Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.1.8 (cholinesterase)
12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Acetylcholinesterase (AchE) is reported to have a narrowly restricted distribution among human tissues. Three strains of human fibroblasts which are trisomic for chromosome 2 had an average level of AchE activity over 28 times higher than the average level in 19 control strains of human fibroblasts. In contrast, the mean pseudocholinesterase activity of the trisomy-2 strains did not differ appreciably, or significantly, from the mean for the control strains. The 19 control strains included 10 strains trisomic for autosomes other than 2, and 9 euploid strains. Our estimate of the mean AchE activity in the control strains did not differ significantly from zero and might, in any case, have originated from a minute amount of activity contributed to the cells by an esterase in our culture medium. Despite the striking elevation of AchE activity in fibroblasts trisomic for chromosome 2, extracts of these cells had only about 1.5% of the specific AchE activity (per microgram DNA) present in extracts of human cerebral cortex. None of the 22 strains studied had detectable activity for two other enzymes which, like AchE, have a restricted distribution among human tissues: xanthine oxidase and choline acetyltransferase.
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PMID:Evidence for a striking increase in acetylcholinesterase activity in cultured human fibroblasts which are trisomic for chromosome two. 69 21

25 iodomethylates of acetic, propionic, butyric, isobutyric and valeric esters of N-(beta-hydroxyethyl)-derivatives of ephedrine (I) pseudo-ephedrine (II), salsoline (III), salsolidine (IV) and cytisine (V) are studied as substrates and inhibitors of acetylcholine esterase (EC 3.1.1.8) from human erythrocytes and butyrylcholine esterase (EC 3.1.1.8) from horse serum. Butyrylcholine esterase found to increase the hydrolysis rate of all the alkaloid esters studied with the increase of acyl radical either to valerates (for ephedrine and pseudo-ephedrine derivatives), or to butyrates (for the rest alkaloids) and then it did not considerably change under further elongation of carbon chain up to valerate. Isobutyrates were observed to be similar to propionates in their hydrolysis rates. Acetylcholine esterase hydrolyzed acetates with the highest rate, while butyrates of ephedrine and pseudoephedrine derivatives were hydrolyzed by the enzyme 2,5-3-fold as slow as acetates. The rate of choline esterase hydrolysis decreased in the row: ephedrine--salsoline--cytisine with the volumetric increase of the cationic group. The decrease was almost 10-fold for butyrylcholine esterase, while a transition from "poor" substrates to reversible inhibitors was observed for acetylcholine esterase (3 of 5 cytisine esters were reversible inhibitors of the enzyme). The data obtained are compared with literary data on other cyclic choline esterase substrates; they are discussed from the viewpoint of unproductive binding hypothesis and on the basis of the structure of active centres of acetyl- and butyrylcholine esterases.
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PMID:[Ephedrine, salsoline and cytisine derivatives as substrates and inhibitirs of cholinesterases]. 69 1

The structure and histochemistry of the palmar and plantar skin were studied in four adult male marmosets (two Callithrix jacchus and two Callithrix penicillata). In this skin there exist well-developed epidermal ridges, to which are attached one or two ducts of sweat glands. A thick stratum corneum can be seen in the epidermis, while a distinct stratum lucidum cannot be isolated from the other layers. The stratum granulosum is constituted by one or three layers of cells containing keratohyalin granules. Melanin granulations are mainly concentrated in the basal cells of the epidermal ridges. Dendritic melanocytes and amelanotic melanocytes containing alkaline phosphatase are found among the epidermal cells. Glycogen, UDPG-GT and phosphorylases are mainly present in the middle and lower Malpighian cells of the epidermal ridges. Alkaline phosphatase, ATPase, alanyl amino-peptidase and leucine aminopeptidase were absent in the epidermal cells. SDH, cytochrome oxidase, MAO and a certain number of NAD-dependent dehydrogenases (LDH, ADH, MDH, alpha-GPDH, beta-OHBDH and GDH) showed a stronger reactivity in the basal cells and Malpighian layer. The NADP-dependent enzymes (G-6-PDH, 6-PGDH, cis-aconistase and ICDH) were more reactive in the upper Malpighian layer and stratum granulosum. The stratum corneum showed some acid phosphatase and nonspecific esterase reactivity. The collagenous fibers intertwined with a small number of very thin elastic ones and a larger amount of reticular fibers run almost parallel to the epidermal ridges in the papillary body. In the reticular dermis some fibers are disposed transversely to the epidermal ridges. Meissner corpuscles reactive to butyrylcholinesterase, acetylcholinesterase, nonspecific esterase and G-6-PA are disposed at regular intervals and frequently at each side of the epidermal ridges. Pacinian corpuscles were found only in the hypodermis. The eccrine sweat glands contain glycogen, UDPG-GT and phosphorylase in their secretory, ductal and myoepithelial cells. The secretory part shows a uniform reactivity for every dehydrogenase because it contains only one type of cells (clear cells). The intraepidermal segment of the ducts shows a stronger reactivity to nonspecific esterase and NADP-dependent dehydrogenases than the epithelial cells around it.
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PMID:The skin of the palms and soles of the marmosets (Callithrix jacchus and Callithrix penicillata). 82 86

