Microsequential injection analysis/lab-on-valve system for the automatic evaluation of acetylcholinesterase inhibitors
| Autor: | Marieta L.C. Passos, Diana I. S. P. Resende, Thierno Moussa Ndongo, Fernando Durães, Emília Sousa, Madalena Pinto, Maria Lúcia M. F. S. Saraiva |
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| Rok vydání: | 2021 |
| Předmět: |
Xanthones
Pharmaceutical Science Rivastigmine 01 natural sciences Xanthone Derivatives chemistry.chemical_compound Structure-Activity Relationship Docking (dog) Drug Discovery Xanthone Galantamine medicine Animals Humans Donepezil EC50 Chromatography 010405 organic chemistry Chemistry Reproducibility of Results Acetylcholinesterase 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry Electrophorus Flow Injection Analysis Cholinesterase Inhibitors medicine.drug |
| Zdroj: | Archiv der PharmazieREFERENCES. 354(10) |
| ISSN: | 1521-4184 |
| Popis: | A miniaturized microsequential injection/lab-on-valve (µSIA-LOV) system was developed and shown to be a useful alternative to perform inhibitory studies on acetylcholinesterase. These studies are essential for the evaluation of the potential therapeutic effect of drugs commonly used in the treatment of Alzheimer's disease. Donepezil, galantamine, and rivastigmine were tested, in addition to compounds based on the xanthone scaffold. Four of these xanthone derivatives were identified as having EC50 values between 676 and 4466 µmol/l, showing a potential inhibitory effect higher than the clinical agent rivastigmine. The developed automatic system added advantages of reduction of reagents and sample consumption (around 55 µl per analysis), lower cost per analysis, and the generation of less waste (around 1.2 ml per analysis). The µSIA-LOV system is also a robust, rapid, reliable, and simple system to use. Docking studies suggested a possible mode of interaction with the target acetylcholinesterase protein. |
| Databáze: | OpenAIRE |
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