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)

The Dutch aquatic environment was monitored from September 1969 to December 1975 for organochlorine pesticides and their metabolites, cholinesterase inhibitors, and aromatic amines. The 1,492 samples analyzed included surface water, rainwater, groundwater, and drinking water. The highest concentrations of hexachlorobenzene (HCB) and alpha- and beta-benzene hexachloride (BHC) were found in the Rhine River and its tributaries. Concentrations of the compounds in the Dutch part of the Rhine River decreased downstream. Other organochlorine pesticides and their metabolites, heptachlor, heptachlor epoxide, aldrin, dieldrin, endrin alpha- and beta-endosulfan, and sigmaDDT were detected occasionally, but only in low concentrations. Cholinesterase inhibitors and aromatic amines were always present in the Rhine River and its tributaries.
Pestic Monit J 1978 Dec
PMID:Organochlorines, cholinesterase inhibitors, and aromatic amines in Dutch water samples, September 1969--December 1975. 74 May 17

Rapid and reliable measurement of acetylcholinesterase (AChE) activity is of crucial importance to the pharmacodynamic monitoring of anticholinesterase drugs. A new assay has been developed to measure AChE from 10 microliter samples of capillary blood. AChE activity was calculated from the change in pH of the reaction medium caused by the hydrolysis of acetylcholine and measured with a highly sensitive differential pH apparatus (CL-10, Eurochem, Rome, Italy). Interference by butyrylcholinesterase was eliminated by a specific inhibitor, quinidine sulfate. The assay lasts 1 min. The coefficient of variation (CV) for replicated measurements was 2.8% (3267 U/L, n = 33). Linearity ranged from 0 to 10,000 U/L. The correlation coefficient between the new technique and Ellman's colorimetric method on washed erythrocytes was r = 0.987 (y = 1.299x - 63, n = 29). The correlation coefficient between assays on capillary and venous samples was r = 0.979 (y = 0.974x + 174, n = 47). A cross-laboratory validation study was performed in 10 centers using glycerol-stabilized hemolysates with normal and reduced AChE activity. Samples were assayed in triplicate. The within- and between-laboratory CVs for samples with normal AChE activity (6,018 U/L) were 2.2 and 8.1%, respectively. The new method was applied to a double-blind, placebo-controlled multicenter study of eptastigmine in Alzheimer patients and proved to be a simple, noninvasive, rapid, and reliable method for pharmacodynamic monitoring of this drug.
Ther Drug Monit 1995 Jun
PMID:A patient-side technique for real-time measurement of acetylcholinesterase activity during monitoring of eptastigmine treatment. 762 18

The objective of this prospective study was to assess the prognostic value of dynamic and static liver function tests and clinical symptoms in pediatric patients with chronic end-stage liver disease in a serial examination including three evaluations at 3-month intervals. Of the 24 patients entering the study, six were given transplants within the observation period of 10 months. Of the remaining 18 patients who were considered in the final evaluation, five died before transplantation was possible. The variables included in the analysis were monoethylglycinexylidide (MEGX) formation from lidocaine, bilirubin, albumin, and creatinine serum concentrations, catalytic serum concentration of cholinesterase (CHE), prothrombin time (PT), factors II and V, serum amino acids, body weight, and presence of ascites. In nonsurvivors (n = 5), MEGX serum concentrations 30 min after intravenous administration of lidocaine (1 mg/kg body weight) were < 10 micrograms/L at the first examination. Statistically significant differences between nonsurvivors and survivors were observed for initial MEGX test results (p = 0.0089) and serum bilirubin concentrations (p = 0.009), as well as for the last available MEGX and bilirubin data from each patient (p = 0.017 and 0.016, respectively). At a diagnostic sensitivity of 100%, the corresponding diagnostic specificities for MEGX and bilirubin from the first examination were 77 and 62%, respectively. These data show that consistently low MEGX test results < 10 micrograms/L, obtained 30 min after intravenous administration of lidocaine (1 mg/kg body weight), are a prognostically unfavorable sign in pediatric transplant candidates.
Ther Drug Monit 1996 Aug
PMID:Prognostic value of the monoethylglycinexylidide test in pediatric liver transplant candidates. 885 54

