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- Title
Identification of Human UDP-Glucuronosyltransferase 1A4 as the Major Isozyme Responsible for the Glucuronidation of 20(S)-Protopanaxadiol in Human Liver Microsomes.
- Authors
Jia Li; Chunyong He; Lianxiang Fang; Li Yang; Zhengtao Wang
- Abstract
20(S)-protopanaxadiol (PPD), one of the representative aglycones of ginsenosides, has a broad spectrum of pharmacological activities. Although phase I metabolism has been investigated extensively, information regarding phase II metabolism of this compound remains to be elucidated. Here, a glucuronidated metabolite of PPD in human liver microsomes (HLMs) and rat liver microsomes (RLMs) was unambiguously identified as PPD-3-O-β-d-glucuronide by nuclear magnetic resonance spectroscopy and high resolution mass spectrometry. The chemical inhibition and recombinant human UDP-Glucuronosyltransferase (UGT) isoforms assay showed that the PPD glucuronidation was mainly catalyzed by UGT1A4 in HLM, whereas UGT1A3 showed weak catalytic activity. In conclusion, PPD-3-O-β-d-glucuronide was first identified as the principal glucuronidation metabolite of PPD in HLMs, which was catalyzed by UGT1A4.
- Subjects
GINSENOSIDES; LIVER microsomes; GLUCURONIDATION; GLUCURONOSYLTRANSFERASE; NUCLEAR magnetic resonance spectroscopy; MASS spectrometry
- Publication
International Journal of Molecular Sciences, 2016, Vol 17, Issue 3, p205
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms17030205