Abstract
We investigated the inhibitory activity of the furanocoumarin derivatives from grapefruit juice to the drug metabolizing enzyme, cytochrome P450 (CYP) 3A4. Although two known furanocoumarin dimers GF-I-1 (1) and GF-I-4 (2) showed potent CYP3A4 inhibition with IC50 value of 0.07 microM, a semi-synthetic dihydroxybergamottin caproate (11), which was more stable and more simple than the dimers, exhibited comparable activity against CYP3A4.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Caproates / chemistry
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Caproates / pharmacology*
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Citrus / chemistry
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme Inhibitors*
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Drug Stability
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Furocoumarins / chemistry
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Furocoumarins / pharmacology*
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Inhibitory Concentration 50
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Mixed Function Oxygenases / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Caproates
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Cytochrome P-450 Enzyme Inhibitors
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Enzyme Inhibitors
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Furocoumarins
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Mixed Function Oxygenases
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CYP3A protein, human
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Cytochrome P-450 CYP3A
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CYP3A4 protein, human