The Use of Isomeric Testosterone Dimers to Explore Allosteric Effects in Substrate Binding to Cytochrome P450 CYP3A4 [PDF]
, 2016 : Cytochrome P450 CYP3A4 is the main drug-metabolizing enzyme in the human liver, being responsible for oxidation of 50% of all pharmaceuticals metabolized by human P450 enzymes.
Bastien, Dominic +6 more
core +2 more sources
CYP3A4 Inhibitors Isolated from Licorice
Biological and Pharmaceutical Bulletin, 2005 The extract of licorice (Glycyrrhiza uralensis FISHER, Leguminosae) showed CYP3A4 inhibitory activity with the IC50 value of 0.022 mg/ml. Bioassay-guided purification afforded nine compounds, 3-(p-hydroxyphenyl)propionic acid (1), isoliquiritigenin (2), (3R)-vestitol (3), licopyranocoumarin (4), 4-hydroxyguaiacol apioglucoside (5), liquiritin (6 ...
Sachiko, Tsukamoto +5 more
openaire +3 more sources
Administration of Vitamin D Metabolites Affects RNA Expression of Xenobiotic Metabolising Enzymes and Function of ABC Transporters in Rats [PDF]
, 2019 From studies on different species and in cell culture systems, it has been suggested that vitamin D metabolites might affect themetabolism and elimination of xenobiotics.
Hansen, Kathrin +7 more
core +1 more source
Interactions between CYP3A4 and Dietary Polyphenols [PDF]
Oxidative Medicine and Cellular Longevity, 2015 The human cytochrome P450 enzymes (P450s) catalyze oxidative reactions of a broad spectrum of substrates and play a critical role in the metabolism of xenobiotics, such as drugs and dietary compounds. CYP3A4 is known to be the main enzyme involved in the metabolism of drugs and most other xenobiotics.
Loai Basheer, Zohar Kerem
openaire +2 more sources
Induced fit for cytochrome P450 3A4 based on molecular dynamics
ADMET and DMPK, 2019 The present study aims at numerically describing to what extent substrate - enzyme complexes in solution may change over time as a natural process of conformational changes for a liganded enzyme in comparison to those movements which occur independently ...
Thomas R.F. Scior, Israel Quiroga
doaj +1 more source
In vitro study on the effect of peucedanol on the activity of cytochrome P450 enzymes
Pharmaceutical Biology, 2021 Context Peucedanol is a major extract of Peucedanum japonicum Thunb. (Apiaceae) roots, which is a commonly used herb in paediatrics. Its interaction with cytochrome P450 enzymes (CYP450s) would lead to adverse effects or even failure of therapy ...
Cun Zhang +4 more
doaj +1 more source
Effects of curcumin on the pharmacokinetics of amlodipine in rats and its potential mechanism
Pharmaceutical Biology, 2020 Context Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and amlodipine.
Na Jiang +3 more
doaj +1 more source
Drug Interaction Study Of Apixaban With Cyclosporine Or Tacrolimus: Results From A Phase 1, Randomized, Open-Label, Crossover Study In Healthy Volunteers [PDF]
, 2018 BACKGROUND Solid organ transplant recipients commonly require anticoagulation. Apixaban (APX) is principally metabolized by CYP3A4, undergoes direct intestinal excretion, and is a substrate to P-glycoprotein (P-gp) and Breast Cancer Resistance Protein ...
Bashir, MD, Babar +5 more
core +1 more source
7‑hydroxymitragynine is an active metabolite of mitragynine and a key mediator of its analgesic effects [PDF]
, 2019 Mitragynina speciosa, more commonly known as kratom, is a plant native to Southeast Asia, the leaves of which have been used traditionally as a stimulant, analgesic, and treatment for opioid addiction.
Ansonoff, Michael +12 more
core +3 more sources
FEBS Open Bio, EarlyView.We investigated the toxicity of 12 active compounds commonly found in herbal weight loss supplements (WLS) using human liver and colon cell models. Epigallocatechin‐3‐gallate was the only compound showing significant toxicity. Metabolic profiling revealed protein degradation, disrupted energy and lipid metabolism suggesting that the inclusion of EGCG ...
Emily C. Davies +3 more
wiley +1 more source