César TB, Manthey JA, Myung K
Journal of Natural Products, 2009
ABSTRACT:
A new cyclic acetal (1) of marmin (6′,7′-dihydroxy-7-geranyloxycoumarin), two new cyclic acetals (5, 6) of 6′,7′-dihydroxybergamottin, and the known compounds marmin (2), 7-geranyloxycoumarin (3), bergamottin (4), and 6′,7′-dihydroxybergamottin (7) were isolated from grapefruit peel oil. All compounds were tested for inhibitory activity against intestinal cytochrome P450 3A4, an enzyme involved in the “grapefruit/drug” interactions in humans. Coumarins (1-3) exhibited negligible inhibitory activity, while the furanocoumarins (4-7) showed potent in vitro inhibitory activity with IC(50) values of 2.42, 0.13, 0.27, and 1.58 microM, respectively.
CITATION:
César TB, Manthey JA, Myung K. Minor Furanocoumarins and Coumarins in Grapefruit Peel Oil as Inhibitors of Human Cytochrome P450 3A4. J Nat Prod. 2009;72(9):1702-1704.
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