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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F07%3A00004833%21RIV10-MSM-15310___
rdf:type
n11:Vysledek skos:Concept
dcterms: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
dcterms:title
Silybin is metabolized by cytochrome P4502C8 in vitro Silybin is metabolized by cytochrome P4502C8 in vitro
skos:prefLabel
Silybin is metabolized by cytochrome P4502C8 in vitro Silybin is metabolized by cytochrome P4502C8 in vitro
skos:notation
RIV/61989592:15310/07:00004833!RIV10-MSM-15310___
n3:aktivita
n8:Z
n3:aktivity
Z(MSM6198959216)
n3:cisloPeriodika
11
n3:dodaniDat
n5:2010
n3:domaciTvurceVysledku
n7:4316851 n7:8321124 n7:3649768 n7:2439085 n7:5975700 n7:7271859 n7:2249456
n3:druhVysledku
n12:J
n3:duvernostUdaju
n6:S
n3:entitaPredkladatele
n15:predkladatel
n3:idSjednocenehoVysledku
449798
n3:idVysledku
RIV/61989592:15310/07:00004833
n3:jazykVysledku
n14:eng
n3:klicovaSlova
Human liver-microsomes; milk thistle; mass-spectrometry; silibinin; pharmacokinetics; inhibition; indinavir; marianum; enzymes; assays ENZYMES; ASSAYS
n3:klicoveSlovo
n4:assays%20ENZYMES n4:mass-spectrometry n4:Human%20liver-microsomes n4:ASSAYS n4:inhibition n4:silibinin n4:enzymes n4:marianum n4:indinavir n4:milk%20thistle n4:pharmacokinetics
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[1A4718096A5F]
n3:nazevZdroje
Drug Metabolism and Disposition
n3:obor
n16:CE
n3:pocetDomacichTvurcuVysledku
7
n3:pocetTvurcuVysledku
7
n3:rokUplatneniVysledku
n5:2007
n3:svazekPeriodika
35
n3:tvurceVysledku
Lužná, Pavla Papoušková, Barbora Lemr, Karel Anzenbacher, Pavel Veinlichová, Alena Anzenbacherová, Eva Jančová, Petra
n3:zamer
n17:MSM6198959216
s:issn
0090-9556
s:numberOfPages
5
n18:organizacniJednotka
15310