研究生英文文献汇报.pptx

研究生英文文献汇报 Keywords scutellarin; scutellarein; UGT; enzyme inhibition、 Contents1、 Introduction2、 Experimental section3、 Results and discussion4、 Conclusion 1、 Introduction In the recent years,another important drug metabolizing enzyme UDP-glucuronosyltransferase (UGT) has been demonstrated to exhibit significant contribution towards the metabolism of clinical drugs and herbal ponents,and more and more attention has been given to this enzymes (Malik and Black, 2012; Li etal、, 2012)、UGTs have been demonstrated to be involved in the metabolic elimination of many important endogenous substances, such as bilirubin, bile acid and estradiol (Erichsen et al、, 2010)、 Guo et al、 showed deglycosylation process of liquiritin strongly enhanced the inhibitory capability towards UGTs (2012)、 Huang et al、 showed strong inhibition of glycyrrhetinic acid towards UGT1A3 and 2B7 (2012)、 Liu et al、 also used in vitro incubation system to find the strong inhibition of deoxyschizandrin and schisantherin A towards UGT1A3 (2012)、 Chemicals and reagents、 Scutellarin,Scutellarein,4-MU,Tris-HCl, 7-hydroxycoumarin,UDPGA(缓冲盐), 重组UGTs亚型(UGT1A1,UGT1A6, UGT1A9,UGT2B7),HPLC reagents、2、 Experimental section Incubation and analysis methods for inhibition evaluation、 After 5min pre-incubation at 37℃, the UDPGA was added in the mixture to initiate the reaction、 The incubation time was 120min for UGT1A1 and UGT2B7, 30min,or UGT1A6 and UGT1A9, respectively、 The reactions were terminated by adding 100 mL acetonitrile with 7-hydroxycoumarin (100mM) as internal standard、The mixture was centrifuged at 20000×g for 10min, HPLC analysis、 Data fitting for determination of inhibition type and parameters (Ki)、The reaction velocity was determined using various concentrations of 4-MU and scutellarein、 The data were fitted using Dixon plot and Lineweaver–Burk double reciprocal plot、 The second plot with the slopes from the Lineweaver–Burk plot versus the concentrations of scutellarein was utilized