- Paradisin C: A new CYP3A4 inhibitor from grapefruit juice
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A new furanocoumarin derivative, paradisin C, was isolated from grapefruit juice as an inhibitor of cytochrome P450 (CYP) 3A4. Its stereochemistry was elucidated by spectroscopic methods. The stereochemistries of 17,18-dihydroxybergamottin and 17-epoxybergamottin were also elucidated.
- Ohta, Tomihisa,Maruyama, Takuro,Nagahashi, Minoru,Miyamoto, Yasuyo,Hosoi, Shinzo,Kiuchi, Fumiyuki,Yamazoe, Yasushi,Tsukamoto, Sachiko
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- Synthesis and biological evaluation of 6',7'-dihydroxybergamottin (6,7-DHB, a naturally occurring inhibitor of cytochrome P450 3A4
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The recently isolated inhibitor of cytochrome P450 CYP3A4, 6',7'-dihydroxybergamottin (6,7-DHB), was synthesized by an efficient route that is readily adaptable to the production of analogues. The compound was evaluated as an inhibitor of 3A4 in a purified enzyme preparation, as well as against human liver microsomes and human 3A4 expressed in Escherichia coil membrane. In each case, 6,7-DHB proved to be a potent NADPH- and time dependent inactivator of 3A4.
- Bellevue III, Frank H.,Woster, Patrick M.,Edwards, David J.,He, Kan,Hollenberg, Paul F.
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- Design, synthesis and evaluation of furanocoumarin monomers as inhibitors of CYP3A4
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A number of furanocoumarins isolated from grapefruit juice have been found to inhibit CYP3A4 activity in vitro. In this study, we have designed and synthesised a range of analogues based on bergamottin to investigate the relationship between chemical stru
- Row,Brown,Stachulski,Lennard
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p. 1604 - 1610
(2008/02/03)
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- SYNTHESIS OF SPIRO ORTHO ESTERS, SPIRO ORTHO CARBONATES, AND INTERMEDIATES
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Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synt
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