鞣花酸作用機制 - Medchemexpress - MCE中國

1、Product Data SheetEllagic acidCat. No.: HY-B0183CAS No.: 476-66-4分式: CHO分量: 302.19作靶點: Casein Kinase; Reactive Oxygen Species; Endogenous Metabolite作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; Immunology/Inflammation; MetabolicEnzyme/Protease; NF-B儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mo

2、nths-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 3.33 mg/mL (11.02 mM; Need ultrasonic)H2O : 40 M). Ellagic acid (5-100 M) shows inhibitoryactivities against Karpas299, SUDHL1, SR786, and FE-PD cell lines1. Ellagic acid (10 M) exhibits cytotoxic effects onMCF-7 cells after treatment of radiation. Ellagic acid (10 M

3、) in combination with Irradiation (IR) significantly abridgesPage 1 of 2 www.MedChemEthe capacity of MCF-7 cells to form colonies equated with individual treatments. Ellagic acid with IR also induces cellapoptosis, and facilitates the upregulation of pro-apopttotic Bax and downregulation of Bcl-2 in

4、 MCF-7 cells3.體內(nèi)研究 Ellagic acid (EA; 10 mg/kg/day; p.o., 14 days) strongly decreases MDA brain content by 17%, and reduces the levels ofbrain TNF- by 42% in rats. Ellagic acid markedly increases the reduced brain contents of 5-HT (39%), dopamine (DA,71%), and norepinephrine (NE, 77%). Ellagic acid (

5、10 mg/kg, p.o., 14 days) causes decreased histopathologicalchanges induced by Doxorubicin in rats2.PROTOCOLKinase Assay 1 CK2 and CK1 phosphorylation assays are carried out at 37C in the presence of increasing amounts of each inhibitor (Ellagic acid) in a final volume of 25 L containing 50 mM, Tris-

6、HCl pH 7.5, 100 mM NaCl, 12 mM MgCl2, 0.02 mM 33P-ATP (500-1000 cpm/pmol), unless otherwise indicated. The phosphorylatable substrates are the synthetic peptidesubstrate RRRADDSDDDDD (100 M) and RRKHAAIGDDDDAYSITA (200 M) for CK2 and CK1, respectively. Reactionstarted with the addition of the kinase

7、 and is stopped after 10 min. by addition of 5 L of 0.5 M orthophosphoric acidbefore spotting aliquots onto phosphocellulose filters. Filters are washed in 75 mM phosphoric acid substratefollowing SDSof the radiolabeled samples. DYRK1A, assayed on the peptide RRRFRPASPLRGPPK, and tyrosinekinase acti

8、vities are determined1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 ALCL cell viability is measured by MTT assay. Briefly, 0.1 105 cells are seeded onto 96-well microculture plates 12hrs before adding ellagic acid. The cells are grown in

9、 200 L of complete RPMI-1640 medium, under standard tissue-culture conditions, in the presence or absence of the drug (Ellagic acid) for 48 hours. Twenty L of MTT solution (5mg/mL) are then added to the cell suspension for 4h. The intracellular formazan crystals are dissolved with 150 L ofDMSO and o

10、ptical density, measured on a spectrophotometer at 540 nm, represents the mean ( SD) of triplicatecultures1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Fifty male adult Sprague-Dawley rats are divided randomly into five groups as follow: Grou

11、p (1) receives corn oil Administration 2 orally as a vehicle and served as normal control. Group (2) receives doxorubicin (DOX) injection (5 mg/kg, i.p.) twice a week for 14 days. Group (3) receives Ellagic acid (10 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.) twice aweek for 14 days. Gro

12、up (4) receives rosmarinic acid (RA; 75 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.)twice a week for 14 days. Group (5) receives Ellagic acid (10 mg/kg, p.o.; daily) with RA (75 mg/kg, p.o.; daily) for 14days and DOX injection (5 mg/kg, i.p.) twice a week for 14 days2.MCE has not independ

13、ently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Cozza G, et al. Identification of ellagic

14、 acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem.2006 Apr 20;49(8):2363-6.Page 2 of 3 www.MedChemE2. Rizk HA, et al. Prophylactic effects of ellagic acid and rosmarinic acid on doxorubicin-induced neurotoxicity in rats. J Biochem Mol Toxicol. 2017Dec;31(12).3. Ahire V, et al. Ellagic Acid Enhances Apoptotic Sensitivity of Breast Cancer Cells to -Radiation. Nutr Cancer. 2017 Aug-Sep;69(6):904-910.Mce