Molecular Insights on the Modulated Acetylcholinesterase Inhibition Activity of Tacrine Adsorbed on Biocompatible Graphene Oxide

Abstract

Graphene oxide (GO) based nano‐formulation has gained much attention because of its carbonaceous composition with biologically benign properties. In this study, the interactions of GO with tacrine (TAC), an FDA approved Alzheimer's disease (AD) drug, are explored using various analytical tools and theoretical modeling techniques. Furthermore, the modulatory effect of these nano‐conjugates toward the in‐vitro catalytic activity of the neurodegenerative enzyme acetylcholinesterase (AChE) is also quantified. The maximal rate for enzyme inhibition in presence of the nanoconjugate decreases up to an extent of 16 and 34 % in comparison with TAC and GO, respectively. Interestingly, these results are in sharp contrast to the increased AChE activity on adsorption into spherical gold and silver nanoparticles. The current findings demonstrate the synergistic use of TAC−GO hybrid material with augmented AChE inhibition efficacy towards the treatment of Alzheimer's disease (AD). Additionally, GO presents a sustainable alternative for biomedical applications to inorganic equivalents.

Bio-Nano Synergy in Therapeutic Applications: Drug–Graphene Oxide Nanocomposites for Modulated Acetylcholinesterase Inhibition and Radical Scavenging

“…In a recent communication, it has been reported that certain antidiabetic drugs of sulfonylurea class are extremely potent in inhibiting acetylcholinesterase (AChE) activity, suggesting their possible application in the treatment of Alzheimer’s disease (AD) . Additionally, latest research findings from one of the present research groups indicate that tacrine (TAC), an FDA-approved AD medication, might also be effective in reversing the DNA oxidative stress caused by reactive oxygen species (ROS). , Intriguingly, in an earlier study, it is shown that the presence of graphene oxide (GO) enhances the anticholinergic effects of TAC, hinting at a synergistic interaction …”

“…8,9 Intriguingly, in an earlier study, it is shown that the presence of graphene oxide (GO) enhances the anticholinergic effects of TAC, hinting at a synergistic interaction. 10 The incorporation of nanotechnology into medical research marks a significant advancement, especially in the development of innovative therapeutic strategies. 11−15 This is particularly visible in the judicious integration of nanomaterials with biological mechanisms, which holds the promise of transforming the way diseases are treated at both the molecular and cellular scales.…”