当前位置： SCI文献检索 > EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS期刊下所有文献 > Inhibition of ethoxy- and pentoxy-resorufin dealkylases of rat liver by flavones and flavonols: structure-activity relationship.

Inhibition of ethoxy- and pentoxy-resorufin dealkylases of rat liver by flavones and flavonols: structure-activity relationship.

Abstract：

:The inhibitory effects of 17 flavones and flavonols on ethoxy- and pentoxy-resorufin dealkylases of rat liver were investigated. Several findings concerning the relationship between structure and activity can be pointed out. The presence or lack of hydroxyl groups on the flavane nucleus has no influence on the efficiency of inhibition. Flavone and quercetin result in the same degree of inhibition. For polyhydroxylated moleculse, the position of hydroxyl groups on A and B rings was an important factor. The more powerful inhibitors were the flavones having hydroxyl groups only on the A ring (e.g. chrysin) and the inhibitory effect was decreased by addition of hydroxyl substituents on the B group (e.g. quercetin). EROD activities were more responsive than PROD activities. Flavone and quercetin were competitive inhibitors of EROD activity whereas chrysin and morin were mixed type inhibitors. In the case of PROD activity, all four flavones were of the mixed type inhibitors.

journal_name

Eur J Drug Metab Pharmacokinet

journal_title

European journal of drug metabolism and pharmacokinetics

authors

Siess MH,Pennec A,Gaydou E

doi

10.1007/BF03190104

subject

Has Abstract

pub_date

1989-07-01 00:00:00

pages

235-9

issue

3

eissn

0378-7966

issn

2107-0180

journal_volume

14

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS文献大全
  • Effect of induced hypoalbuminemia on distribution, total clearance and unbound clearance of piroxicam in vivo in the rat.

    abstract：:The influence of decreased albumin concentration on the pharmacokinetic behaviour of Piroxicam was studied in vivo in rats that had undergone plasmapheresis. Reductions of approximately 25% and 50% in the plasma albumin concentration were achieved, the former in rats not given plasma expander, the latter in animals gi...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03188792

    authors： Troconiz JI,Lopez-Bustamante LG,Fos D

    更新日期：1993-04-01 00:00:00

  • Parameterization of Microsomal and Cytosolic Scaling Factors: Methodological and Biological Considerations for Scalar Derivation and Validation.

    abstract：:Mathematical models that can predict the kinetics of compounds have been increasingly adopted for drug development and risk assessment. Data for these models may be generated from in vitro experimental systems containing enzymes contributing to metabolic clearance, such as subcellular tissue fractions including micros...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-020-00666-w

    authors： Doerksen MJ,Jones RS,Coughtrie MWH,Collier AC

    更新日期：2020-12-19 00:00:00

  • Pharmacokinetics of natural borneol after oral administration in mice brain and its effect on excitation ratio.

    abstract：:Previous studies have indicated that borneol has double side effects on the central nervous system (CNS), but the mechanism is unknown. The aim of this study was to clarify the relationship between excitation ratio [contents of excitatory amino acids (AAs) versus that of inhibitory] and the content of natural borneol ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-011-0058-5

    authors： Li WR,Chen RY,Yang L,Huang TL,Xu QW,Mi SQ,Wang NS

    更新日期：2012-03-01 00:00:00

  • The metabolic fate of the anti-parkinsonian drug budipine in rats.

    abstract：:The metabolic fate of the anti-Parkinsonian drug budipine was studied in rats after oral administration. The presence of an aromatic hydroxylation product, metabolite M1, and its O-sulphate conjugate was confirmed. Three new minor metabolites, budipine N-oxide, metabolite M1 N-oxide and a secondary metabolite derived ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189947

    authors： Caputo O,Grosa G,Ceruti M,Rocco F,Biglino G

    更新日期：1991-04-01 00:00:00

  • 4-Hydroxy-5-oxo-4,5-dihydrobenzo(a)pyrene, a new metabolite of benzo(a)pyrene.

    abstract：:The detection and the isolation in phenobarbital-induced rat liver microsomal incubation systems of a new metabolite of benzo(a)pyrene are described. The structure of this metabolite and the way in which it is formed are described. ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189442

    authors： Lhoëst G

    更新日期：1980-01-01 00:00:00

  • Metabolism of ticlopidine in rats: identification and quantitative determination of some its metabolites in plasma, urine and bile.

