Minor furanocoumarins and coumarins in grapefruit peel oil as inhibitors of human cytochrome P450 3A4
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2009-09-25
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César, Thaïs B.
Manthey, John A.
Myung, Kyung
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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 IC50 values of 2.42, 0.13, 0.27, and 1.58 μM, respectively.
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Journal of Natural Products, v. 72, n. 9, p. 1702-1704, 2009.