PXR-Mediated Upregulation of CYP3A Expression by Herb Compound Praeruptorin C from Peucedanum praeruptorum Dunn
Joint Authors
Bi, Hui-Chang
Wang, Yi-Tao
Wu, Qian
Huang, Ling
Li, Yu-Hua
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-9, 9 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-11-26
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Abstract EN
We recently reported that Praeruptorin C effectively transactivated the mRNA, protein expression, and catalytic activity of CYP3A4 via the CAR-mediated pathway, but whether and how PC could affect the expression and catalytic activity of CYP3A4 via PXR pathway remains unknown.
Therefore, in this study, the effect of PC on the CYP3A gene expression was investigated in mice primary hepatocytes after knockdown of PXR by transient transfection of PXR siRNA, and the gene expression, protein expression, and catalytic activity of CYP3A4 in the LS174T cells with PXR overexpression were determined by real-time PCR, western blot analysis, and LC-MS/MS-based CYP3A4 substrate assay, respectively.
We found that the level of CYP3a11 gene expression in mouse primary hepatocytes was significantly increased by praeruptorin C, but such an induction was suppressed after knockdown of pregnane X receptor by its siRNA.
In PXR-overexpressed LS174T cells, PC significantly enhanced CYP3A4 mRNA, protein expression, and functional activity through PXR-mediated pathway; conversely, no such increase was found in the untransfected cells.
These findings suggest that PC can significantly upregulate CYP3A level via the PXR-mediated pathway, and this should be taken into consideration to predict any potential herb-drug interactions between PC, Qianhu, and the other coadministered drugs.
American Psychological Association (APA)
Huang, Ling& Wu, Qian& Li, Yu-Hua& Wang, Yi-Tao& Bi, Hui-Chang. 2013. PXR-Mediated Upregulation of CYP3A Expression by Herb Compound Praeruptorin C from Peucedanum praeruptorum Dunn. Evidence-Based Complementary and Alternative Medicine،Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-450289
Modern Language Association (MLA)
Huang, Ling…[et al.]. PXR-Mediated Upregulation of CYP3A Expression by Herb Compound Praeruptorin C from Peucedanum praeruptorum Dunn. Evidence-Based Complementary and Alternative Medicine No. 2013 (2013), pp.1-9.
https://search.emarefa.net/detail/BIM-450289
American Medical Association (AMA)
Huang, Ling& Wu, Qian& Li, Yu-Hua& Wang, Yi-Tao& Bi, Hui-Chang. PXR-Mediated Upregulation of CYP3A Expression by Herb Compound Praeruptorin C from Peucedanum praeruptorum Dunn. Evidence-Based Complementary and Alternative Medicine. 2013. Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-450289
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-450289