Ceftriaxone是一种具有广谱杀菌作用的β-内酰胺类抗生素，对多种革兰氏阴性和阳性菌有良好的抗菌活性。
Cas No.:73384-59-5
Sample solution is provided at 25 µL, 10mM.
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Ceftriaxone is a β -lactam antibiotic with broad-spectrum bactericidal activity, which has good antibacterial activity against a variety of Gram-negative and Gram-positive bacteria. Ceftriaxone is used for a variety of infections such as community-acquired pneumonia, meningitis and gonorrhea. Ceftriaxone is a covalent inhibitor of Glycogen Synthase Kinase 3β (GSK3β), with an IC50 value of 0.78μM under the condition of 60 minutes preincubation. GSK3β is a serine/threonine kinase that has been suggested as a putative drug target for several diseases. In cancer, Ceftriaxone excerts antiproliferative, cell cycle arresting and apoptosis induction properties; in Alzheimer's Disease (AD), Ceftriaxone decreases amyloid-β peptide production and upregulate glutamate transporter-1 mediated by the inhibition of tau hyperphosphorylation[1][2].
In vitro, treatment with 500-1000μM Ceftriaxone for 10 days (A549), 7 days (H520), or 14 days (H1650) resulted in a significant and dose-dependent reduction in colony formation by targeting Aurora B[2]. Ceftriaxone (100μg/mL; 3h) upregulated NOD-like receptor family pyrin domain containing 3 (NLRP3) and pro-caspase-1 transcription but attenuated NLRP3 protein expression in LPS-induced A549 and PC3 cells[4].
In vivo, Ceftriaxone (100mg/kg; i.p.; three times a week) significantly slowed tumor growth and reduced tumor size in athymic nude mice bearing A549 (57d) or H520 (32d) xenografts by inhibiting Aurora B activity[2]. Ceftriaxone (200mg/kg/d; i.p.; 6w) improved functional indicators, oxidative stress, and inflammatory parameters in the D-galactose (DGL)-induced liver and kidney injury rat model[3].
References:
[1] Nassar H, Sippl W, Dahab RA, Taha M. Molecular docking, molecular dynamics simulations and in vitro screening reveal cefixime and ceftriaxone as GSK3β covalent inhibitors. RSC Adv. 2023;13(17):11278-11290.
[2] Li X, Li H, Li S, et al. Ceftriaxone, an FDA-approved cephalosporin antibiotic, suppresses lung cancer growth by targeting Aurora B. Carcinogenesis. 2012;33(12):2548-2557.
[3] Hakimizadeh E, et al. Ceftriaxone improves hepatorenal damages in mice subjected to D-galactose-induced aging. Life Sci. 2020 Oct 1;258:118119.
[4] Tezcan G, Alsaadi M, Hamza S, Garanina EE, Martynova EV, Ziganshina GR, Farukshina ER, Rizvanov AA, Khaiboullina SF. Azithromycin and Ceftriaxone Differentially Activate NLRP3 in LPS Primed Cancer Cells. International Journal of Molecular Sciences. 2022; 23(16):9484.
Ceftriaxone是一种具有广谱杀菌作用的β-内酰胺类抗生素，对多种革兰氏阴性和阳性菌有良好的抗菌活性。Ceftriaxone用于治疗多种感染，如社区获得性肺炎、脑膜炎和淋病。Ceftriaxone是糖原合成酶激酶3β（GSK3β）的一种共价抑制剂，在60分钟的预孵育条件下，其IC50值为0.78μM。GSK3β是一种丝氨酸/苏氨酸激酶，已被认为是多种疾病潜在的药物靶点。在癌症领域，Ceftriaxone具有抗增殖、细胞周期停滞和诱导细胞凋亡的特性；在阿尔茨海默病（AD）方面，Ceftriaxone能够减少β-淀粉样肽的生成，并通过抑制tau蛋白的过度磷酸化而上调谷氨酸转运蛋白-1的表达[1][2]。
体外实验中，500-1000μM的Ceftriaxone处理10天（A549），7天（H520）或14天（H1650），通过靶向Aurora B，以剂量依赖性显著抑制细胞集落形成[2]。Ceftriaxone（100μg/mL, 3h）在LPS诱导的A549和PC3细胞中上调NOD样受体家族含pyrin结构域蛋白3（NLRP3）和caspase-1的无活性酶原前体（pro-CASP1）转录，但降低NLRP3蛋白表达[4]。
Ceftriaxone（100mg/kg；i.p.；每周3次）通过抑制Aurora B活性显著减缓A549（57天）或H520（32天）异种移植裸鼠的肿瘤生长并缩小肿瘤大小[2]。Ceftriaxone （200mg/kg/d；i.p.；6周）能改善D-半乳糖（DGL）诱导的大鼠肝肾损伤模型的功能指标、氧化应激和炎症参数[3]。
| Kinase experiment [1]: | |
