Metabolism of flavonolignans in human hepatocytes

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F18%3A73588074" target="_blank" >RIV/61989592:15110/18:73588074 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61388971:_____/18:00489013 RIV/61989592:15310/18:73588074

Výsledek na webu

<a href="https://reader.elsevier.com/reader/sd/pii/S0731708517328790?token=536998082A11DD8D459B26DFEBDE755AAD012F73D9ED1423DF59A4F695FC5FD49A6BC2ED6C00E9FA26DCA8A590AEBAAA" target="_blank" >https://reader.elsevier.com/reader/sd/pii/S0731708517328790?token=536998082A11DD8D459B26DFEBDE755AAD012F73D9ED1423DF59A4F695FC5FD49A6BC2ED6C00E9FA26DCA8A590AEBAAA</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jpba.2018.01.048" target="_blank" >10.1016/j.jpba.2018.01.048</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Metabolism of flavonolignans in human hepatocytes

Popis výsledku v původním jazyce

Anotace: Biotransformation of silybin, 2,3-dehydrosilybin, silychristin, 2,3-dehydrosilychristin, silydianin, 2,3-dehydrosilydianin, isosilybin A and isosilybin B was examined using primary cultures of human hepatocytes and recombinant human cytochromes P450 (CYPs). The metabolites were analyzed by UPLC/MS. Eeach of the tested compounds was metabolized by one or more CYP enzymes which catalyzed O-demethylation, hydroxylation, hydrogenation and dehydrogenation reactions. In human hepatocytes, silybin, 2,3-dehydrosilybin, silychristin, 2,3-dehydrosilychristin, and isosilybins A and B were conjugated by sulfation or glucuronidation. Isosilybin A was also converted to a methyl derivative, while isosilybin B was hydroxylated and methylated. Silydianin and 2,3-dehydrosilydianin underwent hydrogenation and/or glucuronidation. In addition, the main metabolite of 2,3-dehydrosilydianin was a cleavage product corresponding to a loss of CO. We conclude that the hepatic biotransformation of flavonolignans primarily involves the phase II conjugation reactions, however in some cases the phase I reactions may also occur.

Název v anglickém jazyce

Metabolism of flavonolignans in human hepatocytes

Popis výsledku anglicky

Anotace: Biotransformation of silybin, 2,3-dehydrosilybin, silychristin, 2,3-dehydrosilychristin, silydianin, 2,3-dehydrosilydianin, isosilybin A and isosilybin B was examined using primary cultures of human hepatocytes and recombinant human cytochromes P450 (CYPs). The metabolites were analyzed by UPLC/MS. Eeach of the tested compounds was metabolized by one or more CYP enzymes which catalyzed O-demethylation, hydroxylation, hydrogenation and dehydrogenation reactions. In human hepatocytes, silybin, 2,3-dehydrosilybin, silychristin, 2,3-dehydrosilychristin, and isosilybins A and B were conjugated by sulfation or glucuronidation. Isosilybin A was also converted to a methyl derivative, while isosilybin B was hydroxylated and methylated. Silydianin and 2,3-dehydrosilydianin underwent hydrogenation and/or glucuronidation. In addition, the main metabolite of 2,3-dehydrosilydianin was a cleavage product corresponding to a loss of CO. We conclude that the hepatic biotransformation of flavonolignans primarily involves the phase II conjugation reactions, however in some cases the phase I reactions may also occur.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10608 - Biochemistry and molecular biology

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)

Rok uplatnění

2018

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

—

Svazek periodika

152

Číslo periodika v rámci svazku

April

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

8

Strana od-do

94-101

Kód UT WoS článku

000428362000013

EID výsledku v databázi Scopus

2-s2.0-85042904574