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)

Affinity electrophoresis of three purified molecular forms of human plasma cholinesterase (monomer C1, dimer C3, tetramer C4) was carried out in polyacrylamide gels at various total acrylamide concentrations ranging from 3.48 to 9% in a discontinuous buffer system. A water-soluble linear copolymer supporting procainamide, a ligand of the anionic site of cholinesterase, was physically entrapped at various concentrations within the gel network. The combined effects of gel concentration and ligand concentration on the affinity pattern of the three molecular forms were studied. It was found that gel concentration influences the apparent binding activity of their anionic site: The apparent strength of interaction varied with the gel concentration: the denser the gel was, the higher the apparent affinity. The ligand-induced isomerization process was also depending on the gel concentration: the ligand concentration from which each zone is splitting into two moving zones decreased as the total gel concentration increased. These results show that the electrophoretic matrix plays an important role in the affinity process in affinity electrophoresis presumably by controlling kinetic effects: kinetics of protein-ligand complex formation and dissociation reactions, and mass transfer kinetics.
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PMID:[Affinity electrophoresis in polyacrylamide gel. Influence of the concentration in the gel on the apparent affinity of cholinesterase for an anionic ligand site]. 403 Sep 68

A study was made of the activity of acetylcholinesterase (AChE), cholinacetyl transferase (CAT), butyril cholinesterase (BCE) and water-soluble proteins in the structures of the CNS and in the autonomous ganglia in rabbits predisposed to cardiovascular disorders under emotional stress. It was established that unlike resistant animals, in those predisposed to cardiovascular disorders, the CAT content in the periphornical area of the hypothalamus did not differ from the control, the content of water-soluble proteins in the CNS structures and the ganglia remained unchanged either as compared with the control. The authors assume that the data obtained confirm a previously advanced concept of the involvement of the cholinergic system of the periphornical area of the hypothalamus in the maintenance of the stability of cardiovascular functions by regulation of the water-salt metabolism.
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PMID:[Acetylcholinesterase and choline acetyltransferase in the nervous system of rabbits predisposed to cardiovascular disorders under emotional stress]. 403 3

A 1:1 mixture of aldicarb sulfoxide/aldicarb sulfone was administered to young adult Wistar rats via the drinking water at nominal concentrations of 19.2, 4.8, 1.2., 0.3, 0.075, or 0 ppm for 29 d. Blood was collected after 8, 15, and 29 d of treatment for plasma and erythrocyte cholinesterase determinations, and brain cholinesterase was determined at sacrifice. Body weight, food intake, and water consumption were measured weekly. Body weight gain and water consumption were reduced at 7, 14, 21, and 29 d in male and female rats at 19.2 ppm. Food consumption was reduced in males at 7, 14, 21, and 29 d but was reduced in females only on d 7. Both plasma and erythrocyte cholinesterase activity were reduced after 8, 15, and 29 d in male and female rats at 19.2 ppm. Males at 4.8 ppm showed reductions in plasma activity only after d 8 and in erythrocyte activity only after d 29. Female rats at 19.2 ppm also displayed depressions in brain cholinesterase activity not observed in similarly treated males. Since the only effects noted at 4.8 ppm were reductions in plasma and red blood cell cholinesterase activity in males only and at only one of three sampling periods, these two instances are not believed to be of any biological significance. The data suggest that 4.8 ppm in drinking water is a no observable ill-effect level for exposure of rats to aldicarb residues based on the parameters measured in this study.
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PMID:Aldicarb sulfoxide/aldicarb sulfone mixture in drinking water of rats: effects on growth and acetylcholinesterase activity. 407 30

An automated colorimetric method using the substrate acetylthiocholine was modified to measure red blood cell (RBC) and plasma cholinesterase (ChE) in samples from rhesus monkeys. The kinetic parameters Km and V(max) were calculated for ChE from both sources. Nonenzymatic hydrolysis of acetylthiocholine was uniform and small, and reproducibility of RBC and plasma ChE values was extremely high. Hemolyzing RBC (by freezing, or by using water or a nonionic detergent as diluents) did not affect ChE activity significantly, but hemolysis did increase nonenzymatic activity. The anticoagulants heparin and EDTA had no effect on RBC or plasma ChE measurements.A microdilution technique was devised for RBC ChE measurements using 13 microliters of RBC packed in a standard microhematocrit tube. Reproducibility was quite high, but values using this technique were significantly greater than in duplicate samples assayed using standard techniques. Since plasma ChE activity is much lower than that of RBC, the more efficient extrusion of plasma in RBC samples packed in microhematocrit tubes probably accounted for the higher values. Normal levels of plasma and RBC ChE in adult rhesus monkeys were calculated. There were no significant differences between sexes.
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PMID:An automated method for measuring Rhesus monkey erythrocyte and plasma cholinesterase. 426 94

The latex of Euphorbia royleana which has high molluscicidal and anti-cholinesterase activity against Lymnaea acuminata reduced the levels of 5-hydroxytryptamine (5HT) and dopamine (DA) in the nervous tissue of L. acuminata. There was, however, no significant change in the level of 5-hydroxyindole acetic acid (5HIAA). The changes were found to be dependent on concentration of the latex extract. Similar changes were produced by both water and organic solvent extracts of the latex. The latex of E. royleana thus affects all the known neurotransmission mechanisms in the snail either separately or through a complex interaction between the different neurotransmitters. This may account for its high toxicity to snails.
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PMID:Alteration in biogenic amine levels in the snail Lymnaea acuminata by the latex of Euphorbia royleana. 620 25

