... of this project was to determine and compare the time-related changes in blood, brain, and tissue acetylcholinesterase (AChE) activity during the ...

The roots of the Thai medicinal plant, Tabernaemontana divaricata (L.) R. Br. ex Roem. & Schult., were investigated for their content of acetylcholinesterase inhibitors. Bioassay-guided fractionation using the Ellman colorimetric method led to the isolation of two bisindole alkaloids, 19,20-dihydrotabernamine and 19,20-dihydroervahanine A. The compounds showed higher ...

Synthesis of four new pyrimidone analogues of the acetyicholinesterase (AChE) inhibitor huperzine A are reported together with the inhibitory potendes of these compounds for foetal bovine calf serum AChE; t3-lactone formation followed by a thermal cyclore...

The authors have studied the binding properties and inhibitory activity of AE-2, a monoclonal antibody which binds to acetylcholinesterase(AChE) and inhibits its activity by up to 50%. This antibody was compared to C1B7, another inhibitory enzyme. It was ...

Two unusual pyridine alkaloids, 7'-multijuguinone (1) and 12'-hydroxy-7'-multijuguinone (2), were isolated from the leaves of Senna multijuga, together with the known flavonoid rutin. The structures of the new alkaloids were established on the basis of spectroscopic data interpretation. Compounds 1 and 2 exhibited moderate in vitro acetylcholinesterase (AChE) ...

Objectives? Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of the most general form of dementia, Alzheimer's disease. In this study selected components of essential oils, which carry a variety of important functional groups, were tested for their in-vitro anti-acetylcholinesterase activity. Methods? ...

Disclosed are methods for the preparation and use of labeled AChE and labeled AChE inhibitory conjugate compositions for detecting accumulation of toxic materials such as organophosphates, insecticides, and other nerve agents. Also disclosed are methods f...

The purpose of this project was to determine and compare the time- related changes in blood, brain, and tissue acetylcholinesterase (AChE) activity during the first hour after exposure to six organophosphorus nerve agents (GA, GB, GD, GF, VR, and VX) in H...

The methanol extracts from five different plant families (Asteraceae, Euphorbiaceae, Melastomataceae, Rubiaceae, and Solanaceae) collected at Regional Natural Park Ucumar� (Colombia), were screened for their acetylcholinesterase inhibitory activity through the modified Ellman's spectrophotometric method. The best ...

Monoclonal antibodies have been raised against acetyicholinesterase isolated from a variety of sources and species. Although none of these antibodies bind to the esteratic site, some of them appear to interact with the region of the catalytic subunit referred to as the peripheral anionic site. We describe here the production and characterization of six inhibitory monoclonal ...

Looking for acetylcholinesterase (AChE) inhibiting compounds within the plant kingdom, we came across the triterpene alpha-onocerin, which has recently been described as the active principle (IC(50) of 5.2 microM) of Lycopodium clavatum L. In order to discover related terpenoid structures with similar AChE inhibitory ...

... Inhibitory Potencies of Chlorpyrifos Oxon, Chlorpyrifos Methyl Oxon, and Mipafox for Acetylcholinesterase Versus Neuropathy Target Esterase. ...

We screened 42 Korean traditional tea plants to determine the inhibitory effect of acetylcholinesterase and attenuation of toxicity induced by amyloid-beta peptide, which were related to the treatment of Alzheimer's disease (AD). The methanolic extract from Artemisia asiatica among tested 42 tea plants, showed the highest inhibitory ...

Cholinesterase (ChE) inhibitory activities of three coumarins (mansorins A-C) and five naphthoquinones (mansonone C, E, G and H) were evaluated to determine the relationships between the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects and the core structures of these compounds. Among ...

Disodium 2?,3?-dihydroxy-5?-cholestan-6-one disulfate (8) has been synthesized using cholesterol (1) as starting material. Sulfation was performed using trimethylamine-sulfur trioxide complex in dimethylformamide as the sulfating agent. The acetylcholinesterase inhibitory activity of compound 8 was evaluated and compared to that of ...

