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... Eight inhibitors of acetylcholinesterase (AChE), tacrine, bis-tacrine, donepezil, rivastigmine, galantamine, heptyl-physostigmine, TAK-147 and metrifonate, were compared with regard to their effects on AChE and butyrylcholinesterase (BuChE) in normal human brain cortex. Additionally, the IC50 values of different molecular forms of AChE (monomeric, G1, and tetrameric, G4) were ...
... A presenilin 2 mutation is believed to be involved in the development of Alzheimer's disease. In addition, transgenic mice with a presenilin 2 mutation have been reported to have learning and memory impairments. In this study, exposing PC12 cells expressing mutant presenilin 2 to 50 μM Aß₂₅–₃₅, 30 mML-glutamate and 50 μM H₂O₂ caused a significant increase in acetylcholine esterase activity. Anin v ...
acetylcholinesterase; enzyme inhibition; Rhodiola rosea; rhizomes; plant extracts; hydroquinone; chemical constituents of plants; Alzheimer disease
Abstract:
... An activity-directed fractionation and purification process was used to identify the acetylcholinesterase inhibitory-active components of Rhodiola rosea L. (RR). Dried rhizome of RR was extracted with boiled ethanol. After removal of tannins, the extract was separated into chloroform, ethyl acetate, n-butanol and water fractions. Among these, chloroform and n-butanol fractions showed stronger acti ...
... Galanthamine, an isoquinoline alkaloid acetylcholinesterase inhibitor, is an important agent used all around the world for the symptomatic treatment of senile dementia of the Alzheimer's type. The production of this metabolite and the availability of the plant are limited and prompted the search for an alternative way to obtain this valuable metabolite using in vitro cultures of Leucojum aestivum ...
... The amyloid beta (Abeta) peptide is responsible for toxic amyloid plaque formation and is central to the aetiology of Alzheimer's disease (AD). It is generated by proteolytic processing of the amyloid precursor protein (APP) by beta-secretase (BACE-1) and gamma-secretase. Consequently, inhibition of BACE-1, a rate-limiting enzyme in the production of Abeta, is an attractive therapeutic approach to ...
... The cholinergic hypothesis of Alzheimer's disease (AD) has provided the rationale for the current pharmaco-therapy of this disease, in an attempt to reduce the cognitive decline caused by cholinergic deficits. Nevertheless, the search for potent and long-acting acetylcholinesterase (AChE) inhibitors that exert minimal side effects in AD patients is still ongoing. AChE inhibitors are currently the ...
... The current pharmacotherapy for Alzheimer's disease (AD) is the use of acetylcholinesterase inhibitors (AChE-Is). A previous in vitro study showed that Tabernaemontana divaricata extract (TDE) can inhibit AChE activity. However, neither the AChE inhibitory effects nor the effect on neuronal activity of TDE has been investigated in vivo. To determine those effects of TDE in animal models, the Ellma ...
... As part of this study on the isolation of cholinesterase inhibitors from natural marine products, the bioactivity of the ethanolic extracts from 27 Korean seaweeds were screened using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory assays. Ecklonia stolonifera exhibited promising inhibitory properties against both AChE and BChE. Bioassay-guided fractionation of the active n ...
... Acetylcholinesterase is an enzyme associated with senile plaques. Biochemical studies have indicated that acetylcholinesterase induces amyloid fibril formation by interaction throughout the peripherical anionic site of the enzyme forming highly toxic acetylcholinesterase-amyloid-β peptide (Aβ) complexes. The pro-aggregating acetylcholinesterase effect is associated with the intrinsic amyloidogenic ...
Huperzia; medicinal plants; micropropagation; callus culture; Oriental traditional medicine; phytochemicals; sesquiterpenoids; cholinesterase inhibitors; acetylcholinesterase; Alzheimer disease; disease control; human health
Abstract:
... Alzheimer's disease (AD) is growing in impact on human health. With no known cure, AD is one of the most expensive diseases in the world to treat. Huperzine A (HupA), a anti-AD drug candidate from the traditional Chinese medicine Qian Ceng Ta (Huperzia serrata), has been shown to be a powerful and selective inhibitor of acetylcholinesterase and has attracted widespread attention because of its uni ...
... Aim of the study: Bacopa monnieri (Brahmi) is extensively used in traditional Indian medicine as a nerve tonic and thought to improve memory. To examine the neuroprotective effects of Brahmi extract, we tested its protection against the beta-amyloid protein (25-35) and glutamate-induced neurotoxicity in primary cortical cultured neurons. Materials and Methods: Neuroprotective effects were determin ...
... This review explores the possibility that acetylcholinesterase may play a pivotal, non-hydrolytic role in neurodegeneration. More specifically, C-terminal sequences of acetylcholinesterase may act as signalling molecules in key brain regions characteristically vulnerable to Alzheimer's, Parkinson's and motor neuron disease. ...
... Field-amplified sample stacking (FASS) in capillary electrophoresis (CE) was used to determine the concentration of donepezil, an acetylcholinesterase inhibitor, in human plasma. A sample pretreatment by liquid-liquid extraction with isopropanol/n-hexane (v/v 3:97) and subsequent quantification by FASS-CE was used. Before sample loading, a water plug (0.5 psi, 6 s) was injected to permit FASS. Ele ...
