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Journal of Zhejiang University SCIENCE B 2007 Vol.8 No.10 P.756-764


Stereoselective glucuronidation of carvedilol by Chinese liver microsomes

Author(s):  YOU Lin-ya, YU Chun-na, XIE Sheng-gu, CHEN Shu-qing, ZENG Su

Affiliation(s):  Department of Drug Metabolism and Pharmaceutical Analysis, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China

Corresponding email(s):   zengsu@zju.edu.cn

Key Words:  Carvedilol (CARV), Derivatization, Stereoselectivity, Enzyme kinetics, Chinese liver microsomes

YOU Lin-ya, YU Chun-na, XIE Sheng-gu, CHEN Shu-qing, ZENG Su. Stereoselective glucuronidation of carvedilol by Chinese liver microsomes[J]. Journal of Zhejiang University Science B, 2007, 8(10): 756-764.

@article{title="Stereoselective glucuronidation of carvedilol by Chinese liver microsomes",
author="YOU Lin-ya, YU Chun-na, XIE Sheng-gu, CHEN Shu-qing, ZENG Su",
journal="Journal of Zhejiang University Science B",
publisher="Zhejiang University Press & Springer",

%0 Journal Article
%T Stereoselective glucuronidation of carvedilol by Chinese liver microsomes
%A YOU Lin-ya
%A YU Chun-na
%A XIE Sheng-gu
%A CHEN Shu-qing
%J Journal of Zhejiang University SCIENCE B
%V 8
%N 10
%P 756-764
%@ 1673-1581
%D 2007
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.2007.B0756

T1 - Stereoselective glucuronidation of carvedilol by Chinese liver microsomes
A1 - YOU Lin-ya
A1 - YU Chun-na
A1 - XIE Sheng-gu
A1 - CHEN Shu-qing
A1 - ZENG Su
J0 - Journal of Zhejiang University Science B
VL - 8
IS - 10
SP - 756
EP - 764
%@ 1673-1581
Y1 - 2007
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.2007.B0756

Objective: To study the stereoselective glucuronidation of carvedilol (CARV) by three chinese liver microsomes. Methods: The metabolites of CARV were identified by a hydrolysis reaction with β-glucuronidase and HPLC-MS/MS. The enzyme kinetics for CARV enantiomers glucuronidation was determined by a reversed phase-high pressure liquid chromatography (RP-HPLC) assay using (S)-propafenone as internal standard after precolumn derivatization with 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosylisothiocyanate. Results: Two CARV glucuronides were found in three chinese liver microsomes incubated with CARV. The non-linear regression analysis showed that the values of Km and Vmax for (S)-CARV and (R)-CARV enantiomers were (118±44) µmol/L, (2 500±833) pmol/(min·mg protein) and (24±7) µmol/L, (953±399) pmol/(min·mg protein), respectively. Conclusion: These results suggested that there was a significant (P<0.05) stereoselective glucuronidation of CARV enantiomers in three chinese liver microsomes, which might partly explain the enantioselective pharmacokinetics of CARV.

Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article


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