Phytochemical Analysis and Cholinesterase Inhibitory and Antioxidant Activities of Enhydra fluctuans Relevant in the Management of Alzheimer’s Disease

Lopa, Simin Shabnam; Al-Amin, M.; Hasan, Kamrul; Ahammed, Salim; Islam, K. M.; Alam, Anwar; Tanaka, Toshihisa; Sadik, Golam

doi:10.1155/2021/8862025

Cited by 14 publications

(7 citation statements)

References 30 publications

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“…However, AChE is reported as the major cholinesterase enzyme in the brain that catalyzes the hydrolysis of acetylcholine and shows higher specificity toward acetylcholine. Therefore, AChE enzyme has been an attractive target for AD therapy (26). In our study, P. galeata extract showed moderate inhibition against the AChE enzyme in a dose-dependent manner.…”

Section: Discussionsupporting

confidence: 50%

Antioxidant and Acetylcholinesterase Inhibitor Potentials of the Stem Extract of Pternandra galeata

Suciati

Inayah

Widyawaruyanti

et al. 2022

Vitae

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Background: Pternandra galeata belongs to the family Melastomataceae. It is a native flowering plant in Borneo Island that serve as food for monkey habitat. There has been limited study on the medicinal and chemical properties of this plant. Objectives: We investigated the acetylcholinesterase inhibitory activity and evaluated the antioxidant activity of the ethanolic extract of Pternandra galeata stem. The total phenolic content in the sample was also determined. Methods: The acetylcholinesterase inhibitory assays were performed using Ellman’s method. Two different methods were used to evaluate the antioxidant activity of 2,2-diphenyl-1-picryl hydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The total phenolic content was determined by the Folin-Ciocalteu method by employing gallic acid as a reference. Results: The ethanolic extract of the P. galeata stems inhibited the AChE enzyme with an IC50value of 74.62 ± 0.89 µg/mL. The sample exhibited antioxidant activity in the DPPH assay with an IC50 value of 20.21 ± 0.08 µg/mL and 7.68 ± 0.09µg/mL in the ABTS scavenging assay. The total phenolic content was 164.71 ± 3.33 mg GAE/g extract. Conclusion: The ethanolic extract of the P. galeata stem can be a promising cholinesterase inhibitor and antioxidant for treating Alzheimer’s disease.

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Section: Discussionsupporting

confidence: 50%

Antioxidant and Acetylcholinesterase Inhibitor Potentials of the Stem Extract of Pternandra galeata

Suciati

Inayah

Widyawaruyanti

et al. 2022

Vitae

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“…It has previously been shown that a number of flavonoids can scavenge OH radicals [ 36 ]. Since free radicals have a detrimental role in Alzheimer’s disease progression, radical scavenging activities are crucial [ 37 ]. The present study indicates the half maximal inhibitory concentration (IC 50 ) values denoted the concentration of OPE required to scavenge 50% of free radicals.…”

Section: Discussionmentioning

confidence: 99%

Characterization of Orange Peel Extract and Its Potential Protective Effect against Aluminum Chloride-Induced Alzheimer’s Disease