Alzheimer disease; Kaempferia; acetylcholinesterase; cholinesterase; flavones; nuclear magnetic resonance spectroscopy; plant extracts; rhizomes; screening; structure-activity relationships; traditional medicine
Abstract:
... The rhizome of Kaempferia parviflora or kra-chai-dum (in Thai) is used traditionally as a folk medicine. The preliminary cholinesterase inhibitory screening of this plant extract exhibited significant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Thirteen known methoxyflavones (1-13) were isolated and their structures were completely elucidated based on NMR an ...
... Ethnopharmacological relevance: Salvia species and Melissa officinalis are used for their memory-enhancing effects in European folk medicine. Teucrium polium was reported to be used in Anatolia for memory-enhancement in a very old book written by an Ottoman herbalist-physician. Aim of the study: Alzheimer's disease (AD) is a progressive neurological disorder mostly affecting the elder population. ...
... The cholinergic theory of aging states that dysfunction of cholinergic neurons arising from the basal forebrain and terminating in the cortex and hippocampus may be involved in the cognitive decline that occurs during aging and Alzheimer’s disease. Despite years of research, pharmacological interventions to treat or forestall the development of Alzheimer’s disease have primarily focused on enhanci ...
... Aim of the study: The cognitive-enhancing and antioxidant activities of KD-501, a standardized extract of the roots of Scrophularia buergeriana Miquel (Scrophulariceae) were investigated. Materials and methods: KD-501 was orally administered to amnesic mice induced by scopolamine and we performed passive avoidance and the Morris water maze tests. To elucidate the mechanism of cognitive-enhancing a ...
... A simple and sensitive MEKC with UV detection was developed and validated for the simultaneous determination of acetylcholinesterase inhibitors including galantamine, rivastigmine and major metabolite NAP 226-90 in plasma. A sample pretreatment by liquid-liquid extraction with diethylether and subsequent quantification by MEKC was used. The optimum separation for these analytes was achieved in <10 ...
Alzheimer disease; DNA damage; acetylcholinesterase; antioxidant activity; bioassays; enzymatic hydrolysis; feeds; fish meal; hydrogen peroxide; hydrolysates; hydrolysis; hydroxyl radicals; liver; liver protein; meat and bone meal; molecular weight; peptides; plasmids; protein hydrolysates; subtilisin; tuna; ultrafiltration
Abstract:
... Tuna liver is fish by-product, which is normally discarded and/or used as fish meal and animal feed because of poor functionality. In this study, we attempt to recover functional peptides from tuna liver protein by enzymatic hydrolysis using various proteases, and further hydrolysates were fractionated into four categories base on their molecular weight (MW) by ultrafiltration membranes. All fract ...
... In the current work, our target was to screen inhibitory potentials of 55 Turkish Salvia taxa, 28 of which are endemic, against acetylcholinesterase (AChE), which is a chief enzyme in pathogenesis of Alzheimer's disease (AD). The dichloromethane, ethyl acetate, and methanol extracts prepared from 55 Salvia taxa were tested for their AChE inhibitory activity at 25, 50, and 100μg/ml using an ELISA m ...
... Eclipta prostrata has been used as a traditional medicinal plant to prevent dementia and to enhance memory in Asia. Its potential as a nootropic and as an antioxidant have been reported in mice. We hypothesized that Eclipta may affect the formation of neurotransmitters and the inhibition of oxidative stress. Charles River cesarean-derived rats (male, 180 ± 10 g) were fed experimental diets supplem ...
... Butyrylcholinesterase (BChE), a serine hydrolase biochemically related to the cholinergic enzyme Acetylcholinesterase (AChE), is found in many mammalian tissues, such as serum and central nervous system, but its physiological role is still unclear. BChE is an important human plasma esterase, where it has detoxifying roles. Furthermore, recent studies suggest that brain BChE can have a role in Alzh ...
... Alzheimer's disease (AD) is the most common type of dementia in the aging population. Enhancement of acetylcholine levels in the brain is one means of treating the disease. However, the drugs presently used in the management of the disease have various drawbacks. New treatments are required and in this study, extracts of Salvia tiliifolia Vahl. (whole plant), Chamaecrista mimosoides L. Greene (roo ...
... In the present study, we investigated the acetylcholinesterase (AChE) inhibitory activity of the ethanolic extracts of a number of mushroom species growing in Turkey, including mainly Polyporus species (Polyporus gilvus, Polyporus sulphureus, Polyporus annosus, Polyporus radiatus, Polyporus pinicola, Polyporus volvatus, Polyporus fomentarius, Polyporus stevenii, Polyporus badius), as well as Canth ...
