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Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7.
MedLine Citation:
PMID:  23148031     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The aim of the present study is to evaluate the inhibitory effects of liver UDP-glucuronosyltransferases (UGTs) by glycyrrhizic acid and glycyrrhetinic acid, which are the bioactive ingredients isolated from licorice. The results showed that glycyrrhetinic acid exhibited stronger inhibition towards all the tested UGT isoforms, indicating that the deglycosylation process played an important role in the inhibitory potential towards UGT isoforms. Furthermore, the inhibition kinetic type and parameters were determined for the inhibition of glycyrrhetinic acid towards UGT1A3 and UGT2B7. Data fitting using Dixon and Lineweaver-Burk plots demonstrated that the inhibition of UGT1A3 and UGT2B7 by glycyrrhetinic acid was best fit to competitive and noncompetitive type, respectively. The second plot using the slopes from Lineweaver-Burk plots versus glycyrrhetinic acid concentrations was employed to calculate the inhibition kinetic parameters (K(i) ), and the values were calculated to be 0.2 and 1.7 μM for UGT1A3 and UGT2B7, respectively. All these results remind us the possibility of UGT inhibition-based herb-drug interaction. However, the explanation of these in vitro parameters should be paid more caution due to complicated factors, including the probe substrate-dependent UGT inhibition behaviour, environmental factors affecting the abundance of herbs' ingredients, and individual difference of pharmacokinetic factors. Copyright © 2012 John Wiley & Sons, Ltd.
Authors:
Yin-Peng Huang; Yun-Feng Cao; Zhong-Ze Fang; Yan-Yan Zhang; Cui-Min Hu; Xiao-Yu Sun; Zhen-Wen Yu; Xu Zhu; Mo Hong; Lu Yang; Hong-Zhi Sun
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-12
Journal Detail:
Title:  Phytotherapy research : PTR     Volume:  -     ISSN:  1099-1573     ISO Abbreviation:  Phytother Res     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-13     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8904486     Medline TA:  Phytother Res     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 John Wiley & Sons, Ltd.
Affiliation:
The First Affiliated Hospital of Liaoning Medical University, Jinzhou, 121001, China.
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