An operational-scale trial, using residual fenitrothion, for control of malaria was carried out in Central Java, Indonesia, from 1980 to 1982. Two areas, each comprising about 70 km(2) and a population of about 50 000, were treated with fenitrothion (40% water dispersible powder) at a target dosage of 2 g/m(2) for 3 cycles at 6-monthly intervals. One area was treated with full coverage (i.e., the interiors of houses and cattle shelters were sprayed to a height of 3 m) for 2 cycles, followed by a third cycle with selective coverage (i.e., the interiors of houses were sprayed with one 75 cm horizontal swath between 10 cm and 85 cm from the floor while the cattle shelters were sprayed to a height of 3 m). The other area was treated for 3 cycles with only selective coverage. While both treatment methods reduced malaria rates and vector populations to very low levels, the full coverage treatment was more rapidly effective and also reduced the Plasmodium falciparum index. However, the selective coverage treatment was 68% less expensive than full coverage and greatly reduced the degree of cholinesterase depressions among the spraymen. The trial also showed that a dosage of 1 g/m(2) with full coverage was nearly as effective as the 2 g/m(2) dosage.
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PMID:Malaria control with residual fenitrothion in Central Java, Indonesia: an operational-scale trial using both full and selective coverage treatments. 639 17

Acephate was incubated in distilled water of three different pH's at 37 degrees C for 7 days. Three hydrolytic products were formed: methamidophos, O,S-dimethyl phosphorothiolate (DMPT), and O-methylacetyl phosphoramidothiolate (OMPT). A single dose of acephate was also fed to mice, and their livers were excised and analyzed for metabolic products up to 30 hours. Three products were detected: methamidophos, DMPT, and S-methylacetyl phosphoramidothiolate (SMPT). The anticholinesterase properties of acephate, methamidophos, DMPT, SMPT, and OMPT were determined. Only acephate and methamidophos had measurable inhibitory effects on the mouse erythrocyte enzyme, methamidophos being about ten times more effective than acephate. The amount of methamidophos formed in the water and mouse liver was too low to have any direct effect on the toxicity of acephate. Acephate toxicity to aquatic insects would depend on its persistence in water, its uptake by the insects, its conversion to methamidophos, and the combined inhibitory effect of acephate and methamidophos on the cholinesterase enzyme. The toxicity of acephate to mammals would depend on the direct anticholinesterase effect of the chemical and to a small extent on methamidophos.
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PMID:Hydrolytic and metabolic products of acephate in water and mouse liver. 649 Nov 73

To study the role of acetylcholine metabolism system in the mechanisms responsible for animals' resistance to emotional stress, the activity of acetylcholinesterase (AChE), butyrylcholinesterase and cholinacetyltransferase (CAT) was evaluated in brain structures and autonomous vegetative nervous system of rabbits after experimental emotional stress. In the course of experiments, arterial pressure and heart rate were recorded. The rabbits whose cardiovascular functions appeared to be resistant showed an increase in the activity of AChE and CAT in the perifocal area of the hypothalamus. It is suggested that the involvement of the perifocal area of the hypothalamus in the formation of the mechanisms responsible for the resistance is linked with the effects on water-salt metabolism.
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PMID:[Acetylcholinesterase and choline acetyltransferase in the nervous system of rabbits resistant to emotional stress]. 668 79

Hexamethylene diisocyanate, HDI, a starting material in the production of many polyurethane products, was found to inhibit stoichiometrically mammalian and electric eel cholinesterases in an in vivo system (W. E. Brown, A. H. Green, M. H. Karol, and Y. Alarie , 1982, Toxicol . Appl. Pharmacol. 62, 45-52). The current study examined in vivo effects on guinea pig cholinesterases resulting from inhalation of HDI. Guinea pigs were exposed to atmospheres of 0.5, 1.8, or 4.0 ppm HDI (ceiling value = 0.02 ppm) for up to 6 hr. Blood samples were drawn prior to exposure and at specified times during exposure. No inhibition of serum cholinesterase was detected following exposure to 0.5 ppm HDI for 6 hr, to 1.8 ppm HDI for 2 hr, or to 4.0 ppm HDI for 3 hr. Similarly, no inhibition was detected when erythrocytes from each blood sample were assayed for acetylcholinesterase activity. Last, animals were sacrificed and cholinesterase activity determined in bronchial lavage fluid. Enzyme levels of HDI-exposed animals were not significantly different (P greater than 0.05) from those of control animals exposed to water vapor. In conclusion, although in vitro experiments had demonstrated potent anticholinesterase activity by HDI, in vivo inhalation exposure of guinea pigs to HDI at concentrations 25-200 times above the recommended (ACGIH) ceiling value did not produce measurable inhibition of cholinesterase activity.
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PMID:Effects of inhaled hexamethylene diisocyanate (HDI) on guinea pig cholinesterases. 672

Adult, male rats (300-325 g) were treated with pyridostigmine bromide (n = 22) or saline (n = 22) to quantitate the effects of cholinesterase inhibition (64%) on the ability to work (9.14 m/min, level treadmill) in the heat (35 degrees C). Pyridostigmine-treated rats had a mean endurance of 23 min, whereas saline-treated animals ran for nearly 35 min (P less than 0.001). Rates of rectal and skin temperature increments were significantly higher (P less than 0.001) in pyridostigmine-treated rats as were water losses (P less than 0.001). Exercise in the heat to hyperthermic exhaustion effected anticipated increments in circulating urea nitrogen, creatinine, lactate dehydrogenase, and potassium levels, whereas pyridostigmine pretreatment had additive effects on lactate and creatine kinase concentrations. Additionally, pyridostigmine elicited a significant (P less than 0.01) hyperglycemia before exercise, an effect noted also with other organophosphate simulants. We concluded that pyridostigmine-induced cholinesterase inhibition had a variety of debilitating effects during work in the heat.
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PMID:Effects of pyridostigmine on ability of rats to work in the heat. 672 66


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