Alzheimer disease; Leucojum aestivum; Narcissus; acetylcholinesterase; bulbs; gas chromatography-mass spectrometry; high performance liquid chromatography; leaves; metabolomics; methanol; nuclear magnetic resonance spectroscopy; pharmaceutical industry; principal component analysis; quality control; rapid methods; raw materials
Abstract:
... Galanthamine, an acetylcholinesterase inhibitor marketed as a hydrobromide salt for the treatment of Alzheimer's disease, is obtained from some Amaryllidaceae plants. A new method was developed and validated for its quantification by GC–MS in different plant sources: bulbs and leaves from Narcissus confusus; bulbs from N. pseudonarcissus cv. Carlton; and leaves and in vitro cultures from L. aestiv ...
... Dichloromethane, ethyl acetate, acetone, methanol, and water extracts prepared from the fruits and leaves of Laurocerasus officinalis Roem. (LO) (Rosaceae) were screened for their cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the key enzymes in pathogenesis of Alzheimer's disease (AD), using ELISA microplate reader at 50, 100, and 200μgmL ...
... Aluminium, a well established neurotoxicant, is reported to be involved in the aetiology of Alzheimer’s disease (AD) due to its easy admittance and accumulation in central nervous system (CNS). Simultaneous curcumin treatment during the induction of neurotoxicity by AlCl₃ is reported to provide protection. However, the therapeutic potential of curcumin in terms of reversing the neuronal damage onc ...
Alzheimer disease; Juniperus; acetone; acetylcholinesterase; antimicrobial properties; antioxidant activity; antioxidants; food preservatives; fruit extracts; fruits; hexane; linoleic acid; medicine; methanol; oxidation; oxidative stress; pathogenesis; raw foods; shelf life
Abstract:
... BACKGROUND: Juniperus L. (Cupressaceae) species are mostly spread out in the Northern Hemisphere of the world, and some of them are used as folkloric medicines. The fruits of some species are eaten. Since oxidative stress is one of the reasons for neurodegeneration and is associated with the Alzheimer's disease (AD), the extracts prepared from the fruits of six Juniperus species were screened for ...
... Several extracts of the leaves and fruits of Juglans regia L. were assessed for their neuroprotective effects through antioxidant and anti-cholinesterase methods. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the enzymes vital for Alzheimer's disease, at 50, 100 and 200 μg ml⁻ ¹. Antioxidant activity was tested using radical scaven ...
... This paper discusses acetylcholinesterase inhibitory properties of gallic acid-grafted-chitosans (GA-g-chitosans) with different grafting ratios. The GA-g-chitosans exhibited potent acetylcholinesterase inhibitory effects in a dose-dependent manner, and their IC₅₀ values ranged from 138.5±0.25 to 397.6±5.2μg/mL. The acetylcholinesterase inhibition kinetics of the GA-g-chitosan (I) by Lineweaver–Bu ...
Alzheimer disease; Cyrtanthus; Lycoris; Narcissus; Zephyranthes; acetylcholinesterase; bulbs; chromatography; enzyme inhibition; enzyme inhibitors; lycorine; medicinal plants; nuclear magnetic resonance spectroscopy; traditional medicine; South Africa
Abstract:
... ETHNOPHARMACOLOGICAL RELEVANCE: Plants of the family Amaryllidaceae are used widely in traditional medicine in South Africa. Several of these, including representatives of the genus Cyrtanthus find use in the treatment of mental illness and age-related dementia. AIM OF THE STUDY: Based on the distribution of central nervous system-activating alkaloidal constituents within the genus Cyrtanthus, Cyr ...
... ETHNOPHARMACOLOGICAL RELEVANCE: The rhizomes of Alpinia galanga (L.) Willd (Zingiberaceae), a ginger substitute for flavouring food was traditionally used as nervine tonic and stimulant. AIM OF THE STUDY: This investigation is designed to screen cognitive improvement of Alpinia galanga (AG) fractions in Alzheimer's type of amnesia in mice induced by Aβ₍₂₅–₃₅₎. MATERIALS AND METHODS: Alzheimer's di ...
Alzheimer disease; Amaryllis belladonna; Haemanthus; Scadoxus; acetylcholinesterase; alkaloids; drugs; flowers; gas chromatography; internal transcribed spacers; mass spectrometry; phylogeny; rain; serotonin; summer; transport proteins
Abstract:
... We present phylogenetic analyses of 37 taxa of Amaryllidaceae, tribe Haemantheae and Amaryllis belladonna L. as an outgroup, in order to provide a phylogenetic framework for the selection of candidate plants for lead discoveries in relation to Alzheimer's disease and depression. DNA sequences from the nuclear ribosomal internal transcribed spacer (ITS) and the plastid trnL-F regions were used. Max ...
... Brain senescence plays an important role in cognitive dysfunction and neurodegenerative disorders. Curcumin was reported to have beneficial effect against several neurodegenerative disorders including Alzheimer's disease. Therefore, the present study was conducted in order to explore the possible role of curcumin against d-galactose-induced cognitive dysfunction, oxidative damage, and mitochondria ...
Alzheimer disease; acetonitrile; acetylcholine; acetylcholinesterase; brain; detection limit; equations; formic acid; hydrophilicity; liquid chromatography; mice; monitoring; pH; tandem mass spectrometry
Abstract:
... Cholinergic dysfunction is known as a hallmark feature of Alzheimer's disease (AD). Measurement of endogenous acetylcholine (ACh) in specific brain regions is important in understanding the pathology of AD and in designing and evaluating novel cholinomimetic agents for the treatment of AD. Since ACh is an endogenous neurotransmitter, there is no real blank matrix available to construct standard cu ...