Hexacyclic derivatives share vital pharmacological properties, considered useful in Alzheimer's disease. The aim of this study was synthesis and its evaluation for acetyl cholinesterase inhibitory activity of novel hexacyclic analogues. Compound 4f, showed potent inhibitory activity against acetyl cholinesterase ...

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 ...

Aqueous and methanolic extracts of 11 plants, used in Danish folk medicine for improvement of memory and cognition, and 3 Corydalis species were tested for acetylcholinesterase inhibitory activity using the Ellman colorimetric method. Significant inhibitory activity in dose-dependent manner was ...

Synthesis of four new pyrimidone analogues of the acetyicholinesterase (AChE) inhibitor huperzine A are reported together with the inhibitory potendes of these compounds for foetal bovine calf serum AChE; t3-lactone formation followed by a thermal cycloreversion reaction serves as the key step for introduction of the ethylidene appendage of analogue 12 in the stereochemically ...

Hartree-Fock and density functional methods were used to analyze electronic and structural properties of known drugs to evaluate the influence of these data on acetylcholinesterase inhibition. The energies of the frontier orbitals and the distances between the more acidic hydrogen species were investigated to determine their contributions to the activity ...

The present study aimed to test the validity of Balanites aegyptiaca remedies used for the treatment of rheumatisms and mental disorders by examining the antioxidant, xanthine oxidase and acetylcholinesterase inhibitory activities of galls and leaves extracts and fractions. The total phenolics and flavonoids were measured using ...

Twelve isoquinoline alkaloids including two new nitro-containing tetrahydroprotoberberines, (-)-2,9-dihydroxyl-3,11-dimethoxy-1,10-dinitrotetrahydroprotoberberine ( 1) and (+)-4-nitroisoapocavidine ( 2), were isolated from the whole plant of CORYDALIS SAXICOLA Bunting. The structures of the new compounds were established by spectroscopic analysis and chemical evidence. The ...

The green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) was investigated for its enhancement effect of huperzine A on inhibiting acetylcholinesterase (AChE). The inhibitory effect of huperzine A on acetylcholinesterase is quite weak in the whole phase. EGCG hardly inhibits the AChE activity within the range ...

Ethanol extract of the aerial portion of Chelidonium majus L. inhibited acetylcholinesterase (AChE) activity without a significant inhibition of butyrylcholinesterase (BuChE). Using mass spectrometry and NMR studies, three active constituents were isolated and identified: 8-hydroxydihydrochelerythrine (1), 8-hydroxydihydrosanguinarine ...

... 4. TITLE AND SUBTITLE Reactivation of acetylcholinesterase activity and its therapeutic benefits in nerve agent 5a. CONTRACT NUMBER ...

... Database of articles on military and naval science, operational warfare, joint ... of Acetylcholinesterase Activity and Its Therapeutic Benefits in Nerve ...

A new triterpenoid 3alpha-hydroxy-ursane-5-ene (1) and a known steroid stigma sterol (2) have been isolated for the first time from the fruit of Rhazya stricta. The structures of these compounds were elucidated and identified by spectral studies. The crude ethanolic extract of R. stricta fruit has led to the determination of good results of antibacterial, lipoxygenase and ...

The aim of this study was to investigate structures and acetylcholinesterase inhibitory activities of lycopodane-type alkaloids isolated from an Icelandic collection of Lycopodium annotinum ssp. alpestre. Ten alkaloids were isolated, including annotinine, annotine, lycodoline, lycoposerramine M, anhydrolycodoline, gnidioidine, ...

The plant Melissa officinalis L. has been used traditionally in the treatment of cognitive dysfunction. Based on its traditional medicinal use, it was assessed for its clinical efficacy in mild to moderate Alzheimer's patients. The plant was effective in the management of the disease. Therefore, based on this result, a similar plant extract was prepared in order to be screened for bioactivities ...

Galanthamine, an acetylcholinesterase inhibitor marketed as a hydrobromide salt (Razadyne�, Reminyl�) for the treatment of Alzheimer's disease (AD), is obtained from Amaryllidaceae plants, especially those belonging to the genera Leucojum, Narcissus, Lycoris and Ungernia. The growing demand for galanthamine has prompted searches for new sources of this compound, as well as ...

