor volume reached 100mm3, the tumor-bearing mice were randomly divided into 3 groups, with 5 mice in each group. All mice were intraperitoneally injected with 30mg/kg Corilagin once every 3 days. The tumor volume was measured every 4 days for a total of 28 days. The length and width of the subcutaneous transplanted tumors were measured using a vernier caliper. The formula for calculating tumor volume (V) is: V = 0.5×width2×length. After treatment (28 days), the mice were anesthetized with isoflurane and euthanized, the xenograft tumor samples of the nude mice were embedded in paraffin, rinsed with cold saline, and cut into 5µm sections. Then, the samples were fixed in 10% formaldehyde neutral buffer solution and stained with hematoxylin-eosin. |
Dosage form | 30mg/kg, once every 3 days for 28 days; i.p. |
Applications | Corilagin treatment inhibited growth of transplanted tumors and resulted in tumor chromatin condensation and structure loosening in the xenograft tumor mouse models. |
References: | |
| Cas No. | 23094-69-1 | SDF | |
| 别名 | 柯里拉京 | ||
| Canonical SMILES | C1C2C(C(C(C(O2)OC(=O)C3=CC(=C(C(=C3)O)O)O)O)OC(=O)C4=CC(=C(C(=C4C5=C(C(=C(C=C5C(=O)O1)O)O)O)O)O)O)O | ||
| 分子式 | C27H22O18 | 分子量 | 634.45 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at 2-8°C |
| 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 | 1.5762 mL | 7.8808 mL | 15.7617 mL |
| 5 mM | 0.3152 mL | 1.5762 mL | 3.1523 mL |
| 10 mM | 0.1576 mL | 0.7881 mL | 1.5762 mL |
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| 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 | ||||||||||
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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，
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2.
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