    abstract：:The fate of Ticlopidine, a new inhibitor of platelet aggregation, has been studied in rats following single oral doses. The compound was quickly absorbed as evaluated by the time of the peak plasma concentration. The metabolism of Ticlopidine involved N-oxidation, cleavage of the N-C bond, oxidation of aliphatic carbo...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189474

    authors： Tuong A,Bouyssou A,Paret J,Cuong TG

    更新日期：1981-01-01 00:00:00

  • Is RPMI 2650 a Suitable In Vitro Nasal Model for Drug Transport Studies?

    abstract：:The evaluation of new intranasal medications requires the development of in vitro cell model suitable for high-throughput screening studies. The aim of a pharmacological model is to closely mimic the barrier properties of human nasal mucosa that will influence drug pharmacokinetics. In this context, the human nasal ce...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章,评审

    doi：10.1007/s13318-017-0426-x

    authors： Mercier C,Perek N,Delavenne X

    更新日期：2018-02-01 00:00:00

  • Tolerability and Pharmacokinetics of Hydronidone, an Antifibrotic Agent for Hepatic Fibrosis, after Single and Multiple Doses in Healthy Subjects: an Open-Label, Randomized, Dose-Escalating, First-in-Human Study.

    abstract：BACKGROUND AND OBJECTIVES:Hydronidone is a novel pyridine derivative with therapeutic potential for hepatic fibrosis. The aim of this study was to investigate the safety, tolerability, and pharmacokinetics of hydronidone in healthy subjects. Effects of sex and food on hydronidone pharmacokinetics were also evaluated. ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章,随机对照试验

    doi：10.1007/s13318-015-0316-z

    authors： Liu Y,Wu J,Li Z,Luo Y,Zeng F,Shi S

    更新日期：2017-02-01 00:00:00

  • Effect of metal salts on UDPglucuronosyltransferase activity of various aglycones in rat liver microsomes in vitro.

    abstract：:The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubi...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189441

    authors： Aitio A,Ahotupa M,Parkki MG

    更新日期：1980-01-01 00:00:00

  • The Effects of CYP3A5 Genetic Polymorphisms on Serum Tacrolimus Dose-Adjusted Concentrations and Long-Term Prognosis in Chinese Heart Transplantation Recipients.

    abstract：BACKGROUND AND OBJECTIVES:Effective management of immunosuppressants is extemely important to improve prognosis of heart transplant recipients. We aim to investigate the effects of cytochrome P450 (CYP) 3A5 (rs776746) single nucleotide polymorphisms (SNPs) on serum tacrolimus concentrations/doses (C/Ds, ng/mL per mg/kg...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-019-00563-x

    authors： Liu BY,Chen WQ,Chen ZG,Huang J,Liao ZK,Liu Q,Zheng Z,Song YH,Wang W,Hu SS

    更新日期：2019-12-01 00:00:00

  • The pharmacokinetics of ceftriaxone based on population pharmacokinetics and the prediction of efficacy in Japanese adults.

    abstract：OBJECTIVE:By using a population pharmacokinetic analysis method, we predicted the efficacy of Ceftriaxone (CTRX) based on the pharmacokinetics of CTRX in Japanese adults and the sensitivity of infective organisms to CTRX in 2004. In addition, we clarified the difference in efficacy between once-a-day administration and...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03191159

    authors： Iida S,Kinoshita H,Kawanishi T,Hayashi M

    更新日期：2009-04-01 00:00:00

  • Hepatic clearance of gitoxin: pharmacokinetic study on rabbit isolated liver. Influence of protein binding and comparison with digoxin.

    abstract：:Hepatic clearance of gitoxin has been studied in the rabbit and compared with that of digoxin using an isolated perfused liver technique. During 1.5 hour perfusions with a modified Krebs-Henseleit solution, gitoxin perfusate levels decreased biexponentially; the distribution and elimination half-lives were estimated t...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189574

    authors： Pellegrin P,Lesne M

    更新日期：1983-01-01 00:00:00

  • Interspecies similarities in the disposition of 3H-dihydroergotamine following subcutaneous administration in man and rabbits.

    abstract：:The disposition of dihydroergotamine methanesulfonate following single subcutaneous doses was studied in man and the rabbit using radiotracer techniques. 3H-Dihydroergotamine was almost immediately and completely absorbed from the injection site; peak blood radioactivity levels were attained within 1 h of drug adminis...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189606

    authors： Tse FL,Jaffe JM

    更新日期：1984-01-01 00:00:00

  • Intraocular penetration of fusidic acid with topical Fucithalmic.

