Geraniin是一种TNF-α释放抑制剂，IC50值为43µM，具有多种活性，包括抗癌、抗炎和抗高血糖活性。
Cas No.:60976-49-0
Sample solution is provided at 25 µL, 10mM.
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Geraniin, a TNF-α releasing inhibitor with an IC50 value of 43μM, exhibits numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities[1]. Geraniin can induce the nuclear translocation of nuclear factor Nrf2 and enhance glutathione (GSH) levels, thus reducing intracellular ROS levels in cells [2]. Geraniin has been widely used in cell and animal models to inhibit tumor growth and interfere with mitochondrial function[3].
In vitro, Geraniin treatment for 48 hours significantly inhibited the viability of OVCAR3 and SKOV3 cells with IC50 values of 34.5μM and 23.6μM, respectively[4]. Geraniin treatment at 36µM for 24h abrogated HT-29 cell growth and induced nuclear morphological changes and DNA fragmentation[5]. Treatment of T24 cells with 20µM Geraniin for 24 hours induced cell cycle arrest, decreased the proportion of T24 cells in S phase, promoted cell apoptosis, and regulated the PI3K/AKT signaling pathway[6].
In vivo, Geraniin (20mg/kg/day) administered daily by gavage for 14 days alleviated lipopolysaccharide (LPS)-induced cognitive impairment, ameliorated LPS-induced nerve/synaptic damage, and reduced Aβ production in mice[7]. Daily gavage administration of Geraniin (8mg/kg/day) for 10 consecutive weeks could reduce the body weight of ApoE−/− mice on a high-fat diet, and lower the levels of serum triglycerides (TG) and low-density lipoprotein cholesterol (LDL-C)[8].
References:
[1] Okabe S, Suganuma M, Imayoshi Y, et al. New TNF-α releasing inhibitors, geraniin and corilagin, in leaves of Acer nikoense, Megusurino-ki[J]. Biological and Pharmaceutical Bulletin, 2001, 24(10): 1145-1148.
[2] Cheng H S, Ton S H, Abdul Kadir K. Ellagitannin geraniin: a review of the natural sources, biosynthesis, pharmacokinetics and biological effects[J]. Phytochemistry reviews, 2017, 16(1): 159-193.
[3] Li J, Wang S, Yin J, et al. Geraniin induces apoptotic cell death in human lung adenocarcinoma A549 cells in vitro and in vivo[J]. Canadian Journal of Physiology and Pharmacology, 2013, 91(12): 1016-1024.
[4] Wang X, Chen Z, Li X, et al. Geraniin suppresses ovarian cancer growth through inhibition of NF‐κB activation and downregulation of Mcl‐1 expression[J]. Journal of Biochemical and Molecular Toxicology, 2017, 31(9): e21929.
[5] Chan C K, Tang L Y, Goh B H, et al. Targeting apoptosis via inactivation of PI3K/Akt/mTOR signaling pathway involving NF-κB by geraniin in HT-29 human colorectal adenocarcinoma cells[J]. Progress in Drug Discovery & Biomedical Science, 2019, 2(1).
[6] Xu J, Qin N, Yao Y, et al. Geraniin inhibits bladder cancer cell growth via regulation of PI3K/AKT signaling pathways[J]. Tropical Journal of Pharmaceutical Research, 2020, 19(2): 253-257.
[7] Wang D, Dong X, Wang B, et al. Geraniin attenuates lipopolysaccharide-induced cognitive impairment in mice by inhibiting toll-like receptor 4 activation[J]. Journal of Agricultural and Food Chemistry, 2019, 67(36): 10079-10088.
[8] Xie Y, Liu S, Wei Z, et al. Geraniin Alleviates High‐Fat Diet‐Induced Atherosclerosis in ApoE−/− Mice[J]. Food Science & Nutrition, 2025, 13(7): e70693.
