五味子甲素和戈米辛 A 对细胞色素 P450 3A4 活性的抑制作用。
Inhibition of cytochrome P450 3A4 activity by schisandrol A and gomisin A isolated from Fructus Schisandrae chinensis.
机构信息
National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, MD 20892, USA.
出版信息
Phytomedicine. 2010 Jul;17(8-9):702-5. doi: 10.1016/j.phymed.2009.12.005. Epub 2010 Jan 25.
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.
我们研究了五味子醇甲（SCH）和五味子甲素（GOM）这两种五味子的主要生物活性成分对细胞色素 P450-3A4（CYP3A4）活性和细胞内谷胱甘肽（GSH）水平的影响。在无细胞体系中，SCH 和 GOM 对 CYP3A4 活性的抑制作用的 IC50 值分别为 32.02μM 和 1.39μM。SCH 或 GOM 的浓度高达 100μM 时，不会改变普通 HepG2 细胞和 P-糖蛋白过度表达的 HepG2-DR 细胞中的细胞内 GSH 水平。由于 SCH 和 GOM 可能通过阻碍 P-糖蛋白（一种膜外源性药物外排泵）的活性来逆转多药耐药（MDR），因此 SCH 或 GOM 除了影响药物摄取外，还可能影响细胞内药物代谢。
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