... BACKGROUND: Many persons with Alzheimer's disease (AD) treated with galantamine appear to receive additional cognitive benefit from citalopram. Both drugs inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These enzymes co-regulate acetylcholine catabolism. In AD brain, AChE is diminished while BuChE is not, suggesting BuChE inhibition may be important in raising acetylcholine ...
... The stem with hooks of Uncaria rhynchophylla is a component herb of many traditional formulae for the treatment of neurodegenerative diseases. However, scientific evidence of the efficacy of Uncaria rhynchophylla in the treatment of Alzheimer's disease (AD) in animal models is lacking. Thus, in the present study, we investigated whether the 70 % aqueous ethanol extract of Uncaria rhynchophylla (EU ...
... As part of our ongoing project of new acetylcholinesterase inhibitors from lower marine and terrestrial species, a phytochemical investigation was conducted on a foliose lichen, Lobaria pulmonaria (L.) Hoffm. (Lobariaceae), from Bosnia and Herzegovina. The study led to the isolation of a mixture of acetylated depsidones which showed a moderate activity (0.5 µg) in the acetylcholinesterase inhibiti ...
... A bienzymatic choline biosensor was constructed by coimmobilizing acetylcholinesterase (AChE) and choline oxidase (ChO) onto nanocomposite of carboxylated multiwalled carbon nanotubes (c-MWCNTs) and zirconium oxide nanoparticles (ZrO₂NPs) electrodeposited on the surface of a glassy carbon electrode (GCE) and using it (AChE–ChO/c-MWCNT/ZrO₂NPs/GCE) as working electrode, Ag/AgCl as reference electro ...
... Satureja thymbra was used as a spice in Anatolia and Greece. The essential oil and the methanol extract of Satureja thymbra were evaluated for cholinesterase inhibitory effects against acetylcholinesterase and butyrylcholinesterase which are the chief enzymes of Alzheimer’s disease. The antioxidative effects of the essential oil and the extract were also determined by using β-carotene-linoleic aci ...
... It is necessary to develop food additives to help treat chronic disorders like neurodegenerative diseases from medicinal plants. Ethanol extracts of paper mulberry were found to display significant inhibition against cholinesterases, enzymes that are strongly linked with Alzheimerâs disease (AD). The active components were identified as prenylated flavonols (2â4) that inhibited two related hum ...
... Tricholoma species, known as odorous mushrooms, are consumed in Anatolia as well as in the world. The antioxidant activity of extracts of Tricholoma fracticum, Tricholoma imbricatum and Tricholoma terreum was determined using five complementary tests: β-carotene/linoleic acid, DPPH[Symbol: see text] scavenging, ABTS[Symbol: see text]+ scavenging, ferrous ion chelating assay and cupric-reducing an ...
... Alzheimer’s disease (AD) is the most prevalent cause of dementia in the elderly people. The disease is pathologically characterized by extracellular deposition of beta-amyloid peptide (Aβ), cholinergic neurodegeneration and elevation of acetylcholine esterase (AChE) activity in the affected regions. In this study, we investigated the effects of obovatol on memory dysfunction, which was caused by s ...
Alzheimer disease; Ayurvedic medicine; Semecarpus anacardium; Torpedo californica; acetylcholinesterase; active sites; catechol; cholinesterase; computer software; databases; fractionation; fruits; high performance liquid chromatography; inhibitory concentration 50; mass spectrometry; methylene chloride; nuclear magnetic resonance spectroscopy; screening
Abstract:
... ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Semecarpus anacardium L. f. (Anacardiaceae) are used in Ayurvedic medicine and also in Iranian Traditional Medicine for various indications, among those for retarding and treatment of dementia. AIM OF THE STUDY: The severity of Alzheimer's disease obviously correlates with a cholinergic deficit. In a screening for acetylcholinesterase (AChE) inhibitory ...
Alzheimer disease; acetates; acetylcholinesterase; bioactive properties; drug formulations; electrophoresis; micellar electrokinetic capillary chromatography; pH; temperature
Abstract:
... The aim of this work is the development, validation and application of an MEKC method for the chiral separation of Huperzine A. Huperzine A is an important compound that is used to treat Alzheimer's disease. However, only the (â)âform of this compound is biologically active and behaves as a potential acetylcholinesterase inhibitor. Therefore, the separation of the (â)âform from the (+)âf ...
... To investigate the anti-amnesic effect of quercetin by using in vivo Y-maze and passive avoidance tests, the learning and memory impairment in ICR mice was induced by neurotoxic trimethyltin. Quercetin pre-administration attenuated TMT-induced memory injury in both in vivo tests. Acetylcholinesterase (AChE), prepared from mice brain tissues, was inhibited by quercetin in a dose-dependent manner. M ...
