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Author:

Zhang Zhao-Yan (Zhang Zhao-Yan.) | Yang Liang (Yang Liang.) | Huang Xiao-Yan (Huang Xiao-Yan.) | Wang Mei-Xi (Wang Mei-Xi.) | Ma Zeng-Chun (Ma Zeng-Chun.) | Tang Xiang-Lin (Tang Xiang-Lin.) | Wang Yu-Guang (Wang Yu-Guang.) | Gao Yue (Gao Yue.)

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PKU PubMed CSCD

Abstract:

The rapid screening technology was used to investigate the transcriptional regulation effect of main chemical constituents in tubers of Polygonum multiflorum, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside(THSG) and anthraquinones (such as rhein, chrysophanol, aloe-emodin, emodin) on CYP3A4 drug inducers induced by human pregnancy X receptor (PXR).The effect of chemical composition on the cell activity was detected by MTS cell viability assay. IC₅₀ was calculated. The expression vector and the reporter vector were co-transfected into HepG2 cells, with 10 μmol•L⁻¹ rifampicin (RIF) as a positive control, and 10 μmol•L⁻¹ ketoconazole (TKZ) as a negative control. After treated with different concentrations of anthraquinones (2.5, 5, 10 μmol•L⁻¹) for 24 h, the cells were tested for dual luciferase activity. The results show that the inhibitory effect of THSG, chrysophanol, emodin, rhein and aloe-emodin on CYP3A4 was inhibited by co-transfection of pcDNA3.1 and pGL4.17-CYP3A4. The expressions of pcDNA3.14-PXR and pGL4.17-CYP3A4 were induced by the four compounds. Besides, emodin had a direct inducing effect. In conclusion, the four anthraquinone compounds have an inducing effect on CYP3A4 by PXR, but emodin can directly induce CYP3A4. THSG can inhibit CYP3A4, but plasmid can induce CYP3A4 after intervened with PXR.These results suggest that we should pay attention to the liver function and avoid liver damage in the combined administration of drugs.

Keyword:

anthraquinones CYP3A4 Polygonum multiflorum human progesterone X receptor (PXR) THSG

Author Community:

  • [ 1 ] [Zhang Zhao-Yan]College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China
  • [ 2 ] [Yang Liang]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 3 ] [Huang Xiao-Yan]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 4 ] [Wang Mei-Xi]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 5 ] [Ma Zeng-Chun]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 6 ] [Tang Xiang-Lin]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 7 ] [Wang Yu-Guang]Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • [ 8 ] [Gao Yue]College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China

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Source :

China journal of Chinese materia medica

ISSN: 1001-5302

Year: 2017

Issue: 24

Volume: 42

Page: 4827-4833

Cited Count:

WoS CC Cited Count:

SCOPUS Cited Count:

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 0

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