Evaluation of Bioactive Compounds as Acetylcholinesterase Inhibitors from Medicinal Plants

Bhadra, Santanu; Dalai, Manoj Kumar; Chanda, Joydeb; Mukherjee, Pulok K.

doi:10.1016/b978-0-12-800874-4.00013-1

Cited by 14 publications

(11 citation statements)

References 118 publications

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“…Additionally, a diet rich in fruits and vegetables could prevent 20% of most types of cancers [ 16 , 24 , 25 ]. Several epidemiological and empirical studies have reported that the consumption of fruits and vegetables containing polyphenol compounds plays an important role in the inhibition of carbohydrate-hydrolyzing enzymes such as α-amylase, α-glucosidase [ 26 , 27 , 28 , 29 ], and acetylcholine esterase (AChE) [ 30 ].…”

Section: Introductionmentioning

confidence: 99%

GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties

et al. 2021

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The inhibition of certain digestive enzymes by target food matrices represents a new approach in the treatment of socially significant diseases. Proving the ability of fruits to inhibit such enzymes can support the inclusion of specific varieties in the daily diets of patients with diabetes, obesity, Alzheimer’s disease, etc., providing them with much more than just valuable micro- and macromolecules. The current study aimed atidentifying and comparing the GC-MS metabolic profiles of eight peach varieties (“Filina”, “Ufo 4, “Gergana”, “Laskava”, “July Lady”, “Flat Queen”, “Evmolpiya”, and “Morsiani 90”) grown in Bulgaria (local and introduced) and to evaluate the inhibitory potential of their extracts towards α-glucosidase, α-amylase, lipase, and acetylcholinesterase. In order to confirm samples’ differences or similarities, principal component analysis (PCA) and hierarchical cluster analysis (HCA) were also applied to the identified metabolites. The results provide important insights into the metabolomic profiles of the eight peach varieties and represent a first attempt to characterize the peels of the peach varieties with respect to α-glucosidase-, α-amylase-, lipase-, and acetylcholinesterase-inhibitory activities. All of the studied peach extracts displayed inhibitory activity towards α-glucosidase (IC50: 125–757 mg/mL) and acetylcholinesterase (IC50: 60–739 mg/mL), but none of them affected α-amylase activity. Five of the eight varieties showed inhibitory activity towards porcine pancreatic lipase (IC50: 24–167 mg/mL). The obtained results validate the usefulness of peaches and nectarines as valuable sources of natural agents beneficial for human health, although further detailed investigation should be performed in order to thoroughly identify the enzyme inhibitors responsible for each activity.

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Section: Introductionmentioning

confidence: 99%

GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties

et al. 2021

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“…Herbal medicines have been used for the treatment of memory and cognitive functions [ 42 ]. 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 ].…”

Section: Resultsmentioning

confidence: 99%

“…AChE is a key of enzyme that plays important roles in cholinergic transmission by hydrolyzing the neurotransmitter acetylcholine (ACh) [8]. Inhibition of AChE in the cholinergic framework is intimately linked with the therapy of neurodegenerative-related diseases [9]. Therefore, by inhibiting AChE, the levels of this neurotransmitter can be elevated and thus improve the learning and memory functions.…”

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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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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“…Such compounds, isolated from the Strychnos species, have also been found to inhibit quinine-and choloquinine-resistant P. falciparum [50]. One of the more studied indole alkaloids would be physostigmine, the template that led to the development of rivastigmine, globally licensed in 2006 to fight the symptoms of dementia associated with Parkinson's disease, also prescribed for the symptomatic treatment of Alzheimer's disease [51]. Figure 24.…”

Section: Natural and Synthetic Indolesmentioning

confidence: 99%

Breakthroughs in Indole and Indolizine Chemistry – New Synthetic Pathways, New Applications

Ghinea¹,

Dinică²

2016

Scope of Selective Heterocycles From Organic and Pharmaceutical Perspective

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Indole and indolizines heterocyclic aromatic compounds structurally and chemically isomeric with indoles are an important class of N-fused heterocyclic compounds due to their interesting biological and optical properties. Different strategies for generating diverse collections of small molecules with indole and indolizine moieties have been developed. They can be synthesized by means of classical and nonclassical pathways. The present study discusses the versatile nature of indole/indolizine derivatives, new green methods for their synthesis, their possible mechanism of action and also provides information about current/future prospects of the topics and different indole/indolizine derivatives in pharmaceutical/clinical trials. With the remarkable number of approved indole-containing drugs as well as the importance of the indolizine moiety, it can be easily concluded that indole and indolizine derivatives offer perspectives on how pyrrole scaffolds might be exploited in the future as bioactive molecules against a broad range of diseases.

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Evaluation of Bioactive Compounds as Acetylcholinesterase Inhibitors from Medicinal Plants

Cited by 14 publications

References 118 publications

GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties

GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties

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

Breakthroughs in Indole and Indolizine Chemistry – New Synthetic Pathways, New Applications

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