Metabolism of palmatine by human hepatocytes and recombinant cytochromes P450

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F15%3A33149675" target="_blank" >RIV/61989592:15310/15:33149675 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15110/15:33149675

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S073170851400452X" target="_blank" >http://www.sciencedirect.com/science/article/pii/S073170851400452X</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jpba.2014.09.015" target="_blank" >10.1016/j.jpba.2014.09.015</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Metabolism of palmatine by human hepatocytes and recombinant cytochromes P450

Popis výsledku v původním jazyce

In this study, we developed a new liquid chromatography-mass spectrometry (LC-MS) method for analysis of the protoberberine alkaloid palmatine and its metabolites with separation performed on acyanopropyl-modified stationary phase. Palmatine was metabolized using suspensions of human hepatocytes and human recombinant cytochrome P450 (CYP) enzymes. Our analyses using electrospray ionization-quadrupole time-of-flight mass spectrometry revealed that palmatine was relatively resistant to the metabolic activity of human hepatocytes and recombinant CYP enzymes. However, we found that the biotransformation of palmatine in human hepatocytes included O-demethylation or hydroxylation, and that the product of palmatine demethylation was conjugated by glucuronidation or sulfation. Moreover, we found that human recombinant CYP2D6 and, to a lesser extent, CYP1A2 can mediate O-demethylation of palmatine. These results provide fundamental insights into the biotransformation of palmatine in human in vi

Název v anglickém jazyce

Metabolism of palmatine by human hepatocytes and recombinant cytochromes P450

Popis výsledku anglicky

In this study, we developed a new liquid chromatography-mass spectrometry (LC-MS) method for analysis of the protoberberine alkaloid palmatine and its metabolites with separation performed on acyanopropyl-modified stationary phase. Palmatine was metabolized using suspensions of human hepatocytes and human recombinant cytochrome P450 (CYP) enzymes. Our analyses using electrospray ionization-quadrupole time-of-flight mass spectrometry revealed that palmatine was relatively resistant to the metabolic activity of human hepatocytes and recombinant CYP enzymes. However, we found that the biotransformation of palmatine in human hepatocytes included O-demethylation or hydroxylation, and that the product of palmatine demethylation was conjugated by glucuronidation or sulfation. Moreover, we found that human recombinant CYP2D6 and, to a lesser extent, CYP1A2 can mediate O-demethylation of palmatine. These results provide fundamental insights into the biotransformation of palmatine in human in vi

Druh

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

CEP obor

CB - Analytická chemie, separace

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Journal of Pharmaceutical and Biomedical Analysis

ISSN

0731-7085

e-ISSN

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Svazek periodika

102

Číslo periodika v rámci svazku

JAN

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

6

Strana od-do

193-198

Kód UT WoS článku

000347277500023

EID výsledku v databázi Scopus

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