... β-Amyloid peptides (Aβ) are neurotoxic and contribute to the development of Alzheimer’s disease (AD). Ergothioneine (EGT) has been shown to protect against loss of memory and learning abilities in mice. In this study, mice were orally fed EGT (0.5 or 2mg/kg body weight) for 16days before treatment (i.c.v) with a single dose of Aβ1–40 in the hippocampus. After resting for 12days to restore the body ...
Alzheimer disease; acetylcholinesterase; acids; antioxidant activity; apigenin; biphenyl; bleaching; chemical composition; citrus peels; foods; free radical scavengers; gas chromatography; human health; kaempferol; leaf extracts; leaves; liquid chromatography; mass spectrometry; methanol; monoterpenoids; phenol; quercetin; rutin; screening; sesquiterpenoids; vegetables
Abstract:
... BACKGROUND: The replacement of synthetic antioxidants by safe natural antioxidants fosters research on the screening of vegetables and food as sources of new antioxidants. Moreover, oxidative degeneration of cells is associated with neurodegenerative diseases such as Alzheimer's disease. On the basis of these considerations this work aimed to investigate the antioxidant properties [by using the di ...
... Microwave-assisted synthesis of oxo-/thioxopyrimidines and tetrazoles linked to furanoses with d-xylo and d-ribo configuration, and to a d-galacto pyranose is reported and compared to conventional methods. Reaction of dialdofuranoses and dialdopyranoses with a β-keto ester and urea or thiourea under microwave irradiation at 300W gave in 10min the target molecules containing the 2-oxo- or 2-thioxo- ...
... Huperzine A, a Lycopodium alkaloid produced by Chinese folk herb Huperzia serrata (Lycopodiaceae), has been shown to be a promising agent for the treatment of Alzheimer's disease due to its potent acetylcholinesterase (AChE) activity, as well its efficacy in the treatment of memory of aged patients. Thus, the effects of two Huperzia species of habitats in Brazil (H. quadrifariata and H. reflexa) w ...
... Ginger has been reportedly used for the management or treatment of Alzheimer's disease in folklore medicine. Therefore, this study sought to investigate the inhibitory effects of water extractable phytochemicals of red and white ginger on acetylcholinesterase activities, and sodium nitroprusside (SNP) and quinolinic acid (QA)-induced lipid peroxidation in rat brain –in vitro. Both extracts inhibit ...
Alzheimer disease; Camellia sinensis; acetylcholinesterase; bioavailability; caffeine; cardiovascular diseases; enzyme inhibition; epigallocatechin gallate; flavanols; gallic acid; green tea; health promotion; in vitro digestion; inhibitory concentration 50; intestines; lactones; metabolites; neoplasms; polyphenols; pyrogallol; tea (beverage); white tea
Abstract:
... By 2034 it is forecast that 5% of the global population will be aged 85 years or over—approximately two and half fold increase on present day figures—which will inevitably lead to an increase in age-associated disorders such as Alzheimer's disease. There is mounting evidence that green tea (Camellia sinensis) possesses numerous health-promoting properties, and may potentially be beneficial to thos ...
... Inhibition of cholinesterase has attracted much attention recently because of its potential for the treatment of Alzheimer's disease. In this work, the anticholinesterase activities of plant oils were investigated using Ellman's colorimetric method. The results indicate that essential oils obtained from Melissa officinalis leaf and Citrus aurantifolia leaf showed high acetylcholinesterase and buty ...
Alzheimer disease; Artemia; Buddleja; acetylcholinesterase; bronchitis; cough; ethyl acetate; flowers; inhibitory concentration 50; leaves; lethal concentration 50; memory; methylene chloride; neurodegenerative diseases; socioeconomics; toxicity; traditional medicine; South America
Abstract:
... Alzheimer's disease (AD) is a neurodegenerative disorder resulting in impaired memory and behaviour of remarkable socio-economic impact. A decrease in cholinergic activity is a key event in the biochemical of AD. Buddleja thyrsoides is a plant widely distributed in Southern parts of South America. In Brazilian traditional medicine, the infusion of its leaves and flowers is used for the treatment o ...
... Alzheimer's disease (AD) is the most common chronic neurodegenerative disorder associated with aging. This study aimed to explore new markers for AD as total homocysteine (tHcy), insulin, insulin like growth factor-1 (IGF-1), interlukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α); to determine the modulatory effects of vitamin E (VE), acetyl-l-carnitine (ALC) and α-lipoic acid (LA) on the inves ...
... In this study, black chokeberry concentrate was added (5% w/v) to lemon juice, since previous reports suggested potential health benefits of this blend. The phytochemical composition, antioxidant capacity (scavenging of DPPH, superoxide and hydroxyl radicals, and hypochlorous acid), and inhibitory activity against cholinesterase of the new blend were determined and compared with those of lemon jui ...
... The kinetics of single-amperometric exocytotic events has been measured in chromaffin cells of C57 mice and in an APP/PS1 mouse model of Alzheimer’s disease (AD). K⁺ depolarisation causes a burst of spikes that indicate the quantal release of the single-vesicle content of catecholamine. The kinetic analysis of 278 spikes from 10 control cells and 520 spikes from 18 APP/PS1 cells shows the followin ...