In a bioassay-guided search for acetylcholinesterase (AChE) inhibitors from 180 medicinal plants, an ethyl acetate extract of whole plants of Agrimonia pilosa ledeb yielded tiliroside (1), 3-methoxy quercetin (2), quercitrin (3) and quercetin (4). We report herein for the first time that all four flavonol compounds showed significant inhibitory effects on ...

Commercially available essential oils extracted from Artemisia dracunculus L., Inula graveolens L., Lavandula officinalis Chaix, and Ocimum sanctum L. and the components of these oils were screened by the microplate assay method for determining their acetylcholinesterase (AChE) inhibitory activity. The composition profiles of the oils ...

Tubers of Corydalis cava were extracted with ethanol and fractionated using n-hexane, chloroform and ethanol. Repeated column chromatography, preparative TLC and crystallization led to the isolation of fifteen isoquinoline alkaloids. The chemical structures of the isolated compounds were determined on the basis of spectroscopic techniques and by comparison with literature data. All isolated ...

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 ...

Acetylcholinesterase (AChE) inhibitor has been used as a drug for the symptomatic treatment of Alzheimer's disease. In order to search for new AChE inhibitors, 32 plants used in Thai traditional rejuvenating and neurotonic remedies were collected. The plant methanolic extracts were tested for AChE inhibitory activity using Ellman's ...

... by isomalathion: inhibitory reactions with (1R)- and ... Millard, CB, Kryger, G., Ordentlich, A ... acetylcholinesterase: nerve agent reaction products at the ...

The mechanism of enhanced effect of (-)-epigallocatechin-3-gallate (EGCG) on huperzine A's (HUP) inhibition of acetylcholinesterase (AChE) activity in rats was investigated. The inhibitory effects of HUP at 10 and 5 microg/kg on AChE activity were quite weak in the whole phase. In contrast, upon addition of EGCG ...

With the accelerated aging of human society Alzheimer's disease (AD) has become one of the most threatening diseases in the elderly. However, there is no efficient therapeutic agent to combat AD. Berberine is a natural isoquinoline alkaloid that possesses a wide range of pharmacological effects. In the present paper, we review the multiple activities of berberine, including ...

The commercial essential oils of Citrus aurantium L., Cupressus sempervirens L., Eucalyptus globulus Labill., Foeniculum vulgare Mill. and Thymus vulgaris L., isolated by steam distillation by a company of Morocco were evaluated in terms of in vitro antioxidant activity through several methods. In vitro acetylcholinesterase inhibitory ...

transition-state analogues [2], organophosphorus compounds are unique active-site probes of serine hydrolases. � The acute toxicity of organophosphorus compounds is mainly due to their inhibitory action on acetylcholinesterase and related serine hydrolases such as chymotrypsin (Scheme 1) [1]. Hence, the exact knowledge

In the course of screening natural products for anti-acetylcholinesterase (AChE) activity, we found that a total methanolic extract of the underground parts of Caragana chamlague (Leguminosae) had significant inhibition towards AChE. Bioactivity-guided fractionation of the total methanolic extract resulted in the isolation and identification of two ...

A series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), AChE-induced and self-induced ?-amyloid (A?) aggregation. The new hybrids consist of a unit of 1-azabenzanthrone and a tacrine or its congener, connected through an oligomethylene linker containing an ...

Lithium has been used as an effective antimanic drug in humans and it is well known for its effects on neuropsychiatric disorders and neuronal communication. ATP and adenosine are important signaling molecules, and most nerves release ATP as a fast co-transmitter together with classical neurotransmitters such as acetylcholine. In this study, we evaluated the in vitro and in vivo effects of lithium ...

The in vitro acetylcholinesterase (AChE) inhibitory potential of the hydroalcoholic extract and of the essential oil from Acorus calamus (AC) rhizomes and that of its major constituents were evaluated based on the Ellman's method. GC/MS analysis of the oil revealed that the major constituents were beta-asarone (79.54%) and alpha-asarone (8.47%). The IC50 ...

