Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors

Abstract

Among neurodegenerative diseases, Alzheimer’s disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treatment of AD. The study aims to evaluate the interactions between natural molecules and AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols and substrates of AChE have been considered for the study with a major emphasis on affinity and kinetics. To better understand the activity of small molecules, the investigation is supported by both experimental and theoretical approach such as fluorescence, Circular Dichroism (CD) and molecular docking studies. Amongst the screened ones tannic acid showed promising results compared with others. The methodology followed here have highlighted many molecules with a higher affinity towards AChE and these findings may take lead molecules generated in preclinical studies to treat neurodegenerative diseases. Additionally, we suggest a unique signature for the heterogeneous analyte model using competitive experiments for analyzing simultanous interactions of both the analytes.

Phytochemical Composition, Antioxidant, Antiacetylcholinesterase, and Cytotoxic Activities of Rumex crispus L.

“…This study showed that the anti-AchE activity of the MeOH extract was higher than that of the other extracts obtained. Indeed, Patil et al [ 63 ] proved that the presence of some phenolic compounds such as Rutin hydrate (with IC 50 = 1.1 × 10 3 μ g/ml) could contribute to the inhibition of AChE. In addition, the present results were better than those found by Ahmad et al [ 62 ] when working with R. hastatus extracts.…”

Laccase-Catalyzed 1,4-Dioxane-Mediated Synthesis of Belladine N-Oxides with Anti-Influenza A Virus Activity

“…Belladine 1 and norbelladine 2 (firstly extracted from the Amaryllidaceae family [ 1 ]) are bioactive precursors in the synthesis of drugs acting on the central nervous system, such as galantamine 3 , lycorine 4 , and haemanthamine 5 ( Figure 1 , Panel a) [ 2 , 3 ]. They are natural substances emerging in therapy, showing a cholinesterase inhibitory activity comparable to that of 3 in the treatment of Alzheimer’s disease [ 4 , 5 ].…”

Assessment of the In Vitro Cytotoxicity Effects of the Leaf Methanol Extract of Crinum zeylanicum on Mouse Induced Pluripotent Stem Cells and Their Cardiomyocytes Derivatives

“…Amaryllidaceae is the leading family of genera holding anticholinesterase inhibitors (AChE) activity [12]. In fact, several secondary metabolites such as alkaloids, terpenoids, polyphenols, and quinones and many further compounds from natural sources have been reported as cholinesterase inhibitors [13,14]. For example, alkaloids and flavonoids have been shown to give protection against chronic diseases.…”