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PubMed1985

The effect of storage at different temperatures on cholinesterase activity in human serum.

The effect of storage on the catalytic concentration of cholinesterase and on the reference values of cholinesterase in human serum were studied. When serum was stored at room temperature (20 degrees C), at 4 degrees C and at - 20 degrees C (one year) there was no change in catalytic activity. Even after nine times freezing and thawing (over nine weeks) the catalytic activity was unaffected. The average reference value was significantly higher for males than for females (3.11 +/- 0.57 vs 2.50 +/- 0.43 kU/l).

Acetylthiocholine↗
PubMed1977

Effect of plasma-cholinesterase preparation on the phase II block of succinylcholine chloride in man.

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.

Adult↗
PubMed2006

Influence of body size on swimming performance of four species of neonatal natricine snakes acutely exposed to a cholinesterase-inhibiting pesticide.

Locomotor performance is an important fitness-related trait in reptiles because of its potential influence on prey capture and predator avoidance. Because cholinesterase-inhibiting pesticides disrupt neuromuscular signaling, reduction in performance seems to be a logical translation of this biochemical disruption to the organism level. In the present study, we compared the swimming performance of four species of natricine snakes acutely exposed to a formulation of carbaryl to determine whether neonatal body size or skin permeability influences responsiveness. Exposure to high concentrations of carbaryl (2.5-5.0 mg/L) resulted in reduced swimming performance in all four species of snakes, and species responded similarly to the pesticide once body size was accounted for allometrically. Using traditional methods in physiological ecology to estimate skin permeability (a parameter that influences the dose of contaminant absorbed), we found that water flux across the integument also scaled allometrically with body surface area and, therefore, was similar among species after controlling for this relationship. We suggest that future studies examining the effects of repeated low-dose exposure to cholinesterase inhibitors on performance parameters will be useful in assessing the ecological significance of our findings.

Animals↗
PubMed2003

Pharmacoeconomics of cholinesterase inhibitors in the treatment of Alzheimer's disease.

Cholinesterase inhibitors constitute one of few treatment options available for Alzheimer's disease, the most common cause of dementia. The modest effects and relatively high acquisition costs of these drugs make the health economics of dementia an important subject of study. Simulation models can be used to bring together existing data and make predictions of the long-term cost effectiveness of treatment. Most models have been built around cognitive function as a key parameter based on the observed relationship between cognitive function and costs of care. Patients with more severe disease attain higher total costs of care. Also, these patients have a higher share of formal care costs than do patients with mild disease, who are usually looked after by informal caregivers. The valuation of unpaid care is controversial, and the choice of method may affect results considerably. Another important issue is the measurement of health-related QOL in patients with Alzheimer's disease. The few existing studies have used proxy respondents to elicit utility weights in different disease states; however, this methodology has not been validated. It is likely that the increased drug costs incurred by the use of cholinesterase inhibitors will be offset (at least partly) by savings in other healthcare costs. However, these results should be viewed as preliminary, since we are still awaiting data from long-term follow-up studies. Also, the value of treatment for patients and caregivers in terms of QOL improvements has yet to be established.

Alzheimer Disease↗
PubMed2004

Cholinesterase inhibitors and vascular dementia: another string to their bow?

