scholarly journals Intraperitoneal Exposure to Nano/Microparticles of Fullerene (C60) Increases Acetylcholinesterase Activity and Lipid Peroxidation in Adult Zebrafish (Danio rerio) Brain

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Gonzalo Ogliari Dal Forno ◽  
Luiza Wilges Kist ◽  
Mariana Barbieri de Azevedo ◽  
Rachel Seemann Fritsch ◽  
Talita Carneiro Brandão Pereira ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Oxidative Damage ◽  
Ache Activity ◽  
Transcriptional Control ◽  
Direct Action ◽  
Acetylcholinesterase Activity ◽  
Biological Properties ◽  
Adult Zebrafish ◽  
Antioxidant Responses

Even though technologies involving nano/microparticles have great potential, it is crucial to determine possible toxicity of these technological products before extensive use. Fullerenes C60are nanomaterials with unique physicochemical and biological properties that are important for the development of many technological applications. The aim of this study was to evaluate the consequences of nonphotoexcited fullerene C60exposure in brain acetylcholinesterase expression and activity, antioxidant responses, and oxidative damage using adult zebrafish as an animal model. None of the doses tested (7.5, 15, and 30 mg/kg) altered AChE activity, antioxidant responses, and oxidative damage when zebrafish were exposed to nonphotoexcited C60nano/microparticles during 6 and 12 hours. However, adult zebrafish exposed to the 30 mg/kg dose for 24 hours have shown enhanced AChE activity and augmented lipid peroxidation (TBARS assays) in brain. In addition, the up-regulation of brain AChE activity was neither related to the transcriptional control (RT-qPCR analysis) nor to the direct action of nonphotoexcited C60nano/microparticles on the protein (in vitroresults) but probably involved a posttranscriptional or posttranslational modulation of this enzymatic activity. Taken together these findings provided further evidence of toxic effects on brain after C60exposure.

Effects of phenytoin on acetylcholinesterase activity and cell protein in cultured chick embryonic skeletal muscle

1978 ◽  
Vol 56 (2) ◽  
pp. 287-293 ◽  
Author(s):  
C. Michael Cisson ◽  
Richard K. Entrikin ◽  
Barry W. Wilson
Keyword(s):  
Ache Activity ◽  
Creatine Phosphokinase ◽  
Direct Action ◽  
Acetylcholinesterase Activity ◽  
Lactic Dehydrogenase ◽  
Pectoral Muscle ◽  
Cell Protein ◽  
Leucine Incorporation ◽  
Chick Embryos

Cultured pectoral muscle from 11-day-old chick embryos was treated for 48 h with phenytoin (diphenylhydantoin, DPH) in concentrations ranging from 15 to 270 μg/ml on days 7–9 in vitro. Acetylcholinesterase (AChE, EC 3.1.1.7), creatine phosphokinase (CPK, EC 2.7.3.2), and lactic dehydrogenase (LDH, EC 1.1.1.27) activities, [3H]leucine incorporation into protein, and total protein of the cultures decreased in a dose-related manner with DPH concentrations of 30 μg/ml and greater. Total AChE activity and AChE activity released into the medium were specifically decreased with 15 μg DPH per millilitre. In cultures treated chronically with 15 μg DPH per millilitre on days 5–13 in vitro, total AChE activity and AChE activity released into the medium were 66.0 ± 13.2 and 64.7 ± 11.8% of untreated controls, respectively, but cellular AChE activity, cell protein, and [3H]leucine incorporation into protein were unaffected. The results indicate that DPH specifically decreases the total net synthesis of AChE activity by a direct action on cultured chick embryo muscle.

Spirocyclohexadienones as an Uncommon Scaffold for Acetylcholinesterase Inhibitory Activity

2019 ◽  
Vol 15 (4) ◽  
pp. 373-382 ◽  
Author(s):  
Ralph C. Gomes ◽  
Renata P. Sakata ◽  
Wanda P. Almeida ◽  
Fernando Coelho
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Population Aging ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Activity ◽  
Docking Study ◽  
Biological Properties ◽  
Ache Inhibitor ◽  
Molecular Docking Study

