Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice.

@article{He1998InactivationOC,
  title={Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice.},
  author={Kan Lian He and Krishna R Iyer and Roger N. Hayes and Michael W. Sinz and Thomas F Woolf and Paul F. Hollenberg},
  journal={Chemical research in toxicology},
  year={1998},
  volume={11 4},
  pages={252-9}
}
Grapefruit juice has been found to significantly increase oral bioavailability of several drugs metabolized by cytochrome P450 3A4 (P450 3A4) through inhibiting the enzymatic activity and decreasing the content of intestinal P450 3A4. HPLC/MS/MS and HPLC/UV analyses of ethyl acetate extracts from grapefruit juice revealed the presence of several furanocoumarins of which bergamottin (BG) is the major one. BG was shown to inactivate P450 3A4 in a reconstituted system consisting of purified P450… CONTINUE READING

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