Two of the four licensed cholinesterase inhibitors, galantamine and donepezil, have recently featured in published work showing how they act in dementia associated with cerebrovascular disease (CVD). It is timely to review this new evidence and place it within the current consensus understanding of what makes up a clearly heterogeneous dementia population. To do this, the current review explores the relationship between Alzheimer's disease, for which this group of compounds originally received licensing approval, and vascular pathology within the brain, highlighting the significant overlap in risk factors and the frequent coexistence of the two conditions in the patients that are studied. Whether they are inter-related or separate entities is discussed, followed by a description of the current classifications of Alzheimer's disease with CVD, and the three subtypes of 'pure' vascular dementia - subcortical, cortical and strategic infarct. Understanding these entities allows more accurate diagnostic and prognostic information to be given to patients, and leads towards matching the published clinical evidence discussed with more predictable clinical syndromes. This distinction is particularly relevant in terms of the studies conducted thus far. Galantamine has been studied in a placebo-controlled study of patients with Alzheimer's disease and CVD as well as patients with vascular dementia, whereas donepezil was studied exclusively in patients with vascular dementia. Differences in the way the placebo groups acted in these studies confirmed the fact that these actually are two distinct groups. Galantamine showed efficacy across the combined groups studied, with placebo deterioration similar to previous Alzheimer's disease studies, while donepezil produced a positive effect in vascular dementia - with this placebo group relatively unchanged. The symptomatic improvements seen were not really surprising, as cholinergic deficits are a common factor across all of these syndromes. Wherever this is the predominant biological finding, it would be expected that cholinesterase inhibitors would have a similar effect, whatever the condition causing it.

Alzheimer Disease↗
PubMed2006

Cholinesterase inhibitors slow decline in executive functions, rather than memory, in Alzheimer's disease: a 1-year observational study in the Sunnybrook dementia cohort.

To determine if there are differential treatment effects of second-generation cholinesterase inhibitors over one year, 130 patients (untreated=65, treated=65) meeting NINCDS-ADRDA criteria for mild or moderate probable AD underwent standardized cognitive testing at baseline and 12 months later at a university memory clinic. Patients were followed either prior to or after the availability of treatment and were matched on education and baseline Mini Mental State Examination (MMSE). A detailed medical history evaluation was conducted. In this well matched longitudinal observational cohort study, there were no differences in the prevalence of comorbid illnesses, concomitant medication use or vascular risk factors except for a greater number of treated patients with a previous history of smoking. Separate repeated measures MANCOVAs on the MMSE, Mattis Dementia Rating Scale (DRS), and its 5 subscores (attention, initiation/perseveration, conceptualization, construction and memory) (Bonferroni corrected), after covarying for the effects of smoking, and SSRI use, showed less decline over one year in the treated group in overall cognition and in all subscores of the DRS except for memory (effect sizes 0.5-0.7). Less decline was also seen in the treated group in function and in instrumental and basic activities of daily living as measured with the Disability Assessment for Dementia Scale (DAD) (effect sizes 0.4-0.8). Executive, language and visuospatial functions, rather than memory, appeared to be more amenable to stabilization over one year by cholinesterase inhibitors in AD.

Aged↗
PubMed1983

Cholinesterase activity of seminal plasma and human spermatozoa in normal and infertile subjects.

Cholinesterase activity was determined in seminal plasma and human spermatozoa from 23 fertile volunteer subjects (N), 23 asthenospermic patients (A), and 25 oligoasthenospermic patients (OA). Cholinesterase activity determined in human seminal plasma for group N was 0.227 +/- 0.023 U/ml; for group A, 0.232 +/- 0.016 U/ml; and for group OA, 0.205 +/- 0.027 U/ml. The differences were not statistically significant. Sperm enzymatic activity in group N was 0.048 +/- 0.008 U per million sperms; in group A, 0.072 +/- 0.019 U per million sperms; and in group OA, 0.135 +/- 0.044 U per million sperms. These differences were not statistically significant.

Adult↗
PubMed2001

Hematological, protein electrophoresis and cholinesterase values of free-living nestling peregrine falcons in Spain.

Protein electrophoresis, hematological and cholinesterase values were determined in 32 nestling free-living peregrine falcons (Falco peregrinus) (15- to 27-days-old) in order to establish normal reference values for this population. The following values (mean +/- SD) were observed: prealbumin 0.31 +/- 0.04 g/dl, albumin 1.25 +/- 0.06 g/dl, alpha1 and alpha2-globulin 0.23 +/- 0.02 and 0.16 +/- 0.02 g/dl respectively, beta-globulin 1.02 +/- 0.05 g/dl, gamma-globulin 0.060 +/- 0.08 g/dl, total protein 3.79 +/- 0.18 g/dl, 21.26 +/- 1.30 white blood cells/microl (1 x 10(3)), 2.17 +/- 0.07 red blood cells/microl (1 x 10(6)), packed cell volume 37.58 +/- 0.82%, hemoglobin 20.96 +/- 0.29 g/dl, heterophils 61.14 +/- 2.50% and cholinesterase 1,184 +/- 75 IU/L. There were no difference in any of these parameters among males and females. The hematological values obtained could be considered as representative values in free-living nestling peregrine falcons.

