http://dx.doi.org/10.1016/j.phymed.2009.12.005">
 

Document Type

Journal Article

Department/Unit

School of Chinese Medicine

Title

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

Language

English

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. © 2009 Elsevier GmbH. All rights reserved.

Keywords

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

Publication Date

2010

Source Publication Title

Phytomedicine

Volume

17

Issue

9-8

Start Page

702

End Page

705

Publisher

Elsevier

ISSN (print)

09447113

ISSN (electronic)

1618095X

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