Geraniin是一种TNF-α释放抑制剂，IC50值为43µM，具有多种活性，包括抗癌、抗炎和抗高血糖活性[1]。Geraniin可诱导核因子Nrf2的核转位，并提高谷胱甘肽（GSH）水平，从而降低细胞内的活性氧（ROS）水平[2]。Geraniin已被广泛用于细胞和动物模型中，以抑制肿瘤生长并干扰线粒体功能[3]。
在体外，Geraniin处理48小时显著抑制了OVCAR3和SKOV3细胞的活力，IC50值分别为34.5µM和23.6µM[4]。使用36µM的Geraniin处理24小时，抑制了HT-29细胞的生长，并诱导了细胞核形态改变和DNA片段化[5]。使用20µM的Geraniin处理T24细胞24小时，诱导了细胞周期阻滞，降低了T24细胞在S期的比例，促进了细胞凋亡，并调节了PI3K/AKT信号通路[6]。
在体内，每日灌胃给予Geraniin（20mg/kg/day），持续14天，减轻了脂多糖（LPS）诱导的小鼠认知障碍，改善了LPS诱导的神经/突触损伤，并减少了Aβ的产生[7]。连续10周每日灌胃给予Geraniin（8mg/kg/day），可降低高脂饮食喂养的ApoE−/−小鼠的体重，并降低血清甘油三酯（TG）和低密度脂蛋白胆固醇（LDL-C）水平[8]。
| Cell experiment [1]: | |
Cell lines | OVCAR3 cells |
Preparation Method | OVCAR3 cells were cultured in Dulbecco's Modified Eagle's medium containing 10% fetal bovine serum at 37℃ in the presence of 5% CO2. OVCAR3 cells were seeded at a density of 5×103 cells/well in 96-well flat-bottom plates and cultured for 24 hours. Cells were treated with different concentrations of Geraniin (0, 5, 10, 20, 40, and 80µM), and the cell viability was detected after 48 hours. |
Reaction Conditions | 0, 5, 10, 20, 40, and 80µM; 48h |
Applications | Geraniin treatment reduced the cell viability of OVCAR3 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male ApoE−/− mice |
Preparation Method | Male ApoE−/− mice (six weeks old) were housed in a Specific Pathogen-Free (SPF) experimental environment, with the temperature set at 24°C±1°C, relative humidity controlled between 40% and 50%, and exposed to a 12-h light–dark cycle. All mice were adaptively fed for one week. The ApoE−/− mice were randomly assigned to one of 2 groups (n=6 per group): (1) ApoE−/− mice model group; (2) Geraniin 8mg/kg/day (p.o.). All ApoE−/− mice were fed a high-fat diet (40% kcal fat) containing 0.5% cholesterol for 10 weeks. Mice were weighed weekly, and blood was collected for analysis. |
Dosage form | 8mg/kg/day for 10 weeks; p.o. |
Applications | Geraniin treatment reduced the body weight of ApoE−/− mice on a high-fat diet, and decreased the levels of TG and LDL-C. |
References: | |
| Cas No. | 60976-49-0 | SDF | |
| 别名 | 老鹳草素 | ||
| Canonical SMILES | OC1=C(O)C(O)=C(C(C(O)=C(O)C(O)=C2)=C2C(O[C@H]3[C@@H]4OC(C(C=C(O)C(O)=C5OC6(O)C(O)7O)=C5C7C8=CC6=O)=O)=O)C(C(OC[C@H](O[C@@H]4OC(C9=CC(O)=C(O)C(O)=C9)=O)[C@@H]3OC8=O)=O)=C1 | ||
| 分子式 | C41H28O27 | 分子量 | 952.08 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | 储存条件 | 4°C, away from moisture and 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 | 1.0503 mL | 5.2517 mL | 10.5033 mL |
| 5 mM | 210.1 μL | 1.0503 mL | 2.1007 mL |
| 10 mM | 105 μL | 525.2 μL | 1.0503 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。
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