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Statements

Subject Item
n2:RIV%2F61989592%3A15110%2F14%3A33150147%21RIV15-MSM-15110___
rdf:type
n15:Vysledek skos:Concept
rdfs:seeAlso
http://pubs.acs.org/doi/ipdf/10.1021/jf404643w
dcterms:description
Anthocyanidins and anthocyanins are pharmacologically active constituents of various berry fruits, such as blueberry and cranberry. These compounds are also contained in massively used nutritional supplements based on extracts or dry matter from berry fruits. The current study evaluated the effects of anthocyanidins and anthocyanins on the expression and catalytic activity of major drug-metabolizing enzymes CYP2C9, CYP2A6, CYP2B6, and CYP3A4 in primary cultures of human hepatocytes and human liver microsomes. Expression of mRNA was quantified by qRT-PCR. Expression of proteins was evaluated by Western blotting and immunochemiluminescence. The catalytic activity of CYP enzymes was measured by HPLC using specific enzyme substrates. Tested anthocyanidins (6) and anthocyanins (21) did not induce the expression of mRNA and protein of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 genes in human hepatocytes. Catalytic activities of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 enzymes were inhibited by all anthocyanidins to different extents (e.g., delphinidin inhibits CYP3A4 by }90% at 100 mýM with IC50 = 32 mýM). Of 21 anthocyanins tested, only cyanidin-3-O-rhamnoside (CYP3A4 by }75% at 100 mýM with IC50 = 44 mýM) and two glycosides of delphinidin significantly inhibited examined cytochromes P450. It may be concluded that in the ranges of common ingestion of either food or dietary supplement an induction or significant inhibition of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 activity is most probably not expected. Anthocyanidins and anthocyanins are pharmacologically active constituents of various berry fruits, such as blueberry and cranberry. These compounds are also contained in massively used nutritional supplements based on extracts or dry matter from berry fruits. The current study evaluated the effects of anthocyanidins and anthocyanins on the expression and catalytic activity of major drug-metabolizing enzymes CYP2C9, CYP2A6, CYP2B6, and CYP3A4 in primary cultures of human hepatocytes and human liver microsomes. Expression of mRNA was quantified by qRT-PCR. Expression of proteins was evaluated by Western blotting and immunochemiluminescence. The catalytic activity of CYP enzymes was measured by HPLC using specific enzyme substrates. Tested anthocyanidins (6) and anthocyanins (21) did not induce the expression of mRNA and protein of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 genes in human hepatocytes. Catalytic activities of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 enzymes were inhibited by all anthocyanidins to different extents (e.g., delphinidin inhibits CYP3A4 by }90% at 100 mýM with IC50 = 32 mýM). Of 21 anthocyanins tested, only cyanidin-3-O-rhamnoside (CYP3A4 by }75% at 100 mýM with IC50 = 44 mýM) and two glycosides of delphinidin significantly inhibited examined cytochromes P450. It may be concluded that in the ranges of common ingestion of either food or dietary supplement an induction or significant inhibition of CYP2C9, CYP2A6, CYP2B6, and CYP3A4 activity is most probably not expected.
dcterms:title
Effects of Anthocyanidins and Anthocyanins on the Expression and Catalytic Activities of CYP2A6, CYP2B6, CYP2C9, and CYP3A4 in Primary Human Hepatocytes and Human Liver Microsomes Effects of Anthocyanidins and Anthocyanins on the Expression and Catalytic Activities of CYP2A6, CYP2B6, CYP2C9, and CYP3A4 in Primary Human Hepatocytes and Human Liver Microsomes
skos:prefLabel
Effects of Anthocyanidins and Anthocyanins on the Expression and Catalytic Activities of CYP2A6, CYP2B6, CYP2C9, and CYP3A4 in Primary Human Hepatocytes and Human Liver Microsomes Effects of Anthocyanidins and Anthocyanins on the Expression and Catalytic Activities of CYP2A6, CYP2B6, CYP2C9, and CYP3A4 in Primary Human Hepatocytes and Human Liver Microsomes
skos:notation
RIV/61989592:15110/14:33150147!RIV15-MSM-15110___
n3:aktivita
n9:S n9:P
n3:aktivity
P(ED0030/01/01), P(ED2.1.00/03.0058), P(GBP303/12/G163), S
n3:cisloPeriodika
3
n3:dodaniDat
n4:2015
n3:domaciTvurceVysledku
n13:3828506 n13:8321124 n13:7271859 n13:2637812
n3:druhVysledku
n5:J
n3:duvernostUdaju
n18:S
n3:entitaPredkladatele
n11:predkladatel
n3:idSjednocenehoVysledku
13681
n3:idVysledku
RIV/61989592:15110/14:33150147
n3:jazykVysledku
n14:eng
n3:klicovaSlova
xenobiotics; human hepatocytes; food?drug interactions; cytochrome P450; anthocyans
n3:klicoveSlovo
n7:xenobiotics n7:anthocyans n7:human%20hepatocytes n7:cytochrome%20P450 n7:food%3Fdrug%20interactions
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[F365D870DD1A]
n3:nazevZdroje
Journal of Agricultural and Food Chemistry
n3:obor
n19:FR
n3:pocetDomacichTvurcuVysledku
4
n3:pocetTvurcuVysledku
7
n3:projekt
n10:GBP303%2F12%2FG163 n10:ED2.1.00%2F03.0058 n10:ED0030%2F01%2F01
n3:rokUplatneniVysledku
n4:2014
n3:svazekPeriodika
62
n3:tvurceVysledku
Švécarová, Michaela Srovnalová, Alžběta Anzenbacherová, Eva Bachleda, Petr Kopečná Zapletalová, Michaela Dvořák, Zdeněk Anzenbacher, Pavel
n3:wos
000330202700031
s:issn
0021-8561
s:numberOfPages
8
n16:doi
10.1021/jf404643w
n20:organizacniJednotka
15110