Cynaroside
(Synonyms: 木犀草苷; Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside) 目录号 : GN10690
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。
Cas No.:5373-11-5
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | HGC27 cells |
Preparation Method | The HGC27 cells were cultured in a DMEM medium containing 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin, and were incubated in a humidified environment at 37°C and 5% CO2. The logarithmic phase cells were inoculated into 96-well plates (1000 cells per well), and pre-cultured for 24 hours. Then, different concentrations (0, 25, 50, 75 and 100µM) of Cynaroside were added and incubated for 48 hours. The control group was treated with DMSO. MTT (5mg/ml; 20µl per well) was added to the cells and incubated in the cell culture box for 2 hours. The absorbance of the cells at 560nm was measured. |
Reaction Conditions | 0, 25, 50, 75 and 100µM; 48h |
Applications | Cynaroside significantly inhibited the viability of HGC27 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Female BALB/c nude mice, aged 4-6 weeks, were raised in a specified pathogen-free environment with a 12-hour light-dark cycle. HCT116 cells were resuspended at a density of 2×106 cells/ml, and 100μl of the cell suspension was subcutaneously injected into the right side of each mouse. On the 7th day, the tumor size was measured, and mice with a volume between 50 and 70mm3 were selected for further study. Each mouse was intraperitoneally injected with DMSO or 50mg/kg of Cynaroside every 3 days. The tumor size was calculated as (length×width2)/2. After 18 days of treatment, the mice were sacrificed, and the tumor tissues were collected for analysis. |
Dosage form | 50mg/kg; every 3 days for 18 days; i.p. |
Applications | Cynaroside treatment significantly inhibited tumor growth and reduced tumor weight in mice. |
References: | |
| Cas No. | 5373-11-5 | SDF | |
| 别名 | 木犀草苷; Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside | ||
| 化学名 | 2-(3,4-dihydroxyphenyl)-5-hydroxy-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one | ||
| Canonical SMILES | C1=CC(=C(C=C1C2=CC(=O)C3=C(C=C(C=C3O2)OC4C(C(C(C(O4)CO)O)O)O)O)O)O | ||
| 分子式 | C21H20O11 | 分子量 | 448.38 |
| 溶解度 | DMSO : 83.33 mg/mL (185.85 mM; Need ultrasonic) | 储存条件 | Store at 2-8°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 | 2.2303 mL | 11.1513 mL | 22.3025 mL |
| 5 mM | 446.1 μL | 2.2303 mL | 4.4605 mL |
| 10 mM | 223 μL | 1.1151 mL | 2.2303 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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