Preparation Method | Ceftriaxone was dissolved in 100% (v/v) DMSO to form a 10mM stock solution (2ml). Ceftriaxone was initially screened at 100μM against GSK3β. The bioassay was conducted in black 384-well plates. For testing Ceftriaxone, 100nl of the stock solution (10mM) was mixed with 5μl of the peptide/kinase mixture, 2.4μl of the kinase buffer (50mM HEPES pH 7.5, 0.01% BRIJ-35, 10mM MgCl2, 1mM EGTA) and 2.5μl of the ATP solution. The final 10μl kinase reaction included the tested cephalosporin concentration (100μM), 1% (v/v) DMSO, kinase peptide substrate and 25μM ATP in 50mM HEPES pH 7.5, 0.01% BRIJ-35,10mM MgCl2, and 1mM EGTA. The mixture was shaken for 30s then incubated at room temperature for 60min to complete the kinase reaction. Subsequently, 5μl of the development reagent solution was added to each reaction mixture, shaken for 30s and left for another 60min at room temperature. Ultimately, fluorescence emissions were measured at λex of 445 and λem of 520nm. To assess the potential of Ceftriaxone to irreversibly inhibit GSK3β, it was initially incubated at 10μM with the kinase for 60min before adding the ATP solution. |
Reaction Conditions | 100μM; 30s+60min or 60min+60min |
Applications | Ceftriaxone resulted in more than 60% inhibition and were considered for further screening to calculate its IC50 value. The IC50 value for GSK3β without preincubation is 7.35μM. After 60 minutes preincubation with GSK3β, the IC50 value decreased to 0.78μM. |
| Cell experiment [2]: | |
Cell lines | A549, H520 and H1650 cells |
Preparation Method | Cells were cultured with different concentrations of Ceftriaxone for 10 days (A549), 7 days (H520) or 14 days (H1650) and then colonies were counted. |
Reaction Conditions | 500 or 1000μM; 7, 10 or 14d |
Applications | A549, H520 or H1650 cells treated with Ceftriaxone had a significant reduction in colony formation compared with untreated control cells. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice (Cr:NIH(S), NIH Swiss nude, 6–9 weeks old) |
Preparation Method | Mice were randomly divided into three groups: (i) vehicle group; (ii) 100mg/kg Ceftriaxone-treated group; (iii) no cells-injected group. Treated with 100mg/kg Ceftriaxone A549 or H520 cells were inoculated subcutaneously (2×106 cells) into the left flank of each mouse in the first two groups. Treatment was started when the tumors reached a mean tumor volume of 100mm3. For the Ceftriaxone group, 2.5mg Ceftriaxone, formulated in 500µl physiological saline, was administered to each mouse three times per week by intraperitoneal (i.p.) injection. For the vehicle group, 500µl physiological saline was administered to each mouse three times per week by i.p. injection. The duration of the animal study was 57 days for A549 cells and 32 days for H520 cells. |
Dosage form | 100mg/kg; 3 times a week; i.p. |
Applications | The tumors treated with 100mg/kg Ceftriaxone grew significantly more slowly and the sizes of the tumors were smaller compared with the vehicle group. Expression of phosphorylated histone H3 was substantially decreased in the ceftriaxone-treated group compared with the vehicle group. Ceftriaxone suppressed tumor growth by inhibiting Aurora B activity in vivo. |
References: | |
| Cas No. | 73384-59-5 | SDF | |
| 别名 | 头孢曲松 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC(N(C)NC3=O)=NC3=O)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)O | ||
| 分子式 | C18H18N8O7S3 | 分子量 | 554.58 |
| 溶解度 | DMSO:≥100mg/mL | 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 | 1.8032 mL | 9.0158 mL | 18.0317 mL |
| 5 mM | 360.6 μL | 1.8032 mL | 3.6063 mL |
| 10 mM | 180.3 μL | 901.6 μL | 1.8032 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） | ||||||||||
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % 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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