By targeting the dual active sites of acetylcholinesterase (AChE), a new series of berberine derivatives was designed, synthesized, and evaluated as AChE inhibitors. Most of the derivatives inhibited AChE in the sub-micromolar range. Compound 8c, berberine linked with phenol by a 4-carbon spacer, showed the most potent inhibition of AChE. A kinetic study ...

By targeting multi-active sites of acetylcholinesterase (AChE), a series of huperzine A (Hup A) derivatives with various aromatic ring groups were designed and synthesized by Schiff reaction. They were evaluated as AChE and butyrylcholinesterase (BChE) inhibitors. Results showed very significant specificity that the group of imine derivatives could inhibit ...

The present study evaluated the anticholinesterase activity of cold and hot aqueous extracts of Ficus racemosa stem bark against rat brain acetylcholinesterase in vitro. Both the cold aqueous extract (FRC) and the hot aqueous extract (FRH) exhibited a dose dependent inhibition of rat brain acetylcholinesterase. FRH showed significantly ...

The present study evaluated the anticholinesterase activity of cold and hot aqueous extracts of Ficus racemosa stem bark against rat brain acetylcholinesterase in vitro. Both the cold aqueous extract (FRC) and the hot aqueous extract (FRH) exhibited a dose dependent inhibition of rat brain acetylcholinesterase. FRH showed significantly ...

Bioassay-guided extraction of the stem bark of Knema laurina showed the acetylcholinesterase (AChE) inhibitory activity of DCM and hexane fractions. Further repeated column chromatography of hexane and DCM fractions resulted in the isolation and purification of five alkenyl phenol and salicylic acid derivatives. New compounds, ...

The hydrolysis of acetylthiocholine by acetylcholinesterase from Electrophorus electricus was investigated in the presence of the inhibitors tacrine, gallamine and compound 1. The interaction of the enzyme with the substrate and the inhibitors was characterized by the parameters K(I), alpha', b or beta, K(m) and V(max), which were determined directly and simultaneously from ...

Currently acetylcholinesterase inhibitor (AChEI) therapy is one of the most frequently used methods in the treatment of Alzheimer's disease; tacrine, donepezil, rivastygmine and galantamine are applied in different stages of AD. In the present study, we propose a new series of 2-benzoxazolinone derivatives as potential cholinesterase inhibitors. These compounds were ...

ABSTRACT In the present study the in vitro hypoglycemic and anti-acetylcholinesterase activities of hot pepper fruits (Capsicum annuum var. acuminatum L.) at different ripening stages were investigated. The mature, green-stage fruits had the highest activity against alpha-amylase and alpha-glucosidase with 50% ...

Plants are a potential source of bioactive compounds and offer a promising strategy for the treatment of neurological disorders such as Alzheimer's disease. The inhibitory effect of 73 native and naturalized plants collected from the central region of Argentina on acetylcholinesterase (AChE) was tested using microplate and TLC assays after solvent ...

Three natural products, 1,5-diphenylpentan-1-one, 1,5-diphenylpent-2-en-1-one, and 3-hydroxy-1,5-diphenylpentan-1-one, with good insecticidal activities were extracted from Stellera chamaejasme L. Based on their shared diaryl ketone moiety as 'pharmacophores', a series of diaryl ketones were synthesized and tested for insecticidal activity, ...

... orthologous and -paralogous acetylcholinesterase precursors (AO- and AP-AChE precursors, respectively), were identified from the body louse, ... louse strain exhibited a simplex inhibitory response of ACh...

Linarin (acacetin-7-O-beta-d-rutinoside) from the flower extract of Mentha arvensis showed selective dose dependent inhibitory effect on acetylcholinesterase. PMID:16815640

... Title : CONFORMATIONAL STUDIES ON THE ACTIVE SITE OF ACETYLCHOLINESTERASE BY ELECTRON PARAMAGNETIC RESONANCE,. ...

Two new xanthone glycosides, corymbiferin 3-O-beta-D-glucopyranoside (1) and swertiabisxanthone-I 8'-O-beta- d-glucopyranoside (2), were isolated from Gentianella amarella ssp. acuta, along with eight known xanthones: triptexanthoside C, veratriloside, corymbiferin 1-O-glucoside, swertianolin, norswertianolin, swertiabisxanthone-I, bellidin, and bellidifolin, four of them identified for the first ...

