| CAS |
No.186763-78-0 |
| 中文名称 |
人参皂苷Rg5 |
| 英文名称 |
Ginsenoside Rg5 |
| 分子式 |
C42H70O12 |
| 分子量 |
767 |
| 溶解性 |
Soluble in DMSO ≥5mg/mL |
| 纯度 |
HPLC≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 靶点 |
IGF-1R |
| 通路 |
Protein Tyrosine Kinase/RTK |
| 背景说明 |
Ginsenoside Rg5 是 IGF-1R 的竞争型激动剂， 竞争 IGF-1R 的结合位点，并阻断 IGF-1 与 IGF-1R 的结合。 |
| 生物活性 |
Ginsenoside Rg5 is the main component of Red ginseng and IGF-1R agonist. Ginsenoside Rg5 compets for the binding site of IGF-1R and blocks the binding of IGF-1 to IGF-1R (IC50 about 90 nM). Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.[1-3] |
| In Vitro |
Ginsenoside Rg5 是 IGF-1R 激动剂。Ginsenoside Rg5 具有血管生成活性，可被 IGF-1R 敲低抑制。为了研究人参皂苷 Rg5 与 IGF-1R 可能的相互作用，进行了对接分析。对接结果表明，人参皂苷 Rg5 在 A 和 B 两个位点与 IGF-1R 富含半胱氨酸的结构域结合，Kd 值分别为 20 和 27 nM。用 Rg5 预处理可阻断放射性标记的 IGF-1 与 HUVEC 的结合，IC50 值为~90 μM，大于 IC50 值~1.4 nM未标记的 IGF-1[1]。MTT 法结果显示人参皂苷 Rg5 处理 24、48 和 72 小时后，MCF-7 细胞增殖受到剂量依赖性抑制。不同浓度 (0、25、50 和 100 μM) 的 Ginsenoside Rg5 通过调节 MCF-7 细胞周期相关蛋白诱导细胞周期停滞于 G0/G1 期[3]。 |
| In Vivo |
Ginsenoside Rg5 通过抑制脂多糖 (LPS) 刺激的 BV2 小胶质细胞中 NF-κB p65 的 DNA 结合活性来抑制 COX-2 的 mRNA 表达。Rg5 预处理组小鼠的 NF-κB p65 和 COX-2 表达下降。在低剂量 Ginsenoside Rg5 (10mg/kg) 处理组中，肾小管损伤明显，炎症细胞浸润。然而，在较高剂量的人参皂苷 Rg5 (20 mg/kg) 下，肾小管在组织学上明显正常，在肾组织中未观察到炎症和管型形成[2]。 |
| 细胞实验 |
MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) human breast cancer cell lines are maintained using RPMI 1640 medium supplemented with 10% (vol/vol) FBS plus 100 units/mL Penicillin and Streptomycin in a 5% carbon dioxide air incubator at 37°C. Cell cytotoxicity is measured by MTT assay. Cells are seeded in 96-well tissue culture plates at the density of 0.2×104 cells per well with 100 μL medium， and are allowed to become attached for 24 h. One hundred microliters of the medium with different concentrations of Ginsenoside Rg5 (e.g.， 0 μM， 25 μM， 50 μM， and 100 μM) are added to each well. At indicated times， 30 μL MTT stock solution (3 mg/mL) are added to each well. After culturing the cells at 37°C for 2 h， DMSO is added to dissolve the formazan crystals. The absorbance is read at the wavelength of 540 nm with a microplate reader[3]. |
| 动物实验 |
Mice[2]Male ICR mice (6 to 8 weeks old)， weighing 25-27 g， are used. After acclimation for one week， mice are randomly assigned into 4 experimental groups with 8 mice in each group: normal control， Cisplatin control， and Cisplatin+Ginsenoside Rg5 groups (10 and 20 mg/kg， respectively). Ginsenoside Rg5 is administered intragastrically at the dose of 10 and 20 mg/kg for 10 days. On the 7th day， animals in Cisplatin control and Ginsenoside Rg5-treated groups receive a single intraperitoneal injection of Cisplatin (25 mg/kg) to induce nephrotoxicity in mice. Mice are anaesthetized with pentobarbital， subsequently sacrificed at 72 h after Cisplatin injection (Day 10). Blood samples are collected and then centrifuged at 3000 rpm to separate the serum and stored at -20 °C for determining blood urea nitrogen (BUN) and creatinine (CRE) levels. |
| 激酶实验 |
HUVECs are cultured in 24-well plates overnight. The cells are changed to serum-free M199 and incubated for 1 h. The medium is removed， and cells are incubated with fresh serum-free medium containing 0.1 μM-50 mM Ginsenoside Rg5 at 37°C for 20 min followed by the addition of 50 μL (1 μCi) of [125I]IGF-1 and then further incubated for 10 min. The medium is decanted， and cell plates are washed twice with serum-free medium. Cells are lysed in 300 μL of 0.1 N NaOH solution containing 0.1% SDS， transferred to scintillation vials， and mixed with 1 mL of Ultima Gold mixture solution. Cell-associated [125I]IGF-1 is analyzed in a scintillation counter. The nonspecific binding is determined by coincubation with unlabeled IGF-1 (50 nM)[1]. |
| 数据来源文献 |
[1]. Cho YL， et al. Specific activation of insulin-like growth factor-1 receptor by ginsenoside Rg5 promotes angiogenesis and vasorelaxation. J Biol Chem. 2015 Jan 2;290(1):467-77.
[2]. Li W， et al. Ginsenoside Rg5 Ameliorates Cisplatin-Induced Nephrotoxicity in Mice through Inhibition of Inflammation， Oxidative Stress， and Apoptosis. Nutrients. 2016 Sep 13;8(9). pii: E566.
[3]. Kim SJ， et al. Anti-breast cancer activity of Fine Black ginseng (Panax ginseng Meyer) and ginsenoside Rg5. J Ginseng Res. 2015 Apr;39(2):125-34. |
| 规格 |
1mg 5mg 10mg |
| 单位 |
瓶 |
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