Inhibition of cytochrome P450 3A4 activity by schisandrol A and gomisin A isolated from Fructus Schisandrae chinensis

C. K. Wan, Anfernee K W TSE, Zhiling YU, G. Y. Zhu, H. Wang, David W F FONG*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

24 Citations (Scopus)

Abstract

We studied the effects of schisandrol A (SCH) and gomisin A (GOM), two of the main bioactive components of Fructus Schisandrae chinensis, on cytochrome P450-3A4 (CYP3A4) activity and cellular glutathione (GSH) level. In a cell-free system both SCH and GOM inhibited CYP3A4 activity with IC50 values of 32.02 μM and 1.39 μM, respectively. SCH or GOM at concentrations up to 100 μM did not alter cellular GSH level in regular HepG2 cells and P-glycoprotein overexpressing HepG2-DR cells. Since SCH and GOM may reverse multidrug resistance (MDR) by impeding the activity of P-glycoprotein, a membrane xenobiotic exporter, SCH or GOM could affect cellular drug metabolism in addition to drug uptake.

Original languageEnglish
Pages (from-to)702-705
Number of pages4
JournalPhytomedicine
Volume17
Issue number8-9
DOIs
Publication statusPublished - Jul 2010

Scopus Subject Areas

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine

User-Defined Keywords

  • Cytochrome P450 3A4
  • Glutathione
  • Gomisin A
  • Multidrug resistance
  • Schisandra chinensis
  • Schisandrol A

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