The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review

Kód výsledku v IS VaVaI

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Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review

Popis výsledku v původním jazyce

Silymarin, a standard extract from Silybum marianum L. seeds, contains at least 7 flavonolignans and flavonoid taxifolin. It has been used to date, as a hepatoprotectant and chemoprotectant. Flavonolignan silybin, the main component of silymarin, is composed of two diastereomers A and B in an approximately 1:1 ratio. Silybin can inhibit the activities of cytochrome P450 enzymes (CYP) (Beckmann-Knopp S. et al., 2000). In our study, the most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 ?M). In the second part of our study, the metabolism of silybin in vitro was analyzed in detail. The results indicated that silybin is subjected to O-demethylation by CYP2C8, enzymes of Phase I in xenobiotic metabolism. The contribution of UDP-glucuronosyltransferases (main phase II enzymes) to the metabolism of silybin and its A and B diastereomers was also investigated. Four main metabolites of silybin, namely silybin A-7-O-?-D-glucuronide, B-7-O-?-D-glucuronide, A-20-O

Název v anglickém jazyce

The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review

Popis výsledku anglicky

Silymarin, a standard extract from Silybum marianum L. seeds, contains at least 7 flavonolignans and flavonoid taxifolin. It has been used to date, as a hepatoprotectant and chemoprotectant. Flavonolignan silybin, the main component of silymarin, is composed of two diastereomers A and B in an approximately 1:1 ratio. Silybin can inhibit the activities of cytochrome P450 enzymes (CYP) (Beckmann-Knopp S. et al., 2000). In our study, the most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 ?M). In the second part of our study, the metabolism of silybin in vitro was analyzed in detail. The results indicated that silybin is subjected to O-demethylation by CYP2C8, enzymes of Phase I in xenobiotic metabolism. The contribution of UDP-glucuronosyltransferases (main phase II enzymes) to the metabolism of silybin and its A and B diastereomers was also investigated. Four main metabolites of silybin, namely silybin A-7-O-?-D-glucuronide, B-7-O-?-D-glucuronide, A-20-O

Druh

D - Stať ve sborníku

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

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Návaznosti

V - Vyzkumna aktivita podporovana z jinych verejnych zdroju

Rok uplatnění

2010

Kód důvěrnosti údajů

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

Název statě ve sborníku

Biomedical Papers of the Faculty of Medicine of Palacký University in Olomouc

ISBN

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ISSN

1213-8118

e-ISSN

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Počet stran výsledku

1

Strana od-do

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Název nakladatele

Univerzita Palackého v Olomouci

Místo vydání

Olomouc

Místo konání akce

Vyškov

Datum konání akce

1. 1. 2010

Typ akce podle státní příslušnosti

CST - Celostátní akce

Kód UT WoS článku

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