About: 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     Goto   Sponge   NotDistinct   Permalink

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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. (en)
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 (en)
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 (en)
skos:notation
  • RIV/61989592:15110/14:33150147!RIV15-MSM-15110___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(ED0030/01/01), P(ED2.1.00/03.0058), P(GBP303/12/G163), S
http://linked.open...iv/cisloPeriodika
  • 3
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 13681
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15110/14:33150147
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • xenobiotics; human hepatocytes; food?drug interactions; cytochrome P450; anthocyans (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [F365D870DD1A]
http://linked.open...i/riv/nazevZdroje
  • Journal of Agricultural and Food Chemistry
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 62
http://linked.open...iv/tvurceVysledku
  • Dvořák, Zdeněk
  • Anzenbacher, Pavel
  • Anzenbacherová, Eva
  • Bachleda, Petr
  • Srovnalová, Alžběta
  • Švécarová, Michaela
  • Kopečná Zapletalová, Michaela
http://linked.open...ain/vavai/riv/wos
  • 000330202700031
issn
  • 0021-8561
number of pages
http://bibframe.org/vocab/doi
  • 10.1021/jf404643w
http://localhost/t...ganizacniJednotka
  • 15110
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