et al. 2022

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Alzheimer’s disease (AD) is a devastating neurodegenerative disorder without a cure. Hence, developing an effective treatment or protective agent is crucial for public health. The present study aims to characterize orange peel extract (OPE) through in vitro and in silico studies. Furthermore, it examines the protective effect of OPE against experimentally-induced Alzheimer’s disease in rats. The total phenolic and flavonoid content of OPE was 255.86 ± 1.77 and 52.06 ± 1.74 (mg/100 g), respectively. Gallic acid, the common polyphenol in OPE detected by HPLC was 3388.60 μg/100 g. OPE antioxidant IC50 was 67.90 ± 1.05, 60.48 ± 0.91, and 63.70 ± 0.30 by DPPH, ABTS and Hydroxyl radical scavenging activity methods, respectively. In vitro anti-acetylcholinesterase (AChE) IC50 was 0.87 ± 0.025 mg/mL for OPE and 2.45 ± 0.001 mg/mL for gallic acid. Molecular docking analysis for human AChE (4EY7) with donepezil, gallic acid, and acetylcholine showed binding energy ΔG values of −9.47, −3.72, and −5.69 Kcal/mol, respectively. Aluminum chloride injection (70 mg/Kg/day for 6 weeks) induced Alzheimer’s-like disease in male rats. OPE (100 and 200 mg/kg/d) and gallic acid (50 mg/kg/d) were administered orally to experimental animals for 6 weeks in addition to aluminum chloride injection (as protective). OPE was found to protect against aluminum chloride-induced neuronal damage by decreasing both gene expression and activity of acetylcholinesterase (AChE) and a decrease in amyloid beta (Aβ42) protein level, thiobarbituric acid-reactive substances (TBARS), and nitric oxide (NO), and increased reduced glutathione (GSH) level and activity of the antioxidant enzymes in the brain tissues. Additionally, gene expressions for amyloid precursor protein (APP) and beta secretase enzyme (BACE1) were downregulated, whereas those for presinilin-2 (PSEN2) and beta cell lymphoma-2 (BCL2) were upregulated. Furthermore, the reverse of mitochondrial alternation and restored brain ultrastructure might underlie neuronal dysfunction in AD. In conclusion, our exploration of the neuroprotective effect of OPE in vivo reveals that OPE may be helpful in ameliorating brain oxidative stress, hence protecting from Alzheimer’s disease progression.

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“…Thus antioxidants may be more effective to prevent and reverse AD progression ( Gezici et al, 2020 ; Veurink et al, 2020 ). Phenols and flavonoids are considered potential natural antioxidants having the ability to scavenge free radicals and reactive oxygen species because of their conjugated ring structures and OH group’s substitution ( Lopa et al, 2021 ). A study by Wang et al, 2014 suggested that treatment of the polyphenols combination resulted in improved protection against cognitive impairments in mice.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Mollugo oppositifolia Linn. as cholinesterase and β-secretase enzymes inhibitor

Das

Bhardwaj²,

Sharma³

et al. 2023

Front. Pharmacol.

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Mollugo oppositifolia Linn. is traditionally used in neurological complications. The study aimed to investigate in-vitro neuroprotective effect of the plant extracts through testing against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase linked to Alzheimer’s disease (AD). To understand the safety aspects, the extracts were tested for CYP450 isozymes and human hepatocellular carcinoma cell (HepG2) inhibitory potential. The heavy metal contents were estimated using atomic absorption spectroscopy (AAS). Further, the antioxidant capacities as well as total phenolic content and total flavonoid content (TFC) were measured spectrophotometrically. UPLC-QTOF-MS/MS analysis was employed to identify phytometabolites present in the extract. The interactions of the ligands with the target proteins (AChE, BChE, and BACE-1) were studied using AutoDockTools 1.5.6. The results showed that M. oppositifolia extract has more selectivity towards BChE (IC50 = 278.23 ± 1.89 μg/ml) as compared to AChE (IC50 = 322.87 ± 2.05 μg/ml). The IC50 value against β-secretase was 173.93 μg/ml. The extract showed a CC50 value of 965.45 ± 3.07 μg/ml against HepG2 cells and the AAS analysis showed traces of lead 0.02 ± 0.001 which was found to be within the WHO prescribed limits. Moreover, the IC50 values against CYP3A4 (477.03 ± 2.01 μg/ml) and CYP2D6 (249.65 ± 2.46 μg/ml) isozymes justify the safety aspects of the extract. The in silico molecular docking analysis of the target enzymes showed that the compound menthoside was found to be the most stable and showed a good docking score among all the identified metabolites. Keeping in mind the multi-targeted drug approach, the present findings suggested that M. oppositifolia extract have anti-Alzheimer’s potential.

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Phytochemical Analysis and Cholinesterase Inhibitory and Antioxidant Activities of Enhydra fluctuans Relevant in the Management of Alzheimer’s Disease

Cited by 14 publications

References 30 publications

Antioxidant and Acetylcholinesterase Inhibitor Potentials of the Stem Extract of Pternandra galeata

Antioxidant and Acetylcholinesterase Inhibitor Potentials of the Stem Extract of Pternandra galeata

Characterization of Orange Peel Extract and Its Potential Protective Effect against Aluminum Chloride-Induced Alzheimer’s Disease

Evaluation of Mollugo oppositifolia Linn. as cholinesterase and β-secretase enzymes inhibitor

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