Search results for "Cholinesterase Inhibitor"
showing 10 items of 57 documents
Effect of bioclimatic area on the composition and bioactivity of Tunisian Rosmarinus officinalis essential oils
2014
The chemical composition of eight Tunisian Rosmarinus officinalis L. populations (A-H) from different bioclimatic areas has been examined by gas chromatography (GC) and GC-mass spectrometry. The essential oils are characterised by high amounts of oxygenated monoterpenes (58.2-71.7%) followed by monoterpene hydrocabons (15.1-26.7%). 1,8-Cineole, camphor, α-pinene and borneol are the main representative components. The antioxidant activity was investigated by 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), ferric reducing ability power assay and β-carotene bleaching test. Samples showed antiradical activity by inhibiting DPPH radical with IC50 values ranging from 375.3 to 592.8 μg mL(- 1) for s…
(±)- BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3β Inhibition with Calcium Channe…
2021
Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer's disease (AD). Novel MTDLs have been designed as inhibitors of human acetylcholinesterases/butyrylcholinesterases, monoamine oxidase A/B, and glycogen synthase kinase 3β and as calcium channel antagonists via the Biginelli multicomponent reaction. Among these MTDLs, (±)-BIGI-3h was identified as a promising new hit compound showing in vitro balanced activities toward the aforementioned recognized AD targets. Additional in vitro studies demonstrated antioxidant effects and brain penetration, along with the ability to inhibit the aggregation of both τ protein…
Hairy Garlic (Allium subhirsutum) from Sicily (Italy): LC-DAD-MSn Analysis of Secondary Metabolites and In Vitro Biological Properties
2020
Allium subhirsutum, known as hairy garlic, is a bulbous plant widespread in the Mediterranean area and locally used as a food and spice. In the present study, the chemical profile of the ethanolic extracts from bulbs (BE) and aerial parts (APE) were analyzed by HPLC-ESI-MSn, and antioxidant properties were evaluated by DPPH, ABTS and TEAC assays. The traditional use in the diet, and the well documented biological activity of Allium species suggest a potential as a new nutraceutical. For this reason, the potential usefulness of this food can be considered in the treatment and prevention of degenerative Alzheimer disease. For this reason, acetylcholinesterase inhibitory property was investiga…
Comparative chemical composition and bioactivity of leaves essential oils from nine Sicilian accessions of Myrtus communis L.
2019
In this study, the essential oils obtained from the leaves of Myrtus communis L. stored in a collection orchard located at the experimental station ‘Orleans’ of the Department of Agricultural and Forest Sciences of the University of Palermo (Italy) were investigated. The essential oils, analysed by gas chromatography–mass spectrometry, revealed the presence of α-pinene, 1,8-cineole, linalool, limonene and myrtenyl acetate as dominant constituents. The neuroprotective effects of M. communis essential oils were investigated by analysing the antioxidant properties and cholinesterases (acetylcholinesterase, AChE, and butyrylcholinesterase, BChE) inhibitory activity. Essential oils from Scopello…
Alterations on AChE Activity of the Fish Anguilla anguilla as Response to Herbicide-Contaminated Water
2000
Abstract The inhibition of both total and specific acetylcholinesterase activities was measured in the whole eyes of the yellow eel Anguilla anguilla after exposure to the carbamate thiobencarb. In vivo assays were conducted under a constant flow-through system of thiobencarb-contaminated water (1/60 LC50 96 h=0.22 ppm for 96 h) followed by a recovery period in clean water (192 h more). The results indicated a measurable level of AChE activity on eyes of control eels, which resulted in a sensitive indicator of the presence of thiobencarb in the water. The pesticide induced significant inhibitory effects on AChE activity ranging from 35% in total AChE activity to 75% in specific AChE activit…
Inhibitory and excitatory muscarinic receptors modulating the release of acetylcholine from the postganglionic parasympathetic neuron of the chicken …
1992
The effects of muscarinic receptor antagonists on ACh release were studied in the absence or presence of cholinesterase (ChE) inhibition using the isolated perfused chicken heart. Presynaptic inhibitory muscarinic autoreceptor were characterized by determining the potency of various antagonists to enhance [3H]-ACh release evoked by field stimulation (3 Hz, 1 min). The order of potencies was: (±)-telenzepine > atropine > 4-DAMP > silahexocyclium > pirenzepine > hexahydro-siladifenidol > AF-DX 116. The comparison with known pA2 values for M1-, M2- and M3-receptors revealed that the presynaptic autoreceptor meets the criteria of an M1-receptor. Basal, not electrically evoked overflow of unlabe…
Effects of diazinon exposure on cholinesterase activity in different tissues of European eel (Anguilla anguilla).
1996
Cholinesterase (ChE) activity was measured in brain, plasma, and whole eye of Anguilla anguilla experimentally exposed to a sublethal concentration of 0.042 mg/liter (0.50 of the 96-hr LC50) of the organophosphorous pesticide diazinon. Whole eye was the tissue which revealed higher values of ChE activity (8.17 micromol/min/g) in nonexposed animals. Brain, plasma, and whole eye ChE activity of A. anguilla was inhibited at 6, 24, 48, 72, and 96 hr of diazinon exposure. Pesticide induced significant inhibitory effects on the ChE activity of this species ranging from >70% inhibition in brain tissue to >90% in plasma samples. Brain and plasma presented technical difficulties in their collection.…
In vivo inhibition of AChE activity in the European eel Anguilla anguilla exposed to technical grade fenitrothion.
1998
European eel (Anguilla anguilla) were exposed to sublethal fenitrothion concentrations in a continuous flow-through system for 4 days. Plasma acetylcholinesterase (AChE) activity was evaluated after 2, 8, 12, 24, 32, 48, 56, 72 and 96 h pesticide exposure. AChE activity in the plasma of the eel decreased as concentration of fenitrothion increased. Pesticide induced significant inhibitory effects on the AChE activity of A. anguilla ranging from 51% inhibition at sublethal concentration of 0.02 ppm to 57% inhibition at sublethal concentration of 0.04 ppm. Eel were exposed to both fenitrothion concentrations for 96 h and then allowed a period of recovery in pesticide-free water. Following 1 we…
Use of drug treatments for Alzheimer's disease in France: a study on a national level based on the National Alzheimer's Data Bank (Banque Nationale A…
2012
Purpose To examine the way in which specific drug treatments for Alzheimer's disease are used and whether their use complies with clinical practice guidelines issued by the French National Authority for Health in patients with Alzheimer's disease. Methods We analysed a cross-section of the French National Alzheimer's databank (BNA). Participants were individuals who consulted centres contributing to the BNA in 2010 and diagnosed with Alzheimer's disease and with at least one Mini Mental State Examination (MMSE) score recorded during the course of the year. Results Of 191 919 consultations recorded in the database, 29.9% involved a diagnosis of Alzheimer's disease, and 26 809 patients had co…
Allosteric sensitization of nicotinic receptors by galantamine, a new treatment strategy for Alzheimer’s disease
2001
Cholinesterase inhibitors are the only approved drug treatment for patients with mild to moderately severe Alzheimer's disease. Interestingly, the clinical potency of these drugs does not correlate well with their activity as cholinesterase inhibitors, nor is their action as short lived as would be expected from purely symptomatic treatment. A few cholinesterase inhibitors, including galantamine, produce beneficial effects even after drug treatment has been terminated. These effects assume modes of action other than mere esterase inhibition and are capable of inducing systemic changes. We have recently discovered a mechanism that could account, at least in part, for the above-mentioned unex…