Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
| Autor: | Sai-Sai Xie, Long-Fei Pan, Xiao-Bing Wang, Su-Yi Li, Ling-Yi Kong |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Pharmacology
Chemistry Monoamine oxidase Aché Organic Chemistry Pharmaceutical Science Resveratrol Ligand (biochemistry) Inhibitory postsynaptic potential Biochemistry language.human_language Pathogenesis chemistry.chemical_compound Monoamine neurotransmitter Drug Discovery language Molecular Medicine IC50 |
| Zdroj: | MedChemComm. 5:609-616 |
| ISSN: | 2040-2511 2040-2503 |
| DOI: | 10.1039/c3md00376k |
| Popis: | Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 μM; BuChE, IC50 = 8.04 μM; SI = 1.23), significant inhibition of Aβ42 aggregation (57.78%, at 20 μM) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 μM; MAO-B, IC50 = 12.19 μM), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy. |
| Databáze: | OpenAIRE |
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