Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Measurement of blood cholinesterase activity and of the urinary metabolites of fenitrothion (p-nitrocresol) and malathion (monocarboxylic acid) was used to assess the exposure to these insecticides of workers in the Haitian malaria control programme and of residents in the sprayed houses. Cholinesterase activity was significantly reduced at the end of the working week in 3 out of 28 fenitrothion workers. Urinary levels of p-nitrocresol (PNC) in the spraymen ranged from 2.2 to 25.2 mg/l. In fenitrothion workers who had no direct contact with spraying (weighers and supervisors), the cholinesterase activity remained >/= 75% of the normal control value, and the urinary PNC levels were relatively low. Urinary malathion monocarboxylic acid (MCA) levels at the end of the working week ranged between 1.1 and 5.3 mg/l in workers using malathion and their blood cholinesterase activity remained essentially normal. In both groups of workers the cholinesterase levels improved and the urinary excretion of metabolites decreased after 2 days of rest from the spraying operations. In the residents of the sprayed houses, low concentrations of PNC and MCA were detected in the urine 1 day after spraying and measurable but reduced levels were still present after 7 days. In all these cases the cholinesterase activity remained >/= 75% of the normal control value.
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PMID:Assessment of exposure to organophosphate insecticides during spraying in Haiti: monitoring of urinary metabolites and blood cholinesterase levels. 387 16

Cholinesterase activity have been estimated in rectal biopsies of 19 children with Hirschsprung's disease and 80 normal children. A high level of acetyl-cholinesterase is a strong argument for the diagnosis of aganglionosis. However the ratio acetylcholinesterase over butyrylcholinesterase seems to be a better sign allowing a right diagnosis in 99% of the cases.
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PMID:[Value of the assay of cholinesterase activity in superficial biopsies of the rectum in the diagnosis of Hirschsprung's disease]. 388 81

Serum cholinesterase activity decreases 30% during pregnancy and remains depressed during the postpartum period. However, succinylcholine recovery is not prolonged in term-pregnant patients. This contrasts with results obtained in other patients with decreased serum cholinesterase activity. To better understand this paradox, the authors compared serum cholinesterase activity and recovery from succinylcholine, 1 mg/kg, in nonpregnant (with and without oral contraceptive use), in term-pregnant, and in postpartum patients. Serum cholinesterase activity was lower in both term-pregnant (3.66 +/- 0.39 U/ml, means +/- SE) and postpartum (2.84 +/- 0.35 U/ml) patients than in nonpregnant patients not taking oral contraceptives (5.01 +/- 0.33 U/ml, P less than 0.05). Cholinesterase activity in postpartum patients also was significantly lower than in nonpregnant patients taking oral contraceptives (4.81 +/- 0.63, P less than 0.05). In contrast, the time to 25% twitch-height recovery did not differ between term-pregnant (470 +/- 56 s) and nonpregnant patients taking (499 +/- 29 s) or not taking (501 +/- 21 s) oral contraceptives, but was significantly increased in postpartum patients (685 +/- 22 s, P less than 0.001). The similar duration of action of succinylcholine in term-pregnant patients (with decreased serum cholinesterase activities) and nonpregnant patients may be related to the increased volume of distribution of succinylcholine at term.
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PMID:Succinylcholine pharmacodynamics in peripartum patients. 394 7

