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Neurochem Res ; 46(4): 905-920, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33486698

RESUMO

Alzheimer's disease (AD) is age-dependent neurological disorder with progressive loss of cognition and memory. This multifactorial disease is characterized by intracellular neurofibrillary tangles, beta amyloid plaques, neuroinflammation, and increased oxidative stress. The increased cellular manifestations of these markers play a critical role in neurodegeneration and pathogenesis of AD. Therefore, reducing neurodegeneration by decreasing one or more of these markers may provide a potential therapeutic roadmap for the treatment of AD. AD causes a devastating loss of cognition with no conclusive and effective treatment. Many synthetic compound containing isoxazolone nucleus have been reported as neuroprotective agents. The aim of this study was to explore the anti-Alzheimer's potential of a newly synthesized 3,4,5-trimethoxy isoxazolone derivative (TMI) that attenuated the beta amyloid (Aß1-42) and tau protein levels in streptozotocin (STZ) induced Alzheimer's disease mouse model. Molecular analysis revealed increased beta amyloid (Aß1-42) protein levels, increased tau protein levels, increased cellular oxidative stress and reduced antioxidant enzymes in STZ exposed mice brains. Furthermore, ELISA and PCR were used to validate the expression of Aß1-42. Pre-treatment with TMI significantly improved the memory and cognitive behavior along with ameliorated levels of Aß1-42 proteins. TMI treated mice further showed marked increase in GSH, CAT, SOD levels while decreased levels of acetylcholinesterase inhibitors (AChEI's) and MDA intermediate. The multidimensional nature of isoxazolone derivatives and its versatile affinity towards various targets highpoint its multistep targeting nature. These results indicated the neuroprotective potential of TMI which may be considered for the treatment of neurodegenerative disease specifically in AD.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Isoxazóis/uso terapêutico , Fármacos Neuroprotetores/uso terapêutico , Acetilcolinesterase/metabolismo , Doença de Alzheimer/induzido quimicamente , Doença de Alzheimer/patologia , Peptídeos beta-Amiloides/metabolismo , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/patologia , Avaliação Pré-Clínica de Medicamentos , Teste de Labirinto em Cruz Elevado , Feminino , Isoxazóis/metabolismo , Masculino , Camundongos , Simulação de Acoplamento Molecular , Fármacos Neuroprotetores/metabolismo , Teste de Campo Aberto/efeitos dos fármacos , Fragmentos de Peptídeos/metabolismo , Ligação Proteica , Estreptozocina , Proteínas tau/metabolismo
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