科研之友
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摘要
The flavonoid wogonin has been reported to exhibit inhibition towards one of the most important drug-metabolizing enzymes (DMEs) cytochrome P450 (CYP), including CYP1A2. The present study aims to investigate the inhibition of UDP-glucuronosyltransferases (UGTs) by wogonin, trying to broaden the inhibition profile of wogonin towards DMEs. The inhibition of wogonin towards UGT1A1 and UGT1A3 was investigated using 4-methylumbelliferone glucuronidation reaction as probe reaction. Concentration-dependent inhibition behaviour of wogonin towards UGT1A1 and UGT1A3 was detected. Both Dixon plot and Lineweaver-Burk plot demonstrated that the inhibition of wogonin towards UGT1A1 and UGT1A3 was best fit the competitive inhibition type, and the inhibition kinetic parameters (K-i) were calculated to be 1.4 mu M and 0.02 mu M for UGT1A1 and UGT1A3, respectively. All these information was very helpful for guidance of safe application of clinical drugs when co-administration of wogonin-containing herbs.
- 出版日期2013-6
- 单位锦州医科大学