In order to determine whether a structural modification at the active center of cholinesterase may alter the conformational stability of the enzyme we compared the urea-induced unfolding of the tetrameric form of non-inhibited and irreversibly inhibited human plasma cholinesterase (acylcholine acylhydrolase, EC 3.1.1.8). We studied enzyme inhibited by methanesulfonyl fluoride, diisopropylfluorophosphonate (DFP) and racemic soman. DFP- and soman-inhibited cholinesterases are converted spontaneously into non-reactivable forms called 'aged' enzymes through a process involving dealkylation of the bound organophosphate residue. The unfolding was followed by transverse urea-gradient polyacrylamide electrophoresis at various temperatures ranging from 0 to 60 degrees C. Unfolding of cholinesterase appears to be a complex process. The denaturation patterns showed that partially unfolded states are thermodynamically unstable, but that several intermediates are involved; the lifetime of these depends on the temperature at which electrophoreses are carried out. Cholinesterase inhibited by methanesulfonyl fluoride behaved like the non-inhibited enzyme. On the other hand, small but significant differences in stability between non-inhibited and aged enzymes were observed. Whatever the temperature, the urea concentration at the mid-point of transition was always greater for aged enzyme than for the non-inhibited enzyme. In addition, aged enzymes showed more complex denaturation patterns at the lower temperatures (under 20 degrees C). These findings suggest that the overall stability of aged-cholinesterases is slightly increased as compared with the stability of non-inhibited or methanesulfonyl fluoride-inhibited enzymes. The denaturation pattern obtained at 0 degree C for soman-inhibited cholinesterase under non-aging conditions (inhibition at 0 degree C, pH 10.7) was similar to that of non-inhibited enzyme at this temperature, although splitting in two of the denaturation curve over the transition zone reflects the heterogeneity of soman-inhibited enzyme. The slight difference in denaturation behavior between these species may be due to stereoisomerism in soman. The differences in electrophoretic behavior and apparent stability observed between non-inhibited and aged enzymes were interpreted as the result of a conformational change induced by the dealkylation reaction of enzyme-inhibitor conjugates.
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PMID:Evidence that the conformational stability of 'aged' organophosphate-inhibited cholinesterase is altered. 394 40

The disposition of [3H]diisopropylfluorophosphate (DFP) and its metabolites was studied in mice after iv treatment. In addition, disposition of [3H]DFP in selected tissues was correlated with cholinesterase activity and spontaneous activity following DFP treatment. Within 1 min of administration [3H]DFP had penetrated tissues and was already irreversibly bound. The tissue concentrations of [3H]DFP declined in a rapid fashion so that after 2 hr all concentrations were below 50 pg/mg tissue. The major portion of radioactivity was bound to tissue in the form of [3H]diisopropylphosphoric acid (DIP). There was a decline in [3H]DIP with time in all tissues except liver, kidneys, and fat, which reached a maximum at 30 min before declining. The only appreciable quantities of [3H]DIP remaining after 3 days were in liver and kidneys. There was also evidence that [3H]DFP was rapidly hydrolyzed to free [3H]DIP which was found in all tissues within 1 min of [3H]DFP administration. [3H]DIP concentrations were equivalent to or exceeded those of [3H]DFP in all tissues, except brain. Cholinesterase inhibition in plasma, diaphragm, and brain following DFP treatment (1 mg/kg, iv) was temporarily correlated with the concentrations of bound [3H]DIP in these same tissues between 1 hr and 3 days. Cholinesterase inhibition in brain and diaphragm did not correlate well with bound [3H]DIP at earlier time points which suggested the presence of noncholinesterase binding. DFP treatment (1 mg/kg) also induced motor hypoactivity which lasted up to 6 hr after iv injection. The time course of motor hypoactivity was not correlated with free [3H]DFP, bound [3H]DIP concentrations in the brain, or with cholinesterase inhibition in the brain, which suggested that noncholinesterase bound [3H]DIP was responsible for this CNS depression.
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PMID:Biodisposition of [3H]diisopropylfluorophosphate in mice. 397

Pregnant CD-1 mice were exposed to 2.45-GHz continuous wave microwave radiation at an incident power density of 30 mW/cm2. The local specific absorption rate near the uterine area (deep colonic location), as determined from time-temperature profiles measured with a Vitek thermistor probe, was 40.2 mW/g. Groups of mice were exposed 8 hr per day through Days 1-6 or 6-15 of pregnancy. Other groups of animals were exposed to an elevated ambient temperature of 31 degrees C which increased the colonic temperature 2.3 degrees C, the same as that produced by the microwaves. Sham-irradiated groups of animals were treated exactly the same as the microwave-exposed animals. For the two conditions, temperature exposed and sham exposed, two groups of animals were used. One group was handled in the same manner as the microwave-irradiated group and the other group was not handled so as to evaluate the effects of stressing the animals by handling. Eleven groups of animals were used in the complete study: five groups for gestational Days 1-6, five groups for gestational Days 6-15, and one group of cage control animals. On Day 18 of gestation the dams of all experimental groups were sacrificed and their reproductive status was determined. The fetuses were examined for visceral and skeletal alterations. Brain cholinesterase activity and histology were evaluated in the groups exposed on Days 6-15. The results show that microwave radiation increases embryo lethality at the early stages of gestation (exposure Days 1-6). Fetal toxicity and teratogenicity were not significantly increased by exposure to microwaves on either Days 1-6 or 6-15 of gestation. Cholinesterase activity and histology of the brain of 18-day-old fetuses were not adversely affected.
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PMID:Teratogenic, biochemical, and histological studies with mice prenatally exposed to 2.45-GHz microwave radiation. 398 69

