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Inhibition of Cytochrome P450 3A4 Activity by Schisandrol A and Gomisin A Isolated From Fructus Schisandrae Chinensis

Inhibition of Cytochrome P450 3A4 Activity by Schisandrol A and Gomisin A Isolated From Fructus Schisandrae Chinensis

C-K Wan, A K Tse, Z-L Yu, G-Y Zhu, H Wang, D W F Fong

Phytomedicine. 2010 Jul;17(8-9):702-5.

PMID: 20089387

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 IC(50) values of 32.02 microM and 1.39 microM, respectively. SCH or GOM at concentrations up to 100 microM 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP7432282-A	Schisandrol A		7432-28-2	Price

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