Acetylcholinesterase inhibition of Alzheimer’s disease: identification of potential phytochemicals and designing more effective derivatives to manage disease condition

Koly, Hazera Khatun; Sutradhar, Kakan; Rahman, Mustafizur

doi:10.1080/07391102.2023.2166992

Cited by 6 publications

(2 citation statements)

References 67 publications

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“…Thus, glycosylation in positions 3 (C ring) or 5 (A ring) decreases their potency, whereas the presence of hydroxyls in 3' and 5' (B ring) promotes AChE inhibition [122]. Accordingly, anthocyanins have become lead compounds for the development of more effective AChE inhibitors [123].…”

Section: Altered Cholinergic Transmissionmentioning

confidence: 99%

Anthocyanins: Molecular Aspects on Their Neuroprotective Activity

Zaa,

Marcelo,

et al. 2023

Biomolecules

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Anthocyanins are a type of flavonoids that give plants and fruits their vibrant colors. They are known for their potent antioxidant properties and have been linked to various health benefits. Upon consumption, anthocyanins are quickly absorbed and can penetrate the blood–brain barrier (BBB). Research based on population studies suggests that including anthocyanin-rich sources in the diet lower the risk of neurodegenerative diseases. Anthocyanins exhibit neuroprotective effects that could potentially alleviate symptoms associated with such diseases. In this review, we compiled and discussed a large body of evidence supporting the neuroprotective role of anthocyanins. Our examination encompasses human studies, animal models, and cell cultures. We delve into the connection between anthocyanin bioactivities and the mechanisms underlying neurodegeneration. Our findings highlight how anthocyanins’ antioxidant, anti-inflammatory, and anti-apoptotic properties contribute to their neuroprotective effects. These effects are particularly relevant to key signaling pathways implicated in the development of Alzheimer’s and Parkinson’s diseases. In conclusion, the outcome of this review suggests that integrating anthocyanin-rich foods into human diets could potentially serve as a therapeutic approach for neurological conditions, and we identify promising avenues for further exploration in this area.

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Section: Altered Cholinergic Transmissionmentioning

confidence: 99%

Anthocyanins: Molecular Aspects on Their Neuroprotective Activity

Zaa,

Marcelo,

et al. 2023

Biomolecules

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“…Another target is the NMDA receptor, which is associated with memantine as a drug (Figure 1) [13][14][15]. Unfortunately, none of the above mentioned are cures for this disease, since they only stop the progression and are not completely efficient [3,[16][17][18]. Therefore, the formation of the β-amyloid peptide, in which the β-secretase protease, particularly type 1, has been associated with an increase in the concentration of β-amyloid insoluble, which has a commercial inhibitor, verubecestat [19][20][21][22].…”

Section: Introductionmentioning

confidence: 99%

β-Secretase-1: In Silico Drug Reposition for Alzheimer’s Disease

Galeana-Ascencio

Mendieta

Limón

et al. 2023

IJMS

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The β-secretase-1 enzyme (BACE-1) performs a key role in the production of beta-Amyloid protein (Aβ), which is associated with the development of Alzheimer’s disease (AD). The inhibition of BACE-1 has been an important pharmacological strategy in the treatment of this neurodegenerative disease. This study aims to identify new potential candidates for the treatment of Alzheimer’s with the help of in silico studies, such as molecular docking and ADME prediction, from a broad list of candidates provided by the DrugBank database. From this analysis, 1145 drugs capable of interacting with the enzyme with a higher coupling energy than Verubecestat were obtained, subsequently only 83 presented higher coupling energy than EJ7. Applying the oral route of administration as inclusion criteria, only 41 candidates met this requirement; however, 6 of them are associated with diagnostic tests and not treatment, so 33 candidates were obtained. Finally, five candidates were identified as possible BACE-1 inhibitors drugs: Fluphenazine, Naratriptan, Bazedoxifene, Frovatriptan, and Raloxifene. These candidates exhibit pharmacophore-specific features, including the indole or thioindole group, and interactions with key amino acids in BACE-1. Overall, this study provides insights into the potential use of in silico methods for drug repurposing and identification of new candidates for the treatment of Alzheimer’s disease, especially those targeting BACE-1.

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Berberine-loaded iron oxide nanoparticles alleviate cuprizone-induced astrocytic reactivity in a rat model of multiple sclerosis

Ibrahim Fouad,

Mabrouk,

El-Sayed

et al. 2024

Biometals

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Berberine (BBN) is a naturally occurring alkaloid as a secondary metabolite in many plants and exhibits several benefits including neuroprotective activities. However, data on the neuromodulating potential of nanoformulated BBN are still lacking. In the present study, BBN loaded within iron oxide nanoparticles (BBN-IONP) were prepared and characterized by transmission electron microscopy FTIR, X-ray photoelectron spectroscopy particle-size distribution, zeta potential, and HPLC. The remyelinating neuroprotective potential of BBN-IONP relative to free BBN was evaluated against cuprizone (CPZ)-induced neurotoxicity (rats administered 0.2% CPZ powder (w/w) for five weeks). CPZ rats were treated with either free BBN or IONP-BBN (50 mg/kg/day, orally) for 14 days. Cognitive function was estimated using Y-maze. Biochemically, total antioxidant capacity lipid peroxides and reduced glutathione in the brain tissue, as well as, serum interferon-gamma levels were estimated. Moreover, the genetic expression contents of myelin basic protein Matrix metallopeptidase-9 Tumor necrosis factor-α (TNF-α), and S100β were measured. The histopathological patterns and immunohistochemical assessment of Glial Fibrillary Acidic Protein in both cerebral cortex and hippocampus CA1 regions were investigated. CPZ-rats treated with either free BBN or IONP-BBN demonstrated memory restoring, anti-oxidative, anti-inflammatory, anti-astrocytic, and remyelinating activities. Comparing free BBN with IONP-BBN revealed that the latter altered the neuromodulating activities of BBN, showing superior neuroprotective activities of IONP-BBN relative to BBN. In conclusion, both forms of BBN possess neuroprotective potential. However, the use of IONPs for brain delivery and the safety of these nano-based forms need further investigation.

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Acetylcholinesterase inhibition of Alzheimer’s disease: identification of potential phytochemicals and designing more effective derivatives to manage disease condition

Cited by 6 publications

References 67 publications

Anthocyanins: Molecular Aspects on Their Neuroprotective Activity

Anthocyanins: Molecular Aspects on Their Neuroprotective Activity

β-Secretase-1: In Silico Drug Reposition for Alzheimer’s Disease

Berberine-loaded iron oxide nanoparticles alleviate cuprizone-induced astrocytic reactivity in a rat model of multiple sclerosis

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