Dexamethasone Sodium Phosphate
(Synonyms: 地塞米松磷酸钠) 目录号 : GC16239
Dexamethasone Sodium Phosphate是一种糖皮质激素，也是白细胞介素受体抑制剂，抑制环氧化酶-2（COX-2）的IC50值为7.3μM。
Cas No.:55203-24-2
Sample solution is provided at 25 µL, 10mM.
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Dexamethasone Sodium Phosphate is a glucocorticoid and an interleukin receptor inhibitor. The IC50 value for inhibiting cyclooxygenase-2 (COX-2) is 7.3μM [1-2]. COX is an enzyme in the prostaglandin-prostaglandin-prostanoid pathway, and the expression of COX-2 can be induced by inflammatory stimuli or mutagens, inflammatory cytokines, and transcription factor CCAAT enhancer binding protein (c/EBP) β [3]. Dexamethasone Sodium Phosphate has been used to treat various inflammatory diseases, arthritis, and endocrine disorders [4].
In vitro, in the presence of cytokines and basic fibroblast growth factor (bFGF), Dexamethasone Sodium Phosphate (1-1000nM; 24h) can increase DNA synthesis in airway smooth muscle cells (ASM) in a concentration-dependent manner [5]. Dexamethasone Sodium Phosphate (0.1-100μM; 24h) treatment of human lens epithelial cells (HLEC) promotes HLEC cell proliferation at a concentration of 0.1μM, while at concentrations of 1-100μM, it increases cell apoptosis in a dose-dependent manner [6].
In vivo, oral administration of Dexamethasone Sodium Phosphate (0.075 and 0.15mg/kg/day; 4 weeks;) can significantly improve the rigidity state of Parkinsonian rats in a concentration-dependent manner [7]. Dexamethasone Sodium Phosphate (5 and 10mg/kg/day; 7 days; i.p.) treatment of mice with acute lung injury (ALI) induced by lipopolysaccharide (LPS) significantly reduces the expression of COX-2, iNOS, and NF-κB p65 in mice, lowers the levels of malondialdehyde (MDA) and myeloperoxidase (MPO) activity, increases the content of glutathione (GSH), and has an effective anti-inflammatory effect [8].
References:
[1] Hui, B., Yao, X., Zhang, L., et al. Naunyn Schmiedebergs Arch. Pharmacol. 393(9), 1761-1768 (2020) .
[2] Blanco FJ, Guitian R, Moreno J, de Toro FJ, Galdo F. Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes. J Rheumatol. 1999;26(6):1366-1373.
[3] Ristimäki A, Narko K, Hla T. Down-regulation of cytokine-induced cyclo-oxygenase-2 transcript isoforms by dexamethasone: evidence for post-transcriptional regulation[J]. Biochemical Journal, 1996, 318(1): 325-331.
[4] Tsao P W, Suzuki T, Totsuka R, et al. The effect of dexamethasone on the expression of activated NF-κB in adjuvant arthritis[J]. Clinical immunology and immunopathology, 1997, 83(2): 173-178.
[5] Vlahos R, Stewart AG. Interleukin-1alpha and tumour necrosis factor-alpha modulate airway smooth muscle DNA synthesis by induction of cyclo-oxygenase-2: inhibition by dexamethasone and fluticasone propionate. Br J Pharmacol. 1999;126(6):1315-1324.
[6] Petersen A, Carlsson T, Karlsson J O, et al. Effects of dexamethasone on human lens epithelial cells in culture[J]. Molecular vision, 2008, 14: 1344.
[7] Ardestani M S, Mehrab H, Sadeghzadeh N. Effects of dexamethasone and betamethasone as COX-2 gene expression inhibitors on rigidity in a rat model of Parkinson′ s disease[J]. Indian Journal of Pharmacology, 2007, 39(5): 235-239.
[8] Al-Harbi N O, Imam F, Al-Harbi M M, et al. Dexamethasone attenuates LPS-induced acute lung injury through inhibition of NF-κB, COX-2, and pro-inflammatory mediators[J]. Immunological Investigations, 2016, 45(4): 349-369.