... AIMS: Inhibition of acetylcholinesterase (AChE) is still considered as a strategy for the treatment of neurological disorders such as Alzheimer's disease (AD). Many plant derived alkaloids (such as huperzine A, galanthamine and rivastigmine) are known for their AChE inhibitory activity. The aim of the present work was to isolate and identify new AChE inhibitors from Holarrhen antidysenterica. MAIN ...
... Tacrine is a medication applied in cases of mild to moderate dementia in Alzheimer’s disease. By blocking acetylcholinesterase activity the drug increases the concentration of acetylcholine, whose effects influence the functions of different organs and systems of the body. The effect of tacrine on smooth muscle preparations isolated from rat stomach was studied by isometric registration of muscle ...
... To find the multi-target-directed compounds for the treatment of Alzheimer’s disease (AD), we synthesized 7-(4-(diethylamino)butoxy)-5-hydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, a novel 7-O-modified genistein derivative (GS-14), and investigated its acetylcholinesterase (AChE) inhibitory effect, estrogenic activity and neuroprotective effect. GS-14 acted as a selective AChE inhibitor in vitro, ...
... The use of immobilized capillary enzyme reactors (ICERs) and enzymes coated to magnetic beads ((NT or CT)-MB) for ligand screening has been adopted as a new technique of high throughput screening (HTS). In this work the selected target was the enzyme acetylcholinesterase (AChE), which acts on the central nervous system and is a validated target for the treatment of Alzheimer’s disease, as well as ...
... Ammocharis coranica (Ker-Gawl.) Herb. (Amaryllidaceae) is used in southern Africa for the treatment of mental illnesses. The ethanol extracts of the bulb of A. coranica and its total alkaloids rich fractions were screened for inhibition of acetylcholinesterase enzyme (AChE), which is implicated in the pathophysiology of Alzheimer's disease. The ethanolic extracts significantly inhibited AChE with ...
... In the current study, in vitro neuroprotective effect of the ethyl acetate, methanol, and water extracts of Hypericum perforatum L. growing in Turkey was investigated through testing against acetylcholinesterase and butyrylcholinesterase at 50, 100, and 200μgmL−1, linked to Alzheimer's disease, and tyrosinase at 250μgmL−1, related to Parkinson's disease. As neurodegeneration is strongly correlated ...
... The neuroprotective effects of catalpol, an iridoid glycoside isolated from the fresh rehmannia roots, on the cholinergic system and inflammatory cytokines in the senescent mice brain induced by d-galactose were assessed. The results showed that acetylcholinesterase (AChE) activity increased in senescent mice brain and choline acetyltransferase (ChAT) positive neurons, detected by immunohistochemi ...
Alzheimer disease; Cistus creticus; acetylcholinesterase; antioxidant activity; beta-carotene; bleaching; chemical composition; essential oils; food additives; functional foods; functional properties; gas chromatography; inhibitory concentration 50; iron; mass spectrometry; neurodegenerative diseases; oils
Abstract:
... The chemical composition of Cistus creticus, Cistus salvifolius, Cistus libanotis, Cistus monspeliensis and Cistus villosus essential oils has been examined by GC and GC–MS analysis. Height-nine constituents were identified in C. salvifolius oil, sixty in C. creticus, fifty-six in C. libanotis, fifty-four in C. villosus, forty-five in C. monspeliensis. Although the five species belong to the same ...
... Many plant varieties of Narcissus (Amaryllidaceae) are cultivated on a large scale for ornamental purposes but they are also known to contain galanthamine, a bioactive alkaloid used in antiacetylcholinesterasic therapy in Alzheimer's disease.More than 100 ornamental varieties of Narcissus, using leaves and bulbs separately, were screened for their galanthamine content as well as their acetylcholin ...
... The lichen-forming fungus Cladonia macilenta strain KoLRI003786 is capable of producing an acetylcholinesterase inhibitor, biruloquinone, which effectively prevents neurodegeneration in Alzheimer’s disease. Laying the foundation to unravel the biruloquinone biosynthetic pathway, we present the 37.11-Mb draft genome sequence of strain KoLRI003786. ...
... A simple but robust droplet-based microfluidic system was developed for dose–response enzyme inhibition assay by combining concentration gradient generation method with electrochemical detection method. A slotted-vials array and a tapered tip capillary were used for reagents introduction and concentration gradient generation, and a polydimethylsiloxane (PDMS) microfluidic chip integrated with micr ...
... Acetylcholinesterase inhibitors (AChEIs) are important for treatment of Alzheimer’s disease and other neurological disorders. Search for potent and safe AChEIs from plant sources still continues. In the present work, we explored fragrant plant extracts that are traditionally used in flavoring foods, namely, Hemidesmus indicus and Vanilla planifolia, as possible sources for AChEI. Root and pod extr ...
Manuela Bartolini; Marina Naldi; Dan V. Nicolau; Falco C. M. J. M. van Delft; Jeroen van Zijl; Jaap Snijder; Eric F. C. van den Heuvel; Emile P. Naburgh; Natalia Calonghi; Vincenza Andrisano
... Human acetylcholinesterase (AChE) is a widely studied target enzyme in drug discovery for Alzheimer’s disease (AD). In this paper we report evaluation of the optimum structure and chemistry of the supporting material for a new AChE-based fluorescence sensing surface. To achieve this objective, multilayered silicon wafers with spatially controlled geometry and chemical diversity were fabricated. Sp ...
