AI Article Synopsis

  • The study examined how fenugreek seeds powder and its alcoholic extract impact drug-metabolizing enzymes CYP2D6 and CYP3A4.
  • In vitro results showed that fenugreek extract can inhibit CYP2D6 activity at higher concentrations, but in vivo findings indicated it did not significantly affect the metabolism of dextromethorphan in humans.
  • Overall, the research suggests that fenugreek may not have a major influence on the metabolic activity of these enzymes, based on the lack of significant changes in drug metabolite levels.

Article Abstract

Background: The present study investigated the effect of fenugreek seeds powder and its alcoholic extract on metabolic activity of drug-metabolizing enzymes CYP2D6 and CYP3A4.

Materials And Methods: Dextromethorphan (DEX) was used as a probe for measuring metabolic activity, based on its CYP2D6- and CYP3A4-mediated metabolism to dextrorphan (DOR) and 3-methoxymorphinan (3-MM), respectively. For the in vitro investigations, DEX (25µM) was incubated with human liver microsomes and NADPH and tested with and without the fenugreek extract. For the in vivo study, phase I, 6 subjects received a single dose of DEX (30 mg); in phase II, after washout period, the fenugreek seeds powder was administered for 1 week and DEX was administered with its last dose.

Results: In vitro, fenugreek extract inhibits CYP2D6-mediated O-demethylation of DEX. Higher concentrations (50 and 100µg/ml) of extract inhibit CYP2D6 and CYP3A4 activity. In vivo results indicated that fenugreek does not significantly inhibit CYP2D6 and CYP3A4 metabolic activity. There was no significant change in the levels of DEX metabolites (DOR 12% and 3-MM 9%) excreted in urine and their urine metabolic ratios (P values: 0.257 and 0.333 DEX/DOR and DEX/3-MM, respectively).

Conclusion: In vitro and in vivo observations suggested that fenugreek may not have substantial effect on the metabolic activity of CYP2D6 and CYP3A4.

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http://dx.doi.org/10.1159/000432412DOI Listing

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