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Urolithin A is a microbial metabolite of ellagic acid in the gut and an inducer of mitophagy. It has anti-inflammatory, antiproliferative, and antioxidant activities. Urolithin A shifts mitochondria from CI- to CII-driven respiration, extends lifespan and improves muscle function.
| ln Vitro |
Micromolar quantities of urolithin A cause cell closure and autophagy. In the human sw620 colorectum, urolithin A suppresses DNA synthesis and the development of the cell cycle [2]. T24 and Caco-2 cell growth is inhibited by urolithin A, which also has anti-proliferative effects. In G2/M and S phase, urolithin A was dose- and time-dependent when compared to control cells, with 50 and 100 μM at 24 and 48 hours, respectively. IC 50 values are 43.9 and 49 μM, in that order [3]. At 50 and 100 μM, it causes apoptosis [4]. HepG2 cells exhibit strong antiproliferative activity in response to urolithin A. TCF/LEF fast activation was markedly downregulated and the expression of β-catenin, c-Myc, and cyclin D1 was reduced when urolithin A promoted cell death. In addition, urolithin A upregulates the expression of caspase-3, p38-MAPK, and p53, while suppressing NF-κB, p65, and other neuromediators [5].
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| ln Vivo |
Furthermore, an hour following the delivery of urolithin A in the vessel wall, the amount of paw edema decreased. Furthermore, the treated cell stems exhibited high oxygen radical antioxidant capacity (ORAC) scores an hour after urolithin A was added to the blood vessel wall, with the remaining unformed levels comparable to A [6].
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| References |
[1]. Gong Z, et al. Urolithin A attenuates memory impairment and neuroinflammation in APP/PS1 mice.
[2]. Wang Y, et al. In vitro antiproliferative and antioxidant effects of urolithin A, the colonic metabolite of ellagic acid, on hepatocellular carcinomas HepG2 cells. Toxicol In Vitro. 2015 Aug;29(5):1107-15. [3]. Zhao W, et al. Metabolite of ellagitannins, urolithin A induces autophagy and inhibits metastasis in human sw620colorectal cancer cells. Mol Carcinog. 2018 Feb;57(2):193-200. [4]. Ishimoto H, et al. In vivo anti-inflammatory and antioxidant properties of ellagitannin metabolite urolithin A. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5901-4. [5]. Qiu Z, et al. In vitro antioxidant and antiproliferative effects of ellagic acid and its colonic metabolite, urolithins, on human bladder cancer T24 cells. Food Chem Toxicol. 2013 Sep;59:428-37. [6]. González-Sarrías A, et al. Antiproliferative activity of the ellagic acid-derived gut microbiota isourolithin A and comparison with its urolithin A isomer: the role of cell metabolism.Eur J Nutr. 2017 Mar;56(2):831-841 |
| Molecular Formula |
C13H8O4
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|---|---|
| Molecular Weight |
228.2002
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| CAS # |
1143-70-0
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| SMILES |
O1C(C2C([H])=C(C([H])=C([H])C=2C2C([H])=C([H])C(=C([H])C1=2)O[H])O[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~30 mg/mL (~131.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (10.96 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (21.91 mM) in 0.5% CMC/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3821 mL | 21.9106 mL | 43.8212 mL | |
| 5 mM | 0.8764 mL | 4.3821 mL | 8.7642 mL | |
| 10 mM | 0.4382 mL | 2.1911 mL | 4.3821 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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