Albumins↗
PubMed1976

[Bioptical diagnostics of hirschsprung disease by the membrane technique for the histochemical demonstration of cholinesterases (author's transl)].

50 biopsies of the rectum and 8 of the large intestine from male and female children aged 4 months to 7 years, obtained by resection were investigated. The absence of ganglion cells in the intrinsic nerve plexuses is in agreement with the increased cholinesterases reaction. The presence of muscularis mucosae is necessary in the biopsy for the evaluation of the cholinesterase reaction. The instrument used for the excision must fulfill those demands.

Biopsy↗
PubMed1998

Effects of synthetic (-)-huperzine A on cholinesterase activities and mouse water maze performance.

AIM: To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance. METHODS: Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect. RESULTS: The IC50 of synthetic Hup A for acetylcholinesterase (AChE) of rat cortex and rat erythrocyte membrane determined in vitro were 64.7 (52.6-79.5) and 53.9 (43.6-66.6) nmol.L-1, respectively, and for butyrylcholinesterase of rat serum was 53.6 (44.9-63.8) mumol.L-1. Synthetic Hup A 0.12-0.48 mg.kg-1 ig produced a dose-dependent inhibition of brain AChE in mice. Synthetic Hup A 0.05 mg.kg-1 ig attenuated scopolamine-induced impairment of spatial memory. The efficacy of synthetic Hup A was the same as natural Hup A. CONCLUSION: Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A.

Acetylcholinesterase↗
PubMed1975

Survey of local anesthetic toxicity in the families of patients with atypical plasma cholinesterase.

There have been reports of toxic reactions to ester-type local anesthetics in patients with genetic anomalies of plasma cholinesterase in so-called dibucaine-resistant homozygotes or heterozygotes. Because of these reports, 23 patients with prolonged apnea after administration of succinylcholine were studied with Kalow's method for abnormal dibucaine number (DN), which characterizes this condition, and for the history of local anesthetic toxicity. Thirty-eight relatives of abnormal individuals were studied in the same manner. Two atypical dibucaine-resistant homozygotes and the relative of one of these had toxic reactions to ester-type local anesthetics. Although low doses of ester-type local anesthetics may be tolerated by atypical homozygotes, these agents are best avoided and amide-type local anesthetics or tetracaine, which is hydrolyzed at a normal rate, should be used. Individuals with atypical plasma cholinesterase should wear a Medic-Alert bracelet or amulet so that complications and fatalities can be avoided.

Anesthetics, Local↗
PubMed1975

Cholinesterase in embryonic development.

I. Cholinesterase (ChE) activity was studied histochemically during early development of the sea urchin, the amphibian, the chick and the rat embryo. After formalin fixation and embedding in water-soluble carbowax, the enzyme reaction was carried out in serial section. 2. Independent from innervation ChE appears in every embryonic blastema in a very early stage of development. It disappears from the embryonic cells after they have assembled into definite organ structures. Thus, ChE plays a role in embryonic development which is different from its known function in the adult. Therefore, ChE activity present in differentiating cells during a limited phase of development, is termed "embryonic cholinesterase". 3. Embryonic ChE was invariably found in cells engaged in morphogenetic movements. This observation has led us to suppose that the enzyme in involved in the regulation of cellular movements during development. 4. In particular, embryonic ChE is described in the following locations: a) During sea urchin gastrulation ChE is present in the primary mesenchymal cells emigrating from the blastula wall and in the archenteron cells which are known to bring about the invagination movement by contraction of their pseudopods. b) In the early chick blastoderm ChE active "droplet cells" are described which are supposed to emigrate from the epiblast layer in order to form the hypoblast. c) During development of notochord and somites, during closure of the neural tube and development of the head anlage, the close correlation of ChE activity with various morphogenetic movements is demonstrated: ChE appears during aggregation and desaggregation of epithelial compounds. The active bending of preexisting epithelial sheets, such as the neural plate, is also accompanied by ChE activity in epithelial cells...

