2-Deoxy-D-glucose (2-DG) 是一种葡萄糖类似物,为葡萄糖代谢抑制剂,通过作用于己糖激酶 (hexokinase) 来抑制糖酵解 (glycolysis)。可用于小鼠多能干细胞的诱导和维持,以及癫痫的相关研究。
Cell Death Dis. 2025 Aug 12;16(1):613.
Commun Biol. 2025 Aug 30;8(1):1314.
Mol Med Rep. 2025 Aug 29;32(5):301.
J Transl Med. 2024 Aug 12;22(1):754.
Transl Cancer Res. 2023 Oct 31;12(10):2823-2836.
Front Immunol. 2021 Feb 25;12:620365.
Circulating Neutrophil Dysfunction in HBV-Related Acute-on-Chronic Liver Failure
Redox Biol. 2020 Oct;37:101761.
Cell Death Dis. 2020 Oct 23;11(10):902.
| 分子量 | 164.16 |
| 分子式 | C6H12O5 |
| CAS号 | 154-17-6 |
| 中文名称 | 2-脱氧-D-葡萄糖 |
| 溶解性(仅列举部分溶剂) | Water 30 mg/mL DMSO 15 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
| 运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*不同实验中用到的溶剂可能不同,具体实验所需溶剂及溶解方法请参考相关文献描述。
2-Deoxy-D-glucose (2-DG) 是一种葡萄糖类似物,为葡萄糖代谢抑制剂,通过作用于己糖激酶 (hexokinase) 来抑制糖酵解 (glycolysis)。在所有 16 种肿瘤细胞系中,DG 摄取量与 3-O-MG 转运之间有明显的相关性(p = 0.0012,F 检验),但 DG 摄取量与己糖激酶活性之间没有相关性。肿瘤细胞的己糖激酶活性与处于指数生长期的人类成纤维细胞相当。胰岛素(ED(50) = 0.6 mU/ml)能以剂量依赖的方式增加离体大鼠比目鱼肌中经 2-脱氧葡萄糖(2DG)培养后的 2DG6P 含量,最大反应量约为体外基础含量的 5 倍。2-DG increased mitochondrial dysfunction and upregulated Bax/Bcl-2, promoting cytochrome c release to initiate procaspase 3 cleavage induced by buforin IIb.
2-DG plus BCNU significantly suppressed tumor growth with lower side effects compared with BCNU alone in tumor-bearing mice. 2-DG also exerts anticonvulsant effects in vivo against perforant path kindling in rats.
Rats fed the 2-DG diet exhibited significant reductions in resting BP, attenuated BP responses during stress, and accelerated recovery to baseline after stress. Plasma concentrations of ACTH and corticosterone were elevated under nonstress conditions in rats fed the 2-DG diet and exhibited differential responses to single (enhanced response) and multiple (reduced response) stress sessions compared with rats fed control rat chow ad libitum. The 2-DG diet improved glucose metabolism, as indicated by decreased concentrations of blood glucose and insulin under nonstress conditions, but glucose and insulin responses to stress were maintained.
DEN and 2-DG model in the rat
Male 10–12 week old Sprague Dawley rats, weighing 220–240 g were maintained at an animal facility under pathogen-free conditions. To induce HCC, N-diethylnitrosamine (DEN) at a dilution of 1/10,000 (95 mg/l), was added to the drinking water of rats for 13 weeks. Subsequently, the water was replaced by normal sterile water and certain rats received 0.75 g/kg 2-DG, dissolved in normal saline solution via intraperitoneal (IP) injection once every 3 days until the end of the 17th week after initial DEN administration. A total of 30 rats (control group, n=5; 2-DG group, n=5; DEN group, n=10; DEN+2-DG group, n=10) were kept and assessed for survival time and 20 rats (DEN group, n=10; DEN+2-DG group, n=10) were sacrificed through cervical dislocation at 17 weeks in order to observe their primary liver tumors. The tumors were measured with a micrometer up to a maximum diameter of 3 mm. The tumor volumes were calculated using the following formula: Volume=axb2/2 (‘a’ is the maximal diameter and ‘b’ was the minimal diameter).
