KTZ is also a potent inhibitor of human cytochrome P450 3A4 (CYP3A4) enzyme, the major drug-metabolizing CYP isozyme in the human liver. We examined the enantioselective differences of KTZ in the inhibition of human CYP3A4 and in antifungal action. Dextro- and levo-KTZ exhibited modest ...
Conclusion In ordinary condition, no significant interaction between KDZi and CYP3A4 is de-tected in vitro, which indicates that KDZi might be used with CYP3A4 enzyme substrates.%目的:观察苦碟子注射液对大鼠肝微粒体CYP3A4的体外抑制作用与CYP3A4酶底物合用药时可能产生的相互作用。方法采用SD大鼠...
cytochrome P450 is linked to the co-ordination of the nucleophilic nitrogen of the azole heterocyclic ring to the P450 haem iron in the ferric state; potency of the azole drug is determined by the remainder of the molecule (N1-substituent), which interacts with the apoprotein of the enzyme [...
Molecular modeling computations were utilized to generate pharmaceutical grade CYP3A4-enzyme inhibitors. In vitro metabolism of felodipine in human intestinal and liver microsomes (HLM and HIM) was optimized yielding a MichaelisMenten plot from where the Km and Vmax values were estimated by nonlinear ...
Quercetin inhibited CYP3A4 enzyme activity in a concentration-dependent manner with a 50% inhibition concentration (IC 50 ) of 1.97 渭M. In addition, quercetin significantly enhanced the intracellular accumulation of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp. The pharmacokinetic parameters...
Caco-2 cells are widely used as an in vitro intestinal epithelial cell model because they can form a monolayer and predict drug absorption with high accuracy. However, Caco-2 cells hardly express cytochrome P450 (CYP), a drug-metabolizing enzyme. It is k
In silico analysis and molecular docking studies of potential angiotensin-converting enzyme inhibitor using quercetin glycosides Pharmacogn. Mag., 11 (2015), pp. 123-126 CrossrefGoogle Scholar [77] Md.A. Hasan, Md.H.H. Mazumder, A.S. Chowdhury, A. Amit Datta, Md.A. Khan Molecular-docking...
Main drug-metabolizing enzyme systems in human breast tumors and peritumoral tissues. Cancer Res 1993; 53: 3541–6. CAS PubMed Google Scholar Czerwinski M, McLemore TL, Gelboin HV . Quantification of CYP2B7, CYP4B1 and CYPOR messenger RNAs in normal human lung and lung tumors. Cancer...
CYP3A4isamajordrugmetabolitingenzyme,invitro,CYP3A4inhibitorerythromycinaffectedvoriconazolemetabolism.Objective:ToassesstheeffectsofCYP2C19genotypesandCYP3A4一m ediatedinhibitoryeffectsonthepharmacokineticsoftheantimycoticvoriconazoleinChinesesubjects.Methods:ThestudyWascarriedoutasasingle-center,open,two-waycrossover...
(DDIs) involving cytochrome P450 3A4 (CYP3A4), the most abundant P450 in the human liver and intestine, are due to time-dependent inhibition consequent to metabolism of the inhibitor to a reactive intermediate that binds irreversibly or quasi-irreversibly to the enzyme (Silverman, 1995, Venkata...