Topic:Cholinesterase
Cholinesterase refers to a group of enzymes responsible for the hydrolysis of choline esters, which are essential for normal nervous system function in horses. These enzymes, primarily acetylcholinesterase and butyrylcholinesterase, are involved in the breakdown of acetylcholine, a neurotransmitter critical for muscle function and neural communication. Variations in cholinesterase activity can be indicative of exposure to certain toxins, such as organophosphates or carbamates, or may reflect liver function and other metabolic conditions. Monitoring cholinesterase levels can aid in diagnosing and managing these conditions. This page gathers peer-reviewed research studies and scholarly articles that explore the role, activity, and clinical implications of cholinesterase in equine physiology and health.
Novel Organoruthenium(II) Complex C1 Selectively Inhibits Butyrylcholinesterase without Side Effects on Neuromuscular Transmission. Enzyme butyrylcholinesterase (BChE) shows increased activity in some brain regions after progression of Alzheimer's disease and is therefore one of the therapeutic targets for symptomatic treatment of this neurodegenerative disorder. The organoruthenium(II) complex [(η--cymene)Ru(II)(1-hydroxy-3-methoxypyridine-2(1)-thionato)pta]PF () was designed based on the results of our previous structure-activity studies. Inhibitory activity toward cholinesterase enzymes shows that this complex selectively, competitively, and reversibly inhibits horse serum BChE (hsBChE) with an IC value of 2.88 µM. Wh...
Amiridine-piperazine hybrids as cholinesterase inhibitors and potential multitarget agents for Alzheimer’s disease treatment. We synthesized eleven new amiridine-piperazine hybrids 5a-j and 7 as potential multifunctional agents for Alzheimer's disease (AD) treatment by reacting N-chloroacetylamiridine with piperazines. The compounds displayed mixed-type reversible inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Conjugates were moderate inhibitors of equine and human BChE with negligible fluctuation in anti-BChE activity, whereas anti-AChE activity was substantially dependent on N4-substitution of the piperazine ring. Compounds with para-substituted aromatic moieties (5g, 5h, and bis-amirid...
[How aliphatic alcohols and ph affect reactional capability of the horse blood serum cholinesterase at its interaction with organophosphorus inhibitors]. There was studied action of aliphatic alcohols (ethanol, propanol, isopropanol, n-butanol, isobutanol, secbutanol, tretbetanol) and pH on various kinds of reactional capability the serum cholinesterase. At the alcohols-affected inhibition of the cholinesterase hydrolytic activity, the determining role was played not the total number carbon atoms in the alcohol molecule, but by the "effective length" of the carbohydrate chain. The fact that the presence of alcohols did not affect parameters of the reverse cholinesterase inhibition with onium ions tetramethylammonium and choline allows suggestin...
[The influence of pH on cholinesterase hydrolysis of alpha-naphthylacetate in the presence of some cationic detergents]. The influence of some cationic detergents on the catalytic activity of the horse blood plasma cholinesterase in reaction of hydrolysis of alpha-naphthylacetate at different pH were investigated. It was shown, that in the absence of detergents in acid pH of the reaction medium the Km value increases, but V remain constant. In the range of pH from 8.5 to 5.0 in the presence of detergents the Km and V values are not practically changed. That is why the activation of cholinesterase hydrolysis of alpha-naphthylacetate in the presence of detergents is considerably higher than that of the neutral pH....
Role of oligosaccharides in the pharmacokinetics of tissue-derived and genetically engineered cholinesterases. To understand the role of glycosylation in the circulation of cholinesterases, we compared the mean residence time of five tissue-derived and two recombinant cholinesterases (injected intravenously in mice) with their oligosaccharide profiles. Monosaccharide composition analysis revealed differences in the total carbohydrate, galactose, and sialic acid contents. The molar ratio of sialic acid to galactose residues on tetrameric human serum butyrylcholinesterase, recombinant human butyrylcholinesterase, and recombinant mouse acetylcholinesterase was found to be approximately 1.0. For Torpedo ca...
