Acetylcholinesterase: Inhibitory activity of some Indonesian vegetables and fraction of selected plants

doi:10.7324/japs.2020.101014

Cited by 3 publications

(2 citation statements)

References 18 publications

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“…The mix was incubated at 37 °C for 15 min for binding with the enzyme. Thereafter, the substrate acetylthiocholine iodide was added to the well, and the increase in absorbance was monitored at 412 nm . Galantamine was used as a reference.…”

Section: Methodsmentioning

confidence: 99%

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Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Srivastava,

Sharma,

Deep

et al. 2023

ACS Omega

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Alzheimer's disease (AD) is a neurodegenerative disorder that impairs neurocognitive function. Acetylcholinesterase (AChE) and β-site APP cleaving enzyme 1 (BACE1) are the two main proteins implicated in AD. Indeed, the major available commercial drugs (donepezil, rivastigmine, and galantamine) against Alzheimer's are AChE inhibitors. However, none of these drugs are known to reverse or reduce the pathophysiological condition of the disease since there are multiple contributing factors to AD. Therefore, there is a need to develop a multitarget-directed ligand approach for its treatment. In the present study, plant bioactive compounds were screened for their AChE and BACE1 inhibition potential by conducting molecular docking studies. Considering their docking score and pharmacokinetic properties, limonin, peimisine, serratanine B, and withanolide A were selected as the lead compounds. Molecular dynamics simulations of these protein−ligand complexes confirmed the conformational and energetically stabilized enzyme−inhibitor complexes. The inhibition potential of the lead compounds was validated by in vitro enzyme assay. Withanolide A inhibited AChE (IC 50 value of 107 μM) and showed mixedtype inhibition. At this concentration, it inhibited BACE1 activity by 57.10% and was stated as most effective. Both the compounds, as well as their crude extracts, were found to have no cytotoxic effect on the SH-SY5Y cell line.

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Section: Methodsmentioning

confidence: 99%

“…Thereafter, the substrate acetylthiocholine iodide was added to the well, and the increase in absorbance was monitored at 412 nm. 47 Galantamine was used as a reference. Based on enzyme activity, the inhibitory potential of the commercial and extracted compounds was determined, and the IC 50 value was calculated.…”

Section: Methodsmentioning

confidence: 99%

Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Srivastava,

Sharma,

Deep

et al. 2023

ACS Omega

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Biological properties and HPLC analyses of four medicinal plants extracts obtained at different extraction temperatures

Eyüpoğlu

Etienne²,

Sinan

et al. 2021

Food Processing Preservation

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In the present study, extracts of four medicinal plants (Cajanus cajan, Carica papaya, Morinda morindoides, and Senna alexandrina) obtained at two different extraction temperatures (24 and 45°C) were investigated for their polyphenolic contents, antioxidant, and enzyme inhibitory properties. For instance, extracts of the studied species yielded total phenolic and flavonoid contents in the range of 17.8-66.3 mg GAE/g and 4.18-26.8 mg RE/g, respectively. High performance liquid chromatography (HPLC) coupled with antioxidant assays (HPLC-FRAP and HPLC-DPPH) was employed for direct identification of antioxidant compounds. The extracts showed moderate to high antioxidant potentials in various assays performed (radical scavenging activity: 10.15-240.08 mg TE/g; reducing activity: 24.88-229.59 mg TE/g; metal chelating activity: 5.56-18.32 mg EDTAE/g and total antioxidant capacity: 1.40-2.18 mM TE/g). Additionally, the extracts were found to exert inhibitory properties against all the studied enzymes (anti-acetylcholinesterase: 1.80-2.29 mg GALAE/g; anti-butyrylcholinesterase: 0.19-3.13 mg GALAE/g; anti-amylase: 0.39-0.58 mmol ACAE/g; anti-glucosidase: 0.17-1.36 mmol ACAE/g and anti-tyrosinase: 60.97-73.71 mg KAE/g). Of all, C. cajan extracts were revealed to be the best antioxidants and inhibitors of most enzymes. Therefore, this study demonstrated the pharmacological potentials of the four medicinal plants, especially C. cajan as viable sources of phyto-ingredients that could be of interest in nutraceutical development. Novelty impact statement• The methanol extracts from four medicinal plant with different extraction temperatures (24 and 45°C) were investigated.• HPLC-DPPH and HPLC-FRAP methodologies were used.• Different levels of phenolics in the tested extracts were determined.

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An Insight into Diverse Activities and Targets of Flavonoids

Tiwari¹,

Mishra²,

Mazumder³

et al. 2023

CDT

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Background: Flavonoids belong to the chemical class of polyphenols and are in the category of secondary metabolites imparting a wide protective effect against acute and chronic diseases. Objective: The study aims to investigate and summarize the information of various flavonoids which were extracted, isolated from various sources, and possess different pharmacological properties by acting on multiple targets. Methods:: This comprehensive review summarizes the research information related to flavonoids and their pharmacological action targets from various sources like PubMed. google scholar and google websites. Result: Extracted information in the paper discusses various therapeutic effects of flavonoids isolated from medicinal plant sources which have the property to inhibit several enzymes which finally results in health benefits like anti-cancer, anti-bacterial, antioxidant, anti-allergic, and anti-viral effects. This study also showed the different solvents and methods involved in the extraction and characterization of the isolated phytochemical constituents. Conclusion: The findings showed the contribution of several flavonoids in the management and inhibition of various acute and chronic sicknesses by acting on different sites in the body. This study may lead to gaining the interest for more research on the bioactives of different medicinal plants for the discovery of new lead compounds or further improvement of the efficacy of the existing compound.

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Acetylcholinesterase: Inhibitory activity of some Indonesian vegetables and fraction of selected plants

Cited by 3 publications

References 18 publications

Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Biological properties and HPLC analyses of four medicinal plants extracts obtained at different extraction temperatures

An Insight into Diverse Activities and Targets of Flavonoids

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