Budesonide是一种具有高效局部抗炎作用的糖皮质激素。
Cas No.:51333-22-3
Sample solution is provided at 25 µL, 10mM.
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Budesonide is a glucocorticoid with potent local anti-inflammatory effects. Budesonide enhances the stability of endothelial cells, smooth muscle cells, and lysosomal membranes, inhibits immune responses, and reduces antibody synthesis, thereby decreasing the release and activity of allergic mediators such as histamine. Budesonide is used in the treatment of bronchial asthma, asthmatic chronic bronchitis, allergic rhinitis, nasal polyps, Crohn's disease, and ulcerative colitis[1-4].
In vitro, Budesonide (1μM–25μM) was used to treat LS180 and Caco-2 intestinal cell lines for 48h–72h. Budesonide induced the expression of MDR1/P-gp in LS180 cells and down-regulated the expression of MDR1/P-gp in Caco-2 cells[5]. Budesonide (0.1–25μM) was co-treated with SARS-CoV-2 (MOI=0.1) in Vero E6 cells for 24 hours. Budesonide significantly reduced the viral titer in Vero E6 cells without affecting cell viability[6].
In vivo, Budesonide (10mg/kg/day) was administered daily via oral gavage to female C57BL/6 mice for 5 days. Budesonide significantly increased the mortality rate in Clostridium difficile-infected mice[7]. Budesonide (1mg) combined with Calcitriol (100ng) was administered daily via nebulized inhalation and intraperitoneal injection to asthmatic model BALB/c mice for 8 weeks. Budesonide and Calcitriol synergistically inhibited airway remodeling in asthmatic mice[8].
References:
[1] Olivas I, Cobreros M, Londoño MC, et al. Budesonide in the first line treatment of patients with autoimmune hepatitis. Gastroenterol Hepatol. 2022 Aug-Sep;45(7):561-570.
[2] Grossmann C, Scholz T, Rochel M, et al. Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: a comparison of their glucocorticoid and mineralocorticoid properties. Eur J Endocrinol. 2004 Sep;151(3):397-406.
[3] Dong L, Zhu YH, Liu DX, et al. Intranasal Application of Budesonide Attenuates Lipopolysaccharide-Induced Acute Lung Injury by Suppressing Nucleotide-Binding Oligomerization Domain-Like Receptor Family, Pyrin Domain-Containing 3 Inflammasome Activation in Mice. J Immunol Res. 2019 Feb 27;2019:7264383.
[4] Pereira MA, Tao L, Liu Y, et al. Modulation by budesonide of DNA methylation and mRNA expression in mouse lung tumors. Int J Cancer. 2007 Mar 1;120(5):1150-3.
[5] Maier A, Zimmermann C, Beglinger C, et al. Effects of budesonide on P-glycoprotein expression in intestinal cell lines. Br J Pharmacol. 2007 Feb;150(3):361-8.
[6] Heinen N, Meister TL, Klöhn M, et al. Antiviral Effect of Budesonide against SARS-CoV-2. Viruses. 2021 Jul 20;13(7):1411.
[7] Lin Q, Li Z, Lu L, et al. Budesonide, an anti-inflammatory drug, exacerbate clostridioides difficile colitis in mice. Biomed Pharmacother. 2023 Nov;167:115489.
[8] Qian J, Xu Y, Yu Z. Budesonide and Calcitriol Synergistically Inhibit Airway Remodeling in Asthmatic Mice. Can Respir J. 2018 May 2;2018:5259240.
