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Cytochrome P450 2C19 Inhibitory Activity of Common Berry Constituents

  作者 Sand, PG; Dreiseitel, A; Stang, M; Schreier, P; Oehme, A; Locher, S; Hajak, G  
  选自 期刊  Phytotherapy Research;  卷期  2010年24-2;  页码  304-307  
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[摘要]The cytochrome P450 enzyme CYP2C19 is involved in the metabolism of many commonly prescribed drugs, including proton pump inhibitors, antiepileptics; and antidepressants. CYP2C19 inhibitors from food and food supplements may augment the toxicity of these agents and lead to noncompliance with treatment. The present investigation addresses CYP2C19 inhibition by 18 berry constituents using a chemiluminescent assay. Test compounds displayed inhibitory properties in a concentration-dependent fashion, with IC50 values ranging from 20.2 mu m up to >316 mu m. In the order of decreasing effect size, anthocyanidins were followed by anthocyanidin-monoglycosides and procyanidins. Anthocyanidin-diglucosides exhibited weak and biphasic effects. When compared with the CYP2C19 inhibitor fluvoxamine, the flavonoids under study were 50- to 750-fold less potent. It is concluded that the above natural substances are moderate to poor inhibitors of CYP2C19 in vitro. Copyright (C) 2009 John Wiley & Sons, Ltd.

 
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