Urolithin-A _Drug Metabolite - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUrolithin ACat. No.: HY-100599CAS No.: 1143-70-0分式: CHO分量: 228.2作靶點: Drug Metabolite; Autophagy; Reactive Oxygen Species作通路: Metabolic Enzyme/Protease; Autophagy;Immunology/Inflammation; NF-B儲存式: Powder -20C 3 years4C 2 yearsIn

2、solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 33 mg/mL (144.61 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.96 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (10.96 mM); Suspended s

3、olution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.96 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Urolithin A具有抗氧化和抗增殖作的鞣花酸的腸代謝物; 抑制T24和Caco-2細(xì)胞的長的IC50值分別為43.9和49 M。IC50 & Target IC50: 43.9 M (T24 cell) 1, 49 M (Caco-2cell) 2體外研究 Urolithins could mainly inhibit prosta

4、te cancer and colon cancer cell growth. Urolithin A increases mRNA andprotein expression of Phospho-p38 MAPK, and decreases mRNA and protein expression of MEKK1 andPhospho-c-Jun in T24 cells. Caspase-3 is also activated and PPAR- protein expression increased in drug-induced apoptosis 1. Urolithin A

5、exerts a dose- and time-dependent significant arrest at G2/M and S phasesafter treatments with 50 and 100 M at 24 and 48 h compared to control cells. It induces cell apoptosis with50 and 100 M 2. Urolithin A shows potent antiproliferative activity on HepG2 cells. When cell death isinduced by Urolith

6、in A, the expression of -catenin, c-Myc and Cyclin D1 are decreased and TCF/LEFtranscriptional activation is notably down-regulated. Urolithin A also increases protein expression of p53, p38-MAPK and caspase-3, but suppresses expression of NF-B p65 and other inflammatory mediators 3.體內(nèi)研究 The volume

7、of paw edema is reduced at 1 h after oral administration of urolithin A. In addition, plasma intreated mice exhibited significant oxygen radical antioxidant capacity (ORAC) scores with high plasma levelsof the unconjugated form at 1 h after oral administration of urolithin A 4.PROTOCOLCell Assay 2 H

8、uman colon cancer cells HT-29 are treated for 24 and 48 h at 100 and 50 M of Urolithin A and Iso UrolithinA aglycones and their glucuronide conjugates. Cell viability and proliferation are measured using a TC10automated cell counter with the addition of Trypan blue for viability determination. IC50

9、values aredetermined by MTT assay 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Paw edema is induced in the right hind paw of ICR mice by the subcutaneous injection of 1% -Administration 4 carrageenan in pysiological saline (50 L). The

10、inflammation level is quantified by the volume of paw edema.Urolithin A dissolved in 0.5% carboxymethylcellulose suspension is orally administered to the mice at 1 or 6 hbefore carrageenan injection. The anti-inflammatory effects of urolithin A on carrageenan-induced edema inmice are analyzed 4.MCE

11、has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Qiu Z, et al. In vitro antioxidant and antiproliferative effects of ellagic acid and its colonic metabolite, urolithins, on human bladder cancerT24

12、 cells. Food Chem Toxicol. 2013 Sep;59:428-37.2. Gonzlez-Sarras A, et al. Antiproliferative activity of the ellagic acid-derived gut microbiota isourolithin A and comparison with itsurolithin A isomer: the role of cell metabolism.Eur J Nutr. 2017 Mar;56(2):831-841.3. Wang Y, et al. In vitro antiprol

13、iferative and antioxidant effects of urolithin A, the colonic metabolite of ellagic acid, on hepatocellularcarcinomas HepG2 cells. Toxicol In Vitro. 2015 Aug;29(5):1107-15.4. Ishimoto H, et al. In vivo anti-inflammatory and antioxidant properties of ellagitannin metabolite urolithin A. Bioorg Med Chem Lett. 2011Oct 1;21(19):5901-4.McePd