Taurodeoxycholic Acid (sodium salt)
(Synonyms: 牛磺脱氧胆酸钠) 目录号 : GC44995
牛磺脱氧胆酸 (TDCA) 是一种胆汁盐，通常存在于肠腔内。
Cas No.:1180-95-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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| Cell experiment [1]: | |
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Cell lines |
The human colonic epithelial cell line HT-29 |
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Preparation Method |
The human CEC line HT-29 were treated with dilutions of Taurodeoxycholic acid (TDCA). and IL-8 secretion was analyzed in the supernatant 24 h after stimulation.NF-kappa B binding activity was analyzed with EMSA, RelA translocation with immunofluorescence, and RelA-phosphorylation with Western blot analysis. |
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Reaction Conditions |
1,500 μM Taurodeoxycholic acid for 24h. |
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Applications |
Taurodeoxycholic acid induced IL-8 gene expression correlated with enhanced RelA phosphorylation, which was blocked by Ad5dnIKK beta.Taurodeoxycholic acid primarily induced IL-8 gene expression through RelA phosphorylation. |
| Animal experiment [2]: | |
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Animal models |
C57Bl/6J mice |
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Preparation Method |
Mice were fed a liquid diet with or without Taurodeoxycholic acid supplementation. After 6 days, the mice were injected with LPS (10mg/kg) to induce intestinal injury. Specimens were obtained 24 hours later and evaluated for intestinal apoptosis, crypt proliferation, and villus length. A separate cohort of animals were injected with LPS (25mg/kg) and followed 7 days for survival. |
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Dosage form |
50mg/kg/day Taurodeoxycholic acid, oral gavage |
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Applications |
Mice whose diet was supplemented with Taurodeoxycholic acid had significantly increased survival. After LPS-induced injury, mice supplemented with Taurodeoxycholic acid showed decreased intestinal apoptosis by both H&E and caspase-3. Dietary taurodeoxycholic acid supplementation alleviates mucosal damage and improves survival after LPS-induced intestinal injury. Taurodeoxycholic acid is protective of the intestinal mucosa by increasing resistance to injury-induced apoptosis, stimulating enterocyte proliferation and increasing villus length. |
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References: [1]. Mühlbauer M, Allard B, et al. Differential effects of deoxycholic acid and taurodeoxycholic acid on NF-kappa B signal transduction and IL-8 gene expression in colonic epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2004 Jun;286(6):G1000-8. [2]. Perrone EE, Chen C, et al. Warner BW, Sun CC, Alaish SM, Strauch ED. Dietary bile acid supplementation improves intestinal integrity and survival in a murine model. J Pediatr Surg. 2010 Jun;45(6):1256-65. |
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Taurodeoxycholic acid (TDCA) is one of the Bile salts, are normally found within the intestinal lumen. The primary function of bile salts is to aid in the absorption of lipids and lipid-soluble vitamins. However, recent studies have shown that bile salts have other biologic effects independent of their role in digestion[1].
Several effects of bile acids (BAs) on colonic epithelial cells (CECs) have been described, including induction of proliferation and apoptosis.?Taurodeoxycholic acid (TDCA) is capable of inducing classic NF-κB activation in hepatoma cells, and induced IL-8 expression in a dose- and time-dependent manner.??that there seems to be a classical NF-κB-dependent and an independent pathway in BA-induced IL-8 expression in CECs[2].
The bile salt taurodeoxycholic acid (TDCA) has been associated with increased growth of esophageal mucosa in a rabbit explant model. Taurodeoxycholic acid increased gallbladder eicosanoid release in a dose-related manner with 6-keto-PGF1 alpha and PGE2 release 10-fold higher than TXB2.These findings suggest that the increased release of gallbladder PGI2 and PGE2 described in animal models of cholecystitis may, in part, be related to increased gallbladder bile levels of taurodeoxycholic acid[3].
References:
[1].Perrone EE, Chen C, et al. Warner BW, Sun CC, Alaish SM, Strauch ED. Dietary bile acid supplementation improves intestinal integrity and survival in a murine model. J Pediatr Surg. 2010 Jun;45(6):1256-65.
[2]. Mühlbauer M, Allard B, et al. Differential effects of deoxycholic acid and taurodeoxycholic acid on NF-kappa B signal transduction and IL-8 gene expression in colonic epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2004 Jun;286(6):G1000-8.?
[3]. Myers SI, Riva A, et al. Taurodeoxycholic acid stimulates rabbit gallbladder eicosanoid release. Prostaglandins Leukot Essent Fatty Acids. 1995 Jan;52(1):35-9.
