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

1
Drug Discovery and Development Division, Patanjali Research Institute, Patanjali Research Foundation Trust, Roorkee-Haridwar Road, Haridwar 249405, India
2
Department of Allied Sciences, University of Patanjali, Roorkee-Haridwar Road, Haridwar 249405, India
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(22), 4175; https://doi.org/10.3390/molecules24224175
Received: 25 September 2019 / Revised: 6 November 2019 / Accepted: 12 November 2019 / Published: 18 November 2019
(This article belongs to the Section Natural Products Chemistry)
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) 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 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. View Full-Text
Keywords: Alzheimer’s disease; anti-acetylcholinesterase activity; herbal extracts; HPLC; synergistic effect; molecular docking Alzheimer’s disease; anti-acetylcholinesterase activity; herbal extracts; HPLC; synergistic effect; molecular docking
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MDPI and ACS Style

Balkrishna, A.; Pokhrel, S.; Tomer, M.; Verma, S.; Kumar, A.; Nain, P.; Gupta, A.; Varshney, A. Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study. Molecules 2019, 24, 4175. https://doi.org/10.3390/molecules24224175

AMA Style

Balkrishna A, Pokhrel S, Tomer M, Verma S, Kumar A, Nain P, Gupta A, Varshney A. Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study. Molecules. 2019; 24(22):4175. https://doi.org/10.3390/molecules24224175

Chicago/Turabian Style

Balkrishna, Acharya; Pokhrel, Subarna; Tomer, Meenu; Verma, Sudeep; Kumar, Ajay; Nain, Pradeep; Gupta, Abhishek; Varshney, Anurag. 2019. "Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study" Molecules 24, no. 22: 4175. https://doi.org/10.3390/molecules24224175

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