tidepressants that are widely used clinically. As shown in Fig. 1, IMI is oxidized by cytochrome P450 (CYP) mainly via two pathways: side-chain N-demethylation and aromatic ring 2-hydroxylation, forming DMI and 2-hydroxyimipramine (2OH-IMI), respectively. DMI and 2-OH-IMI further undergo 2-hydroxylation and N-demethylation, respectively, forming 2-hydroxy-DMI as the common metabolite (Fig. 1). ...

Enzyme activities of the CYP enzymes (CYP3A4, CYP2C9 and CYP2A6) were determined using classical substrates (testosterone, diclofenac and coumarin, respectively) as well as with luminogenic or fluorogenic substrates in micromethod arrangement. The luciferin-based luminogenic substrates for CYP3A4 and CYP2C9 as well as coumarin in micromethod for assay of CYP2A6 activity gave results well compar...

The mechanism of cis-trans isomerization of prolyl peptides catalyzed by cyclophilin (CyP) was studied computationally via molecular dynamics (MD) simulations of the transition state (TS) and the cis and trans forms of the ground state (GS), when bound to CyP and when free in aqueous solution. The MD simulations include four enzyme-bound species of tetrapeptide (Suc-Ala-XC([double bond]O)-NPro-...

The transport of pesticides from application areas to other results in pesticide contamination and this sort has led unexpected environmental problems worldwide. It is important determine the responses phytoplanktonic organisms these chemicals for an understanding effects on aquatic ecosystems. In study, Arthrospira platensis Gomont cyanobacteria were exposed different concentrations cypermethr...

The neighbourhoods of cytochrome P450 (CYP) genes in deuterostome genomes, as well as those of the cnidarians Nematostella vectensis and Acropora digitifera and the placozoan Trichoplax adhaerens were examined to find clues concerning the evolution of CYP genes in animals. CYP genes created by the 2R whole genome duplications in chordates have been identified. Both microsynteny and macrosynteny...

Benzo[a]pyrene (BaP) is a human carcinogen requiring metabolic activation prior to reaction with DNA. Cytochrome P450 (CYP) 1A1 is the most important hepatic and intestinal enzyme in both BaP activation and detoxification. CYP1A2 is also capable of oxidizing BaP, but to a lesser extent. The induction of CYP1A1/2 by BaP and/or β-naphthoflavone in liver and small intestine of rats was investigate...

1,2-Dichloro-3,3,4,4,5,5-hexafluorocyclopentene (F 6 cypCl 2 ) was functionalized with diphenyl- and dimesitylphosphanyl groups by a salt-elimination reaction of the respecttive chlorophosphane (PPh Cl, PMes Cl) in situ generated lithiated F cyp(Li)Cl. cyp(PR )Cl (R = Ph, Mes) functionalised again to obtain corresponding trimethylstannyl substituted compounds )(SnMe 3 Mes). These tin-precursors...

Caffeic acid phenethyl ester (CAPE), a natural component of propolis, shows anticarcinogenic properties in the modified resistant hepatocyte model when administered before initiation or promotion of hepatocarcinogenesis process; however, information about the mechanism underlying this chemoprotection is limited. The aim of this work was to characterize the effect of CAPE on cytochrome P450 (CYP...

Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP) enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the bacosides from the extract on five major CYP isoforms in vitro ...

Hard conditions of long-term manned spaceflight can affect functions of many biological systems including a system of drug metabolism. The cytochrome P450 (CYP) superfamily plays a key role in the drug metabolism. In this study we examined the hepatic content of some P450 isoforms in mice exposed to 30 days of space flight and microgravity. The CYP content was established by the mass-spectromet...