Influence of sanguinarine on the GABA synthesizing enzyme glutamate decarboxylase in vitro
Jazyk angličtina Země Německo Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
8794470
Knihovny.cz E-zdroje
- MeSH
- alkaloidy chemie farmakologie MeSH
- benzofenantridiny MeSH
- GABA biosyntéza MeSH
- glutamát dekarboxyláza antagonisté a inhibitory MeSH
- inhibitory enzymů chemie farmakologie MeSH
- isochinoliny MeSH
- kinetika MeSH
- krysa rodu Rattus MeSH
- mozek účinky léků enzymologie MeSH
- potkani Wistar MeSH
- techniky in vitro MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- alkaloidy MeSH
- benzofenantridiny MeSH
- GABA MeSH
- glutamát dekarboxyláza MeSH
- inhibitory enzymů MeSH
- isochinoliny MeSH
- sanguinarine MeSH Prohlížeč
The inhibitory activity of the quaternary benzophenanthridine alkaloid sanguinarine on rat brain glutamate decarboxylase (GAD; EC 4.1.1.15) was studied in vitro. A value of Ki 7.10(-4) mol.1(-1) for sanguinarine was found. The inhibition was irreversible and increased during the preincubation time of sanguinarine with the GAD preparation. The results suggest that reaction of the iminium bond in the benzophenanthridine molecule with thiol groups of the enzyme participates in GAD inhibition. As GAD catalyzes the rate-limiting step of GABA synthesis, its inhibition by sanguinarine may contribute to its physiological action in vivo.