Cynaroside is a flavonoid compound that exhibits a significant inhibition of α-glucosidase, with an IC50 value of 18.3µM[1]. Cynaroside inhibits the activity of influenza endonuclease with an IC50 value of 32µM [2]. Cynaroside can inhibit the MET/AKT/mTOR axis by reducing the phosphorylation levels of AKT, mTOR and P70S6K. It has been widely used as an anti-cancer agent to suppress the growth of various cancer cells[3].
In vitro, Cynaroside treatment for 24 hours significantly inhibited the proliferation of U87 cells and Caco-2 cells, with IC50 values of 26.34µg/ml and 97.06µg/ml, respectively[4]. Treatment with 100μM Cynaroside for 48 hours significantly inhibited the viability of HGC27 cells, causing the cell cycle to arrest at the S phase[5]. Pre-treatment with 100μM Cynaroside for 6 hours can alleviate the H2O2-induced damage to APRE-19 cells and reduce the protein expression of caspase 3[6].
In vivo, Cynaroside treatment via intraperitoneal injection at a dose of 50mg/kg every 3 days for 18 days significantly inhibited tumor growth and reduced tumor weight in HCT116 cell-xenograft tumor mouse model[7]. Intraperitoneal injection of 10mg/kg/day dose of Cynaroside was administered daily for 8 consecutive days, which significantly ameliorated renal tubular injury and interstitial fibrosis in the unilateral ureteral obstruction mouse model, accompanied by the improved renal function[8]. For 13 consecutive days, intraperitoneal injection of 20mg/kg/day dose of Cynaroside was administered daily, which effectively improved the anxiety, despair and anhedonia-like states in mice induced by chronic unpredictable mild stress (CUMS), and reduced microglial activation in the hippocampus[9].
References:
[1] Cen C, Li J, Zhou P, et al. The effects of cynaroside on lipid metabolism and lipid-related diseases: a mechanistic overview[J]. Frontiers in Pharmacology, 2025, 16: 1648614.
[2] Zima V, Radilová K, Kožíšek M, et al. Unraveling the anti-influenza effect of flavonoids: Experimental validation of luteolin and its congeners as potent influenza endonuclease inhibitors[J]. European Journal of Medicinal Chemistry, 2020, 208: 112754.
[3] Bouyahya A, Taha D, Benali T, et al. Natural sources, biological effects, and pharmacological properties of cynaroside[J]. Biomedicine & Pharmacotherapy, 2023, 161: 114337.
[4] Pirvu L C, Pintilie L, Albulescu A, et al. Anti-Proliferative Potential of Cynaroside and Orientin—In Silico (DYRK2) and In Vitro (U87 and Caco-2) Studies[J]. International Journal of Molecular Sciences, 2023, 24(23): 16555.
[5] Ji J, Wang Z, Sun W, et al. Effects of cynaroside on cell proliferation, apoptosis, migration and invasion though the MET/AKT/mTOR axis in gastric cancer[J]. International journal of molecular sciences, 2021, 22(22): 12125.
[6] Yu H, Li J, Hu X, et al. Protective effects of cynaroside on oxidative stress in retinal pigment epithelial cells[J]. Journal of Biochemical and Molecular Toxicology, 2019, 33(8): e22352.
[7] Lei S, Cao W, Zeng Z, et al. Cynaroside induces G1 cell cycle arrest by downregulating cell division cycle 25A in colorectal cancer[J]. Molecules, 2024, 29(7): 1508.
[8] Yang A Y, Kim J Y, Gwon M G, et al. Protective effects and mechanisms of cynaroside on renal fibrosis in mice with unilateral ureteral obstruction[J]. Redox Report, 2025, 30(1): 2500271.
[9] Zhou Y, Huang Y, Ye W, et al. Cynaroside improved depressive-like behavior in CUMS mice by suppressing microglial inflammation and ferroptosis[J]. Biomedicine & Pharmacotherapy, 2024, 173: 116425.
Cynaroside是一种黄酮类化合物，对α-葡萄糖苷酶具有显著抑制作用，IC50值为18.3µM[1]。Cynaroside能抑制流感病毒核酸内切酶活性，IC50值为32µM[2]。通过降低AKT、mTOR和P70S6K的磷酸化水平，Cynaroside可有效抑制MET/AKT/mTOR信号轴，目前已作为抗癌剂广泛应用于多种癌细胞的生长抑制研究[3]。
在体外，Cynaroside处理24小时能显著抑制U87细胞和Caco-2细胞的增殖，IC50值分别为26.34µg/ml和97.06µg/ml[4]。使用100μM的Cynaroside处理HGC27细胞48小时，可显著抑制细胞活力并引起S期细胞周期阻滞[5]。用100μM的Cynaroside预处理ARPE-19细胞6小时，能减轻H2O2诱导的细胞损伤，并降低caspase 3蛋白表达[6]。
在体内，每3天腹腔注射50mg/kg剂量的Cynaroside，持续18天，能显著抑制HCT116细胞移植瘤小鼠的肿瘤生长并减轻肿瘤重量[7]。每日腹腔注射10mg/kg/day剂量的Cynaroside（连续8天），可显著改善单侧输尿管结扎小鼠的肾小管损伤和间质纤维化，并伴随肾功能指标恢复[8]。每日腹腔注射20mg/kg/day剂量的Cynaroside连续13天，能有效缓解慢性不可预见性温和应激(CUMS)诱导的小鼠焦虑、绝望和快感缺失样状态，并抑制海马区小胶质细胞的活化[9]。