2002
DOI: 10.1124/dmd.30.9.977
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Effects of Bergamottin on Human and Monkey Drug-Metabolizing Enzymes in Primary Cultured Hepatocytes

Abstract: ABSTRACT:We investigated the effect of bergamottin, a major furanocoumarin in grapefruit juice, on phase I and phase II drug-metabolizing enzymes using cultured human and monkey hepatocytes. Both cultured systems were compared and evaluated for the direct effects of bergamottin as well as control treatments on liver enzymes. Treatment of hepatocytes with 0.1, 1, 5, and 10 M bergamottin resulted in a concentration-dependent reduction in CYP3A4 activity (40-100%) in both human and monkey cells, as measured by te… Show more

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Cited by 42 publications
(31 citation statements)
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“…Testosterone metabolism and EROD activity on cultured hepatocytes were conducted as described by Kostrubsky, et al 40 and Wen et al 41 , respectively. Briefly, hepatocytes were isolated from control, non-transplanted mice or those showing repopulation with human hepatocytes using a standard col-lagenase perfusion protocol 42 .…”
Section: Drug Metabolizing Enzymes In Cultured Hepatocytesmentioning
confidence: 99%
See 1 more Smart Citation
“…Testosterone metabolism and EROD activity on cultured hepatocytes were conducted as described by Kostrubsky, et al 40 and Wen et al 41 , respectively. Briefly, hepatocytes were isolated from control, non-transplanted mice or those showing repopulation with human hepatocytes using a standard col-lagenase perfusion protocol 42 .…”
Section: Drug Metabolizing Enzymes In Cultured Hepatocytesmentioning
confidence: 99%
“…Cells were then plated in HMM media (hepatocyte maintenance media; Lonza, USA) at a density of 1.5 million cells per well in collagen I -coated 6 well plates. Cells were cultured for 48 h without inducers and then for 48 additional hours in the presence of 1 mM Phenobarbital, 10 μM rifampicin or 25 μ M beta-naphthoflavone as previously described 40,41 . Following the induction period, cells were washed 3 times with PBS to remove inducers, and media was replaced with fresh media (without inducers).…”
Section: Drug Metabolizing Enzymes In Cultured Hepatocytesmentioning
confidence: 99%
“…RNA was extracted with Trizol reagent using the method recommended by the manufacturer (Invitrogen, Carlsbad, CA). The microarray was fabricated and used as described previously (Kane et al, 2001;Wen et al, 2002). Briefly, three oligonucleotides per gene were designed and amino-modified 50mer oligos were spotted onto SuModic slides using a Molecular Dynamic Gen III robotic spotter (Amersham Biosciences).…”
Section: Methodsmentioning
confidence: 99%
“…Bergamottin (BG) and 6Ј,7Ј-dihydroxybergamottin (DHBG), the two most abundant furanocoumarins present in grapefruit, have been characterized as reversible inhibitors and as mechanism-based inactivators of CYP3A4 (Schmiedlin-Ren et al, 1997;He et al, 1998;Guo et al, 2000;Ohnishi et al, 2000;Tassaneeyakul et al, 2000). Subsequently, studies in primary cultured hepatocytes and more clinically related research with BG and DHBG were pursued (Wen et al, 2002;Goosen et al, 2004;Kakar et al, 2004;Paine et al, 2004Paine et al, , 2006. Accelerated degradation of CYP3A4 after covalent modification of the apoprotein by BG and DHBG was confirmed to play a role in the grapefruit juice effect by several in vivo studies (Goosen et al, 2004;Kakar et al, 2004;Paine et al, 2006).…”
Section: Introductionmentioning
confidence: 99%