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]。