牛磺脱氧胆酸 (TDCA) 是一种胆汁盐,通常存在于肠腔内。胆汁盐的主要功能是帮助吸收脂质和脂溶性维生素。然而,最近的研究表明,胆汁盐具有与其在消化中的作用无关的其他生物学效应[1]。
已经描述了胆汁酸 (BA) 对结肠上皮细胞 (CEC) 的多种作用,包括诱导增殖和细胞凋亡。 Taurodeoxycholic acid (TDCA) 能够在肝癌细胞中诱导经典的 NF-κB 激活,并以剂量和时间依赖性方式诱导 IL-8 表达。 BA 诱导的 CEC 中 IL-8 表达似乎存在经典的 NF-κB 依赖和独立途径[2]。
在兔外植体模型中,胆汁盐牛磺脱氧胆酸 (TDCA) 与食道粘膜生长增加有关。牛磺脱氧胆酸以剂量相关的方式增加胆囊类花生酸的释放,其中 6-酮基-PGF1 α 和 PGE2 的释放比 TXB2 高 10 倍。这些发现表明,胆囊炎动物模型中描述的胆囊 PGI2 和 PGE2 释放增加可能在部分,与胆囊胆汁中牛磺脱氧胆酸水平升高有关[3]。
| Cas No. | 1180-95-6 | SDF | |
| 别名 | 牛磺脱氧胆酸钠 | ||
| Canonical SMILES | O[C@@H]1CC[C@@]2(C)[C@@](CC[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)CCC(NCCS(=O)([O-])=O)=O)([H])C1.[Na+] | ||
| 分子式 | C26H44NO6S•Na | 分子量 | 521.7 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 3 mg/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。 | ||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9168 mL | 9.5841 mL | 19.1681 mL |
| 5 mM | 0.3834 mL | 1.9168 mL | 3.8336 mL |
| 10 mM | 0.1917 mL | 0.9584 mL | 1.9168 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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Bile acid salt binding with colesevelam HCl is not affected by suspension in common beverages
J Pharm Sci 2006 Dec;95(12):2751-9.PMID:16937334DOI:10.1002/jps.20734.
It has been previously reported that anions in common beverages may bind to bile acid sequestrants (BAS), reducing their capacity for binding bile acid salts. This study examined the ability of the novel BAS colesevelam hydrochloride (HCl), in vitro, to bind bile acid sodium salts following suspension in common beverages. Equilibrium binding was evaluated under conditions of constant time and varying concentrations of bile acid salts in simulated intestinal fluid (SIF). A stock solution of sodium salts of glycochenodeoxycholic acid (GCDC), Taurodeoxycholic Acid (TDC), and glycocholic acid (GC), was added to each prepared sample of colesevelam HCl. Bile acid salt binding was calculated by high-performance liquid chromatography (HPLC) analysis. Kinetics experiments were conducted using constant initial bile acid salt concentrations and varying binding times. The affinity, capacity, and kinetics of colesevelam HCl binding for GCDC, TDC, and GC were not significantly altered after suspension in water, carbonated water, Coca-Cola, Sprite, grape juice, orange juice, tomato juice, or Gatorade. The amount of bile acid sodium salt bound as a function of time was unchanged by pretreatment with any beverage tested. The in vitro binding characteristics of colesevelam HCl are unchanged by suspension in common beverages.
Impairment of rat oesophageal muscle contractility associated with experimental non-erosive oesophageal mucosal damage
Exp Physiol 2019 Feb;104(2):199-208.PMID:30561099DOI:10.1113/EP087244.
New findings: What is the central question of this study? Is the responsiveness of isolated segments of the rat oesophagus to contractile or relaxant stimuli susceptible to acute luminal exposure of the oesophagus to an acid solution that contains pepsin and bile salt? What is the main finding and its importance? The study reveals that luminal acidity is an important factor that disrupts barrier function in the oesophagus to allow the diffusion of noxious agents, such as bile acid, that alter the contractile status of the oesophageal body, even in the absence of inflammation. Abstract: We investigated whether the experimental simulation of duodenogastro-oesophageal reflux alters the contractile responsiveness of rat oesophageal strips. After 30 min of luminal exposure to a solution at acid pH that contained pepsin and Taurodeoxycholic Acid, isolated strips of the rat oesophagus and gastro-oesophageal junction were subjected to contractile or relaxing stimuli. Acid challenge decreased the responsiveness of oesophageal strips to contractile stimulation, especially in oesophageal preparations that were mounted following the circular orientation of the muscularis externa layer. The contractility of longitudinal preparations of the rat oesophagus appeared less susceptible to the deleterious effects of acid challenge. In contrast, the responsiveness of ring-like preparations from the gastro-oesophageal junction to contractile stimulation was unaltered by acid challenge. Taurodeoxycholic Acid decreased the responsiveness of circular oesophageal preparations to KCl, an effect that was exacerbated by luminal acidity. On the contrary, although the relaxant ability of the rat oesophagus did not change, acid challenge increased the relaxant efficacy of sodium nitroprusside and isoprenaline in strips of the gastro-oesophageal junction. A significant decrease in transepithelial electrical resistance was seen when the oesophageal mucosa was challenged at pH 1 but not at pH 4. Treatment with alginate blunted the deleterious effects of acid challenge on transepithelial electrical resistance and the responsiveness of oesophageal preparations to KCl. The present findings support the notion that luminal acidity is an important factor that disrupts barrier function in the oesophagus to allow the diffusion of noxious agents, such as bile acid, that alter the contractile status of the oesophagus.
