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Description
| - Flavonolignan silybin a jeho derivát dehydrosilybin byly navrženy jako kandidátské látky do přípravků chránících kůži před UV zářením. Tato studie se zabývala účinkem silybinu a dehydrosilybinu na aktivitu cytochromu P450 1A1 v lidských keratinocytech (HaCaT) a v lidských hepatomových buňkách (HepG2). Katalytická aktivita CYP1A1 byla monitorována jako O-deethylace 7-ethoxyresorufinu s využitím fluorescenční detekce. Silybin a dehydrosilybin inhibovaly bazální a dioxinem-indukovanou katalytickou aktivitu CYP1A1 v obou typech použitých buněčných linií. Inhibiční účinek testovaných látek byl silnější v buňkách HaCaT ve srovnání s HepG2 buňkami. Dehydrosilybin byl mnohem silnější inhibitor než silybin. Experimenty na lidském rekombinantním CYP1A1 proteinu poskytly hodnoty inhibičních konstant IC50 22,9+/-4,7 mmol/l pro silybin a 0,43+/-0,04 mmol/l pro dehydrosilybin. Jelikož enzymy CYP1A patří mezi prominentí hráče v procesu chemicky vyvolané karcinogeneze, bylo by možné využít inhibiční aktivitu silybinu (cs)
- The flavonolignan silybin and its derivative dehydrosilybin have been proposed as candidate UV-protective agents in skin care products. This study addressed the effect of silybin and dehydrosilybin on the activity of cytochrome P450 isoform CYP1A1 in human keratinocytes (HaCaT) and human hepatoma cells (HepG2). CYP1A1 catalytic activity was assessed as O-deethylation of 7-ethoxyresorufin using fluorescence detection. Silybin and dehydrosylibin inhibited basal and dioxin-inducible CYP1A1 catalytic activity in both cell lines used. The inhibitory effect of tested compounds was more pronounced in HaCaT cells than in HepG2 cells, and dehydrosilybin was a much stronger inhibitor than silybin. Analyses on CYP1A1 human recombinant protein yielded IC(50) values of 22.9 +/- 4.7 micromol/L and 0.43 +/- 0.04 micromol/L for silybin and dehydrosilybin, respectively. Since CYP1A enzymes are some of the most prominent actors in the process of chemically induced carcinogenesis, the inhibitory activity of the flavonol
- The flavonolignan silybin and its derivative dehydrosilybin have been proposed as candidate UV-protective agents in skin care products. This study addressed the effect of silybin and dehydrosilybin on the activity of cytochrome P450 isoform CYP1A1 in human keratinocytes (HaCaT) and human hepatoma cells (HepG2). CYP1A1 catalytic activity was assessed as O-deethylation of 7-ethoxyresorufin using fluorescence detection. Silybin and dehydrosylibin inhibited basal and dioxin-inducible CYP1A1 catalytic activity in both cell lines used. The inhibitory effect of tested compounds was more pronounced in HaCaT cells than in HepG2 cells, and dehydrosilybin was a much stronger inhibitor than silybin. Analyses on CYP1A1 human recombinant protein yielded IC(50) values of 22.9 +/- 4.7 micromol/L and 0.43 +/- 0.04 micromol/L for silybin and dehydrosilybin, respectively. Since CYP1A enzymes are some of the most prominent actors in the process of chemically induced carcinogenesis, the inhibitory activity of the flavonol (en)
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Title
| - Silybin and dehydrosilybin inhibit cytochrome P450 1A1 catalytic activity: a study in human keratinocytes and human hepatoma cells
- Silybin a dehydrosilybin inhibují katalytickou aktivitu cytochromu P450 1A1: studie v lidských keratinocytech a lidských hepatomových buňkách (cs)
- Silybin and dehydrosilybin inhibit cytochrome P450 1A1 catalytic activity: a study in human keratinocytes and human hepatoma cells (en)
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skos:prefLabel
| - Silybin and dehydrosilybin inhibit cytochrome P450 1A1 catalytic activity: a study in human keratinocytes and human hepatoma cells
- Silybin a dehydrosilybin inhibují katalytickou aktivitu cytochromu P450 1A1: studie v lidských keratinocytech a lidských hepatomových buňkách (cs)
- Silybin and dehydrosilybin inhibit cytochrome P450 1A1 catalytic activity: a study in human keratinocytes and human hepatoma cells (en)
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skos:notation
| - RIV/61989592:15110/06:00003104!RIV07-GA0-15110___
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http://linked.open.../vavai/riv/strany
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
| - P(GP303/04/P074), Z(MSM6198959216)
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15110/06:00003104
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - CYP1A1; dehydrosilybin; enzyme inhibition; HaCaT cells; HepG2 cells (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Cell Biology and Toxicology
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Dvořák, Zdeněk
- Ulrichová, Jitka
- Vrzal, Radim
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http://linked.open...n/vavai/riv/zamer
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issn
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number of pages
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http://localhost/t...ganizacniJednotka
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