In-vitro evaluation and in-silico studies applied on newly synthesized amide derivatives of N-phthaloylglycine as Butyrylcholinesterase (BChE) inhibitors

Begum, Sabira; Nizami, Shaikh Sirajuddin; Mahmood, Uzma; Masood, Summyia; Iftikhar, Sahar; Saied, Summayya

doi:10.1016/j.compbiolchem.2018.04.003

Cited by 13 publications

(4 citation statements)

References 32 publications

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“…According to S. Bhadra et al, (2016) asiatic acid, a triterpenoid component of CA, was found to have an inhibitory effect against the AChE enzyme [ 9 ]. N. Omar et al, (2019) reported that asiatic acid that was present in CA could cross the blood–brain barrier (BBB) and maintained in the tight junction of the BBB [ 24 ]. Furthermore, it has been reported that the combination of asiatic acid and madecassic acid could induce neuronal differentiation and neurofilament [ 39 ].…”

Section: Resultsmentioning

confidence: 99%

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Combining In Silico and In Vitro Studies to Evaluate the Acetylcholinesterase Inhibitory Profile of Different Accessions and the Biomarker Triterpenes of Centella asiatica

et al. 2020

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Alzheimer’s disease (AD) is a neurodegenerative disease and the most cause of dementia in elderly adults. Acetylcholinesterase (AChE) is an important beneficial target for AD to control cholinergic signaling deficit. Centella asiatica (CA) has proven to be rich with active ingredients for memory enhancement. In the present study, the chemical profiling of three accession extracts of CA namely SECA-K017, SECA-K018, and, SECA-K019 were performed using high-performance liquid chromatography (HPLC). Four biomarker triterpene compounds were detected in all CA accessions. Quantitative analysis reveals that madecassoside was the highest triterpene in all the CA accessions. The biomarker compounds and the ethanolic extracts of three accessions were investigated for their acetylcholinesterase (AChE) inhibitory activity using Ellman’s spectrophotometer method. The inhibitory activity of the triterpenes and accession extracts was compared with the standard AChE inhibitor eserine. The results from the in vitro study showed that the triterpene compounds exhibited an AChE inhibitory activity with the half-maximal inhibitory concentration (IC50) values between 15.05 ± 0.05 and 59.13 ± 0.18 µg/mL. Asiatic acid was found to possess strong AChE inhibitory activity followed by madecassic acid. Among the CA accession extracts, SECA-K017 and SECA-K018 demonstrated a moderate AChE inhibitory activity with an IC50 value of 481.5 ± 0.13 and 763.5 ± 0.16 µg/mL, respectively from the in silico docking studies, it is observed that asiatic acid and madecassic acid showed very good interactions with the active sites and fulfilled docking parameters against AChE. The present study suggested that asiatic acid and madecassic acid in the CA accessions could be responsible for the AChE inhibitory action and could be used as markers to guide further studies on CA as potential natural products for the treatment of AD.

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Section: Resultsmentioning

confidence: 99%

“…Molecular docking is a tool in computer aided drug designing (CADD) which is used to study the binding interaction between the potential inhibitors, known as ligands, and targeted enzymes [24]. The X-ray crystal structures of AChE from various species can be found in the protein data bank (PDB) [25].…”

Section: Introductionmentioning

confidence: 99%

Combining In Silico and In Vitro Studies to Evaluate the Acetylcholinesterase Inhibitory Profile of Different Accessions and the Biomarker Triterpenes of Centella asiatica

et al. 2020

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“…According to a study, a selective and repeatable HPLC/ESI-MS/MS method was ISSN: 2320-4850 [170] CODEN (USA): AJPRHS developed to measure the amount of AA in rat plasma using colchicine as an internal standard. The proposed method has also been tested according to US Food and Drug Administration rules and used in a pharmacokinetic study with female albino wistar rats (147) .…”

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

Preventive Mechanism, Therapeutic Property,Pharmacokinetics And Benefitsof Asiatic Acid - A Triterpenoid Of Centella Asiatica In Alzheimer Disease: An In-Depth Review

Chakraborty,

Sinha

2023

Asian J Pharm Res Dev

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Alzheimer's disease (AD) remains the most prevalent form of age-related dementia worldwide, and it has no cure. Memory loss, difficulty communicating, depression, agitation, mood swings, and psychosis all develop gradually in this disorder. Reduced physical activity, infection, smoking, and the prevalence of diseases like obesity and diabetes all pose a risk for the development of AD. Current synthetic medications only alleviate symptoms by targeting a single molecule, so they can't deal with the complex pathogenesis of AD. The scientific community is actively working to characterise therapeutic agents derived from plants that have shown promise in the literature in treating AD due to their perceived efficacy, safety, and availability. Traditional Chinese medicine includes the use of the plant Centella asiatica for its purported benefits to cognitive performance and memory. Pentacyclic triterpenes are largely responsible for its therapeutic and medicinal effects, which include accelerated enhanced memory. These pentacyclic triterpenoids are asiaticoside and madecassoside as saponins and their aglycones, asiatic acids and madecassic acids. Amongst other triterpenoid Asiatic acid has several therapeutic properties against AD like anti-cholinesterase, neuroprotective and anti-inflammatory. This review focused on the pathophysiology of AD followed by a detailed account on Asiatic acid and the research findings to date related to its mechanism of action on AD, advantage over other two terpenoid, BBB permeability, Pharmacokinetic, molecular docking and different therapeutic activities.

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“…Benzothiazole (fragment A) and isoquinoline (fragment C) are connected by an amide bond (fragment B) because amide compounds are used to treat illnesses of the central nervous system, such as anxiety, schizophrenia, epilepsy and depression, and have antioxidant pharmacological activity [52][53][54][55]. The most relevant parameters of the newly created MTDLs included physicochemical features of the compounds in connection to their drug-likeness and success in the drug development process.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Activity Evaluation of Benzothiazole-Isoquinoline Derivatives

et al. 2022

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In-vitro evaluation and in-silico studies applied on newly synthesized amide derivatives of N-phthaloylglycine as Butyrylcholinesterase (BChE) inhibitors

Cited by 13 publications

References 32 publications

Combining In Silico and In Vitro Studies to Evaluate the Acetylcholinesterase Inhibitory Profile of Different Accessions and the Biomarker Triterpenes of Centella asiatica

Combining In Silico and In Vitro Studies to Evaluate the Acetylcholinesterase Inhibitory Profile of Different Accessions and the Biomarker Triterpenes of Centella asiatica

Preventive Mechanism, Therapeutic Property,Pharmacokinetics And Benefitsof Asiatic Acid - A Triterpenoid Of Centella Asiatica In Alzheimer Disease: An In-Depth Review

Synthesis and Biological Activity Evaluation of Benzothiazole-Isoquinoline Derivatives

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