Acid lipase activity of human lymphocytes
Biochim Biophys Acta 1979 Feb 26;572(2):225-34.PMID:427176DOI:10.1016/0005-2760(79)90038-9.
Acid lipase activity was examined in human leukocytes using 4-methylumbelliferyl esters in a fluorimetric assay. Mononuclear leukocytes had 10--15 times the acid lipase activity of polymorphonuclear leukocytes. The enzyme activity was highest using the oleate ester of 4-methylumbelliferone at pH 4.0, in the presence of L-alpha-phosphatidylcholine and Taurodeoxycholic Acid (sodium salt). Acid lipase activity was inhibited by diethylaminoethoxyhexestrol, sodium chloride and fluoride, potassium chloride, calcium chloride and albumin, but was unaffected by diethyl p-nitrophenyl phosphate or sulphydryl reagents. There were at least two forms of acid lipase activity: one (A form) was sensitive to heart inactivation (56 degrees C) and corresponded to the enzyme deficient in patients with Wolman's disease; the other (B form) was resistant to heat inactivation and corresponded to the residual enzyme activity found in Wolman's disease.
Comparative evaluation of in vitro efficacy of colesevelam hydrochloride tablets
Drug Dev Ind Pharm 2014 Sep;40(9):1173-9.PMID:23805883DOI:10.3109/03639045.2013.809534.
Context: Colesevelam hydrochloride is used as an adjunct to diet and exercise to reduce elevated low-density lipoprotein (LDL) cholesterol in patients with primary hyperlipidemia as well as to improve glycemic control in patients with type 2 diabetes. This is likely to result in submission of abbreviated new drug applications (ANDA). Objective: This study was conducted to compare the efficacy of two tablet products of colesevelam hydrochloride based on the in vitro binding of bile acid sodium salts of glycocholic acid (GC), glycochenodeoxycholic acid (GCDA) and Taurodeoxycholic Acid (TDCA). Methods: Kinetic binding study was carried out with constant initial bile salt concentrations as a function of time. Equilibrium binding studies were conducted under conditions of constant incubation time and varying initial concentrations of bile acid sodium salts. The unbound concentration of bile salts was determined in the samples of these studies. Langmuir equation was utilized to calculate the binding constants k1 and k2. Results: The amount of the three bile salts bound to both the products reached equilibrium at 3 h. The similarity factor (f2) was 99.5 based on the binding profile of total bile salts to the test and reference colesevelam tablets as a function of time. The 90% confidence interval for the test to reference ratio of k2 values were 96.06-112.07 which is within the acceptance criteria of 80-120%. Conclusion: It is concluded from the results that the test and reference tablets of colesevelam hydrochloride showed a similar in vitro binding profile and capacity to bile salts.
Potential tumor-promoting activity of bile acids in rat glandular stomach
Jpn J Cancer Res 1987 Jan;78(1):32-9.PMID:3102436doi
The potential tumor-promoting and -initiating activities of bile acids in the glandular stomach mucosa of F344 rats after administration by gastric intubation were studied. Taurocholic acid sodium salt at doses of 300 to 1200 mg/kg body weight and glycocholic acid sodium salt at doses of 400 to 1200 mg/kg body weight induced up to 100-fold increases in ornithine decarboxylase activity with maxima after 4 hr and up to 10-fold increases in replicative DNA synthesis with maxima after 16-17 hr in the pyloric mucosa of the stomach. Taurodeoxycholic Acid sodium salt, taurochenodeoxycholic acid sodium salt and glycocholic acid also induced high ornithine decarboxylase activity, and glycodeoxycholic acid sodium salt and glycochenodeoxycholic acid sodium salt caused slight induction of ornithine decarboxylase activity, but taurolithocholic acid sodium salt did not induce ornithine decarboxylase activity at all in the pyloric mucosa of the stomach. Glycocholic acid sodium salt did not induce unscheduled DNA synthesis in the pyloric mucosa of the stomach. The present results suggest that six bile acids, but not taurolithocholic acid sodium salt, have potential tumor-promoting activities in the pyloric mucosa of rat stomach and that glycocholic acid sodium salt has no potential tumor-initiating activity in the pyloric mucosa of rat stomach.