Quinidine (QUINID) substantially inhibited the serum degradation of cocaethylene (CE), an important cocaine analog, when incubated for two hours at 37 degrees C with pooled human serum containing 1.58 micromol/L of CE. In the absence of QUINID, the CE concentration was only 49.4% of its original value after incubation. However, QUINID at subtherapeutic (3.08 micromol/L) and therapeutic (15.4 micromol/L) concentrations preserved 55.1% and 75.9% of the original CE concentration, respectively. At a QUINID concentration of 308 micromol/L, 89.2% of the CE concentration was preserved. There was a marked decrease in the serum cholinesterase (CHE) activity as QUINID concentrations were increased to 154 micromol/L (19.8% decrease in CHE) and to 308 micromol/L (36.8% decrease in CHE). These data suggest that QUINID inhibits the hydrolysis of CE in human serum by suppressing CHE activity. These findings are significant because QUINID may be used in patients who have abused cocaine with ethanol. They also have important implications for individuals receiving QUINID together with other drugs whose hydrolysis may be catalyzed by CHE.
Ther Drug Monit 1999 Jun
PMID:Quinidine inhibition of cocaethylene degradation in human serum in vitro: a preliminary study. 1036 41

The aim of this study was to assess the influence of renal function on the pharmacokinetics, pharmacodynamics, safety, and tolerability of the acetylcholinesterase inhibitor metrifonate. Four groups of six age- and gender-matched subjects with varying degrees of renal function (creatinine clearances more than 90, 60-90, 30-60, and less than 30 mL/min/ 1.73 m2, respectively) were administered a single 50-mg oral dose of metrifonate. Blood and urine samples were collected for 24 hours and concentrations of metrifonate and its metabolites dichlorvos, dichloroacetic acid, and M3 were determined. Inhibition of acetylcholinesterase activity in erythrocytes and butyrylcholinesterase in plasma were also measured. Metrifonate was well tolerated in all treatment groups. The urinary excretion of metrifonate and dichlorvos decreased with decreasing renal function but accounted for less than 2% of the elimination. There were no statistically significant differences in primary pharmacokinetic parameters--Cmax, t(max), area under the concentration-time curve (AUC), and t1/2--of metrifonate and dichlorvos among the different groups. The excretion of dichloroacetic acid and M3 was not influenced by renal impairment. Acetylcholinesterase was not inhibited, whereas butyrylcholinesterase was inhibited markedly but independently of renal function. No metrifonate dose adjustments are needed when treating subjects with renal impairment.
Ther Drug Monit 1999 Jun
PMID:Pharmacokinetics and pharmacodynamics of the acetylcholinesterase inhibitor metrifonate in patients with renal impairment. 1036 43

The effect of lovastatin and thioridazine on the degradation of cocaine in human serum was studied by incubating therapeutic and toxic concentrations of either drug with cocaine in human serum at 37 degrees C. Without these other drugs, cocaine concentrations decreased by an average of 88% in 120 minutes. Lovastatin at all concentrations studied showed a negligible effect on the degradation of cocaine in human serum and did not alter the pseudocholinesterase activity of the serum. In contrast, in the presence of a therapeutic concentration of thioridazine, cocaine concentrations decreased by only 71% during this period of time, and, with a toxic concentration of thioridazine, cocaine concentrations decreased by only 55%. Thioridazine suppressed the pseudocholinesterase activity of human serum by up to 19% during the 120-minute incubation period, and this effect was more pronounced at higher thioridazine concentrations. These findings suggest that thioridazine may prolong the serum half-life of cocaine by inhibiting the pseudocholinesterase-mediated catabolism of cocaine to ecgonine methyl ester. This may be important in cocaine users who are treated with phenothiazines and other structurally similar drugs. They also may be of interest in cocaine-abusing patients who are treated with phenothiazines for schizophrenic disorders.
Ther Drug Monit 2005 Apr
PMID:The effect of lovastatin and thioridazine on the degradation of cocaine in human serum in vitro. 1579 47

