Chemical genomics and molecular medicine
Notice bibliographique
Résumé
Alzheimer's disease (AD) is a progressive neurodegenerative disease that, in its most common form, occurs as dementia in people over 65 years old although early onset form also exists. Currently it afflicts 24 million people worldwide. The disease is characterized in the brain by abnormal clumps (amyloid plaques) and tangled bundles of fibers (neurofibrillary tangles) composed of misplaced proteins. Three neurotransmitters commonly affected by AD are acetylcholine, serotonin, and nor epinephrine. The cholinergic system-the nerve cell system in the brain that uses acetylcholine as a neurotransmitter-is the most dramatic of the neurotransmitter systems affected by Alzheimer's disease. Acetylcholinesterase is one of the most crucial enzymes that hydrolyze acetylcholine in the brain to choline and acetic acid at cholinergic synapses, leading to nerve response and function. Potentiation of central cholinergic activity has been proposed as a therapeutic approach for improving the cognitive function in patients with Alzheimer's disease (AD). Increasing the acetylcholine concentration in the brain by modulating/inhibiting acetylcholinesterase (AchE) activity is among the most promising therapeutic strategies. In our studies attempts were made to produce potential natural acetylcholinesterase inhibitors. More than eight hundred compounds were taken from different natural sources. Initial in-silico screening of molecules was based on docking score between acetylcholinesterase and compounds taken from the natural sources. The hits were further analyzed and narrowed by applying Lipinski's rule-of-five analysis. Molecules with high ability to cross blood brain barrier were taken for energy minimization and quantitative structure activity studies. The biological activity of promising compounds was predicted by using PASS prediction analysis. Ferulic acid and Caffeic acid found in garlic showed very good IC50 values and satisfied the standard drug-like properties with remarkable pharmacokinetics and pharmacodynamics abilities. Thus we hypothesize that ferulic acid and caffeic acid which is obtained from garlic can be used as an effective acetylcholinesterase inhibitors in the early stage of Alzheimer's disease. Wet lab studies were conducted on the Swiss Albino mice as the animal model to check the inhibition of acetycholinestrerase by ferulic acid and caffeic acid.
Récupéré en direct depuis OpenAlex et désinversé. Les résumés ne sont pas conservés dans cette base de données : les index inversés représentent 8,6 Go des 9,3 Go de texte de la base, et le serveur dispose de 13 Go libres.
Comment cette classification a été obtenuedéplier
Prédiction distillée sur la base complète
Imitation des enseignantsNi prévalence calibrée, ni vérité terrain. Validation humaine à venir. Apprise à partir de 10 348 étiquettes directes de Codex et de 10 348 étiquettes directes de Gemma. Le mode candidate est l'union des têtes enseignantes seuillées; le consensus est leur intersection. Ces sorties portent le statut machine_predicted_unvalidated et ne sont ni des étiquettes humaines ni des étiquettes directes de modèles de pointe.
Scores Codex et Gemma par catégorie
| Catégorie | Codex | Gemma |
|---|---|---|
| Métarecherche | 0,000 | 0,000 |
| Méta-épidémiologie (sens strict) | 0,000 | 0,000 |
| Méta-épidémiologie (sens large) | 0,001 | 0,000 |
| Bibliométrie | 0,000 | 0,000 |
| Études des sciences et des technologies | 0,000 | 0,001 |
| Communication savante | 0,000 | 0,000 |
| Science ouverte | 0,000 | 0,000 |
| Intégrité de la recherche | 0,001 | 0,001 |
| Charge utile insuffisante (le modèle a refusé de juger) | 0,000 | 0,000 |
Scores machine (provisoires)
Les deux têtes enseignantes du modèle étudiant, lues sur ce travail. Un score ordonne la base pour la relecture; il n'affirme jamais une catégorie, et le statut de validation accompagne chaque rangée tel quel.
Scores de référence d'un modèle non mature (critères de maturité non atteints, 7 itérations). Un score ordonne; il n'affirme jamais une catégorie.
score_only:v0-immature-baseline · tel quel depuis la passe de notation : score_only signifie que le nombre peut ordonner les travaux, et qu'aucune étiquette de catégorie n'en découleClassification
machine, non validéePrédiction automatique; un appel candidat d’une seule tête enseignante, pas un consensus.
Le détail, modèle par modèle et score par score, se trouve en fin de page sous « Comment cette classification a été obtenue ».