Structure of glycan moieties responsible for the extended circulatory life time of fetal bovine serum acetylcholinesterase and equine serum butyrylcholinesterase. Cholinesterases are serine hydrolases that can potentially be used as pretreatment drugs for organophosphate toxicity, as drugs to alleviate succinylcholine-induced apnea, and as detoxification agents for environmental toxins such as heroin and cocaine. The successful application of serum-derived cholinesterases as bioscavengers stems from their relatively long residence time in the circulation. To better understand the relationship between carbohydrate structure and the stability of cholinesterases in circulation, we determined the monosaccharide composition, the distribution of various oligo...
Effect of time and storage temperature on cholinesterase activity in blood from normal and organophosphorus insecticide-treated horses. Delays between time of sampling and time of testing are common; therefore, the length of time that blood can be stored at various temperatures was evaluated for effects on cholinesterase activity. Six horses were treated with 16 g of trichlorfon per os, 6 horses were treated with 15 g of dichlorvos per os, and 10 horses were untreated controls. The cholinesterase activity in whole blood from each horse was measured using an adaptation of the Ellman colorimetric method. The blood from each horse was then divided into 3 groups and stored at 5 C (refrigerated), 20 C (room temperature), or 38 C (i...
The effect of the organophosphate trichlorfon on the neuromuscular blocking activity of atracurium in halothane-anesthetized horses. To determine whether cholinesterase inhibition by an organophosphate would influence atracurium's neuromuscular blockade, six horses were anesthetized and paralyzed with atracurium (total of five injections per horse) on experimental Day 1, then were given trichlorfon (64 mg/kg per os) 6 days later. On Day 7, horses were anesthetized and paralyzed in the same manner as on experimental Day 1. Blood was taken to measure serum cholinesterase activity prior to anesthesia on Days 1 and 7. No significant difference was noted in atracurium's neuromuscular blocking activity between the 2 experimental ...
Brain cholinesterase activity in animals and birds. Normal cholinesterase activity in brain tissue was measured in various mammalian and avain species. The cholinesterase activity in the cerebrum of cattle, swine, sheep and horses was approximately 2-3 umoles/min/g of tissue in each instance. The whole brain cholinesterase activity of small feral mammals was approximately 2 to 5 fold greater than the domestic animals. Considerable interspecies variability was present in the feral mammals. Similar variability was also observed in the avian brain cholinesterase determinations. The avian whole brain cholinesterase activities ranged from 9.78 to 21...
Use of procainamide gels in the purification of human and horse serum cholinesterases. Two large-scale methods based primarily on the use of procainamide-Sepharose gels were developed for the purification of horse and human serum non-specific cholinesterases. With method I, the procainamide-Sepharose 4B gel was used in the first step to handle large volumes of serum. With method II, the procainamide-Sepharose 4B gel was used in the final step to obtain pure enzyme. Although both methods gave electrophoretically pure cholinesterase preparations in good yields, they were significantly more efficient at purifying the horse enzyme than the human enzyme. To study this problem, the re...
Carcinogenicity of dichlorvos. Dichlorvos, 2,2-dichlorovinyl dimethyl phosphate, an organophosphate insecticide, is widely used for the control of agricultural, industrial, and domestic pests (Fig. 1) [1]. Dichlorvos is administered orally as an anthelmintic to swine, horses, cats, and dogs. It is applied by dermal application to cattle, goats, sheep, swine, and chickens to control fleas, flies, and mites. Cucumbers, radishes, lettuce, and tomatoes are treated with dichlorvos in greenhouses. Aerosols and strips are used for the control of ants, bedbugs, ticks, cockroaches, flies, mosquitoes, silverfish, spiders, and wasps. ...
[Study of hydrolysis of aminoalcohol ethers, phenol and choline under the action of horse blood serum cholinesterase]. Hydrolysis of ethers of saturated and unsaturated alcohols and ethers, e.g. phenol and choline, under the action of horse blood serum cholinesterase, was studied. The reactivity towards enzymatic hydrolysis is decreased due to a greater length of the chain in the alcohol residue of the benzoic acid aminoethers; at nCH2 = 4 the compound is a poor substrate. An increase in nydrophobicity of the acyl residue of the ether molecule also leads to a decrease in the Vmax and Km values. In case of cholinesterase substrates, an increase in the molecule hydrophobicity results in an increase of its non-pr...