https://www.spandidos-publications.com/mmr/11/3/1917
2-DG in an Animal Model With CIA
Bovine type II collagen (2 mg/ml) was mixed with complete Freund's adjuvant (2 mg/ml) at a one to one ratio. One hundred microliters of emulsion was injected intradermally into six-week-old Sprague–Dawley (SD) rats at the tail root (n=12). One week later, these rats received an intradermal booster injection with 100 μL of emulsion of bovine type II collagen and incomplete Freund's adjuvant at a one to one ratio. Other rats injected with phosphate-buffered saline (PBS) were used as healthy controls (n=12). An aqueous solution of 2-DG (100 mg/mL) was prepared by dissolving 0.1 g of 2-DG powder in sterile water and was intraperitoneally injected on 3 day before the first injection of collagen. Those rats receiving collagen injections were intraperitoneally administered PBS (n=6) or 2-DG (n=6) (50 mg/kg) twice per week (a total of 6 times, once every 3.5 days). Additionally, those healthy rats receiving the PBS injection in place of collagen were simultaneously treated with 2-DG as a control (n=6). Clinical arthritis scores were calculated according to paw thickness measurements and histologic evidence. The rats were sacrificed on the 21 day after the first 2-DG injection. The hind paws of the rats were collected, fixed in 4% paraformaldehyde and embedded in paraffin for histochemical analysis.
https://pmc.ncbi.nlm.nih.gov/articles/PMC8440946/
下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 6.0916 mL | 30.4581 mL | 60.9162 mL |
| 5 mM | 1.2183 mL | 6.0916 mL | 12.1832 mL |
| 10 mM | 0.6092 mL | 3.0458 mL | 6.0916 mL |
*吸湿的DMSO对产品的溶解度有显著影响,请使用新开封的DMSO;
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。
| 细胞系 | T cells |
| 方法 | Activated T cells (1 × 10^6 cells/ml) were cultured with 2-DG (1 or 5 mM) or/and Rapamycin (100 nM) for 24 h. 2-DG and Rapamycin were dissolved in dimethylsulfoxide (DMSO). |
| 浓度 | 1 or 5 mM |
| 处理时间 | 24 h |
* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
建议您制定动物给药及实验方案时,尽量参考已发表的相关实验文献(溶剂种类及配比众多,简单地溶解目的化合物,并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题,未必能保证目的化合物在动物体内充分发挥生物学效用)。
体内实验的工作液,建议您现用现配,当天使用;如在配制过程中出现沉淀、析出现象,可以通过超声和(或)加热的方式助溶。
切勿一次性将产品全部溶解。
请在下面的计算器中,输入您的动物实验相关数据并点击计算,即可得到该实验的总需药量和工作液终浓度。
例如您给药剂量是10 mg/kg,平均每只动物的体重为20 g,每只动物的给药体积是100 μL,动物数量为20只,则该动物实验的总需药量为4 mg,工作液终浓度为2 mg/mL。
1:鉴于实验过程的损耗,建议您至少多配1-2只动物的量;
2:为该产品最终给药时的浓度。
| 动物模型 | Wild-type C57BL/6J mice |
| 配制 | Saline |
| 剂量 | 1000 mg/kg |
| 给药处理 | Intraperitoneally |
* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
一、2-Deoxy-D-glucose(2-DG)作用机制
2-DG(2-脱氧-D-葡萄糖,AbMole,M5140)在分子结构上与葡萄糖非常相似,仅在2号位缺失了一个氧原子。进入细胞后,可被己糖激酶磷酸化,生成的2-DG-6P不能像葡萄糖-6-磷酸那样顺利进入后续的糖酵解代谢途径,从而在细胞内积累。随着2-DG6P 浓度的升高,它会反馈性地抑制己糖激酶的活性,导致葡萄糖磷酸化受阻,进而抑制整个糖酵解过程。
图 1. Schematic showing the distribution of glycolytic enzymes in various subcellular compartments[1].
