文档介绍:Comparison of Inhibition Capability of Scutellarein and Scutellarin Towards Important Liver UDP Glucuronosyltransferase (UGT) isoforms
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精品资料
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Keywords
scutellarin;
scutellarein;
UGT;
enzyme inhibition.
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Contents
1. Introduction
2. Experimental section
3. Results and discussion
4. Conclusion
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1. Introduction
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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 components,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).
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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).
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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
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