A single application of a mixture of cholinolytic and reactivator of cholinesterase (TMB-4 compos. SPOFA) administered intravenously in the dose of 10.0 mg of trimedoxim per kg of live weight to sheep for 60 minutes after an intramuscular intoxication with O-ethyl S-(2-dimethylaminoethyl) methyl phosphonothioate (EDMM) in the dose of 0.00835 mg per kg of live weight (i.m. LD50, 2h) produces an immediate clinical effect. The reactivation of the erythrocytary acetyl cholinesterase (AChE, E.C.3.1.1.7.) examined in 15 minutes after the administration of the antidotal mixture is almost 100 p.c., the reactivation of the plasmatic butyryl cholin esterase (ChE, E.C.3.1.1.8.) approx. from 70 to 80 p. c. Restitution ad integrum occurred not later than in 14 days after the intoxication.
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PMID:[Antidotal effect of TMB-4 compos. Spofa in sheep intoxicated with O-ethyl S-(2-dimethylaminoethyl) methyl phosphonothioate]. 82 81

The behaviour of several dehydrogenases(succino-, beta-glycerophosphate-, lactate-, alcohol-, beta-hydroxibutyric acid-, glucose-6-phosphate-, isocitronic acid-dehydrogenase, monoamino-oxidase, and gamma-aminobutyric acid-transaminase) and of several hydrolytic enzymes (non-specific esterase, lipase, acetylcholin-, butyrylcholinesterase, alkaline phosphatase and leucinaminopeptidase) was investigated in the neurons of NSO and NPV, in the infundibulum and in the neurohypophysis and the innervation of the neurons (acetylcholinesterase, monoamino-oxidase, catecholamines) by unmilked and milked cows. The milking stimulus influences the metabolism especially in the neurosecretory cells of the NPV. After the milking stimulus the activity of oxydative enzymes is above all very increased, the anaerobic way of the output of energy is after that also higher. The building up of the carbohydrates through glycolyse in the neurosecretory cells of the NPV after the milking stimulus is increased. The possible participation of the investigated hydrolytic enzymes on the metabolism of the neurosecretory cells is discussed. The neurons of the NPV were innervated for the most part adrenergic. It is discussed the participation of the enzymes succinodehydrogenase and monoaminooxidase on the hormone release in the neurohypophysis.
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PMID:[Enzymhistochemical investigations on the hypothalamo-neurohypophysial system of unmilked and milked cows (author's transl)]. 82 94

The dermal cells in grey, xanthic, and white goldfish integuments were cytochemically characterized for the following enzymatic activities: tyrosinase, DOPA-oxidase, cytochrome oxidase, monoamine oxidase, peroxidase, non-specific esterase, cholinesterase, NAD-diaphorase, NADP-diaphorase, aryl sulfatase, nucleotide phosphodiesterase, beta-glucuronidase, acid phosphatase, alkaline phosphatase, adenosine triphosphatase, thiamine pyrophosphatase, glucose-6-phosphatase, aldolase, as well as succinate, malate, isocitrate, glutamate, glucose-6-phosphate, 6-phosphogluconate, alpha-glycerophosphate, alcohol, lactate, and beta-hydroxybutyrate dehydrogenases. It was found that the epidermis was a significant barrier to the access of cytochemical reaction substrates. Removal of the epidermal barrier provided dermal cell localizations of enzymatic activities which were reproducible. Further, alterations in reaction times and temperatures from the mammalian methodology provided conditions fe various integumental cells were compared for possible interrelationships. The basic foundations for future work with the dermis of poikilothermic vertebrates on an experimental basis were established. In addition, a previously undescribed non-pigmented dermal cell, the "x"-cell, was found to have enzymatic characteristics similar to both melanophores and lipophores. The "x"-cell may be the common precursor of both types of pigment cells.
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PMID:Cytochemical characterization of goldfish (Carassius auratus L.) dermis with special reference to the pigment cells. 82 86

