Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study

Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study

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Alzheimer’s disease (AD), a neurodegenerative disease, is the most common form of dementia.Inhibition of acetylcholinesterase (AChE) is a common strategy for the treatment of AD.In this study, aqueous, hydro-methanolic, and methanolic extracts of five potent herbal extracts were tested for their in vitro anti-AChE activity.Among all, the Tinospora cordifolia (Giloy) Furniture methanolic fraction performed better with an IC50 of 202.

64 µg/mL.Of the HPLC analyzed components of T.cordifolia (methanolic extract), palmatine and berberine performed better (IC50 0.66 and 0.

94 µg/mL, respectively) as compared to gallic acid and the tool compound “galantamine hydrobromide” (IC50 7.89 and 1.45 µg/mL, respectively).Mode of inhibition of palmatine and berberine was non-competitive, while the mode was competitive for the tool compound.

Combinations of individual alkaloids palmatine and berberine resulted in a synergistic effect for AChE inhibition.Therefore, the AChE inhibition by the methanolic extract of T.cordifolia was probably due to the synergism of GUT-EASE the isoquinoline alkaloids.Upon molecular docking, it was observed that palmatine and berberine preferred the peripheral anionic site (PAS) of AChE, with π-interactions to PAS residue Trp286, indicating that it may hinder the substrate binding by partially blocking the entrance of the gorge of the active site or the product release.