Auranofin
(Synonyms: 醋硫葡金; SKF-39162) 目录号 : GC15905
Auranofin是一种高效的硫氧还蛋白还原酶（TrxR）抑制剂（IC50 = 0.2μM）。
Cas No.:34031-32-8
Sample solution is provided at 25 µL, 10mM.
Auranofin is a highly effective thioredoxin reductase (TrxR) inhibitor (IC50 = 0.2μM) [1]. Auranofin binds to the selenocysteine residue embedded in the active site of TrxR through gold ions, inhibiting the activity of this key antioxidant enzyme, resulting in decreased intracellular reducing capacity and increased oxidative stress, which in turn activates signaling pathways such as mitochondria and nuclear factor κB, inducing cell apoptosis [2-3]. Auranofin is commonly used to treat rheumatoid arthritis [4].
In A549 cells, Treatment with different concentrations of Auranofin (0-5μM; 24h) inhibited cell proliferation in a dose-dependent manner [5]. In Calu3 and HCC366 cells, treatment with Auranofin (0.5μM; 24h, 48h) induces massive cell death or apoptosis [6]. In NCI-H460 and NCI-H1299 cells, Auranofin (0-5μM; 24h) inhibited cell growth in a dose-dependent manner [7].
In C. difficile infection (CDI) mouse model, Auranofin (0.125mg/kg, 0.25mg/kg, 0.5mg/kg; po; 5d) significantly prevented CDI recurrence [8]. In mice with diet-induced obesity model, Auranofin (1mg/kg; ip; 4 weeks) exerts antidiabetic effects [9]. In MiaPaCa-2 pancreatic tumors mouse model, Auranofin (5mg/kg, 10mg/kg, 15mg/kg; ip; 21d) presents a survival advantage in nude mice with MiaPaCa-2 pancreatic tumors and inhibits metastasis in a dose-dependent fashion [10].
References:
[1]. Davis P. Auranofin. Clinics in Rheumatic Diseases. 1984 Aug 1;10(2):369-383.
[2]. Shen S, Shen J, Luo Z, et al. Molecular mechanisms and clinical implications of the gold drug auranofin. Coordination Chemistry Reviews. 2023 Oct 15; 493: 215323.
[3]. Madeira JM, Gibson DL, Kean WF, et al. The biological activity of auranofin: implications for novel treatment of diseases. Inflammopharmacology. 2012 Dec; 20: 297-306.
[4]. Finkelstein AE, Walz DT, Batista V, et al. Auranofin. New oral gold compound for treatment of rheumatoid arthritis. Annals of the rheumatic diseases. 1976 Jun 1; 35(3): 251-257.
[5]. Cui XY, Park SH, Park WH. Anti-cancer effects of auranofin in human lung cancer cells by increasing intracellular ROS levels and depleting GSH levels. Molecules. 2022 Aug 15; 27(16): 5207.
[6]. Li H, Hu J, Wu S, et al. Auranofin-mediated inhibition of PI3K/AKT/mTOR axis and anticancer activity in non-small cell lung cancer cells. Oncotarget. 2015 Dec 9; 7(3): 3548.
[7]. Cui XY, Park SH, Park WH. Auranofin inhibits the proliferation of lung cancer cells via necrosis and caspase-dependent apoptosis. Oncology Reports. 2020 Dec; 44(6): 2715-2724.
[8]. Abutaleb NS, Seleem MN. Auranofin, at clinically achievable dose, protects mice and prevents recurrence from Clostridioides difficile infection. Scientific reports. 2020 May 7; 10(1): 7701.
[9]. Cox AR, Masschelin PM, Saha PK, et al. The rheumatoid arthritis drug auranofin lowers leptin levels and exerts antidiabetic effects in obese mice. Cell metabolism. 2022 Dec 6; 34(12): 1932-1946.
[10]. Perez MV, Roife D, Dai B, et al. Antineoplastic effects of auranofin in human pancreatic adenocarcinoma preclinical models. Surgery Open Science. 2019 Oct 1; 1(2): 56-63.
Auranofin是一种高效的硫氧还蛋白还原酶（TrxR）抑制剂（IC50 = 0.2μM） [1]。Auranofin通过金离子与TrxR活性位点的硒代半胱氨酸残基结合，抑制这种关键抗氧化酶的活性，导致细胞内还原能力下降、氧化应激增强，进而激活线粒体和核因子κB等信号通路，诱导细胞凋亡 [2-3]。Auranofin常用于治疗类风湿性关节炎 [4]。
在A549细胞中，不同浓度的Auranofin（0-5μM；24h）处理以剂量依赖性方式抑制细胞增殖 [5]。在Calu3和HCC366细胞中，Auranofin（0.5μM；24h，48h）处理可诱导大量细胞死亡或凋亡 [6]。在NCI-H460和NCI-H1299细胞中，Auranofin（0-5μM；24h）以剂量依赖性方式抑制细胞生长 [7]。
在艰难梭菌感染（CDI）小鼠模型中，Auranofin（0.125mg/kg，0.25mg/kg，0.5mg/kg；po；5d）显著预防CDI复发 [8]。在饮食诱导的肥胖小鼠模型中，Auranofin（1mg/kg；ip；4周）具有抗糖尿病作用 [9]。在MiaPaCa-2胰腺肿瘤小鼠模型中，Auranofin（5mg/kg，10mg/kg，15mg/kg；ip；21d）在MiaPaCa-2胰腺肿瘤裸鼠中表现出生存优势，并以剂量依赖性方式抑制肿瘤转移 [10]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | 1 × 106 cells per well were seeded into 60mm culture dishes for cell counting. After exposure to the indicated concentrations of Auranofin for 24h at 37℃ incubation, the cells were subjected to trypan blue staining. For all experimental conditions, three replicates were used, and the experiment was performed at least twice. |
Reaction Conditions | 0-5μM; 24h |
Applications | Treatment with different concentrations of Auranofin for 24h significantly reduced the number of viable cells and increased the number of dead cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C. difficile infection (CDI) mouse model |
Preparation Method | Following infection, mice were randomly allocated into groups (n = 5) for treatment. Two hours post-infection, three groups were treated orally with Auranofin (0.125mg/kg, 0.25mg/kg and 0.5mg/kg), one group was treated with vancomycin (10mg/kg) via oral gavage, and one group was treated orally with the vehicle (10% DMSO in PBS). Treatments were continued once daily for five days and mice were checked (6 times daily) for disease signs (including weight loss, behavioral changes, hunched posture, decreased activity, wet tail and diarrhea). |
Dosage form | 0.125mg/kg, 0.25mg/kg, 0.5mg/kg; po; 5d |
Applications | Auranofin significantly prevented CDI recurrence. |
References: | |
| Cas No. | 34031-32-8 | SDF | |
| 别名 | 醋硫葡金; SKF-39162 | ||
| 化学名 | A name could not be generated for this structure. | ||
| Canonical SMILES | [S-][C@@H]1O[C@H](COC(C)=O)[C@@H]([C@@H]([C@H]1OC(C)=O)OC(C)=O)OC(C)=O.CCP(CC)CC.[Au+] | ||
| 分子式 | C20H34AuO9PS | 分子量 | 678.48 |
| 溶解度 | ≥ 67.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 1.4739 mL | 7.3694 mL | 14.7388 mL |
| 5 mM | 0.2948 mL | 1.4739 mL | 2.9478 mL |
| 10 mM | 0.1474 mL | 0.7369 mL | 1.4739 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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Quality Control & SDS
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- Purity: >98.00%
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