Budesonide是一种具有高效局部抗炎作用的糖皮质激素。Budesonide能增强内皮细胞、平滑肌细胞和溶酶体膜的稳定性，抑制免疫反应和降低抗体合成，从而使组胺等过敏活性介质的释放减少和活性降低。Budesonide可用于支气管哮喘、哮喘性慢性支气管炎、过敏性鼻炎、鼻息肉、克隆氏症和溃疡性结肠炎等相关疾病的治疗[1-4]。
在体外，Budesonide（1μM–25μM）处理LS180和Caco-2肠道细胞系48h–72h。Budesonide可诱导LS180细胞的MDR1/P-gp的表达，下调Caco-2细胞中MDR1/P-gp的表达[5]。Budesonide（0.1–25μM）与SARS-CoV-2（MOI=0.1）同时处理Vero E6细胞24小时。Budesonide显著降低Vero E6细胞中病毒滴度，且细胞活力不受影响[6]。
在体内，Budesonide（10mg/kg/day）通过口服灌胃每天给药于C57BL/6雌性小鼠5天。Budesonide显著增加了艰难梭菌感染小鼠的死亡率[7]。Budesonide（1mg）联合Calcitriol（100ng）通过雾化吸入和腹腔注射每天给药于哮喘模型BALB/c小鼠，持续8周。Budesonide和Calcitriol协同抑制了哮喘小鼠的气道重塑[8]。
| Cell experiment [1]: | |
Cell lines | LS180 and Caco-2 cells (human intestinal cell lines) |
Preparation Method | LS180 and Caco-2 cells were cultured in Dulbecco's modified Eagle's medium with Glutamax-I, supplemented with 10% fetal bovine serum, 1% non-essential amino acids, 1% sodium pyruvate, 50μg/ml gentamycin. Cells were seeded into 12-well plastic culture dishes and maintained in a humidified 37°C incubator with 5% CO2. Cells were treated with Budesonide (1μM–25μM). |
Reaction Conditions | 1μM–25μM; 48h |
Applications | Budesonide induced MDR1/P-glycoprotein expression in LS180 cells and down-regulated MDR1/P-glycoprotein expression in Caco-2 cells. These changes were confirmed at mRNA, protein, and functional levels. |
| Animal experiment [2]: | |
Animal models | Female BALB/c mice (6-8 weeks old) |
Preparation Method | Mice were sensitized by intraperitoneal injection of 50μg ovalbumin (Ova) with 1mg aluminum hydroxide on days 1 and 14. From day 21, mice were challenged by inhalation of 1% Ova solution for 30min once daily for eight weeks to establish an asthma model. In the Budesonide treatment group, 0.5h before each Ova challenge, mice inhaled 5mL PBS containing 1mg Budesonide via a nebulizer over 30min. |
Dosage form | 1mg; inhalation; daily administration before each Ova challenge; 8 weeks |
Applications | Budesonide monotherapy alleviated pathological changes including airway eosinophil infiltration, mucus secretion, and collagen proliferation in asthmatic mice. Budesonide inhibited the high expression of collagen type I (COL I), collagen type III (COL III), and α-smooth muscle actin (α-SMA), downregulated the expression of TGFβ type I receptor (TGFβRI), phosphorylated Smad2 (pSmad2), and phosphorylated Smad3 (pSmad3), and upregulated the expression of Smad7 in lung tissue. Budesonide decreased the expression of microRNA-21 (miR-21) in lung tissue. |
References: | |
| Cas No. | 51333-22-3 | SDF | |
| 别名 | 布地奈德 | ||
| 化学名 | (6aR,6bS,7S,8aS,8bS,11aR,12aS,12bS)-7-hydroxy-8b-(2-hydroxyacetyl)-6a,8a-dimethyl-10-propyl-6a,6b,7,8,8a,8b,11a,12,12a,12b-decahydro-1H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-4(2H)-one | ||
| Canonical SMILES | O=C(C([H])([H])O[H])[C@@]12OC(C([H])([H])C([H])([H])C([H])([H])[H])([H])O[C@]1([H])C([H])([H])[C@]([C@@](C([H])([H])C3([H])[H])([H])[C@@]4([H])[C@@](C([H])([H])[H])(C([H])=C5[H])C3=C([H])C5=O)([H])[C@]2(C([H])([H])[H])C([H])([H])[C@]4([H])O[H] | ||
| 分子式 | C25H34O6 | 分子量 | 430.53 |
| 溶解度 | ≥ 20.2mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3227 mL | 11.6136 mL | 23.2272 mL |
| 5 mM | 464.5 μL | 2.3227 mL | 4.6454 mL |
| 10 mM | 232.3 μL | 1.1614 mL | 2.3227 mL |
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