Activities of glutathione S-transferases (GST) and cholinesterase (ChE) from Paracentrotus lividus were investigated as possible biomarkers of environmental contamination in the coastal zone. In the first phase of the study, the activity of both enzymes was determined in various tissues in order to select the most appropriate ones to be used in the following assays. In the second phase, the ChEs present in ambulacra were characterized using different substrates and selective inhibitors. In the next phase, laboratory bioassays were performed with dilutions of water-accommodated fraction of #4 fuel-oil (WAF) and benzo[a]pyrene (BaP) to determine the response of those enzymes to these pollutants and, finally, the activity of both enzymes was determined during a year in indigenous specimens from six sites on the Northwest coast of Portugal, with different pollution levels, to determine basal values and seasonal variations of ChE and GST activities. Among the several tissues tested, ambulacra and the anterior portion of the intestine were selected for ChE and GST assays, respectively. The determination of ChE in ambulacra tissue may be performed in a non-destructive way. Ambulacra ChE hydrolysed acetylthiocholine preferentially to propionylthiocholine and butyrylthiocholine and, inhibition by excess of substrate was observed. Enzymatic activity was almost fully inhibited by eserine sulfate (>98%) at concentrations equal or higher than 6.25 microM. Sensitivity to both BW284C51 (reaching 98% at 200 microM) and iso-OMPA (73% at 8 mM) was found. In laboratory bioassays, GSTs activity was inhibited by WAF and induced by BaP, whereas ChE activity was not affected by any of these environmental contaminants. Seasonal variations in enzymatic activities were found. For example, in a reference site, ChE values changed from 52.2 +/- 9.3 U mg(-1) protein in autumn to 71.8 +/- 13.3 U mg(-1) protein in spring, while GST activity changed from 129.9 +/- 29.8 U mg(-1) protein in winter to 279.0 +/- 48.0 U mg(-1) protein in autumn. Sea-urchins from reference sites presented significantly higher values of both ChE and GST than animals from contaminated sites in all seasons. In conclusion, the results of this study indicate that (i) ambulacra and the anterior portion of intestine are the most suitable tissues to measure ChE and GST activities, respectively; (ii) only one form of ChE seems to be present in ambulacra, showing properties of both typical acetylcholinesterase (AChE) and pseudocholinesterase (PChE); (iii)P. lividus GST is sensitive to both WAF and BaP even after acute exposures while ChE is not, and (iv) in spite of the significant seasonal variations observed in both enzymes in the field, P. lividus ChE and GST were capable of discriminate sites with different contamination levels and, thus, they are suitable for use as biomarkers in biomonitoring studies in the coastal zone.
J Environ Monit 2005 Apr
PMID:Sea-urchin (Paracentrotus lividus) glutathione S-transferases and cholinesterase activities as biomarkers of environmental contamination. 1579 94

Dosage regimes of aminoglycosides and vancomycin are modified according to the glomerular filtration rate (GFR). In 130 hospitalized patients who were administered amikacin, gentamicin, tobramycin, and vancomycin by intermittent intravenous infusion, we compared the predicted GFR values from the serum concentrations of creatinine (Cockcroft and Gault. Nephron. 1976;16:31-41) and cystatin C (Larsson et al. Scand J Clin Lab Invest. 2004;64:25-30) with respect to their relevance for proper dosage. In 83% and 67% of the cases, respectively, the serum levels of albumin and cholinesterase were below the corresponding lower limit of the reference range. The ratio of creatinine/cystatin C concentrations presented significant correlations with the predicted rate of creatinine production (r=0.762, P<0.001), serum albumin concentration (r=0.205, P<0.05), and catalytic serum concentrations of cholinesterase (r=0.207, P<0.05), gamma glutamyltransferase (r=-0.273, P<0.01), and alkaline phosphatase (r=-0.289, P<0.01). The GFR (mean+/-SD; median) predicted by the serum creatinine (84.0+/-35.1 mL/min/1.73 m; 82.6 mL/min/1.73 m) was significantly higher (P<0.001) than that predicted by the serum cystatin C (53.1+/-30.2 mL/min/1.73 m; 44.9 mL/min/1.73 m). The ratio between the GFR values predicted by creatinine and cystatin C had a highly significant negative correlation with the rate of creatinine production (r=-0.912, P<0.001). Furthermore, significant differences were found for the peak concentrations and clearances of amikacin and vancomycin estimated by means of the Abbottbase Pharmacokinetic Systems program, and using the GFR values predicted by the serum creatinine and cystatin C (P<0.005). In patients with hepatic dysfunction, the clearance of creatinine predicted by the Cockcroft-Gault formula leads to a significant overestimation of the GFR. Cystatin C seems to be a valid alternative as a GFR marker with regard to drug dose adjustment in these cases.
Ther Drug Monit 2006 Jun
PMID:Serum cystatin C for the prediction of glomerular filtration rate with regard to the dose adjustment of amikacin, gentamicin, tobramycin, and vancomycin. 1677 15

