Deoxycholic acid (Cholanoic Acid)
(Synonyms: 去氧胆酸; Cholanoic Acid; Desoxycholic acid) 目录号 : GC33762
Deoxycholic acid (Cholanoic Acid)是一种胆汁酸，肠道代谢副产物，可以激活G 蛋白偶联胆汁酸受体TGR5。
Cas No.:83-44-3
Sample solution is provided at 25 µL, 10mM.
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Deoxycholic acid (Cholanoic Acid) is a bile acid and a byproduct of intestinal metabolism that can activate the G protein-coupled bile acid receptor TGR5[1]. Deoxycholic acid can induce tyrosine phosphorylation and activate the receptor tyrosine kinase epidermal growth factor receptor in a ligand-independent manner[2]. Deoxycholic acid is the first drug that can be used to reduce submental fat[3].
In vitro, Deoxycholic acid (0-1000µM) treatment of AR42J cells for 24h inhibited cell proliferation in a dose- and time-dependent manner, induced cell apoptosis and necrosis, and significantly increased the activities of transcription factor 2 (ATF2), interferon-stimulated response element (ISRE), NKX-2.5, androgen receptor (AR), p53, and hypoxia-inducible factor-1 (HIF-1), and reduced the activities of peroxisome proliferator-activated receptor (PPAR) and activator protein 1 (AP1)[4]. Treatment of colon cancer cells (SW480 and LoVo) with Deoxycholic acid (5, 50µM) for 30min significantly increased tyrosine phosphorylation of β-catenin, leading to the loss of E-cadherin binding to β-catenin in the cells[5]. Treatment of gastric cancer cell MGC803 cells with Deoxycholic acid (100µM) for 2h enhanced cell survival and proliferation activity under bile acid stress[6].
In vivo, Deoxycholic acid added to drinking water at a concentration of 0.2% for 12 weeks in Apcmin/+ mice increased the incidence of intestinal tumors, increased intestinal permeability and induced low-grade inflammation[7].
References:
[1] Truong J K, Dawson P A. Bile acid metabolism[J]. Biochemistry of Lipids, Lipoproteins and Membranes, 2021: 395-428.
[2] Jean-Louis S, Akare S, Ali M A, et al. Deoxycholic acid induces intracellular signaling through membrane perturbations[J]. Journal of Biological Chemistry, 2006, 281(21): 14948-14960.
[3] Farina G A, Cherubini K, de Figueiredo M A Z, et al. Deoxycholic acid in the submental fat reduction: A review of properties, adverse effects, and complications[J]. Journal of Cosmetic Dermatology, 2020, 19(10): 2497-2504.
[4] Zhang G, Zhang J, Shang D, et al. Deoxycholic acid inhibited proliferation and induced apoptosis and necrosis by regulating the activity of transcription factors in rat pancreatic acinar cell line AR42J[J]. In Vitro Cellular & Developmental Biology-Animal, 2015, 51: 851-856.
[5] Pai R, Tarnawski A S, Tran T. Deoxycholic acid activates β-catenin signaling pathway and increases colon cell cancer growth and invasiveness[J]. Molecular biology of the cell, 2004, 15(5): 2156-2163.
[6] Wang X, Sun L, Wang X, et al. Acidified bile acids enhance tumor progression and telomerase activity of gastric cancer in mice dependent on c‐Myc expression[J]. Cancer Medicine, 2017, 6(4): 788-797.
[7] Liu L, Dong W, Wang S, et al. Deoxycholic acid disrupts the intestinal mucosal barrier and promotes intestinal tumorigenesis[J]. Food & function, 2018, 9(11): 5588-5597.
Deoxycholic acid (Cholanoic Acid)是一种胆汁酸，肠道代谢副产物，可以激活G 蛋白偶联胆汁酸受体TGR5[1]。Deoxycholic acid可以诱导酪氨酸磷酸化，并以不依赖配体的方式激活受体酪氨酸激酶表皮生长因子受体[2]。Deoxycholic acid是第一种可用于减少颏下脂肪的药物[3]。
在体外，Deoxycholic acid（0-1000µM）处理AR42J细胞24h，以剂量和时间依赖的方式抑制了细胞增殖，诱导了细胞凋亡和坏死，显著升高了转录因子2 （ATF2）、干扰素刺激反应元件（ISRE）、NKX-2.5、雄激素受体（AR）、p53、缺氧诱导因子-1（HIF-1）活性，降低了过氧化物酶体增殖激活受体（PPAR）、激活蛋白1（AP1）活性[4]。Deoxycholic acid（5、50µM）处理结肠癌细胞（SW480和LoVo）30min，显著增加β-连环蛋白的酪氨酸磷酸化，导致细胞中E-钙粘蛋白与β-连环蛋白结合的丧失[5]。Deoxycholic acid（100µM）处理胃癌细胞MGC803细胞2h，增强了细胞在胆汁酸应激下的存活和增殖活性[6]。
在体内，Deoxycholic acid以0.2%浓度添加到饮用水中喂养Apcmin/+小鼠12周，增加了肠道肿瘤的发生率，增加了肠道通透性并诱发低度炎症[7]。
| Cell experiment [1]: | |
Cell lines | AR42J cells |
Preparation Method | 2×104 cells in the logarithmic growth phase were seeded in each well of a 96-well plate. The medium was changed on the second day, and the fused cells were maintained for 24 h with medium containing different concentrations of Deoxycholic acid (0-1000µM). Then, 10μL MTT in PBSwith a concentration of 5g/L was added into each well for 4 h at 37°C. |
Reaction Conditions | 0-1000µM; 24h |
Applications | Deoxycholic acid inhibited AR42J cells proliferation in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Apcmin/+ mice |
Preparation Method | Four-week-old female Apcmin/+ mice were obtained and randomly divided into 2 groups (n=10): a control group (receiving sterile water) and a Deoxycholic acid group (0.2% Deoxycholic acid in sterile water). After 12 weeks, the mice were sacrificed and intestinal tissues were obtained. |
Dosage form | Add 0.2% Deoxycholic acid to drinking water |
Applications | Deoxycholic acid increased the multiplicity of intestinal tumors and promoted tumorigenesis in mice. Deoxycholic acid increased intestinal permeability and induced low grade inflammation in mice. |
References: [1]Zhang G, Zhang J, Shang D, et al. Deoxycholic acid inhibited proliferation and induced apoptosis and necrosis by regulating the activity of transcription factors in rat pancreatic acinar cell line AR42J[J]. In Vitro Cellular & Developmental Biology-Animal, 2015, 51: 851-856. [2]Liu L, Dong W, Wang S, et al. Deoxycholic acid disrupts the intestinal mucosal barrier and promotes intestinal tumorigenesis[J]. Food & function, 2018, 9(11): 5588-5597. | |
| Cas No. | 83-44-3 | SDF | |
| 别名 | 去氧胆酸; Cholanoic Acid; Desoxycholic acid | ||
| Canonical SMILES | C[C@@]1([C@@]2([H])[C@H](C)CCC(O)=O)[C@](CC2)([H])[C@@](CC[C@@]3([H])[C@@]4(CC[C@@H](O)C3)C)([H])[C@]4([H])C[C@@H]1O | ||
| 分子式 | C24H40O4 | 分子量 | 392.57 |
| 溶解度 | DMSO : ≥ 100 mg/mL (254.73 mM) | 储存条件 | Store at RT |
| 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 | 2.5473 mL | 12.7366 mL | 25.4732 mL |
| 5 mM | 0.5095 mL | 2.5473 mL | 5.0946 mL |
| 10 mM | 0.2547 mL | 1.2737 mL | 2.5473 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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