    abstract：:Fucithalmic is a newly developed 1% microcrystalline suspension of the antistaphylococcal antibiotic fusidic acid. Penetration into the eye was investigated in twenty patients about to undergo cataract extraction. A single dose produced median antibiotic levels in the aqueous humour of 0.3 mcg/ml, maintained for at le...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189761

    authors： Hansen S

    更新日期：1985-10-01 00:00:00

  • Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis.

    abstract：:Pharmacokinetics of ketoprofen (KTP) enantiomers has been studied in patients with rheumatoid arthritis (RA) following administration of a single oral dose of 100 mg rac-KTP during multidrug therapy taking into consideration the genotype of RA patients Concentrations of (-)-R and (+)-S enantiomers of KTP in plasma, ur...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-011-0041-1

    authors： Główka F,Karaźniewicz-Łada M,Grześkowiak E,Rogozinska D,Romanowski W

    更新日期：2011-09-01 00:00:00

  • Comparative bioavailability and in-vitro antimicrobial activity of two different brands of rifampicin.

    abstract：:A comparative bioavailability study was undertaken between a new formulation of rifampicin 'Famcin' and a standard formulation of rifampicin 'R-cin' in eight healthy male volunteers at two dose levels: 300 mg and 450 mg given orally under both single dose and steady state conditions. Plasma rifampicin was assayed spec...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03189964

    authors： Garg SK,Chakrabarti A,Panigrahi D,Sharma M,Talwar P,Kumar N,Sharma PL

    更新日期：1991-07-01 00:00:00

  • Bioconversion of netobimin pro-drug by gastrointestinal fluids of ruminants.

    abstract：:The biotransformation of netobimin (NTB) pro-drug by ruminal, abomasal and intestinal fluids of sheep and cattle was investigated under anaerobic conditions in vitro. No metabolic conversion of NTB was observed upon incubation with abomasal fluid or boiled samples of different gastrointestinal fluids. NTB pro-drug was...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03188780

    authors： Lanusse CE,Nare B,Gascon LH,Prichard RK

    更新日期：1992-04-01 00:00:00

  • Pharmacokinetics of Polyethylene Glycol-Modified Canine Uricase Following Single and Multiple Intravenous Injections in Cynomolgus Monkeys.

    abstract：BACKGROUND AND OBJECTIVE:Polyethylene glycol-modified canine uricase (PEG-UHC) prepared with a lower-molecular-weight (5 kDa) PEG is used to treat gout. This study investigated the comparative pharmacokinetics of single and multiple doses of PEG-UHC administered intravenously and a single dose of uricase (UHC) administ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-020-00612-w

    authors： Li H,Huo J,Sun D,Jiang L,Hu C,Bai Y,Ma X,Zhang H,Shi X,Zhao Z,Zhou J,Lu Y,Zhang C

    更新日期：2020-08-01 00:00:00

  • Gender difference in ifosfamide metabolism by human liver microsomes.

    abstract：:Pharmacokinetic gender-dependent differences in cytochrome P450-mediated drug metabolism, especially CYP3A4, and their clinical implications are increasingly apparent. CYP3A4 seems to be the most important CYP isoform in both bioactivation and N-dechloroethylation of the alkylating prodrug ifosfamide, but informations...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03190396

    authors： Schmidt R,Baumann F,Hanschmann H,Geissler F,Preiss R

    更新日期：2001-07-01 00:00:00

  • Evaluation of Strategies for the Assessment of Drug-Drug Interactions Involving Cytochrome P450 Enzymes.

    abstract：BACKGROUND AND OBJECTIVES:Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-018-0485-7

    authors： Reinen J,Smit M,Wenker M

    更新日期：2018-12-01 00:00:00

  • Metabolism of small antimicrobial β(2,2)-amino acid derivatives by murine liver microsomes.

    abstract：:We have investigated the in vitro metabolism of three small antimicrobial β(2,2)-amino acid derivatives (M (w) < 500) that are highly potent against methicillin resistant Staphylococcus aureus, and are among the first compounds designed from small cationic antimicrobial peptides with potential ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-012-0086-9

    authors： Hansen T,Moe MK,Anderssen T,Strøm MB

    更新日期：2012-09-01 00:00:00

  • Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics.

    abstract：BACKGROUND AND OBJECTIVES:In the present work, pharmacological and pharmacokinetic properties of the supramolecular complex of non-steroid anti-inflammatory drug ibuprofen (IBU) with natural polysaccharide arabinogalactan (AG) were studied. The main goals of such complexation were the increase of ibuprofen's bioavailab...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-016-0357-y

    authors： Khvostov MV,Borisov SA,Tolstikova TG,Dushkin AV,Tsyrenova BD,Chistyachenko YS,Polyakov NE,Dultseva GG,Onischuk AA,An'kov SV