Plasma levels of C-reactive protein, interleukin-6, tumor necrosis factor-alpha, and lipid peroxides are high whereas those of endothelial nitric oxide are low in insulin resistance, obesity, type 2 diabetes mellitus, hypertension, hyperlipidemias, metabolic syndrome X, and Alzheimer's disease suggesting that these diseases are characterized by low-grade systemic inflammation. Recent studies showed that the plasma and tissue activities of enzymes butyrylcholinesterase and acetylcholinesterase are elevated in patients with Alzheimer's disease, and diabetes mellitus, hypertension, insulin resistance, and hyperlipidemia. As a result of this increase in the activities of enzymes acetylcholinesterase and butyrylcholinesterase, the plasma and tissue levels of acetylcholine (ACh) will be low. The "cholinergic anti-inflammatory pathway" mediated by acetylcholine acts by inhibiting the production of tumor necrosis factor, interleukin-1, macrophage migration inhibitory factor, and high mobility group box-1 and suppresses the activation of nuclear factor-kappa B expression. ACh is a neurotransmitter and regulates the levels and activities of serotonin, dopamine and other neuropeptides and thus, modulates both immune response and neurotransmission. Hence, both acetylcholinesterase and butyrylcholinesterase by inactivating acetylcholine may enhance inflammation. This suggests that increased plasma and tissue activities of acetylcholinesterase and butyrylcholinesterase seen in various clinical conditions could serve as a marker of low-grade systemic inflammation.
Med Sci Monit 2007 Dec
PMID:Acetylcholinesterase and butyrylcholinesterase as possible markers of low-grade systemic inflammation. 1804 45

Studies are increasingly using cholinergic parameters as biomarkers of early neurotoxicity, but few have characterized this system in ecologically relevant model organisms. In the present study, key neurochemicals in the cholinergic pathway were measured and analyzed from discrete parts of brain and blood from captive mink (Mustela vison). Similar to other mammals, the regional distribution of cholinergic parameters in the brain could be ranked from highest to lowest as: basal ganglia > occipital cortex > brain stem > cerebellum (F (3,192) = 172.1, p < 0.001). Higher variation in cholinergic parameters was found in the cerebellum (coefficient of variation = 34.9%), and the least variation was measured in the brain stem (19.7%). Variation was also assessed by calculating the difference between the lowest and highest measures among individual animals: choline acetyltransferase (1.6x fold difference), cholinesterase (2.0x), muscarinic receptor levels (2.4x), acetylcholine (3.7x), nicotinic receptor levels (3.9x), and choline transporter (5.0x). In blood samples, activity and inter-individual variation of cholinesterase was highest in whole blood and lowest in plasma and serum. By using captive mink of a common genetic source, age, gender, and rearing conditions, these data help establish normal levels, ranges, and variations of cholinergic biomarkers among brain regions, blood components, and individual animals. Such information may better enable the utility of cholinergic biomarkers in environmental assessments.
Environ Monit Assess 2010 Mar
PMID:Variation of cholinergic biomarkers in brain regions and blood components of captive mink. 1926 10


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