Xanthohumol _COX 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEXanthohumolCat. No.: HY-N1067CAS No.: 6754-58-1分式: CHO分量: 354.4作靶点: COX; Acyltransferase作通路: Immunology/Inflammation; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO

2、: 150 mg/mL (423.25 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8217 mL 14.1084 mL 28.2167 mL5 mM 0.5643 mL 2.8217 mL 5.6433 mL10 mM 0.2822 mL 1.4108 mL 2.8217 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Xanthohumol是从啤酒花中分离

3、到的黄酮类化合物，是DGAT，COX-1 和 COX-2 的抑制剂，具有抗肿瘤，抗管成的作。体外研究Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces theexpression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets surface 1. Xanthohumol (5-50nM) reduces the frequency of spontaneou

4、sly occurring Ca2+ sparks and Ca2+ waves in control myocytes1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEand in cells subjected to Ca2+ overload caused by: (1) exposure to low K+ solutions, (2) periods of highfrequency electrical stimulation, (3) exposures to isoproterenol or (4) caffeine. Xanth

5、ohumol (50-100 nM)reduces the rate of relaxation of electrically- or caffeine-triggered Ca2+ transients, without suppressing ICa,but this effect is small and reversed by isoproterenol at physiological temperatures. Xanthohumol alsosuppresses the Ca2+ content of the SR, and its rate of recirculation

6、2. Treatment of endothelial cells withXanthohumol leads to increased AMPK phosphorylation and activity. Functional studies using biochemicalapproaches confirm that AMPK mediates Xanthohumol anti-angiogenic activity. AMPK activation byXanthohumol is mediated by CAMMK, but not LKB1. Analysis of the do

7、wnstream mechanisms shows thatXanthohumol-induced AMPK activation reduces nitric oxide (NO) levels in endothelial cells by decreasingeNOS phosphorylation. Finally, AKT pathway is inactivated by Xanthohumol as part of its anti-angiogenicactivity, but independently from AMPK, suggesting that these two

8、 signaling pathways proceed autonomously3. Xanthohumol significantly reduces cell viability and induces apoptosis via pro-caspase-3/8 cleavage andpoly(ADP ribose) polymerase (PARP) degradation. Pro-caspase-9 cleavage, Bcl2 family expressionchanges, mitochondrial dysfunction, and intracellular ROS ge

9、neration also participate in Xanthohumol-induced glioma cell death. Xanthohumols inhibition of the IGFBP2/AKT/Bcl2 pathway via miR-204-3ptargeting plays a critical role in mediating glioma cell death 4.PROTOCOLCell Assay 3 In vitro cell proliferation/viability is measured by the MTT test at differen

10、t time points. 1000 cells/well areplated into 96-multiwell plates in complete medium. Following adhesion, medium is replaced with freshmedium containing the different treatments or vehicle (DMSO in medium). Xanthohumol and EGCG are usedin a concentration range from 2.5 to 40 M, up to 96 hours. 3 hou

11、rs before each time point, MTT reagent (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) is added to the wells and plates are incubated at37C. At the indicated time points, absorbance at 540 nm is then measured by a FLUOstarspectrophotometer.MCE has not independently confirmed the accur

12、acy of these methods. They are for reference only.REFERENCES1. Luzak B, et al. Xanthohumol from hop cones (Humulus lupulus L.) prevents ADP-induced platelet reactivity. Arch Physiol Biochem. 2016Nov 18:1-7.2. Arnaiz-Cot JJ, et al. Xanthohumol modulates calcium signaling in rat ventricular myocytes:

13、Possible Antiarrhythmic properties. JPharmacol Exp Ther. 2016 Nov 4. pii: jpet.116.236588.3. Gallo C, et al. Hop derived flavonoid xanthohumol inhibits endothelial cell functions via AMPK activation. Oncotarget. 2016 Aug 1.4. Chen PH, et al. The miR-204-3p-targeted IGFBP2 pathway is involved in xanthohumol-induced glioma cell apoptotic death.Neuropharmacology. 2016 Nov;110(Pt A):362-75.Mc