    更新日期：2017-06-01 00:00:00

  • Prediction of the pharmacokinetics and tissue distribution of levofloxacin in humans based on an extrapolated PBPK model.

    abstract：:This study developed a physiologically based pharmacokinetic (PBPK) model in intraabdominally infected rats and extrapolated it to humans to predict the levofloxacin pharmacokinetics and penetration into tissues. Twelve male rats with intraabdominal infections induced by Escherichia coli received a single dose of 50 m...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-015-0271-8

    authors： Zhu L,Zhang Y,Yang J,Wang Y,Zhang J,Zhao Y,Dong W

    更新日期：2016-08-01 00:00:00

  • Stereoselective Pharmacokinetics of Ketoprofen After Oral Administration of Modified-Release Formulations in Caucasian Healthy Subjects.

    abstract：BACKGROUND AND OBJECTIVES:Ketoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation ...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 临床试验,杂志文章,随机对照试验

    doi：10.1007/s13318-015-0313-2

    authors： Lorier M,Magallanes L,Ibarra M,Guevara N,Vázquez M,Fagiolino P

    更新日期：2016-12-01 00:00:00

  • Clinical Pharmacokinetics of a Lipid-Based Formulation of Risperidone, VAL401: Analysis of a Single Dose in an Open-Label Trial of Late-Stage Cancer Patients.

    abstract：BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/s13318-018-00538-4

    authors： Dilly SJ,Morris GS,Taylor PC,Parmentier F,Williams C,Afshar M

    更新日期：2019-08-01 00:00:00

  • First pass effect of pinazepam in the rabbit liver.

    abstract：:The liver first pass effect of pinazepam in four anaesthetized rabbits was determined by measuring the concentrations of this compound and those of its metabolite N-desmethyldiazepam in the plasma from the portal and hepatic veins. Anaesthesia was induced with an i.p. injection of urethane (1.5 g/kg). Portal and hepat...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03188728

    authors： Pacifici GM,Placidi GF

    更新日期：1982-01-01 00:00:00

  • Disposition of amiodarone in rats after single and multiple intra-peritoneal doses.

    abstract：:The pharmacokinetics of amiodarone was studied after single and multiple dosing in two groups of male Wistar and Albino rats. The first group (40 rats) received a single intraperitoneal (i.p.) dose of amiodarone (100 mg/kg) and 4 rats sacrificed 1, 2, 4, 6, 12, 18, 24, 36, 48 and 72 hours post dosing. The second group...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03192314

    authors： Najjar TA

    更新日期：2000-07-01 00:00:00

  • Pharmacokinetics, pharmacodynamics and aspects of neurotoxic effects of four inhaled aliphatic chlorohydrocarbon solvents as relevant in man.

    abstract：:Intermittent inhalation exposure of adult male rats to dichloromethane, trichloroethylene, 1,1,1-trichloroethane, perchloroethylene or to a combination of trichloroethylene and 1,1,1-trichloroethane for 5 days, for 6 h daily, induced significantly different accumulations of solvent molecules in the body. Adipose tissu...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章,评审

    doi：10.1007/BF03189473

    authors： Savolainen H

    更新日期：1981-01-01 00:00:00

  • Estimation of hepatic distributional volumes using non-labeled reference markers.

    abstract：:Hepatic distributional volumes were investigated in the in situ perfused rat liver. Perfusion experiments were conducted using Krebs bicarbonate buffer delivered via the portal vein in single-pass mode at a total flow rate of 15 mL/min. A bolus dose of normal erythrocytes (RBC, vascular marker) and Evans blue (EB, ext...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03190469

    authors： Karabey Y,Sahin S

    更新日期：2006-10-01 00:00:00

  • Metabolism of the new alpha-1A-adrenergic receptor antagonist, phthalimide-phenylpiperazine analog (RWJ-69442), in rat, dog and human hepatic S9 fractions, and in rats.

    abstract：:The in vitro and in vivo metabolism of RWJ-69442, an alpha-1A-adrenergic receptor antagonist, was investigated after incubation with rat, dog, and human hepatic S9 fractions in the presence of NADPH-generating system, and a single oral/iv dose administration to rats (oral: 100 mg/kg; iv: 10 mg/kg). Unchanged RWJ-69442...

    journal_title：European journal of drug metabolism and pharmacokinetics

    pub_type： 杂志文章

    doi：10.1007/BF03226416

    authors： Wu WN,McKown LA,Kuo GH

    更新日期：2005-01-01 00:00:00