Search results for "Cholinesterase Inhibitor"
showing 10 items of 57 documents
Response and Recovery of Brain Acetylcholinesterase Activity in the European Eel,Anguilla anguilla,Exposed to Fenitrothion
1998
European eel (Anguilla anguilla) were exposed to sublethal fenitrothion concentrations in a continuous flow-through system for 4 days. Brain acetylcholinesterase (AChE) activity was evaluated after 2, 8, 12, 24, 32, 48, 56, 72, and 96 h pesticide exposure. Results indicated that AChE activity in eel brains decreased as the concentration of fenitrothion increased. The pesticide induced significant inhibitory effects on the AChE activity ofA. anguilla,ranging from >40% inhibition at a sublethal concentration of 0.02 ppm to >60% inhibition at a 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-f…
Essential oil of Citrus lumia Risso: Phytochemical profile, antioxidant properties and activity on the central nervous system
2018
Citrus lumia Risso Essential oil Antioxidant properties Anti-cholinesterase activity Cytotoxicity Neuroactive effects 1. Introduction Plants that produce essential oils (EOs) represent a large part of natural flora and an important resource in various fields such as pharmaceutical, food and cosmetic industries, due to their flavor, fra- grance and biological activity (Swamy et al., 2016). EOs play a pivotal role in the growth and colonization of plants, giving color and scent to reproductive organs, attracting pollinators, favoring seed dispersion (Sharifi-Rad et al., 2017), and defending the plant against abiotic (light, temperature, etc.) and biotics (herbivores, harmful insects and pa- t…
Allosteric modulation of nicotinic acetylcholine receptors as a treatment strategy for Alzheimer's disease
2000
The basic symptoms of Alzheimer's dementia, i.e., a loss in cognitive function, are due to impaired nicotinic cholinergic neurotransmission. To compensate for this impairment by drug treatment, blockers of the acetylcholine-degrading enzyme acetylcholinesterase are applied, even though this approach obviously is prone to many side-effects, including those of muscarinic nature. We have recently described a novel class of nicotinic acetylcholine receptor ligands which, similar to the action of benzodiazepines on GABA(A) receptors, allosterically potentiate submaximal nicotinic responses. The sensitizing effect is a consequence of facilitated channel opening in the presence of allosterically p…
Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet.
2009
In this study the development of a procedure based on capillary electrophoresis after enzymatic reaction at capillary inlet methodology for the screening and in vitro evaluation of the biological activity of acetylcholinesterase (AChE) inhibitors is presented. The progress of the enzymatic reaction of the hydrolysis of acetylthiocholine at pH 8 in the presence of AChE and the inhibitor studied is determined by measuring at 230 nm the peak area of the reaction product thiocholine (TCh). In the method employed the capillary was first filled with 30 mM borate-phosphate buffer (pH 8.0) and subsequently, plugs of: (i) water, (ii) AChE solution, (iii) substrate solution with or without inhibitor,…
Pharmacokinetic rationale for switching from donepezil to galantamine.
2001
Galantamine, the most recently approved acetylcholinesterase inhibitor (AChEI) for use in the United States, has allosteric modulating activity at nicotinic receptors and inhibits acetylcholinesterase. This dual mechanism of action may make galantamine an attractive option for patients with Alzheimer's disease who have not benefited from their current therapy; thus, methods for switching patients from donepezil or rivastigmine to galantamine are needed. Protocols for switching patients from one AChEI to another must consider both the time required for washout of the first drug and the rate of dose escalation of the second drug. Both issues depend on the pharmacodynamics, pharmacokinetics, a…
Chemistry and functional properties in prevention of neurodegenerative disorders of five Cistus species essential oils.
2013
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 genus, the composition showed interesting differences. Essential oils were screened also for their potential antioxidant effects (by DPPH, ABTS, FRAP and b-carotene bleaching test) and their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity, useful for prevention and …
Frequencies of pseudocholinesterase variants in Icelanders, Greeks and Pakistanis.
1968
THE formation of the human pseudocholinesterase variants is controlled by at least four alleles at one autosomal locus termed E1 (ref. 1). The four alleles are , , and (refs. 2–5). The heterozygotes have been found in remarkably uniform frequencies, about 3 to 6 per cent, in Caucasians from Europe and North America3,8–11, and also in Australian aborigines12 and Mexican Indians13, but are relatively rare among Negroes11 and Mongoloids10,11,14.
Increased recovery of brain acetylcholinesterase activity in dichlorvos-intoxicated European eels Anguilla anguilla by bath treatment with N-acetylcy…
2003
Organophosphate (OP) pesticides are widely used as antiparasitic chemicals in finfish aquaculture. However, current antidotes cannot be applied to treat intoxicated fish. We showed in previous studies the importance of glutathione (GSH) metabolism in pesticide resistance of the European eel Anguilla anguilla L. The present work studied the effects of the antioxidant and glutathione pro-drug N-acetyl-l-cysteine (NAC) on the recovery of European eels exposed for 96 h to a sublethal concentration (0.17 mg l^-1; 20% of its 96 h LC50) of the OP pesticide dichlorvos (2,2-dichlorovinyl dimethyl phosphate; DDVP). This insecticide and acaricide decreased muscular GSH content and increased oxidised g…
Toxicity of Dimethoate to Some Soil Animal Species in Different Soil Types
1996
Toxicity of dimethoate (insecticide) to an earthworm (Aporrectodea caliginosa tuberculata), a collembola (Folsomia candida), and an enchytraeid worm (Enchytraeus crypticus/variatus) was studied in three different soil types (artificial soil, clayey soil, and humus sandy soil). Parameters measured were survival and biomass change of the earthworms and survival and reproduction of the collembolas and enchytraeids. The degradation of dimethoate was analyzed too. Toxic effects were observed at the concentrations of some mg/kg dry soil. The biomass reduction of the earthworms occurred at lower concentrations than reduction in survival. The collembolas were more susceptible to dimethoate than the…
Confirmation of Fenthion Metabolites in Oranges by IT-MS and QqTOF-MS
2007
14 pages, 4 figures, 4 tables.-- PMID: 18020315 [PubMed].-- Printed version published Dec 15, 2007.