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- W1986236379 abstract "Sixteen compounds isolated from Zingiber aromaticum and showing concentration-dependent inhibition with IC50 values less than 100 microM, were analyzed for their possibility of time-, concentration-, and NADPH-dependent inhibition of CYP3A4 and four were analyzed for CYP2D6. All seven kaempferol glycosides and two kaempferol derivatives (4, 5, 8-14) appear to be the mechanism-based inhibitors of CYP3A4 enzyme in which the inhibition is irreversible and driven by the catalytic process. The other compounds showed no NADPH-dependent inhibition or reversible inhibition, and thus do not appear to be mechanism-based inhibitors. K(I) values for compounds 4, 5, 8-14 were in the range of 2.21-27.01 microM, whereas the k(inact) values were 0.23-0.65 min(-1). Kaempferol-3-O-(2,3,4-tri-O-acetyl-alpha-L-rhamnopyranoside) (5) was found to be the most potent CYP3A4 inactivator with K(I) and k(inact) values of 2.21 microM and 0.45 min(-1), respectively." @default.
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- W1986236379 date "2005-01-01" @default.
- W1986236379 modified "2023-10-09" @default.
- W1986236379 title "Mechanism-Based Inhibition of CYP3A4 by Constituents of Zingiber aromaticum" @default.
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- W1986236379 doi "https://doi.org/10.1248/bpb.28.495" @default.
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