Title : Inhibition of human CYP3A4 activity by grapefruit flavonoids, furanocoumarins and related compounds.

Pub. Date : 2001 Sep-Dec

PMID : 11737987






3 Functional Relationships(s)
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1 METHODS: The effects of various flavonoids and furanocoumarin derivatives on CYP3A4 activity in two human liver microsomal samples was determined using quinine as a substrate. Quinine cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 RESULTS: The results showed that the inhibition of quinine 3-hydroxylation (CYP3A4 activity) by bergapten (67%), and quercetin (55%) was greater than naringenin (39%) and naringin (6%), at the same inhibitor concentration of 100 M. The results also demonstrated that the furan ring in the furanocoumarins enhanced the inhibitory effect on CYP3A4 activity. Quinine cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 RESULTS: The results showed that the inhibition of quinine 3-hydroxylation (CYP3A4 activity) by bergapten (67%), and quercetin (55%) was greater than naringenin (39%) and naringin (6%), at the same inhibitor concentration of 100 M. The results also demonstrated that the furan ring in the furanocoumarins enhanced the inhibitory effect on CYP3A4 activity. Quinine cytochrome P450 family 3 subfamily A member 4 Homo sapiens