Cholinesterase activity in single nerve cell bodies isolated from the locus ceruleus and nucleus of the facial nerve of the rat was analyzed by the microgasometric method. Acetylcholinesterase activity is about the same in both types of cells. Nonspecific cholinesterase is present in noradrenergic cells of the locus ceruleus but not in the cholinergic cells of the nucleus of the facial nerve. The total activity of cholinesterases and the activity of acetylcholinesterase in nerve cell bodies isolated from the locus ceruleus remains practically unchanged from the tenth postnatal day until the age of 24 months. Depletion of noradrenaline by a high dose of reserpine does not influence the total activity of cholinesterases in nerve cell bodies of locus ceruleus.
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PMID:Cholinesterases in single nerve cells isolated from the locus ceruleus and from nucleus of the facial nerve of the rat: a microgasometric study. 399 29

Cholinesterase activity was detected by histochemical methods in normal human blood smears. In erythrocytes, acetylcholinesterase was found to be localized in the cortical region of the cells and, to a lesser degree, in the inner cytoplasm. In leucocytes, cholinesterase activity was found around the nuclear membrane and in the cytoplasm. The specificity of the enzymic activity was ascertained by using selective inhibitors.
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PMID:Histochemical localization of acetylcholinesterase in blood cells. 402 79

The distribution of acetylcholinesterase (AChE) and pseudocholinesterase (BuChE) activities was studied by histochemical, quantitative and electrophoretical methods during the early development of chick limbs, from stage 16 to stage 32 H.H. (Hamburger & Hamilton, 1951). By quantitative methods, true AChE activity was found, and increased about threefold during the developmental period, together with a smaller amount of BuChE which increased more rapidly in comparison with the AChE activity from stage 25 to 32 H.H. Cholinesterase activity was histochemically localized mainly in interacting tissues, such as the ectoderm (including the apical ectodermal ridge) and the underlying mesenchyme. True AChE was histochemically localized around the nuclei and on the plasma membrane of ectodermal (including AER) and mesenchymal cells, and at the plasma membrane of mesenchymal cell processes reaching the basal lamina between the ectoderm and the mesenchyme. AChE together with BuChE activity was found in the basal lamina between the ectoderm and the mesenchyme, in underlying mesenchymal cells and in deeper mesenchymal cells, especially during their transformation into unexpressed chondrocytes. During limb morphogenesis, the cellular and regional localization of the enzyme activities showed variations depending on the stage of development and on the occurrence of interactions. The possibility of morphogenetic functions of the enzyme id discussed.
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PMID:Acetylcholinesterase (AChE) and pseudocholinesterase (BuChE) activity distribution pattern in early developing chick limbs. 403 48

The biodisposition of [3H]diisopropylfluorophosphate (DFP) and its metabolites was studied in mice after inhalation administration. In addition, the time course of DFP-induced cholinesterase inhibition in selected tissues, hypothermia, and motor coordination were studied to determine a possible correlation with [3H]DFP, or its metabolites. The time course of tissue concentrations of [3H]DFP showed that [3H]DFP rapidly penetrated all tissues and was quickly hydrolyzed to [3H]diisopropylphosphoric acid (free [3H]DIP) or was covalently bound to tissue (bound [3H]DIP). By 1 hr, the greater portion of the radioactivity was in the form of bound [3H]DIP. Cholinesterase inhibition in brain, lung, diaphragm, and plasma was temporally related to concentrations of bound [3H]DIP between 5 min and 1 day, except at early time points for the lung. Motor incoordination (rotarod test) produced by DFP exposure had a rapid onset, with complete recovery by 10 hr. DFP-induced hypothermia (rectal temperature) had a very similar time-course profile to that of motor incoordination. The time course of hypothermia and motor incoordination was correlated with neither free [3H]DFP nor bound [3H]DIP concentrations in the brain, nor with cholinesterase inhibition in brain. These findings suggest that non-cholinesterase bound [3H]DIP may contribute to the depression of these centrally mediated effects.
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PMID:Relationship between the pharmacological effects and the biodisposition of [3H]diisopropylfluorophosphate in mice after inhalation. 403 91


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