Role of carbonyl reducing enzymes in the phase I biotransformation of the non-steroidal anti-inflammatory drug nabumetone in vitro

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F13%3A10144044" target="_blank" >RIV/00216208:11160/13:10144044 - isvavai.cz</a>

Výsledek na webu

<a href="http://informahealthcare.com/doi/full/10.3109/00498254.2012.720048" target="_blank" >http://informahealthcare.com/doi/full/10.3109/00498254.2012.720048</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3109/00498254.2012.720048" target="_blank" >10.3109/00498254.2012.720048</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Role of carbonyl reducing enzymes in the phase I biotransformation of the non-steroidal anti-inflammatory drug nabumetone in vitro

Popis výsledku v původním jazyce

1. Nabumetone is a clinically used non-steroidal anti-inflammatory drug, its biotransformation includes major active metabolite 6-methoxy-2-naphtylacetic acid and another three phase I as well as corresponding phase II metabolites which are regarded as inactive. One important biotransformation pathway is carbonyl reduction, which leads to the phase I metabolite, reduced nabumetone. 2. The aim of this study is the determination of the role of a particular human liver subcellular fraction in the nabumetone reduction and the identification of participating carbonyl reducing enzymes along with their stereospecificities. 3. Both subcellular fractions take part in the carbonyl reduction of nabumetone and the reduction is at least in vitro the main biotransformation pathway. The activities of eight cytosolic carbonyl reducing enzymes - CBR1, CBR3, AKR1B1, AKR1B10, AKR1C1-4 - toward nabumetone were tested. Except for CBR3, all tested reductases transform nabumetone to its reduced metabolite. A

Název v anglickém jazyce

Role of carbonyl reducing enzymes in the phase I biotransformation of the non-steroidal anti-inflammatory drug nabumetone in vitro

Popis výsledku anglicky

1. Nabumetone is a clinically used non-steroidal anti-inflammatory drug, its biotransformation includes major active metabolite 6-methoxy-2-naphtylacetic acid and another three phase I as well as corresponding phase II metabolites which are regarded as inactive. One important biotransformation pathway is carbonyl reduction, which leads to the phase I metabolite, reduced nabumetone. 2. The aim of this study is the determination of the role of a particular human liver subcellular fraction in the nabumetone reduction and the identification of participating carbonyl reducing enzymes along with their stereospecificities. 3. Both subcellular fractions take part in the carbonyl reduction of nabumetone and the reduction is at least in vitro the main biotransformation pathway. The activities of eight cytosolic carbonyl reducing enzymes - CBR1, CBR3, AKR1B1, AKR1B10, AKR1C1-4 - toward nabumetone were tested. Except for CBR3, all tested reductases transform nabumetone to its reduced metabolite. A

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

<a href="/cs/project/EE2.3.20.0235" target="_blank" >EE2.3.20.0235: Vybudování výzkumného týmu experimentální a aplikované biofarmacie</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Xenobiotica

ISSN

0049-8254

e-ISSN

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Svazek periodika

43

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

AU - Austrálie

Počet stran výsledku

9

Strana od-do

346-354

Kód UT WoS článku

000315636400004

EID výsledku v databázi Scopus

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