Background: The most important cause of dementia affecting elderly people is the Alzheimer’s disease (AD). Patients affected by this progressive and neurodegenerative disease have severe memory and cognitive function impairments. Some medicines used for treating this disease in the early stages are based on inhibition of acetylcholinesterase. Population aging should contribute to increase the cases of patients suffering from Alzheimer's disease, thus requiring the development of new therapeutic entities for the treatment of this disease. Methods: The objective of this work is to identify new substances that have spatial structural similarity with donepezil, an efficient commercial drug used for the treatment of Alzheimer's disease, and to evaluate the capacity of inhibition of these new substances against the enzyme acetylcholinesterase. Results: Based on a previous results of our group, we prepared a set of 11 spirocyclohexadienones with different substitutions patterns in three steps and overall yield of up to 59%. These compounds were evaluated in vitro against acetylcholinesterase. We found that eight of them are able to inhibit the acetylcholinesterase activity, with IC50 values ranging from 0.12 to 12.67 µM. Molecular docking study indicated that the spirocyclohexadienone, 9e (IC50 = 0.12 µM), a mixedtype AChE inhibitor, showed a good interaction at active site of the enzyme, including the cationic (CAS) and the peripheral site (PAS). Conclusion: We described the first study aimed at investigating the biological properties of spirocyclohexadienones as acetylcholinesterase inhibitors. Thus, we have identified an inhibitor, which provided valuable insights for further studies aimed at the discovery of more potent acetylcholinesterase inhibitors.

Effect of Ethanol on Erythrocyte Acetylcholinesterase Activity

1986 ◽  
Vol 23 (4) ◽  
pp. 458-462 ◽  
Author(s):  
Nuha A Haboubi ◽  
D I Thurnham
Keyword(s):  
Ache Activity ◽  
Acetylcholinesterase Activity ◽  
Inhibitory Effect ◽  
In Vitro Experiments ◽  
Previous Exposure ◽  
Organophosphorus Poisoning ◽  
The Mean ◽  
Erythrocyte Ache ◽  
Early Indication

Erythrocyte acetylcholinesterase (AchE) activity was measured in the blood of 36 alcoholic subjects and 41 healthy volunteers. The mean activity in the alcoholics was significantly lower than that in the control subjects. In vitro experiments showed that ethanol inhibited the AchE activity immediately and in proportion to the concentration of ethanol used. Incubation times up to 6 h did not increase the inhibition significantly. Incubation of normal red cells with ethanol for 15 h, followed by washing, showed also that AchE activity was inhibited by the previous exposure to ethanol and that washing did not reduce the inhibitory effect. The possibility is considered that depressed erythrocyte AchE activity may be an early indication of potential disturbances of the autonomic nervous system. The importance of reporting ethanol intake in patients with organophosphorus poisoning is stressed.

scholarly journals Therapeutic Potential of Polar and Non-Polar Extracts ofCyanthillium cinereum In Vitro

2011 ◽  
Vol 2011 ◽  
pp. 1-10 ◽  
Author(s):  
Gunjan Guha ◽  
V. Rajkumar ◽  
R. Ashok Kumar ◽  
Lazar Mathew
Keyword(s):  
Lipid Peroxidation ◽  
Free Radical ◽  
Oxidative Damage ◽  
Therapeutic Potential ◽  
Reducing Power ◽  
Total Phenolic ◽  
Xtt Assay ◽  
Polar Extracts ◽  
Scavenging Efficiency

Cyanthillium cinereum(Less.) H. Rob. (Asteraceae) has been traditionally known for its medicinal properties, all aspects of which are yet to be exploited. This study was aimed at investigating the therapeutic potential of polar (methanolic and aqueous) and nonpolar (hexane and chloroform) crude extracts of the whole plant. Several parameters including free-radical (DPPH•, ABTS•+, H2O2and•OH) scavenging, reducing power, protection of DNA against oxidative damage, cytotoxicity, inhibition of oxidative hemolysis in erythrocytes, total phenolic content and inhibition of lipid peroxidation were examined. All the free-radical generating assay models demonstrated positive scavenging efficiency with differential but considerable magnitudes for the four extracts. However, only the hexane extract showed significant H2O2scavenging effect. Lipid peroxidation was estimated by thiobarbituric acid-malondialdehyde (MDA) reaction, and a high degree of inhibition was shown by all the extracts. Reducing power of the polar extracts was higher than the non-polar ones. All extracts showed a concentration-dependent increase in phenolic contents. Oxidative damage to erythrocytes was hindered by all extracts in diverse degrees. XTT assay showed that all extracts have mild cytotoxic property. The aqueous extract evidently demonstrated protective effect on pBR322 plasmid DNA against oxidative breakdown. These results suggested the potential ofC. cinereumas medicine against free-radical-associated oxidative damage and related degenerative diseases involving metabolic stress, genotoxicity and cytotoxicity.

scholarly journals Pyridoxine Decreases Oxidative Stress on Human Erythrocyte Membrane Protein in vitro

