Evaluation of Acetylcholinesterase inhibition by Alnus rugosa L. stems methanol extract and phytochemical content

Rashed, Khaled; Sucupira, Ana Carolina Cardoso; Neto, José Machado Moita; Feitosa, Chistiane Mendes

doi:10.7439/ijbar.v4i9.456

Cited by 4 publications

(4 citation statements)

References 11 publications

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“…Aerial parts of A. rugosa showed antimicrobial and cytotoxic activities [ 4 ]. A. rugosa stem methanolic extract was reported to possess anticholinesterase activity [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Baicalein 5,6-Dimethyl Ether Prevents Memory Deficits in the Scopolamine Zebrafish Model by Regulating Cholinergic and Antioxidant Systems

Brinza

Ayoub

Eldahshan

et al. 2021

Plants

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Baicalein 5,6-dimethyl ether, a bioactive flavonoid isolated for the first time from Alnus rugosa, was explored for its capability to relieve memory deficits and decrease oxidative stress. We examined the neuropharmacological effects of baicalein 5,6-dimethyl ether on scopolamine (Sco)-induced zebrafish (Danio rerio) anxiety, amnesia, and brain oxidative stress and attempted to elucidate the underlying mechanisms. Anxiety-like behavior, exploratory behavior, and memory performance were measured using novel tank-diving test (NTT), Y-maze, and novel object recognition (NOR) tests. For 10 days, baicalein 5,6-dimethyl ether (1, 3, and 5 µg/L) was administered through immersion, whereas Sco (100 μM) was delivered 30 min before behavioral tests. Treatment with baicalein 5,6-dimethyl ether reduced anxiety and memory impairment, and increased exploratory behavior in specific tests, along with significant protection from neuronal oxidative stress in the brain tissue of Sco-treated zebrafish. Antioxidant and anti-acetylcholinesterase (AChE) activities of baicalein 5,6-dimethyl ether in the Sco-induced zebrafish were further confirmed using in vivo assays. In Sco-treated zebrafish, baicalein 5,6-dimethyl ether regulated cholinergic function by inhibiting AChE activity. Baicalein 5,6-dimethyl ether may be a promising candidate compound for treating anxiety and amnesia by restoring cholinergic activity and reducing brain oxidative stress, according to our findings.

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“…Aerial parts of A. rugosa showed antimicrobial and cytotoxic activities [ 4 ]. A. rugosa stem methanolic extract was reported to possess anticholinesterase activity [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Baicalein 5,6-Dimethyl Ether Prevents Memory Deficits in the Scopolamine Zebrafish Model by Regulating Cholinergic and Antioxidant Systems

Brinza

Ayoub

Eldahshan

et al. 2021

Plants

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“…Natural products and their derivatives are known to have efficient biological activities against numerous diseases, including CNS disorders [9]. Numerous plant-derived substances that may be considered as potential AChE drug molecules belong to different classes of compounds characterized by their structures [10].…”

Section: Introductionmentioning

confidence: 99%

Novel ligand-based docking; molecular dynamic simulations; and absorption, distribution, metabolism, and excretion approach to analyzing potential acetylcholinesterase inhibitors for Alzheimer's disease

Vijayakumar¹,

Palani²,

Prabhu³

et al. 2018

Journal of Pharmaceutical Analysis

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Acetylcholinesterase (AChE) plays an important role in Alzheimer's disease (AD). The excessive activity of AChE causes various neuronal problems, particularly dementia and neuronal cell deaths. Generally, anti-AChE drugs induce some serious neuronal side effects in humans. Therefore, this study sought to identify alternative drug molecules from natural products with fewer side effects than those of conventional drugs for treating AD. To achieve this, we developed computational methods for predicting drug and target binding affinities using the Schrodinger suite. The target and ligand molecules were retrieved from established databases. The target enzyme has 539 amino acid residues in its sequence alignment. Ligand molecules of 20 bioactive molecules were obtained from different kinds of plants, after which we performed critical analyses such as molecular docking; molecular dynamic (MD) simulations; and absorption, distribution, metabolism, and excretion (ADME) analysis. In the docking studies, the natural compound rutin showed a superior docking score of −12.335 with a good binding energy value of −73.313 kcal/mol. Based on these findings, rutin and the target complex was used to perform MD simulations to analyze rutin stability at 30 ns. In conclusion, our study demonstrates that rutin is a superior drug candidate for AD. Therefore, we propose that this molecule is worth further investigation using in vitro studies.

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“…Shikimic acid ( 134 ) was found to be the major compound responsible for the wound healing effect [ 88 ]. The methanolic extract of A. rugosa stems showed anticholinesterase activity and it was very interesting for further isolation of acetylcholinesterase inhibitors, which are widely used in the treatment of Alzheimer′s disease [ 138 ].…”

Section: Biological Activitiesmentioning

confidence: 99%

The Genus Alnus, A Comprehensive Outline of Its Chemical Constituents and Biological Activities

et al. 2017

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The genus Alnus (Betulaceae) is comprised of more than 40 species. Many species of this genus have a long history of use in folk medicines. Phytochemical investigations have revealed the presence of diarylheptanoids, polyphenols, flavonoids, terpenoids, steroids and other compounds. Diarylheptanoids, natural products with a 1,7-diphenylheptane structural skeleton, are the dominant constituents in the genus, whose anticancer effect has been brought into focus. Pure compounds and crude extracts from the genus exhibit a wide spectrum of pharmacological activities both in vitro and in vivo. This paper compiles 273 naturally occurring compounds from the genus Alnus along with their structures and pharmacological activities, as reported in 138 references.

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Evaluation of Acetylcholinesterase inhibition by Alnus rugosa L. stems methanol extract and phytochemical content

Cited by 4 publications

References 11 publications

Baicalein 5,6-Dimethyl Ether Prevents Memory Deficits in the Scopolamine Zebrafish Model by Regulating Cholinergic and Antioxidant Systems

Baicalein 5,6-Dimethyl Ether Prevents Memory Deficits in the Scopolamine Zebrafish Model by Regulating Cholinergic and Antioxidant Systems

Novel ligand-based docking; molecular dynamic simulations; and absorption, distribution, metabolism, and excretion approach to analyzing potential acetylcholinesterase inhibitors for Alzheimer's disease

The Genus Alnus, A Comprehensive Outline of Its Chemical Constituents and Biological Activities

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