... A new, easily prepared, inexpensive and facile fluorometric assay method for screening of acetylcholinesterase (AChE) and its inhibitor is successfully established with the supramolecular assemblies of myristoylcholine and heparin. Myristoylcholine, an amphiphilic compound, is chosen as the cationic surfactant as well as the substrate for AChE. The environment-dependent dye pyrene, encapsulated in ...
... Development of effective non-invasive drug delivery systems is of great importance to the treatment of Alzheimer's diseases and has made great progress in recent years. In this work, lactoferrin (Lf), a natural iron binding protein, whose receptor is highly expressed in both respiratory epithelial cells and neurons is here utilized to facilitate the nose-to-brain drug delivery of neuroprotection p ...
Alzheimer disease; acetylcholinesterase; chronic exposure; cognition; drugs; mechanism of action; organophosphorus compounds; pathogenesis; patients; pesticides; public health; toxicology
Abstract:
... There has been a steep increase in the prevalence of dementia in recent decades, which has roughly followed an increase in pesticide use some decades earlier, a time when it is probable that current dementia patients could have been exposed to pesticides. This raises the question whether pesticides contribute to dementia pathogenesis. Indeed, many studies have found increased prevalence of cogniti ...
... Acetylcholinesterase (AChE) inhibitors have been used for the symptomatic treatment of Alzheimer's disease. Eleven whole plants from Panama belonging to the Lycopodiaceae family have been screened for their anticholinesterase inhibitory and antioxidant activities by a thin-layer chromatography (TLC) bioautography method. Of these, only Lycopodium clavatum subsp. clavatum showed strong AChE inhibit ...
... The utility of a simple, low-cost detection platform for label-free electrochemical characterization of acetylcholinesterase (AChE) inhibition is demonstrated as a potential tool for screening of small-molecule therapeutic agents for Alzheimer's disease (AD). Technique validation was performed against the standard Ellman's colorimetric assay using the clinically established cholinesterase inhibito ...
... 3-Nitropropionic acid (3-NP) induces cellular energy deficit and oxidative stress–related neurotoxicity via an irreversible inhibition of mitochondrial complex II enzyme, succinate dehydrogenase. Huntington's disease (HD) is a neurological disorder characterized by cognitive and motor dysfunctions. Lutein is a well-known antioxidant used in the management of oxidative stress related diseases. Clin ...
Alzheimer disease; acetylcholinesterase; agarose; cholinesterase; drug therapy; enzyme activity; erythrocytes; gels; humans; hydrolysis; iodides; ionic strength; molecular weight; pH; polyacrylamide gel electrophoresis; proteins; resins; sulfates; temperature
Abstract:
... The acetylcholinesterase enzyme was purified from human erythrocyte membranes using a simple and effective method in a single step. Tacrine (9-amino-1,2,3,4-tetrahydroacridine) is a well-known drug for the treatment of Alzheimer's disease, which inhibits cholinesterase. We have developed a tacrine ligand affinity resin that is easy to synthesize, inexpensive and selective for acetylcholinesterase. ...
Kim Cho Rong; Choi Soo Jung; Oh Seung Sang; Kwon Yoon Kyung; Lee Na Young; Park Gwi Gun; Kim Youn-Jung; Heo Ho Jin; Jun Woo Jin; Park Cheung-Seog; Shin Dong-Hoon
... To find acetylcholinesterase (AChE) inhibitors for the prevention of neurological disorders, such as Alzheimer's disease, ethanol extracts of promising traditional edible Korean plants were tested. Among them, Rubus coreanus Miquel extract exhibited the most significant AChE inhibitory activity. The effect of R. coreanus extract on trimethyltin-induced memory impairment in mice was investigated us ...
... It is known that selenium (Se) might play different roles in the progression of Alzheimer's disease (AD), but there is a lack of evidence that proves whether supplementation with Se is beneficial or not for the treatment of AD. Thus, the aim of the current study was to investigate the therapeutic effect of p,p'-methoxyl-diphenyl diselenide [(MeOPhSe)2], an organoselenium compound, against streptoz ...
Alzheimer disease; Leucojum aestivum; acetylcholinesterase; biosynthesis; chemotypes; gas chromatography; lycorine; mass spectrometry; medicine; mountains; Balearic Islands; Bulgaria; Danube River
Abstract:
... Leucojum aestivum, an industrial source of the acetylcholinesterase inhibitor galanthamine, shows a great chemodiversity in its alkaloid synthesis. Samples from various geographically distinct populations from Bulgaria and the Balearic Islands were studied by GC–MS. The alkaloid pattern of the plants of L. aestivum (subsp. pulchellum) from the Balearic Islands were dominated by crinine type compou ...