2019 ◽  
Vol 13 (1) ◽  
pp. 37-44 ◽  
Author(s):  
Margarita Velásquez ◽  
Darío Méndez ◽  
Carlos Moneriz
Keyword(s):  
Oxidative Stress ◽  
Lipid Peroxidation ◽  
Membrane Protein ◽  
Oxidative Damage ◽  
Erythrocyte Membrane ◽  
Cumene Hydroperoxide ◽  
Protein Carbonylation ◽  
Human Erythrocytes ◽  
Red Cell Membrane

Background: Pyridoxine has reduction and prevention against the levels of reactive oxygen species in in vitro studies. However, the biochemical mechanism that explains this behavior has not yet been fully clarified. Objective: To evaluate the effect of pyridoxine against oxidative damage on the membrane of human erythrocytes. Methods: Cumene hydroperoxide was used to induce oxidative stress in protein and lipid. Human erythrocytes were incubated with pyridoxine and cumene hydroperoxide, either alone or together for 8 h. Oxidative damage was determined by measuring lipid peroxidation and membrane protein carbonylation. Results: The results indicate that the malondialdehyde concentration decreased with increasing concentration of pyridoxine. The membrane protein content also decreased with increasing concentration of vitamin B6, which was confirmed by the decreased signal intensity in the western blot when compared to control without pyridoxine. Results demonstrate that pyridoxine can significantly decrease lipid peroxidation and protein carbonylation in red cell membrane exposed to high concentrations of oxidant agent. Conclusion: Pyridoxine showed a protective effect against the oxidative stress in human erythrocytes in vitro, inhibiting the carbonylation and the oxidative damage of erythrocyte membrane proteins. To date, such an effect has not yet been reported in terms of protein oxidation.

Antioxidant Activity In vivo and Ex Vivo of Tautomeric Pair of Polyprenylated Benzophenone - Garcinielliptone FC (Platonia insignis Mart Seeds)

2020 ◽  
Vol 16 (3) ◽  
pp. 284-293
Author(s):  
George Laylson da Silva Oliveira ◽  
Maria das Dores Alves de Oliveira ◽  
Maria da Conceição Oliveira Prado ◽  
Alexandre de Barros Falcão Ferraz ◽  
José Carlos Correia Lima da Silva ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Lipid Peroxidation ◽  
Antioxidant Activity ◽  
Oxidative Damage ◽  
Ex Vivo ◽  
Redox Balance ◽  
Oxidative Stress Biomarkers ◽  
Iron Citrate

Background: Garcinielliptone FC corresponds to a polyprenylated acylphloroglucinol having a benzophenonic core (diphenylmethanone) substituted with isoprenyl(s) group(s) (3-methyl-2-butenyl) and 2-isopropenyl-hex-5-enyl. Objective: The present work evaluated the antioxidant activity of garcinielliptone FC (GFC) in vitro against non-biological radicals [2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azinobis-3- ethylbenzothiazoline-6-sulfonic acid (ABTS•+)] and ex vivo against oxidative damage induced by AAPH (2,2'-azobis-2-methylpropionamidine dihydrochloride) and iron/citrate ion in erythrocytes and mitochondria, respectively. Methods: In addition to the protective effect, the main biochemical indexes of oxidative stress, such as lipid peroxidation through the formation of Thiobarbituric Acid Reactive Substances (TBARS), Superoxide Dismutase (SOD), Catalase (CAT) activity and reduced glutathione (GSH) levels. Results: According to the results obtained in erythrocytes, the antioxidant results at concentrations of 0.1, 0.3, 0.7, 1.5 and 3.0 mM were 26.34 ± 0.68, 43.39 ± 2.17, 62.27 ± 2.17, 86.69 ± 0.47 and 92.89 ± 0.45%, respectively, where GFC reduced the rate of oxidative hemolysis when compared to AAPH (p<0.05). The antioxidant activity observed in erythrocytes was also seen in mitochondria in which GFC reduced mitochondrial swelling by increasing the absorbance when compared to iron/citrate ion complex (p<0.05). In both biological models, GFC had an antioxidant effect on erythrocyte and mitochondrial redox balance when analyzing oxidative stress biomarkers, such as reduction of lipid peroxidation and inhibition of depletion in the activity of SOD, CAT and GSH levels. Conclusion: In conclusion, GFC had in vitro and ex vivo antioxidant activity against oxidative damage induced in erythrocytes and mitochondria acting on the erythrocytic and mitochondrial redox balance.

scholarly journals In vivo and in vitro effects of fructose on rat brain acetylcholinesterase activity: an ontogenetic study