Acetylcholinesterase↗
PubMed2001

[Cholinesterases and their importance in the etiology, diagnosis and therapy of Alzheimer's disease].

Cholinesterases belong to esterases and represent important animal enzymes with multiple biological function. Acetylcholinesterase (AChE) plays the key role in cholinergic neurotransmission, whereas the function of butyrylcholinesterase (BuChE) is still unrevealed. Both enzymes seem to act as neurogenic factors during the early embryogenesis and later on they may participate in some pathological alteration. In humans, these degenerative changes are related to the deposition of pathologic proteins in the brain and with the progress of the Alzheimer's dementia (AD). Both AChE) and BuChE become recently the target for the most frequently used therapy of AD--cholinesterase inhibitors.

Acetylcholinesterase↗
PubMedDate not supplied

[Blood cholinesterase in rats with experimental thyrotoxicosis and hypothyroidism].

Changes in the sum total activity of cholinesterase of the plasma and erythrocytes (AC substrate) and also separately of acetyl- and pseudocholinesterase (MeC and ByC substrates) were studied in experiments on rats with thyrotoxin toxicosis and 6-methylthiouracil hypothyroidism. The sum total activity of cholinesterase proved to increase in the erythrocytes of rats with thyrotoxicosis and fell in the erythrocytes and plasma of animals with hypothyroidism. The activity of acetylcholinesterase of erythrocytes and plasma increased in thyrotoxicosis and decreased in hypothyroidism. The activity of pseudocholinesterase of erythrocytes and plasma decreased in thyrotoxicosis and showed no significant difference in hypothyroidism.

Acetylcholinesterase↗
PubMed2001

Interlaboratory study into the proficiency of serum cholinesterase activity measurement.

The measurement of cholinesterase activity is an important function of a clinical laboratory. Participation in appropriate quality assurance schemes is essential in ensuring a high analytical standard. Samples of human serum were distributed to thirty-five laboratories for the measurement of cholinesterase activity. Because of methodological differences between the participants, findings of each laboratory were compared either by the use of duplicate samples or by analysis of six mixtures of two samples, one having a high and one a low activity. Of 4,964 distributed samples 95% were analysed and findings reported in 596 reports. Thirty-four percent of all reports were considered very good (less than 5% within-run error) and 38% less than satisfactory (within-run error over 10%). Access to a proficiency programme such as this enables laboratories to evaluate the quality of their analytical service.

Cholinesterases↗
PubMed1975

[Effect of reversible inhibitors on the thermal denaturation of cholinesterases].

The capacity of reversible inhibitors--galanthamine and tacrine--to protect the cholinesterase of rat and mouse brain from the thermal denaturation with the action of the temperature of 56 and 58 degrees C was revealed. The protective action was also noted when the reversible inhibitors decreased the activity of the enzyme. It appeared that with galanthamine the cholinesterase resistance to the thermal action was greater than with the action of tacrine.

Acridines↗
PubMedDate not supplied

[Effect of alcohols on the rate of cholinesterase decarbamoylation].

Butanol-1 and butandiol-1,4 are shown to increase the decarbamoylation rate of N-methylcarbamoyl- and N,N-dimethylcarbamoyl-cholinesterase. It is mainly due to the formation of a ternary complex NEA which is decomposed in 2,5 times faster than corbamoyl-enzyme EA. This is an evidence for the presence of some allosteric center in cholinesterase which is capable of binding alcohols.

Alcohols↗