... Acetylcholinesterase (AChE) is a serine protease that hydrolyzes the neurotransmitter acetylcholine. Here, the effects of hydroxyl radical (OH) and nitric oxide (NO) on AChE activity were studied using a biochromatographic process. The enzyme was immobilized on an ethylenediamine (EDA) monolithic convective interaction media (CIM) disk. The AChE enzymatic mechanism was demonstrated from the chroma ...
... Alzheimer’s disease (AD), a progressive neurodegenerative disorder, is characterized by the deficits in the cholinergic system and deposition of beta amyloid (Aβ) in the form of neurofibrillary tangles and amyloid plaques. Since the cholinergic system plays an important role in the regulation of learning and memory processes, it has been targetted for the design of anti-Alzheimer’s drugs. Cholines ...
... Application of acetylcholinesterase (AChE) inhibitors is the primary treatment for Alzheimer’s disease. Alkaloids, such as physostigmine, galanthamine, and huperzine A, play an important role as AChE inhibitors. The aim of this work was to evaluate Himatanthus lancifolius (Muell. Arg.) Woodson, a Brazilian species of Apocynaceae, and its main indole alkaloid uleine, in order to identify new AChE i ...
Alzheimer disease; Ferula; acetylcholinesterase; active ingredients; herbal medicines; high performance liquid chromatography; inhibitory concentration 50; physostigmine; solid phase extraction; umbelliferones
Abstract:
... Due to the correlation of Alzheimer's disease with a cholinergic deficit, acetylcholinesterase (AChE) inhibitors from herbal drugs or herbal medicinal preparations have gained a lot of scientific interest.In a previous study, several substances with AChE inhibitory activity were detected in galbanum by TLC bioautography and two of them were identified as auraptene and farnesiferol A. The aim of pr ...
... Leucojum aestivum (summer snowflake) is a plant species used for the extraction of galanthamine, an acetylcholinesterase inhibitor for the treatment of Alzheimer’s disease. Extracts from bulbs collected from 18 Bulgarian populations and from shoot-clumps obtained in vitro from 8 different populations showed variations in their alkaloid composition. Nineteen alkaloids were detected in the studied s ...
Jessié M. Gutierres; Fabiano B. Carvalho; Maria Rosa C. Schetinger; Patrícia Marisco; Paula Agostinho; Marília Rodrigues; Maribel A. Rubin; Roberta Schmatz; Cassia R. da Silva; Giana de P. Cognato; Julia G. Farias; Cristiane Signor; Vera M. Morsch; Cinthia M. Mazzanti; Mauricio Bogo; Carla D. Bonan; Roselia Spanevello
... The aim of this study was to analyze if the pre-administration of anthocyanin on memory and anxiety prevented the effects caused by intracerebroventricular streptozotocin (icv-STZ) administration-induced sporadic dementia of Alzheimer's type (SDAT) in rats. Moreover, we evaluated whether the levels of nitrite/nitrate (NOx), Na⁺,K⁺-ATPase, Ca²⁺-ATPase and acethylcholinesterase (AChE) activities in ...
... Phytochemical investigations of Taxus baccata L. by successive chromatographic methods resulted in the isolation of the lignans lariciresinol (1), taxiresinol (2), 3´-demethylisolariciresinol- 9´-hydroxyisopropylether (3), isolariciresinol (4), and 3-demethylisolariciresinol (5) as well as taxoids. Compounds 1 - 5 were evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BChE), ...
Alzheimer disease; Melissa officinalis; acetylcholinesterase; antioxidant activity; antioxidants; autoxidation; brain; chemical composition; enzyme inhibitors; epinephrine; ethyl acetate; flavonoids; gallic acid; gas chromatography-mass spectrometry; gelatinase A; high performance liquid chromatography; nuclear magnetic resonance spectroscopy; oxidative stress; thiobarbituric acid-reactive substances
Abstract:
... Oxidative stress is associated with various diseases, in particular those related with the central nervous system, such as Alzheimer's disease. Based on the various benefits of Melissa officinalis, we investigated the chemical composition and antioxidant activity of different fractions from M. officinalis extract. Furthermore, the fraction with the highest antioxidant activity was tested as a pote ...
... The aim of this study was to investigate chemical constituents of the leaves of Acanthopanax henryi, and their antioxidant, acetyl cholinesterase inhibitory activities. Caffeoyl quinic acid derivates and flavonoids were obtained from A. henry, through column chromatography technologies, and the content of major constituents was determined by the HPLC–UV method. Anti-oxidant activity of the isolate ...
... Inhibition of cholinesterase has been proposed to be a therapeutic target for the treatment of Alzheimer’s diseases. In our preliminary screening study on the acetylcholinesterase (AChE) inhibitory activity, an ethyl acetate soluble fraction of the roots of Harpagophytum procumbens (Pedaliaceae) was found to inhibit AChE activity at the concentration of 100 μg/mL. Ten compounds (1–10) were isolate ...
... Studies on Alzheimer’s disease have been highlighted due to increasing prevalence of this disease. Oldest hypothesis about the pathophysiology strengthens the research of cholinesterase inhibitors for treatment. Amaryllidaceae plants are well known for alkaloids showing cholinesterase inhibiting activity. Among them, Sternbergia species gained attention as a source of metabolites of these a ...