Inhibitory Effect of Natural Furanocoumarins on Human Microsomal Cytochrome P450 3A Activity

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Author(s)

Abstract

To investigate the possible drug interaction with herbal medicine, furanocoumarin derivatives isolated from several Umbelliferous crude drugs were examined for their inhibitory effects on a typical human drug metabolizing enzyme, cytochrome P450 3A(CYP3A).Most furanocoumarins tested at 0.1mM reduced microsomal testosterone 6β-hydroxylation as an index of CYP3A activity to less than 50% of the control.In particular, the dimer and trimer derivatives of furanocoumarins showed striking inhibition, whose potencies were similar to that of a typical CYP3A inhibitor, ketoconazole.Preincubation of dimer types of furanocoumarins increased suppression but not most of the monomer derivatives, suggesting that the inhibition on CYP3A activity was caused by at least plural mechanisms.These results raised the possibility that the furanocoumarin containing herbal medicines may alter pharmacokinetics of co-ingested drugs similar to the case with grapefruit juice.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 82(2), 122-129, 2000-02-01

    The Japanese Pharmacological Society

References:  33

Cited by:  6

Codes

  • NII Article ID (NAID)
    10008183057
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00215198
  • NDL Article ID
    5283923
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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