Synthesis of Quercetin-Metal Complexes, In Vitro and In Silico Anticholinesterase and Antioxidant Evaluation, and In Vivo Toxicological and Anxiolitic Activities
| Autor: | Francisca Crislândia Oliveira Silva, Emmanuel Silva Marinho, Francisco Ernani Alves Magalhães, Jacilene Silva, Daniela Ribeiro Alves, Jane Eire Silva Alencar de Menezes, Solange de Oliveira Pinheiro, Wildson Max Barbosa da Silva, Selene Maia de Morais |
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| Rok vydání: | 2019 |
| Předmět: |
0301 basic medicine
Antioxidant medicine.drug_class medicine.medical_treatment Drug Evaluation Preclinical Toxicology Anxiolytic Antioxidants Protein Structure Secondary Coordination complex 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine In vivo Coordination Complexes medicine Animals Computer Simulation Zebrafish chemistry.chemical_classification General Neuroscience Acetylcholinesterase Molecular Docking Simulation 030104 developmental biology Enzyme chemistry Biochemistry Anti-Anxiety Agents Quercetin Cholinesterase Inhibitors 030217 neurology & neurosurgery Acetylcholine Iron Compounds Locomotion medicine.drug |
| Zdroj: | Neurotoxicity research. 37(4) |
| ISSN: | 1476-3524 |
| Popis: | The level of acetylcholine, a neurotransmitter essential for processing memory and learning, is lower in the brains of patients with Alzheimer’s disease due to the higher concentration of the enzyme acetylcholinesterase. The main compounds used for Alzheimer’s treatment are acetylcholinesterase inhibitors. Quercetin coordination complexes with the metal ions Cu+2, Zn+2, Ni+2, Co+2, and Fe+2 were synthesized to investigate their potential use against Alzheimer’s disease, by evaluating the inhibition of acetylcholinesterase in vitro and in silico, as well as the antioxidant activity, toxicity, and anxiolytic action in the zebrafish (Danio rerio) model. The organic complexes were characterized by UV-Vis and FT-IR. The spectral information suggested that coordination of metals occurs with the carbonyl group and OH linked to the C-3 carbon of quercetin. The quercetin-Fe (QFe) complex presented the best antioxidant and antiacetylcholinesterase actions, and these results were confirmed by molecular docking. In the toxicity and locomotor evaluation, the quercetin molecules and the synthesized complexes, mainly QCu and QZn derivatives, showed the highest degree of inhibition of the fish’s locomotor activity, suggesting a possible anxiolytic action. Then, quercetin complexes with metals, mainly with Fe+2, represent valuable compounds and deserve more investigation as promising agents against Alzheimer’s disease. |
| Databáze: | OpenAIRE |
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