Back to Search
Start Over
Pharmacological evaluation of newly synthesized benzimidazole derivative for anti-Alzheimer potential.
- Source :
- International Journal of Neuroscience; Jun2024, Vol. 134 Issue 6, p635-651, 17p
- Publication Year :
- 2024
-
Abstract
- Backgound: Alzheimer disease (AD) is a disastrous disease characterized by accretion of amyloid-beta plaques, neurofibrillary tangles inducing oxidative stress, loss of neuronal functions and continuous progression of cognitive impairment leading to severe dementia. Material and Methods: The newly synthesized benzimidazole derivative 4-chloro-3-(2-phenyl-1H-benzimidazole-1-sulfonyl) benzoic acid (CB) was evaluated for its anti-Alzheimer activity using in silico, in vivo, in vitro and molecular techniques (ELISA, WB & IHC). Results:In-silico studies revealed that CB has atomic contact energy values of −3.9 to −8.9 kcal/mol against selected targets. In vitro assay showed that CB caused acetylcholinesterase (AChE) and diphenyl-1-picrylhydrazyl inhibition. In-vivo findings revealed improvement in dementia as observed in the morris water maze test and Ymaze test. Amyloid-beta disaggregation, increased level of anti-oxidants, decreased expressions of inflammatory markers and enhanced cellular architecture were found in the cortex and hippocampus of treated rats in the histopathological examination, immunohistochemistry analysis, enzyme-linked immunosorbent assay and western blot analysis. Conclusions: This study revealed that CB possess different binding affinities with the Alzheimer-related targets and it possess anti-Alzheimer activity, mediated via AChE and amyloid-beta inhibition, anti-oxidant and anti-inflammatory pathways. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00207454
- Volume :
- 134
- Issue :
- 6
- Database :
- Complementary Index
- Journal :
- International Journal of Neuroscience
- Publication Type :
- Academic Journal
- Accession number :
- 177520066
- Full Text :
- https://doi.org/10.1080/00207454.2022.2138382