二、2-Deoxy-D-glucose(2-DG)的研究应用
1. 2-DG抑制细胞增殖与诱导凋亡
2-DG(2-脱氧-D-葡萄糖,AbMole,M5140)可显著抑制细胞增殖,并诱导细胞凋亡。2-Deoxy-D-glucose可抑制多种肿瘤细胞系的增殖,如胰腺癌细胞MIA PaCa2、BxP-3、ASPC-1,卵巢癌细胞OVCAR-3、HEY、SK-OV-3等。也有文献表明2-DG能够破坏线粒体膜电位,促进细胞色素c的释放,激活caspase-3,从而诱导细胞凋亡。
2. 2-DG用于代谢途径调控研究
2-DG(2-Deoxy-D-glucose,AbMole,M5140)常被用于研究细胞内代谢途径的调控网络。例如,在肿瘤细胞中,异常活跃的糖酵解是其重要的代谢特征之一。利用2-DG抑制肿瘤细胞的糖酵解后,可抑制肿瘤细胞的能量供应和相关代谢通路的变化,如乳酸代谢和肿瘤细胞中相关蛋白的乳酸修饰。通过此类研究,有助于开发针对肿瘤细胞异常代谢的干预策略。除了上述功能,2DG还会对细胞内的其他代谢途径产生影响。例如,研究发现2-DG处理细胞后,磷酸戊糖途径(PPP)代谢物的水平会增加。这是因为糖酵解受阻,细胞为了维持正常的代谢功能,会通过调节代谢途径,促
使葡萄糖-6-磷酸更多地流向PPP途径,以满足细胞对 NADPH 等物质的需求。2014年,AbMole的两款抑制剂分别被西班牙国家心血管研究中心和美国哥伦比亚大学用于动物体内实验,相关科研成果发表于顶刊 Nature 和 Nature Medicine。
3. 2-DG用于放射性示踪研究
2-DG(2-Deoxy-D-glucose,AbMole,M5140)可与核素结合,形成放射性示踪剂。通过正电子发射断层扫描(PET)技术,能够观察其在组织和器官中的分布情况。在科研中,这种放射性示踪方法被广泛应用于研究生物体内的葡萄糖代谢分布。例如,在研究动物模型的大脑葡萄糖代谢时,注射核素标记的2-DG后,利用 PET 成像可以清晰地显示不同脑区对葡萄糖类似物的摄取差异,从而了解大脑在不同生理状态下的能量代谢活跃区域。这对于研究神经系统疾病的发病机制、作用靶点以及大脑功能分区等方面具有重要意义。此外,在肿瘤研究中,肿瘤细胞通常具有比正常细胞更高的葡萄糖摄取能力,通过核素标记2-DG,能够更准确地定位动物实验中的肿瘤组织,评估肿瘤的生长和转移情况。
三、范例详解
1. J Transl Med. 2024 Aug 12;22(1):754.
上海交通大学、上海分子医学工程技术中心的科研人员在上述文章中以胃癌原发肿瘤、淋巴转移瘤为起始细胞,分别建立了肿瘤类器官模型(SPDO1P和SPDO1LM),通过STRs分析、核型分析、全外显子测序(WES)和单细胞转录组测序(scRNA-seq)等技术,对类器官模型进行了遗传和表型特征的分析。并使用CCK-8方法测试了类器官对氟尿嘧啶(5-Fu)、铂类和紫杉醇的敏感性。在实验中,科研人员发现SPDO1M类器官中存在过度激活的糖酵解通路,并使用AbMole的2-Deoxy-D-glucose(2-DG,AbMole,M5140)处理SPDO1M类器官,结果表明2-Deoxy-D-glucose可抑制类器官细胞的糖酵解和乳酸的产生[2]。
图 2The lactate concentrations of both organoids significantly declined upon 2-deoxy-D-glucose (DG, 1 mM, 72 h) treatment[2].
2. Front Immunol. 2021 Feb 25;12:620365.
浙江大学的科研人员在上述研究中探讨了中性粒细胞在急性慢性肝衰竭(ACLF)模型中的作用,并研究了中性粒细胞的数量、表型、转录组和功能的变化与ACLF短期预后的关系。科研人员还发现上述模型中性粒细胞的吞噬、脱颗粒、NET(Neutrophil Extracellular Trap,中性粒细胞胞外陷阱)形成和细胞因子产生等功能存在异常变化。因此,实验人员探讨了代谢重编程是否能够逆转中性粒细胞的功能异常,在实验中使用了来自AbMole的2-Deoxy-D-glucose(2-DG,AbMole,M5140)抑制糖酵解[3]。
图 3. The effect of glycolysis inhibition on neutrophil extracellular trap (NET) formation[3].
参考文献及鸣谢
[1] Shanmugasundaram Ganapathy-Kanniappan, Jean-Francois H. Geschwind, Tumor glycolysis as a target for cancer therapy: progress and prospects, Molecular cancer 12(1) (2013) 152.
[2] R. Yang, Y. Qi, W. Kwan, et al., Paired organoids from primary gastric cancer and lymphatic metastasis are useful for personalized medicine, Journal of translational medicine 22(1) (2024) 754.
[3] W. Wu, S. Sun, Y. Wang, et al., Circulating Neutrophil Dysfunction in HBV-Related Acute-on-Chronic Liver Failure, Frontiers in immunology 12 (2021) 620365.
以上参考文献由AI整理,仅供参考,AbMole 尚未独立确认这些文献的准确性。