About: Silybin is metabolized by cytochrome P4502C8 in vitro

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An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Silybin (a flavonolignan, the main component of silymarin, an extract from the seeds of Silybum marianum) has been used to date mostly as a hepatoprotectant. However, it also has other interesting activities, e. g., anticancer and hypocholesterolemic effects. It is also known that silybin can inhibit the activities of the cytochrome P450 (P450) enzymes. In this study, a weak interaction of silybin with human microsomal CYP2E1, 2A6, 2B6, 2C19, and 2D6 (IC50 >= 250 mu M) was found; a moderate inhibition was observed for CYP1A2 and 2C8. The most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 mu M). Using mass spectometry detection, production of O-demethylated (the main metabolite) as well as hydroxylated derivatives of silybin formed by P450 enzymes was detected. The effect of different P450 inhibitors on the formation of O-demethylated product was also studied. In particular, a relatively specific inhibitor of CYP2C8 (quercetin) markedly inhibited the formation of this m Silybin (a flavonolignan, the main component of silymarin, an extract from the seeds of Silybum marianum) has been used to date mostly as a hepatoprotectant. However, it also has other interesting activities, e. g., anticancer and hypocholesterolemic effects. It is also known that silybin can inhibit the activities of the cytochrome P450 (P450) enzymes. In this study, a weak interaction of silybin with human microsomal CYP2E1, 2A6, 2B6, 2C19, and 2D6 (IC50 >= 250 mu M) was found; a moderate inhibition was observed for CYP1A2 and 2C8. The most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 mu M). Using mass spectometry detection, production of O-demethylated (the main metabolite) as well as hydroxylated derivatives of silybin formed by P450 enzymes was detected. The effect of different P450 inhibitors on the formation of O-demethylated product was also studied. In particular, a relatively specific inhibitor of CYP2C8 (quercetin) markedly inhibited the formation of this m (en)
Title	Silybin is metabolized by cytochrome P4502C8 in vitro Silybin is metabolized by cytochrome P4502C8 in vitro (en)
skos:prefLabel	Silybin is metabolized by cytochrome P4502C8 in vitro Silybin is metabolized by cytochrome P4502C8 in vitro (en)
skos:notation	RIV/61989592:15310/07:00004833!RIV10-MSM-15310___
http://linked.open...avai/riv/aktivita	Z
http://linked.open...avai/riv/aktivity	Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	11
http://linked.open...vai/riv/dodaniDat	2010
http://linked.open...aciTvurceVysledku	LUŽNÁ, Pavla Jančová, Petra ANZENBACHER, Pavel Papoušková, Barbora Lemr, Karel Anzenbacherová, Eva Tunková, Alena
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Palackého v Olomouci / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	449798
http://linked.open...ai/riv/idVysledku	RIV/61989592:15310/07:00004833
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Human liver-microsomes; milk thistle; mass-spectrometry; silibinin; pharmacokinetics; inhibition; indinavir; marianum; enzymes; assays ENZYMES; ASSAYS (en)
http://linked.open.../riv/klicoveSlovo	enzymes milk thistle silibinin inhibition pharmacokinetics mass-spectrometry ASSAYS Human liver-microsomes assays ENZYMES indinavir marianum
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[1A4718096A5F]
http://linked.open...i/riv/nazevZdroje	Drug Metabolism and Disposition
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	7 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...UplatneniVysledku	2007
http://linked.open...v/svazekPeriodika	35
http://linked.open...iv/tvurceVysledku	Lemr, Karel Papoušková, Barbora Anzenbacher, Pavel Anzenbacherová, Eva Jančová, Petra Lužná, Pavla Veinlichová, Alena
http://linked.open...n/vavai/riv/zamer	Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0090-9556
number of pages	5 (xsd:int)
http://localhost/t...ganizacniJednotka	15310

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