The ontogeny of esterase isozymes in Brachydanio rerio (zebra danio), Brachydanio albolineatus (pearl danio), and hybrids formed by their reciprocal crosses was investigated using polyacrylamide disc electrophoresis. Seven esterase isozymes were identified in each species from the unfertilized egg stage to nine days posthatch. Electrophoretic analysis of qualitative changes in enzyme pattern indicated that some esterases were present at all stages of development while other esterases abruptly appeared at a specific stage of morphological differentiation. The esterases of both species were classified on the basis differential substrate and inhibitor specificities. In developing hybrids formed by B. rerio eggs inseminated with B. albolineatus sperm, the maternal isozyme pattern persisted until Stage 17 (gastrulation). Embryonic extracts from Stage 17 onward showed a slow-moving, DFP-sensitive carboxylesterase of paternal origin. In developing hybrids formed by B. albolineatus eggs inseminated with B. rerio sperm, a paternal contribution to the esterase pattern was probably present by the end of gastrulation; esterase activity of distinctively paternal origin was present by Stage 22 (retinal pigmentation) The maternal contribution to the total esterase profile appeared to remain high through hatching. Additional evidence for gene activity at gastrulation was obtained in experiments utilizing actinomycin-D and cycloheximide. Results of exposing embryos of B. rerio to 15 mug/ml of actinomycin-D indicated that transcription of the template RNA coding for cholinesterase occurred during gastrulation or some 20-30 hours prior to the appearance of the isozyme at Stage 22. This template RNA was translated sometime during that 10-hour interval immediately preceding Stage 22.
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PMID:Esterase isozyme patterns in developing embryos of Brachydanio rerio (zebra danio), Brachydanio abolineatus (pearl danio), and their hybrids. 83 81

Acetate esters, such as aspirin methylester, aspirin and resorcinol monoacetate, induced contractions of guinea-pig ileum. Their actions were selectively antagonized by atropine, but were not affected by ganglion blocking agents, conduction blockers, aging with cooling, anoxia or antihistaminics. On the other hand, N-acetates, such as acetanilide and p-acetaminophenol, and no contractile action on the ileum. These acetate esters thus seemed to have a cholinergic action, and not a direct action on muscle or other known specific receptors for endogenous active substances. The contractions induced by the acetate esters were selectively potentiated by low concentrations of choline, whereas those induced by acetylcholine, nicotine, 5-hydroxytryptamine and histamine were not. However, N-acetates did not induce the contractions even in the presence of choline. Organophosphorus cholinesterase inhibitors, such as diisopropyl fluorophosphate and paraoxon, selectively and irreversibly inhibited the actions of aspirin and N,O-diacetyl-p-aminophenol with or without choline. From these results, it is concluded that the acetate esters with or without choline act through the cholinergic system. However, their actions cannot be explained in terms of known mechanisms, such as acetylcholine release, cholinesterase inhibition or a direct muscarinic action. Therefore, the acetate esters, including phenyl acetate which was supposed to be a releaser of acetylcholine, seem to have a hitherto undescribed type of cholinergic action whose mechanism is unknown. It seems that organophosphate-sensitive esterase(s) in the preparation may be essential for initiation of the actions of the acetate esters with or without choline, but the mechanism of the effect of choline is unknown.
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PMID:Aspects of the spasmogenic effects of acetate esters on ileal smooth muscle. 85 12

The relationship between pseudocholine esterase [acylcholine acyl-hydrolase, EC 3.1.1.8] and non-specific esterase [carboxylic ester-hydrolase, EC 3.1.1.1] in human serum was investigated. The purified preparation (purified 500-fold) which had both pseudocholine esterase and non-specific esterase activities, was found to give a single band with faint tailing on polyacrylamide gel electrophoresis. The ratio of the specific activity of pseudocholine esterase to that of non-specific esterase remained essentially the same during the purification procedures. Furthermore, the pseudocholine esterase was demonstrated to be identical with the non-specific esterase by immunochemical studies. All these results suggest that activities of pseudocholine esterase and non-specific esterase in human serum derive from the same enzyme molecule. Observation of Yoshida-cho in Ehime after the application of organophosphorus insecticide supported our results: the activity of pseudocholine esterase was found to be reduced with a concomitant decrease in the activity of non-specific esterase. Based on these results, the physiological significance of the esterase is discussed.
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PMID:Identification of acylcholine acyl-hydrolase with carboxylic ester-hydrolase in human serum. 89 81

The effect of enriched human plasma-cholinesterase preparation on the phase II block of succinylcholine chloride was studied in man during anesthesia and surgery. Intravenous administration of 8 esterase units/kg of plasma-cholinesterase did not show any discernible effect on the phase II block of succinylcholine chloride, while edorphonium 10 mg clearly antagonized the block. The finding of the present study suggests that the preparation may be ineffective for patients with a prolonged apnea following the administration of succinylcholine chloride.
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PMID:Effect of plasma-cholinesterase preparation on the phase II block of succinylcholine chloride in man. 91 67


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