Gypsogenin Derivatives: An Unexpected Class of Inhibitors of Cholinesterases
| Autor: | Lucie Heller, Stefan Schwarz, Björn Weber, René Csuk |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
chemistry.chemical_classification
biology Aché Stereochemistry Saponin Pharmaceutical Science biology.organism_classification Acetylcholinesterase Electric eel language.human_language chemistry.chemical_compound Hydrolysis Enzyme chemistry Drug Discovery language Galantamine Hydrobromide Butyrylcholinesterase |
| Zdroj: | Archiv der Pharmazie. 347:707-716 |
| ISSN: | 0365-6233 |
| DOI: | 10.1002/ardp.201400103 |
| Popis: | Gypsogenin (1) was obtained by acidic hydrolysis from its saponin. While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 ± 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-dinitrile (11) and acetylcholinesterase (AChE, from electric eel). Thus, 11 possesses one-fifth of the inhibitory activity of the "gold standard" galantamine hydrobromide; this compound is one of the first pentacyclic triterpenoids described as a potent AChE-selective inhibitor. |
| Databáze: | OpenAIRE |
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