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EFFECTS OF STRUCTURALLY AND FUNCTIONALLY DIVERSE GROUP OF PHYTOCHEMICALS ON ANILINE HYDROXYLATION (CYP2E1) OF CONTROL AND ACETONE‐INDUCED RAT LIVER MICROSOMES
Author(s) -
Parekh Jigna,
Sengupta Amiritaparna,
Ray Sidhartha D.
Publication year - 2008
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.22.1_supplement.1137.3
Subject(s) - chemistry , bioavailability , hydroxylation , pharmacology , quercetin , in vivo , drug metabolism , curcumin , biochemistry , naringin , metabolism , biology , enzyme , chromatography , antioxidant , microbiology and biotechnology
Although the last decade focused on exploring disease fighting properties of hundreds of phytochemicals, major gaps remain to be filled in understanding their mechanisms of actions in vivo. Our laboratory pioneered investigating anti‐toxic properties of several phytochemicals, however, information on their bioavailability, impact on drug metabolism, precise role during pathogenesis of a number of diseases, and drug‐drug interactions remains unclear. Interestingly, CYP2E1 has evolved as a major player in this field. This study investigated the effects of structurally & functionally diverse group of phytochemicals on aniline hydroxylation pattern of control and acetone induced (1% in drinking water for 6 days) rat liver microsomes in vitro. Trans cinnamic acid (TCA), Resorcinol (RSL), Rutin (RUT), Quercetin (QTN), Hesperidin (HES) and Curcumin (CUR) were used at 25, 50, 100μM, 1 and 5mM concentrations. Data show that TCA and HES did not impact aniline hydroxylation at all, whereas RSL turned out to be a potent inhibitor. RUT showed 22% inhibition at 25–100 μM, 33% and 53% inhibition at 1mM & 5mM respectively. CUR and QTN showed slight inhibition, 9% and 33% respectively but only at highest dose. This study suggests that different phytochemicals may have different mechanisms of interfering with drug metabolism; therefore, products containing these phytochemicals must be used with caution during drug therapy.