| Attributes | Values |
|---|
| rdf:type
| |
| Description
| - Sanguinarine (SA), a member of the benzo[c]phenanthridine alkaloids, is a potent anti-microbial agent with anti-inflammatory and anti-neoplastic properties. However, toxicity of the alkaloid severely limits its medical applications. Recent report by Williams et al. implicated rat hepatic cytochrome P450 (CYP) 1A2 as a likely modulator of SA toxicity. Indeed, the in vitro toxicity of SA in primary culture of rat hepatocytes and human hepatic cell line HepG2, demonstrated as lactate dehydrogenase leakage and metabolic capability (MTT assay), was diminished following induction of CYP1A by 2,3,7,8-tetrachlorodibenzo-p-dioxin, 3-methylcholanthrene, and beta-naphtoflavone. Using microsomes containing recombinant CYP1A1 or CYP1A2 we show that SA causes non-competitive inhibition of the former and competitive inhibition of the latter as assessed by ethoxyresorufin de-ethylation (EROD). In human hepatic microsomes SA exhibits competitive inhibition of EROD activity with apparent K(i) of 2 microM, a value ident
- Sanguinarine (SA), a member of the benzo[c]phenanthridine alkaloids, is a potent anti-microbial agent with anti-inflammatory and anti-neoplastic properties. However, toxicity of the alkaloid severely limits its medical applications. Recent report by Williams et al. implicated rat hepatic cytochrome P450 (CYP) 1A2 as a likely modulator of SA toxicity. Indeed, the in vitro toxicity of SA in primary culture of rat hepatocytes and human hepatic cell line HepG2, demonstrated as lactate dehydrogenase leakage and metabolic capability (MTT assay), was diminished following induction of CYP1A by 2,3,7,8-tetrachlorodibenzo-p-dioxin, 3-methylcholanthrene, and beta-naphtoflavone. Using microsomes containing recombinant CYP1A1 or CYP1A2 we show that SA causes non-competitive inhibition of the former and competitive inhibition of the latter as assessed by ethoxyresorufin de-ethylation (EROD). In human hepatic microsomes SA exhibits competitive inhibition of EROD activity with apparent K(i) of 2 microM, a value ident (en)
- Sanguinarin (SA) je benzo[c]fenanthridinový alkaloid s antimikrobiálními, protizánětlivými a protirakovinovými vlastnostmi. Jeho použití v medicíně je však omezeno jeho toxicitou. Podle Williamse et al. [Vet. Hum. Toxicol. 42 (2000) 196] má potkaní jaterní cytochrom P450 (CYP) 1A2 pravděpodobně schopnost ovlivňovat toxicitu SA. Po indukci CYP1A 2,3,7,8-tetrachlorodibenzo-p-dioxinem, 3-methylcholanthrenem a ß-naftoflavonem došlo opravdu v primární kultuře potkaních hepatocytů a v buňkách HepG2 ke snížení in vitro toxicity SA hodnocené stanovením aktivity laktátdehydrogenasy uvolněné do média a stanovením životnosti buněk MTT testem. Při použití mikrosomů obsahujících rekombinantní enzymy SA inhibuje nekompetitivně aktivitu CYP1A1 a kompetitivně aktivitu CYP1A2 sledovanou jako deethylaci 7-ethoxyresorufinu (EROD). U lidských jaterních mikrosomů SA inhibuje kompetitivně EROD aktivitu s hodnotou Ki 2 #M, která je shodná jako u rekombinantního CYP1A2. SA inhibuje také aktivitu NADPH:CYP-reduktasy, enzymu n (cs)
|
| Title
| - Involvement of cytochrome P450 1A in sanguinarine detoxication
- Involvement of cytochrome P450 1A in sanguinarine detoxication (en)
- Zapojení cytochromu P450 1A do detoxikace sanguinarinu (cs)
|
| skos:prefLabel
| - Involvement of cytochrome P450 1A in sanguinarine detoxication
- Involvement of cytochrome P450 1A in sanguinarine detoxication (en)
- Zapojení cytochromu P450 1A do detoxikace sanguinarinu (cs)
|
| skos:notation
| - RIV/61989592:15110/04:00000855!RIV/2005/GA0/151105/N
|
| http://linked.open.../vavai/riv/strany
| |
| http://linked.open...avai/riv/aktivita
| |
| http://linked.open...avai/riv/aktivity
| - P(GP303/01/P085), 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/61989592:15110/04:00000855
|
| http://linked.open...riv/jazykVysledku
| |
| http://linked.open.../riv/klicovaSlova
| - Sanguinarine;cytochrome P450;toxicity;human hepatic microsomes;NADPH : CYP reductase (en)
|
| http://linked.open.../riv/klicoveSlovo
| |
| http://linked.open...odStatuVydavatele
| |
| 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
| - Kosina, Pavel
- Ulrichová, Jitka
- Vrba, Jiří
- Modrianský, Martin
|
| 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)