The inhibitory effect of 3-diethylaminophenyl-N-methylcarbamate methiodide on rat brain acetylcholinesterase and horse plasma butyrylcholinesterase was studied in vitro. This quaternary carbamate is a more potent inhibitor of acetylcholinesterase than butyrylcholinesterase. Complete inhibition of ...

Studies on the seeds of Annona squamosa yielded a novel lipoxygenase inhibitor fatty acid ester, (+) - annonlipoxy (1). Compound 1 was screened for its enzyme inhibitory activity against lipoxygenase (E.C.1.14.18.1), exhibiting activity with IC(50) 69.05 +/- 5.06 microm. Baicalein (IC(50) 22.6 +/- 0.5 microm) was used as a positive ...

Various native Korean plants were screened to find an effective acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease (AD). Among these plants, the ethanol extract of Poncirus trifoliate was selected for isolating the AChE inhibitor because it exhibited the highest inhibitory activity (47.31%). To separate the ...

Leucosidea sericea is an important medicinal plant widely used in traditional medicine in southern Africa. Leaf and stem petroleum ether (PE), dichloromethane (DCM) and 50% aqueous methanol (MeOH) extracts were investigated for antioxidant and acetylcholinesterase inhibitory activities. The safety of the extracts was evaluated using ...

Three Lycopodiaceae species from French Polynesia, Lycopodium venustulum C. Gaudichaud, Lycopodiella cernua (C. Linnaeus) R. E. Pichi Sermolli and Lycopodium henryanum E. D. Brown were investigated for their alkaloidal composition by UHPLC/ESI-TOF-MS. Ten alkaloids were identified, with lycopodine and lycodoline being the main constituents in the three species. The ...

For many decades it has been thought that oxygen analogs (oxons) of organophosphorus insecticides phosphorylate the catalytic site of acetylcholinesterase by a mechanism that follows simple Michaelis-Menten kinetics. More recently, the interactions of at least some oxons have been shown to be far more complex and likely involve binding of oxons to a second site on ...

Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer' s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives, fourteen ...

... is described that measures the sensitivity of acetylcholinesterase (AChE) activity to inhibition by organophosphorus (OP) insecticides in ... for resistant individuals. The technique will also measure ACh...

... C.-Y., and Wu, M.-T. (1986) Kinetic studies and strcture activity relationships akbispyddinium oximes Srseactivator of acetylcholin-esterase inhibited ...

Techniques to distinguish between the activities of human acetylcholinesterase and pseudocholinesterase have been developed. Human neuroblastoma cell lines have been shown to synthesize human acetylcholinesterase and the level of enzyme within these cells...

Acetylcholinesterase from electric eel is selectively immobilized on Amberlite IR-120 resin with Al(3+) ions. Immobilized acetylcholinesterase activity is stable at least for 85 days in the wet state at 10 C and for 180 days in the dry state at room tempe...

A series of novel and highly active acetylcholinesterase and butyrylcholinesterase inhibitors derived from substituted benzothiazoles containing an imidazolidine-2,4,5-trione moiety were synthesized and characterized. The molecular structure of 1-(2,6-diisopropyl-phenyl)-3-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-imidazolidine-2,4,5-trione (3g) was ...

Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6,10,14-trimethylpentadeca-5,10-dien-2,12-dione and (5E,9E,13E)-6,10,4-trimethyl-pentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate ...

Seventy-six plant extracts from the Panamanian flora have been screened for acetylcholinesterase (AChE) inhibitors by thin-layer chromatography (TLC) bioautography. The most promising extracts with AChE inhibitory and free radical scavenging activities at 100 microg were those of Tabernaemontana panamensis (Markgr., Boiteau & L. ...

Organophosphate and carbamate insecticides are widely detected in surface waters of the western United States. These chemicals interfere with acetylcholine-mediated synaptic transmission in the nervous systems of fish and other aquatic animals via the inhibition of AChE (acetylcholinesterase) enzyme activity. Anticholinesterase insecticides commonly ...

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 ...