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Transcriptional Regulation of CYP3A42B62C9 Mediated via Nuclear Receptor PXR by Helicid and Its Metabolites
Joint Authors
Li, Yan
Chen, Qun
Xie, Hai-tang
Wang, Guo
Xu, Zhe
Pu, Zhi-chen
Hu, Hua
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-9, 9 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-04-22
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Abstract EN
Objective.
This study aims at establishing and validating an in vitro system to screen drug inducers of CYPs mediated via hPXR, as well as studying transcriptional regulation of CYPs mediated via hPXR by helicid and its two metabolites.
Methods.
Cloning the nuclear receptor hPXR and the promoters of CYP3A4, CYP2B6, CYP2C9, and inserting the trans-element to the upstream of firefly luciferase reporter gene of the pGL4.17 vectors, then cotransfecting the report vectors and hPXR expression plasmid to HepG2 cell line.
After 24 hours, the transfected cells were treated with helicid (0.004, 0.04, and 0.4 μmol/L) and its metabolite I and metabolite II (0.0004, 0.004, and 0.04 μmol/L) for 48 h, while rifampin (10 μmol/L) was included as the positive control and 0.1% DMSO as the negative control group.
Cells were lysized and luciferase activity was determined using a dual luciferase reporter assay kit.
Results.
Helicid and its metabolites did not significantly increase promoter activities of CYP3A4, CYP2B6, and CYP2C9 in HepG2 cells transfected with PXR expression plasmid (P>0.05).
Conclusion.
PXR-expressed CYP3A4, CYP2B6, and CYP2C9 dual luciferase reporter gene platforms were successfully established, and helicid and its metabolites I, II do not significantly induce the transcription of CYP3A4, CYP2B6, and CYP2C9.
American Psychological Association (APA)
Chen, Qun& Xie, Hai-tang& Li, Yan& Wang, Guo& Xu, Zhe& Pu, Zhi-chen…[et al.]. 2015. Transcriptional Regulation of CYP3A42B62C9 Mediated via Nuclear Receptor PXR by Helicid and Its Metabolites. Evidence-Based Complementary and Alternative Medicine،Vol. 2015, no. 2015, pp.1-9.
https://search.emarefa.net/detail/BIM-1063604
Modern Language Association (MLA)
Chen, Qun…[et al.]. Transcriptional Regulation of CYP3A42B62C9 Mediated via Nuclear Receptor PXR by Helicid and Its Metabolites. Evidence-Based Complementary and Alternative Medicine No. 2015 (2015), pp.1-9.
https://search.emarefa.net/detail/BIM-1063604
American Medical Association (AMA)
Chen, Qun& Xie, Hai-tang& Li, Yan& Wang, Guo& Xu, Zhe& Pu, Zhi-chen…[et al.]. Transcriptional Regulation of CYP3A42B62C9 Mediated via Nuclear Receptor PXR by Helicid and Its Metabolites. Evidence-Based Complementary and Alternative Medicine. 2015. Vol. 2015, no. 2015, pp.1-9.
https://search.emarefa.net/detail/BIM-1063604
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1063604