Purpose: The current drugs for Alzheimer's disease (AD) are only used to slow or delay the progression of the pathology. So using a novel technology is a necessity to synthesize more effective medications to control this most common cause of dementia. In this study, using nanochelating technology, ALZc3 was synthesized and its therapeutic effects were evaluated in comparison with memantine on a well-known rat model of AD, which is based on Amyloid-βeta (Aβ) injection into the brain.
Materials And Methods: Aβ (1-42) was injected bilaterally into the CA1 area of the hippocampus of male rats and then animals were treated daily by oral administration of Alz-C3, memantine or their vehicles. Activities of antioxidant enzymes catalase and superoxide dismutase (SOD), glutathione (GSH) and malondialdehyde (MDA) levels, as well as Bax/Bcl-2 ratio, caspase-3 activation, and TNF-α expression were evaluated 7 days after Aβ injection. Finally, learning and memory of the rats were assessed by Morris water maze test.
Results: ALZc3 and memantine improved memory impairment and antioxidant activity and reduced TNF-α expression, caspase-3 activity and Bax/Bcl-2 ratio in the rat's hippocampus. The results showed a superiority of ALZC3 compared to memantine in reducing caspase-3, increasing CAT activity in Aβ (1-42)-injected groups and improving apoptosis factor in healthy mice.
Conclusion: These results indicated that ALZc3 could significantly prevent the memory impairment and Aβ (1-42) toxicity. Thus, ALZc3 could be a promising novel anti-AD agent.
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http://dx.doi.org/10.1007/s11095-020-2773-6 | DOI Listing |
Alzheimers Res Ther
January 2025
MMDN, Univ Montpellier, EPHE, INSERM, Montpellier, France.
Background: Fluoroethylnormemantine (FENM), a new Memantine (MEM) derivative, prevented amyloid-β[25-35] peptide (Aβ)-induced neurotoxicity in mice, a pharmacological model of Alzheimer's disease (AD) with high predictive value for drug discovery. Here, as drug infusion is likely to better reflect drug bioavailability due to the interspecies pharmacokinetics variation, we analyzed the efficacy of FENM after chronic subcutaneous (SC) infusion, in comparison with IP injections in two AD mouse models, Aβ-injected mice and the transgenic APP/PSEN1 (APP/PS1) line.
Methods: In Aβ-treated mice, FENM was infused at 0.
Neurochem Res
January 2025
College of Pharmacy, Guangxi Medical University, Guangxi Zhuang Autonomous Region, Nanning, 530021, China.
To study the neuronal protective effect and its potential mechanism of C16 against gp120-induced cognitive impairment in vitro and in vivo. The NORT method was used to evaluate the short-term memory abilities of rats, the morphological changes in hippocampus were observed by Nissl staining. Cell viability and damage degree were detected by MTT and LDH.
View Article and Find Full Text PDFFront Pharmacol
December 2024
Department of Neurology, Peking University People's Hospital, Beijing, China.
Background: While memantine has been considered a promising drug for migraine prevention, no conclusive evidence exists comparing its efficacy with other migraine-preventive medications. This network meta-analysis (NMA) aimed to access the effectiveness and acceptability of memantine and other guideline-recommended prophylactic agents for migraine.
Methods: We searched the Cochrane Register of Controlled Trials, Embase, PubMed, and ClinicalTrials databases from their inception to 1 June 2024.
Eur J Pharmacol
December 2024
Department of Pharmacology & Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt. Electronic address:
Metabolic dysfunction-associated steatohepatitis (MASH) is a chronic liver disorder marked by hepatic fat accumulation and inflammatory infiltrates which may evolve to cirrhosis. Clinical studies have demonstrated the higher risk of MASH development after tamoxifen (TAM) therapy, especially in obese patients. Therefore, we aimed to evaluate MASH induction by TAM combined with high fat diet (HFD) and the potential interference of memantine (MEMA) with MASH progression via modulation of SIRT6 and its related signaling pathways.
View Article and Find Full Text PDFInt J Pharm Compd
October 2024
University of Cyberjaya, Selangor, Malaysia.
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