Influence of sanguinarine on the GABA synthesizing enzyme glutamate decarboxylase in vitro
Language English Country Germany Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
8794470
Knihovny.cz E-resources
- MeSH
- Alkaloids chemistry pharmacology MeSH
- Benzophenanthridines MeSH
- gamma-Aminobutyric Acid biosynthesis MeSH
- Glutamate Decarboxylase antagonists & inhibitors MeSH
- Enzyme Inhibitors chemistry pharmacology MeSH
- Isoquinolines MeSH
- Kinetics MeSH
- Rats MeSH
- Brain drug effects enzymology MeSH
- Rats, Wistar MeSH
- In Vitro Techniques MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Alkaloids MeSH
- Benzophenanthridines MeSH
- gamma-Aminobutyric Acid MeSH
- Glutamate Decarboxylase MeSH
- Enzyme Inhibitors MeSH
- Isoquinolines MeSH
- sanguinarine MeSH Browser
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.