Dexamethasone Sodium Phosphate是一种糖皮质激素，也是白细胞介素受体抑制剂，抑制环氧化酶-2（COX-2）的IC50值为7.3μM [1-2]。COX是前列腺素-前列环素-血栓素途径中的一种酶，COX-2的表达可以通过炎症刺激或诱变剂、炎症性细胞因子和转录因子CCAAT增强子结合蛋白（c/EBP）β诱导 [3]。Dexamethasone Sodium Phosphate已被用于治疗各种炎症性疾病、关节炎和内分泌紊乱 [4]。
在体外，在细胞因子和碱性成纤维细胞生长因子（bFGF）存在下，Dexamethasone Sodium Phosphate（1-1000nM; 24h）能够以浓度依赖性方式增加人气道平滑肌细胞（ASM）的DNA合成 [5]。Dexamethasone Sodium Phosphate（0.1-100μM; 24h）处理人晶状体上皮细胞（HLEC），在0.1μM浓度下促进HLEC细胞增殖，而在1-100μM浓度下以剂量依赖性方式增加了细胞凋亡 [6]。
在体内，Dexamethasone Sodium Phosphate（0.075和0.15mg/kg/day; 4 weeks; ）口服治疗能够以浓度依赖性方式显著改善帕金森大鼠的强直状态 [7]。Dexamethasone Sodium Phosphate（5和10mg/kg/day;7 days; i.p.）治疗脂多糖（LPS）诱导的急性肺损伤（ALI）小鼠，显著降低了小鼠COX-2、iNOS和NF-κB p65的表达，降低丙二醛（MDA）水平和髓过氧化物酶（MPO）活性，增加了谷胱甘肽（GSH）含量，具有有效的抗炎作用 [8]。
| Cell experiment [1]: | |
Cell lines | Human lens epithelial cells (HLECs) |
Preparation Method | HLECs were subcultured in medium RPMI-1640 with 10% fetal calf serum, 100U/ml penicillin, 0.1mg/ml streptomycin, and 2mM L-glutamine in a white 96 well plate with a transparent bottom with approximately 105 cells per well to yield a confluent monolayer. Cells were exposed to Dexamethasone Sodium Phosphate for 24h. After subsequent rinsing in PBS, the cells were fixed in 4% paraformaldehyde (pH 7.4). The cells were rinsed in PBS and permeabilized by digitonin (30µg/ml in PBS for 10min at room temperature). The cells were marked with monoclonal mouse anti-proliferating cell protein, Ki-67, and visualized by streptavidin-FITC. The cells were viewed using a fluorescence microscope, and the Ki-67 positive cells were counted. |
Reaction Conditions | 0.1-100μM; 24h |
Applications | At a concentration of 0.1μM, Dexamethasone Sodium Phosphate promoted the proliferation of HLEC cells, while at concentrations ranging from 1 to 100μM, it increased cell apoptosis in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Each rat was anesthetized separately by intraperitoneal injection of 75mg/kg of ketamine combined with 8mg/kg xylazine and placed them in the stereotaxic instrument. By using an electrical injury device to apply an electric current (1mA, 8s) to the left substantia nigra compact part (SNc) of the substantia nigra of the black striatum, Parkinson's disease and its related symptoms were triggered. After recovery from surgery (after 7-10 days) all animals received daily oral Dexamethasone Sodium Phosphate for four weeks-either dexamethasone (0.075 or 0.15mg/kg). Measure the rigidity of the animals 12h after the last oral administration of drug or vehicle; the measurements were made at the following time points: 0, 20, 40, 60, 90, 120, 180 and 240min. |
Dosage form | 0.075 and 0.15mg/kg/day; 4 weeks; oral |
Applications | Dexamethasone Sodium Phosphate can significantly improve the rigidity state of Parkinson's rats in a concentration-dependent manner. |
References: | |
| Cas No. | 55203-24-2 | SDF | |
| 别名 | 地塞米松磷酸钠 | ||
| 化学名 | disodium;[2-[(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] phosphate | ||
| Canonical SMILES | CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)COP(=O)([O-])[O-])O)C)O)F)C.[Na+].[Na+] | ||
| 分子式 | C22H30FO8P.2Na | 分子量 | 516.4 |
| 溶解度 | ≥ 51.6mg/mL in Water, <5.16mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9365 mL | 9.6824 mL | 19.3648 mL |
| 5 mM | 387.3 μL | 1.9365 mL | 3.873 mL |
| 10 mM | 193.6 μL | 968.2 μL | 1.9365 mL |
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