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)

Membrane preparations of erythrocytes from normal and P. chabaudi-infected mice and membrane preparations of P. chabaudi-infected and uninfected erythrocytes from infected mice and separated by zonal centrifugation were characterized by the pattern of proteins and extracted glycoproteins obtained by SDS-polyacrylamide gel electrophoresis and by the specific activities of membrane associated enzymes. The protein pattern of the membrane preparation of infected erythrocytes showed similar differences from membrane preparations of normal erythrocytes as those described by Weidekamm et al. for P. berghei. The pattern of glycoproteins extracted by the chloroform-methanol method showed characteristic differences as compared to the controls. A new band (PASi) with a molecular weight of about 165,000 corresponds with the protein band IIa. In membrane preparations of normal erythrocytes and of nonparasitized erythrocytes separated from parasitized erythrocytes by zonal centrifugation was no difference in specific activities of ATPase, adenylate kinase and acetylcholinesterase. Adenylate kinase activity was markedly increased and acetyl-cholinesterase activity was slightly increased in membrane preparations of infected cells. Specific activities of ATPase of membrane preparations of normal and parasitized erythrocytes did not show significant differences. There was a decrease in enzyme activity of ATPase and an increase of acetylcholinesterase in Triton X 100 containing samples. Specific activities of an acid phosphatase were lower in membrane preparations of parasitized cells than in the controls.
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PMID:Plasmodium chabaudi-infection of mice: specific activities of erythrocyte membrane-associated enzymes and patterns of proteins and glycoproteins of erythrocyte membrane preparations. 19 21

The results of a preliminary rangefinding 13-wk oral toxicity study and of two longer term studies on chloroform in toothpaste base are reported. Significant changes in serum enzymes and certain haemotological parameters were seen at the higher dose-levels in the rangefinding study. Intercurrent disease made it necessary to terminate the first long-term experiment prematurely after 1 yr. No evidence of serious toxicity was recorded. In the second long-term experiment, groups of 50 caesarian-derived SPF Sprague-Dawley rats of each sex received either the equivalent of 60 mg CHCl3/kg/d in toothpaste base or the vehicle only, by gavage on 6 d/wk for 80 wk and were then observed for up to a further 15 wk. Chloroform-treated rats of both sexes survived better than the controls, though both groups had a high incidence of non-neoplastic respiratory and renal disease. Female rats gave a consistent finding of decrease in plasma cholinesterase, shown to be related to activity against butyrylcholine but not acetyl-beta-methylcholine. Tumours of various sites were seen in 39 percent of chloroform-treated rats of both sexes examined histologically, compared with 38 percent of vehicle controls. There were no treatment-related effects on the incidence of liver or kidney tumours. Histologically-malignant mammary tumours were reported in more treated than control rats, but the difference in incidence was not statistically significant.
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PMID:Safety evaluation of toothpaste containing chloroform. II. Long term studies in rats. 42 37

Content of organophosphorous inhibitors (with the structure RO/CH3/P/O/SC2H4SC2H5) of cholinesterase as well as their hydrophobic properties (distribution coefficient in hexan/water system) were studied in subcellular fractions of rat brain. Relative content of organophosphorous inhibitors was distinctly decreased in supermicrosomal fraction with increase of hydrophobic properties of the fraction. Nuclear and mitochondrial fractions contained the more hydrophobic substances in relatively higher amount. When homogenate of supermicrosomal fraction was incubated at 37 degrees, own brain cholinesterase was not depressed by organophosphorous inhibitors, containing in the fraction at low concentration. The phenomenon exhibits that content of free organophosphorous inhibitors is distinctly lower in the subcellular fractions studied than amount of the inhibitors, extracted with chloroform.
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PMID:[Intracellular distribution of phosphoorganic cholinesterase inhibitors in rat brain]. 73 75

