| Attributes | Values |
|---|
| rdf:type
| |
| Description
| - Silybin a jeho příbuzné flavonolignany jsou hlavními složkami extraktu ze Silybum marianum, silymarinu, který byl po stovky let používán k léčbě jaterních onemocnění. Ačkoliv je považován za bezpečný, mnoho jeho složek nebylo nikdy testováno v souvislosti s biotransformací léčiv. Cytochromy P450 (CYP) jsou v tomto ohledu velmi důležité. Testovali jsme účinky čtyř flavonolignanů: silybinu, jeho semisyntetického derivátu dehydrosilybinu, silydianinu a silychristinu na tři specifické CYP aktivity: bufuralol 1´-hydroxylaci (CYP2D6), p-nitrofenol hydroxylaci (CYP2E1) a oxidaci nifedipinu (CYP3A4). Všechny flavonolignany vykazovaly inhibici těchto aktivit v závislosti na dávce, s hodnotou IC50 v mikromolární oblasti. Inhibice byla kompetitivní nebo smíšená, což ukázaly grafy dvojitě reciproké závislosti. Ovšem tato inhibice není relevantní pro terapii, protože fyziologické koncentrace jednotlivých flavonolignanů nepřesahují 0,5 mikromolární. Data podporují využití extraktu jako potravního doplňku. (cs)
- Silybin and related flavonolignans form a major part of the Silybum marianum extract, silymarin, which has been used to treat liver diseases for hundreds of years. Although regarded as safe, many of the extract constituents remain thus far untested for their possible effects on liver biotransformation enzymes. Cytochromes P450 (CYP) are very important in this regard. We tested the effect of four flavonolignans: silybin, its hemisynthetic derivative dehydrosilybin, silydianin, and silycristin on three specific CYP activities: bufuralol 1'-hydroxylation (CYP2D6), p-nitrophenol hydroxylation (CYP2E1), and nifedipine oxidation (CYP3A4). All flavonolignans displayed dose-dependent inhibition of these activities with IC(50) values in the micromolar range. The inhibition was competitive or mixed as revealed by double reciprocal plots of kinetic experiments. However, the inhibition is not considered to be relevant for therapy because physiological concentrations of the individual flavonolignans do not ex
- Silybin and related flavonolignans form a major part of the Silybum marianum extract, silymarin, which has been used to treat liver diseases for hundreds of years. Although regarded as safe, many of the extract constituents remain thus far untested for their possible effects on liver biotransformation enzymes. Cytochromes P450 (CYP) are very important in this regard. We tested the effect of four flavonolignans: silybin, its hemisynthetic derivative dehydrosilybin, silydianin, and silycristin on three specific CYP activities: bufuralol 1'-hydroxylation (CYP2D6), p-nitrophenol hydroxylation (CYP2E1), and nifedipine oxidation (CYP3A4). All flavonolignans displayed dose-dependent inhibition of these activities with IC(50) values in the micromolar range. The inhibition was competitive or mixed as revealed by double reciprocal plots of kinetic experiments. However, the inhibition is not considered to be relevant for therapy because physiological concentrations of the individual flavonolignans do not ex (en)
|
| Title
| - Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities
- Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities (en)
- Účinky silybinu a jeho derivátů na aktivitu cytochromů P450 v mikrosomech lidských hepatocytů (cs)
|
| skos:prefLabel
| - Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities
- Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities (en)
- Účinky silybinu a jeho derivátů na aktivitu cytochromů P450 v mikrosomech lidských hepatocytů (cs)
|
| skos:notation
| - RIV/61989592:15110/02:00006948!RIV09-MSM-15110___
|
| http://linked.open...avai/riv/aktivita
| |
| http://linked.open...avai/riv/aktivity
| - P(GA303/99/P002), Z(MSM 151100003)
|
| http://linked.open...iv/cisloPeriodika
| |
| 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
| |
| http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15110/02:00006948
|
| http://linked.open...riv/jazykVysledku
| |
| http://linked.open.../riv/klicovaSlova
| - cytochrome P450; Silybum marianum; flavonolignans; microsomes; human (en)
|
| http://linked.open.../riv/klicoveSlovo
| |
| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
|
| http://linked.open...ontrolniKodProRIV
| |
| http://linked.open...i/riv/nazevZdroje
| |
| 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
| |
| http://linked.open...iv/tvurceVysledku
| - Dvořák, Zdeněk
- Ulrichová, Jitka
- Anzenbacher, Pavel
- Šimánek, Vilím
- Modrianský, Martin
- Zuber, Roman
- Rohovský, Petr
|
| http://linked.open...n/vavai/riv/zamer
| |
| issn
| |
| number of pages
| |
| http://localhost/t...ganizacniJednotka
| |
![[RDF Data]](/fct/images/sw-rdf-blue.png)
![[cxml]](/fct/images/cxml_doc.png)
![[csv]](/fct/images/csv_doc.png)
![[text]](/fct/images/ntriples_doc.png)
![[turtle]](/fct/images/n3turtle_doc.png)
![[ld+json]](/fct/images/jsonld_doc.png)
![[rdf+json]](/fct/images/json_doc.png)
![[rdf+xml]](/fct/images/xml_doc.png)
![[atom+xml]](/fct/images/atom_doc.png)
![[html]](/fct/images/html_doc.png)