Interactions of omeprazole-based analogues with cytochrome P450 2C19: a computational study

2016 ◽  
Vol 12 (6) ◽  
pp. 1913-1921 ◽  
Author(s):  
Junhao Li ◽  
Hanwen Du ◽  
Zengrui Wu ◽  
Haixia Su ◽  
Guixia Liu ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Computational Study ◽  
Drug Metabolizing Enzymes ◽  
Clinical Use ◽  
Metabolizing Enzymes ◽  
Cytochrome P450 2C19

Cytochrome P450 2C19 (CYP2C19) is one of 57 drug metabolizing enzymes in humans and is responsible for the metabolism of ∼7–10% of drugs in clinical use.

Induction of cytochrome P450 and other drug metabolizing enzymes in rat liver following dietary exposure to Aroclor 1254

1991 ◽  
Vol 108 (2) ◽  
pp. 355-365 ◽  
Author(s):  
Ronald A. Lubet ◽  
Collins R. Jones ◽  
Diana L. Stockus ◽  
Stephen D. Fox ◽  
Raymond W. Nims
Keyword(s):  
Cytochrome P450 ◽  
Rat Liver ◽  
Dietary Exposure ◽  
Drug Metabolizing Enzymes ◽  
Aroclor 1254 ◽  
Metabolizing Enzymes

Cytochrome P450, drug metabolizing enzymes and arachidonic acid metabolism in bovine ocular tissues

1987 ◽  
Vol 6 (4) ◽  
pp. 623-630 ◽  
Author(s):  
Michal L. Schwartzman ◽  
Jaime Masferrer ◽  
Michael W. Dunn ◽  
John C. McGiff ◽  
Nader G. Abraham
Keyword(s):  
Arachidonic Acid ◽  
Cytochrome P450 ◽  
Acid Metabolism ◽  
Arachidonic Acid Metabolism ◽  
Drug Metabolizing Enzymes ◽  
Ocular Tissues ◽  
Metabolizing Enzymes ◽  
Bovine Ocular Tissues

scholarly journals Sesquiterpenes Are Agonists of the Pregnane X Receptor but Do Not Induce the Expression of Phase I Drug-Metabolizing Enzymes in the Human Liver

2019 ◽  
Vol 20 (18) ◽  
pp. 4562
Author(s):  
Michaela Šadibolová ◽  
Tomáš Zárybnický ◽  
Tomáš Smutný ◽  
Petr Pávek ◽  
Zdeněk Šubrt ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Phase I ◽  
Reporter Gene ◽  
Pregnane X Receptor ◽  
Receptor Interaction ◽  
Cytochrome P450 3A4 ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes ◽  
Protein Levels ◽  
Reporter Gene Assays

Sesquiterpenes, the main components of plant essential oils, are bioactive compounds with numerous health-beneficial activities. Sesquiterpenes can interact with concomitantly administered drugs due to the modulation of drug-metabolizing enzymes (DMEs). The aim of this study was to evaluate the modulatory effects of six sesquiterpenes (farnesol, cis-nerolidol, trans-nerolidol, α-humulene, β-caryophyllene, and caryophyllene oxide) on the expression of four phase I DMEs (cytochrome P450 3A4 and 2C, carbonyl reductase 1, and aldo-keto reductase 1C) at both the mRNA and protein levels. For this purpose, human precision-cut liver slices (PCLS) prepared from 10 patients and transfected HepG2 cells were used. Western blotting, quantitative real-time PCR and reporter gene assays were employed in the analyses. In the reporter gene assays, all sesquiterpenes significantly induced cytochrome P450 3A4 expression via pregnane X receptor interaction. However in PCLS, their effects on the expression of all the tested DMEs at the mRNA and protein levels were mild or none. High inter-individual variabilities in the basal levels as well as in modulatory efficacy of the tested sesquiterpenes were observed, indicating a high probability of marked differences in the effects of these compounds among the general population. Nevertheless, it seems unlikely that the studied sesquiterpenes would remarkably influence the bioavailability and efficacy of concomitantly administered drugs.

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