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Leonurine is a potent component of herbal medicine Herba leonuri. The detail information on leonurine metabolism in human has not been revealed so far. Two primary metabolites, leonurine O-glucuronide and demethylated leonurine, were observed and identified in pooled human liver microsomes (HLMs) and O-glucuronide is the predominant one. Among 12 recombinant human UDP-glucuronosyltransferases (UGTs), UGT1A1, UGT1A8, UGT1A9, and UGT1A10 showed catalyzing activity toward leonurine glucuronidation. The intrinsic clearance (CLint) of UGT1A1 was approximately 15-to 20-fold higher than that of UGT1A8, UGT1A9, and UGT1A10, respectively. Both chemical inhibition study and correlation study demonstrated that leonurine glucuronidation activities in HLMs had significant relationship with UGT1A1 activities. Leonurine glucuronide was the major metabolite in human liver microsomes. UGT1A1 was principal enzyme that responsible for leonurine glucuronidation in human liver and intestine microsomes.
Bo Tan, and
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December 2001,
The Journal of pharmacology and experimental therapeutics,
Bo Tan, and
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Jinlian Zhang, and
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Yizhun Zhu
September 2005,
Drug metabolism and disposition: the biological fate of chemicals,
Bo Tan, and
Weimin Cai, and
Jinlian Zhang, and
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Guo Ma, and
Ping Yang, and
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Yizhun Zhu
June 2002,
Drug metabolism and disposition: the biological fate of chemicals,
Bo Tan, and
Weimin Cai, and
Jinlian Zhang, and
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Guo Ma, and
Ping Yang, and
Qing Zhu, and
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July 2006,
Pharmaceutical research,
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Ning Zhou, and
Guo Ma, and
Ping Yang, and
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Yizhun Zhu
August 2008,
Drug metabolism and disposition: the biological fate of chemicals,
Bo Tan, and
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Yizhun Zhu
April 2010,
Drug metabolism and disposition: the biological fate of chemicals,
Bo Tan, and
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March 2016,
International journal of molecular sciences,
Bo Tan, and
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October 2012,
Xenobiotica; the fate of foreign compounds in biological systems,
Bo Tan, and
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Chemosphere,