Hydrophobity (coefficient in distribution in the hexane water system) and the content of cholinesterase organophosphorous inhibitors (OPI) of the structure Ro (CH3) P (O) SC2H4 SC2H5 were studied in the rat brain. When the O-alkyl radical is increased hydrophobity rises and the relative content of free OPI in the brain extracted by chloroform decreases. With an increase in R from the ethyl to butyl one the ability to the additional inhibition of the brain own cholinesterase lowers due to incubation of homogenate at 37 degrees C, that evidences for an essential drop in the studied series of the free OPI fraction relative to the free OPI extracted by chloroform.
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PMID:[Binding of phosphoorganic cholinesterase inhibitors in rat brain tissue]. 98 15

The article deals with the hydrophobic character (distribution coefficient in the systems hexane - water and chloroform - water) and certain peculiarities of distributing three cation-containing phosphoroganic inhibitors of cholinesterase and their uncharged analogues in the organisms. The distribution coefficients in the charged and uncharged compounds in the system hexane - water differ inconsiderably, whereas in the system chloroform-water by the thousands and millions times. In rabbits with intravenous administration the content of all inhibitors in blood decreases rapidly, the uncharged compounds accumulate selectively in the lungs and the charged ones are distributed evenly in the tissues.
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PMID:[The distribution of cholinesterase charged phosphorganic inhibitors and their uncharged analogues in tissues]. 120 7

The content and hydrophobic properties (distribution coefficient in hexan : water) of organophosphorus inhibitors OPT of the following structure--R-O (CH3)/P/O/S C2H4SC2H5 have been studied in rat brain. On enlargement of the O-alkyl radical from ethyl to isopropyl and pinacolin hydrophobecity increases from 1 to 12 and 39, while the relative content of the chloroform extractable free OPT in brain, under conditions of uniform distribution, decreases from 11--18% to 3.2%. On incubation of the homogenate at 37 degrees C the further inhibition of the specific cholinesterase of the brain indicates the presence of an absolutely free form of OPT, the amount of which is not dependent on the degree of its hydrophobicity.
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PMID:[Forms of deposition of phosphoorganic cholinesterase inhibitors in the brain]. 123 72

In female and male mice the effect of exposure to trichloroethylene (TCE) seen at the lowest concentration is an increase in liver weight. The activity of plasma butyrylcholinesterase (BuChE) increases even more than the liver weight at corresponding concentrations, but only in the males. Depletion of testosterone through castration or destruction of the pituitary gland or hypothalamus, are the only other ways to experimentally induce corresponding increases in BuChE. Plasma BuChE activity increase was found to be a common reaction after exposure to TCE, perchloroethylene, chloroform, methylene chloride and carbon tetrachloride and also after exposure to ethanol. Other solvents such as toluene, xylene, benzene and 1,1,1-trichloroethane had little or no effect on BuChE activity. Normal and castrated male mice were continuously exposed for one month to 150 p.p.m. TCE. The increase in BuChE activity after the exposure was of the same magnitude as the increase seen after castration. BuChE activity in castrated males was not further increased by TCE exposure. Administration of testosterone with osmotic minipumps for 13 days almost restored the normal testosterone and BuChE levels in castrates. The effect of TCE exposure on BuChE activity in these animals was the same as on normal males. Testosterone levels were not influenced by the TCE exposure in normal males or in castrates given testosterone. No sex hormone binding globulins (SHBG) could be detected in the mice. BuChE activity changes induced through solvent exposure are therefore neither directly nor indirectly (through SHBG) due to effects on testosterone. The results from these animal experiments do not support the epidemiological findings of decreased testosterone levels in humans exposed to solvents.
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PMID:Effects of solvent exposure on testosterone levels and butyrylcholinesterase activity in mice. 408 34

The methanolysis of choline p-nitrophenylcarbonate in chloroform containing 1% methanol is catalyzed with turnover by ditopic receptors 1 and 2, consisting of a calix[6]arene connected to a bicyclic guanidinium by means of a short spacer. The calix[6]arene subunit strongly binds to the trimethylammonium head group through cation-pi interactions, whereas the guanidinium moiety is deputed to stabilize through hydrogen bonding reinforced by electrostatic attraction the anionic tetrahedral intermediate resulting from methoxide addition to the ester carbonyl. The observed cholinesterase activity had been anticipated on the basis of the ability of the ditopic receptors 1 and 2 to bind strongly to the choline phosphate DOPC, which is a transition state analogue for the BAc2-type cleavage of choline esters.
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PMID:Toward an artifical acetylcholinesterase. 1100

