6-Shogaol是生姜中的一种活性物质，具有抗炎、抗肿瘤和抗氧化作用。
Cas No.:555-66-8
Sample solution is provided at 25 µL, 10mM.
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6-Shogaol, an active substance from ginger, has anti-inflammatory, anti-tumor, and anti-oxidative effects [1]. 6-shogaol inhibits AKT kinase activity by binding to the variable configuration site of Akt, thereby inducing cleavage of the apoptosis markers Caspase-3 and Caspase-7 [2]. 6-Shogaol has been widely used in different cell and animal models to inhibit tumor progression and to develop novel combination therapies to eliminate tumor drug resistance[3].
In vitro, 6-Shogaol treatment for 72 hours significantly inhibited the proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 value of 8µM[4]. Treatment with 50µM 6-Shogaol for 24h induced apoptosis in HepG2 and Huh-7 cells, accompanied by nuclear volume reduction, chromatin condensation, and aggregation at the edge of the nuclear membrane, and totally fragmented nuclear bodies[5]. Treatment with 10μg/ml 6-Shogaol for 24 hours blocked the G2/M phase progression of NCI-H226 cells and promoted caspase cascade to induce apoptosis[6].
In vivo, 6-Shogaol via intraperitoneal administration at a daily dose of 50mg/kg for 12 weeks significantly reduced body weight, reduced fasting blood glucose and serum insulin levels, and alleviated kidney pathological damage in C57BL/KsJ db/db obese mice[7]. Oral administration of 6-Shogaol at 1mg/kg/day for 8 weeks significantly reduced pressure overload-induced cardiac hypertrophy and systolic dysfunction in mice[8].
References:
[1] Li F, Nitteranon V, Tang X, et al. In vitro antioxidant and anti-inflammatory activities of 1-dehydro-[6]-gingerdione, 6-shogaol, 6-dehydroshogaol and hexahydrocurcumin[J]. Food chemistry, 2012, 135(2): 332-337.
[2] Kim M O, Lee M H, Oi N, et al. [6]-Shogaol inhibits growth and induces apoptosis of non-small cell lung cancer cells by directly regulating Akt1/2[J]. Carcinogenesis, 2014, 35(3): 683-691.
[3] Jia Y, Li X, Meng X, et al. Anticancer perspective of 6-shogaol: anticancer properties, mechanism of action, synergism and delivery system[J]. Chinese Medicine, 2023, 18(1): 138.
[4] Bischoff-Kont I, Primke T, Niebergall L S, et al. Ginger constituent 6-shogaol inhibits inflammation-and angiogenesis-related cell functions in primary human endothelial cells[J]. Frontiers in pharmacology, 2022, 13: 844767.
[5] Wu J J, Omar H A, Lee Y R, et al. 6-Shogaol induces cell cycle arrest and apoptosis in human hepatoma cells through pleiotropic mechanisms[J]. European journal of pharmacology, 2015, 762: 449-458.
[6] Itharat A, Rattarom R, Hansakul P, et al. The effects of Benjakul extract and its isolated compounds on cell cycle arrest and apoptosis in human non-small cell lung cancer cell line NCI-H226[J]. Research in Pharmaceutical Sciences, 2021, 16(2): 129-140.
[7] Xu Y, Bai L, Chen X, et al. 6-Shogaol ameliorates diabetic nephropathy through anti-inflammatory, hyperlipidemic, anti-oxidative activity in db/db mice[J]. Biomedicine & Pharmacotherapy, 2018, 97: 633-641.
[8] Kawase Y, Sunagawa Y, Shimizu K, et al. 6-shogaol, an active component of ginger, inhibits P300 histone acetyltransferase activity and attenuates the development of pressure-overload-induced heart failure[J]. Nutrients, 2023, 15(9): 2232.
6-Shogaol是生姜中的一种活性物质，具有抗炎、抗肿瘤和抗氧化作用[1]。6-Shogaol通过与Akt的构象可变位点结合来抑制AKT激酶活性，从而诱导凋亡标志物Caspase-3和Caspase-7的裂解[2]。6-Shogaol已被广泛用于不同的细胞和动物模型，以抑制肿瘤进展并开发消除肿瘤耐药性的新型联合疗法[3]。
在体外，6-Shogaol处理72小时显著抑制了人脐静脉内皮细胞（HUVECs）的增殖，IC50值为8µM[4]。使用50µM的6-Shogaol处理24小时，诱导了HepG2和Huh-7细胞凋亡，伴随细胞核体积缩小、染色质浓缩并聚集于核膜边缘，以及核体完全碎裂[5]。使用10μg/ml的6-Shogaol处理24小时，阻断了NCI-H226细胞的G2/M期进程，并通过促进caspase级联反应诱导细胞凋亡 [6]。
在体内，每日腹腔注射50mg/kg剂量的6-Shogaol，持续12周，显著降低了C57BL/KsJ db/db肥胖小鼠的体重，减少了空腹血糖和血清胰岛素水平，并减轻了肾脏病理损伤[7]。每日口服1mg/kg剂量的6-Shogaol，持续8周，显著减轻了压力超负荷诱导的小鼠心脏肥大和收缩功能障碍[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum, 100units /ml penicillin, and 100µg/ml streptomycin at 37°C in a 5% CO2 incubator. HepG2 cells were seeded at a density of 5×103 cells/well in 96-well flat-bottom plates and cultured in DMEM medium containing 10% FBS for 24 hours. Cells were treated with different concentrations of 6-Shogaol (0, 5, 10, 25, 50, 100, and 200µM). The control group was treated with the same concentration of solvent (DMSO) as the drug treatment group, and the cell viability was detected after 24 hours. |
Reaction Conditions | 0, 5, 10, 25, 50, 100, and 200µM; 24h |
Applications | 6-Shogaol treatment decreased cell viability of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/KsJ db/db obese mice |
Preparation Method | Thirty male C57BL/KsJ db/db obese mice were housed in a specific pathogen-free (SPF) animal house maintained at 23°C with a 12h light/dark cycle and free access to water and food. The db/db mice (9 weeks old) with blood glucose levels>11.1mM, were randomly divided into 2 groups, 15 mice in each group: db/db group (DMSO saline group); 6-Shogaol group (50mg/kg/day). 6-Shogaol was dissolved in DMSO, diluted with saline, and injected intraperitoneally, and the animal experiment lasted for 12 weeks. At the end of the experiment, blood samples were collected, and kidney tissue was obtained for analysis. |
Dosage form | 50mg/kg/day for 12 weeks; i.p. |
Applications | 6-Shogaol treatment significantly reduced body weight, fasting blood glucose, and serum insulin levels, and alleviated kidney pathological damage in db/db mice. |
References: | |
| Cas No. | 555-66-8 | SDF | |
| 别名 | 姜烯酚; [6]-Shogaol; 6-Shogaol | ||
| 化学名 | (E)-1-(4-hydroxy-3-methoxyphenyl)dec-4-en-3-one | ||
| Canonical SMILES | CCCCCC=CC(=O)CCC1=CC(=C(C=C1)O)OC | ||
| 分子式 | C17H24O3 | 分子量 | 276.37 |
| 溶解度 | ≥ 27.6mg/mL in DMSO | 储存条件 | 4°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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6183 mL | 18.0917 mL | 36.1834 mL |
| 5 mM | 723.7 μL | 3.6183 mL | 7.2367 mL |
| 10 mM | 361.8 μL | 1.8092 mL | 3.6183 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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