2014 ◽  
Vol 86 (4) ◽  
pp. 1919-1926 ◽  
Author(s):  
CARINE A. GUIMARÃES ◽  
MAIRIS S. BIELLA ◽  
ABIGAIL LOPES ◽  
PEDRO F. DEROZA ◽  
MARIANA B. OLIVEIRA ◽  
...  
Keyword(s):  
Cerebral Cortex ◽  
Ache Activity ◽  
Young Patients ◽  
Brain Structures ◽  
Acetylcholinesterase Activity ◽  
Control Group ◽  
Inherited Disorders ◽  
Old Rats

Increased fructose concentrations are the biochemical hallmark of fructosemia, a group of inherited disorders on the metabolic pathway of this sugar. The main clinical findings observed in patients affected by fructosemia include neurological abnormalities with developmental delay, whose pathophysiology is still undefined. In the present work we investigated the in vitro and in vivo effects of fructose on acetylcholinesterase (AchE) activity in brain structures of developing rats. For the in vitro experiments, fructose was added at increasing concentrations to the incubation medium. It was observed that fructose provoked an inhibition of acetylcholinesterase activity in cerebral cortex of 30-day-old-rats, even at low concentrations (0.1 mM). For the in vivo experiments, rats were killed 1 h after a single fructose administration (5 µmol/g). Control group received the same volume of saline solution. We found that AchE activity was increased in cerebral cortex of 30- and 60-day-old rats receiving fructose administration. Finally, we observed that AchE activity was unaffected by acute fructose administration in cerebral cortex, striatum or hippocampus of 15- and 90-day-old rats. The present data suggest that a disruption in cholinergic homeostasis may be involved in the pathophysiology of brain damage observed in young patients affected by fructosemia.

scholarly journals The influence of chromone based hydrazones on lipid peroxidation and bFGF concentration in the HL-60 cell line.

2013 ◽  
Vol 60 (2) ◽  
Author(s):  
Andrzej Łazarenkow ◽  
Marta Michalska ◽  
Anna Gorąca ◽  
Marek Mirowski ◽  
Jolanta Nawrot-Modranka ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Cell Line ◽  
Significant Influence ◽  
Biological Properties ◽  
Synthetic Analogues ◽  
Wide Range ◽  
Synthetic Derivatives ◽  
Derivatives Of

Natural and synthetic derivatives of benzo-γ-pyrones (i.e. flavones, chromones, and coumarins) and their synthetic analogues possess a wide range of biological properties in vitro and in vivo. In this paper we investigated the influence of two hydrazone compounds of chromones, 3-{[(2-dimethoxytiophosphoryl)-2-methylhydrazono]-methyl}-chromen-4-one (CH-3) and 2-amino-6-chloro-3-[(2-hydroxyethyl)-hydrazonomethyl]-chromen-4-one (A-12), on lipid peroxidation and bFGF concentration in the HL-60 cells. Both of the studied compounds had a significant influence on bFGF and TBARS in ranges -137.20 ~ 380.26% and -81.66 ~ -28.68%, respectively, in comparison with the control (counted as 0%).

The Effect of Galactose Metabolic Disorders on Rat Brain Acetylcholinesterase Activity

2000 ◽  
Vol 55 (9-10) ◽  
pp. 852-856 ◽  
Author(s):  
Stylianos Tsakiris ◽  
Kleopatra H. Schulpis
Keyword(s):  
Enzyme Activity ◽  
Ache Activity ◽  
Direct Action ◽  
Acetylcholinesterase Activity ◽  
Classical Galactosemia ◽  
Control Value ◽  
Brain Ache ◽  
Cholinergic Dysfunction ◽  
The Brain ◽  
Brain Acetylcholinesterase

Abstract To evaluate whether in classical galactosemia galactose (Gal), galactose-1-phosphate (Gal-1-P) and galactitol (Galtol) affect brain acetylcholinesterase (AChE) activity, various concentrations (1-16 mм) of these compounds were preincubated with brain homogenates of suckling rats as well as with pure eel Electroforus electricus AChE at 37 °C for 1 h. Initially, Galtol (up to 2.0 mм) increased (25%) AChE activity which decreased, thereafter, reaching the control value in high Galtol concentrations. Gal-1-P decreased gradually the enzyme activity reaching a plateau (38%), when incubated with 8-16 mM. However, when the usually found 2 mм of Galtol and 2 mм of Gal-1-P. concentrations in galactosemia were added in the incubation mixture simultaneously, brain AChE was stimulated (16%). Galtol or Gal-1-P modulated brain AChE as well as enzyme activity of E.electricus in the same way. Gal, Glucose (Glu) and glucose-1-phosphate (Glu-1-P) had no effect on AChE activity. It is suggested that Galtol as well as Gal-1-P can affect acetylcholine degradation acting directly on AChE molecule. Consequently the direct action of these substances on the enzyme might explain the brain cholinergic dysfunction in untreated galactosemia patients.

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