Brain insulin receptor and ERK I/II are suggested to play a role in memory formation. We designed a series of experiments to explore if Asiasari radix (AR) extracts could display memory enhancing actions possibly via the activation of insulin receptor and ERK I/II in mice and rats. Methanol extract of AR had significantly increased survival time in the NaNO(2) intoxication assay in mice. Methanol extract of Asiasari radix (fraction 1) and its subfractions, chloroform-soluble fraction (fraction 2) and chloroform-insoluble, methanol-soluble fraction (fraction 4) were further tested for memory formation. In eight-arm radial maze experiments, both reference memory errors and working memory errors were significantly decreased in mice by fractions 1, 2 and 4. In addition, these fractions were also effective in promoting memory in the passive avoidance test in mice and rats. To gain insight into the mechanism of memory enhancing effects by Asiasari radix extracts, the activities of hippocampal insulin receptors and ERK I/II were tested in mice and rats. Fraction 1 significantly stimulated tyrosine phosphorylation of the insulin receptor, whereas ERK I/II were stimulated by fractions 1, 2 and 4. These fractions also inhibited cholinesterase activities in rats. These results suggest that Asiasari radix extracts may exert memory enhancing effects via activation of insulin receptor and ERK I/II as well as decreasing cholinesterase activity.
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PMID:Memory enhancing actions of Asiasari radix extracts via activation of insulin receptor and extracellular signal regulated kinase (ERK) I/II in rat hippocampus. 1274 37

The chloroform:medianol (1:1) extracts of a number of the plant species belonging to eight families, namely Corydalis solida (L.) Swartz subsp. solida and Glaucium corniculatum (L.) J. H. Rudolph (Papaveraceae), Rhododendron ponticum L. subsp. ponticum and Rhododendron luteum Sweet. (Ericaceae), Buxus sempervirens L. (Buxaceae), Vicia faba L. (Fabaceae), Robinia pseudoacacia L. (Caeselpiniaceae), Tribulus terrestris L. and Zygophyllum fabago L. (Zygophyllaceae), Lycopodium clavatum L. (Lycopodiaceae), Fumaria vaillantii Lois., Fumaria capreolata L., Fumaria kralikii Jordan, Fumaria asepala Boiss., Fumaria densiflora DC., Fumaria flabellata L., Fumaria petteri Reichb. subsp. thuretii (Boiss.) Pugsley, Fumaria macrocarpa Boiss. ex Hausskn., Fumaria cilicica Hauskkn., Fumaria parviflora Lam. and Fumaria judaica Boiss. (Fumariaceae) were screened for their anticholinesterase activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro Ellman method at 10 microg/ml and 1 mg/ml concentrations. The extracts did not show any noticeable inhibitory activity against both of the enzymes at 10 microg/ml. The extracts of Rhododendron ponticum subsp. ponticum, Rhododendron luteum, Corydalis solida subsp. solida, Glaucium corniculatum, and Buxus sempervirens showed remarkable inhibitory activity above 50% inhibition rate on AChE at 1 mg/ml. Among them, Rhododendron ponticum subsp. ponticum, Corydalis solida subsp. solida and Buxus sempervirens were the most active extracts against BChE having 95.46 +/- 1.03%, 93.08 +/- 0.97%, and 93.45 +/- 0.88% inhibition rates, respectively. Among the extracts screened, all of the Fumaria extracts displayed highly potent inhibition against both of the enzymes at 1 mg/ml concentration compared to the standard.
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PMID:Acetylcholinesterase and butyrylcholinesterase inhibitory activity of some Turkish medicinal plants. 1503 68


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