Nitrofurantoin with Anticholinergic Effect: A Different in Vitro Approach to Alzheimer's Disease
Öz
Alzheimer's disease (AD), a leading cause of dementia, severely affects cognitive function, with the depletion of acetylcholine being a pivotal factor in its pathogenesis. This study delves into the inhibitory potential of the nitrofuran analogue, nitrofurantoin on cholinesterases (ChEs) using comprehensive in vitro approaches. Our findings indicate that nitrofurantoin exhibits differential inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with inhibition constants (KI) of 6.77 ± 0.56 μM for AChE and 9.48 ± 0.69 μM for BChE. These values, although less potent than those of the reference drug tacrine (KIs of 0.17 ± 0.01 μM for AChE and 0.13 ± 0.01 μM for BChE), suggest a noteworthy anticholinergic capability. By providing detailed insights into the enzyme inhibition dynamics, this study lays the groundwork for optimizing nitrofuran derivatives in the therapeutic landscape of AD. The implications of these findings extend to the broader context of pharmacological advancements, highlighting the significance of targeted enzyme inhibition in managing neurodegenerative diseases. Future research building on these results could lead to the development of more effective treatments, enhancing the quality of life for individuals affected by AD and offering new avenues for clinical intervention.
Anahtar Kelimeler
Acetylcholinesterase, Butyrylcholinesterase, Alzheimer, Nitrofuran derivative, Enzyme-ligand interactions
Kaynakça
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