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Showing 2 results for Alzheimer’s Disease
Ligand-based pharmacophore modeling to identify plant-derived acetylcholinesterase inhibitor natural compounds in Alzheimer’s disease
Saeed Pirmoradi,
Volume 11, Issue 1 (7-2023)
Abstract
Background: Alzheimer’s disease (AD) is a neurodegenerative disease characterized by decreased cognitive function in patients due to forming Aβ peptides and neurofibrillary tangles (NFT) in the brain. Therefore, the need to develop new treatments can reduce this risk. Acetylcholinesterase is one of the targets used in the design of new drugs for the treatment of AD. The researchers obtain new inhibitory ligands based on natural compounds from various medicinal plants, such as the family of Asteroideace, Malvacea, Zingbracea, Hypericacea, and Ebenacea, for treating Alzheimer’s disease. 
Methods: After selecting the reference compound of the enzyme acetylcholinesterase inhibitor with the help of bioinformatics tools such as pharmit and ZINCPHARMER for virtual search through the structural and pharmacologic properties of the reference inhibitor compound, several thousand natural structures of several serious ligands were obtained. Then, the ligands were compared by examining the docking process with the acetylcholinesterase enzyme, and their interactions were visualized with the help of Discovery Studio. Then, the top selected ligands in terms of toxicity, allergy, toxicity, and ADME prediction were evaluated with tools such as molsoft, PKCSM, ADMEtlab2.0, Swiss ADME.
Results: The results revealed that these obtained ligands, like donepezil, have the ability of favorable interactions with different amino acids, the crucial of which are HIS381, TRP385, and GLN527 of AChE, and they all fall in the active site or binding pocket of the active site. The present docking supports this hypothesis that these compounds are possible and valuable small molecule ligands for targeting/inhibiting acetylcholinesterases. Indicatively, according to the binding free energy calculation results, it can be concluded that these ligands can compete with donepezil and affect the formation of acetylcholinesterase complexes. Cholinesterase/donepezil can have an excellent competitive inhibitory effect on it.
Conclusion: On the other hand, the study on the designed ligands showed that with favorable interactions and lower binding energy, they form more stable complexes with acetylcholinesterase and can be proposed as inhibitors competing with donepezil in a bind to this enzyme.
Interactive effects of endurance training combined with saffron and crocin on the hippocampal oxidant-antioxidant system in trimethyltin-induced Alzheimer’s rats
Fatemeh Akbari , Mehrzad Maghdesi , Omid Reza Salehi ,
Volume 13, Issue 1 (9-2025)
Abstract
Background: Alzheimer’s disease (AD) disrupts hippocampal oxidant-antioxidant balance. Although endurance training, saffron, and crocin have shown antioxidant benefits individually, their comparative effects in Alzheimer’s models are not well established. The present study investigated changes in hippocampal oxidant-antioxidant markers in trimethyltin (TMT)-induced Alzheimer’s rats following eight weeks of endurance training (ET), with or without saffron (S) and crocin (Cr) supplementation.
Methods: The current study was performed on 49 male Sprague-Dawley rats (age: 8 weeks old, weight: ~220 g). Forty-two rats received TMT (8 mg/kg, [intraperitoneal] IP) and were randomly assigned to six groups: (1) AD, (2) ET, (3) S, (4) Cr, (5) ET+S, and (6) ET+Cr. Seven healthy rats served as controls (HC). Training groups ran on a treadmill for eight weeks (5 sessions/week, 15-30 min/session, 15-20 m/min). S and Cr groups received daily IP injections (25 mg/kg). Forty-eight hours following the intervention, hippocampal tissue was collected to measure superoxide dismutase (SOD), malondialdehyde (MDA), and total antioxidant capacity (TAC). The data were analyzed using one-way analysis of variance (ANOVA) and Tukey’s post hoc test (SPSS software [version 22], P ≤ 0.05).
Results: Compared to the AD group, MDA levels decreased by 35-56%, and SOD levels increased by 193-257% in all the intervention groups. Moreover, TAC levels showed marked improvement, rising by 185%, 220%, 253%, 309%, and 335% in Cr, S, ET, ET+Cr, and ET+S groups, respectively (P < 0.05). The aforementioned findings highlight the superior antioxidant response in the combined intervention groups, compared to the response in single treatments (P < 0.05).
Conclusion: Endurance training, saffron, and crocin improved hippocampal antioxidant status in Alzheimer’s rats, with combined interventions yielding superior effects.
 

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