• Bulletin of the Korean Chemical Society
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• v.32 no.spc8
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• pp.2997-3002
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• 2011

A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The $IC_{50}$ values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.5{\pm}0.2\;{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $1.52{\pm}0.18\;{\mu}M$.

• Natural Product Sciences
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• v.17 no.2
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• pp.108-112
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• 2011

Several isoquinoline alkaloids (1 - 18), which have basic chemical structures as protoberberine and aporphine skeletones, were evaluated for their inhibitory activities on AChE and BuChE. Among them, compounds 3, 4, 6, 8 and 12 showed the potent AchE activity with the $IC_{50}$ values ranging from $10.2{\pm}0.5\;{\mu}M$ to $24.5{\pm}1.6\;{\mu}M$, meanwhile, compound 14 - 17 exhibited strong inhibitory activity with $IC_{50}$ values from $2.1{\pm}0.2$ to $5.5{\pm}0.3\;{\mu}M$. Compounds 14 - 17 exhibited selective inhibition for AChE compared with BuChE. The isoquinoline alkaloid possesses aromatic methylenedioxy groups and quaternary nitrogen atoms are crucial for the anti-cholinesterase inhibitory activity.

• Journal of the East Asian Society of Dietary Life
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• v.6 no.2
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• pp.127-134
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• 1996

This study was performed to investigate the effects of green tea activites in rats with administration of aluminum in drinking green tea. Male Sprague-Daweley rats were divided into five groups consisting of the control, aqueous green tea at the level of 1.5%, a aquous green tea(1.5%) and aluminum sulfate solution 500ppm, before the 2 weeks administration by aquous green tea(1.5%) and after the 2 weeks aluminum sulfate solution 500ppm, aluminum sulfate solution 500ppm. After 4weeks of feeding, serum enzymes activites were measured for experimental rats, and analyzed the activites of alanine amino trans aminase(ALT), asparate amino transminase(AST) , lactate dehydrogenase(LDH), cholinesterase(ChE). Comparing to control group, Alanine amino trans aminase (ALT) was decreased in aqueous green tea administrated group and increased significantly administration by aluminum sulfate solution 500ppm group. Alanine amino trans aminase(ALT) was decreased administration by aqueous green tea group and Increased addition to aluminum sulfate solution 500ppm group as compared to control group. Lactate dehydrogenase(LDH) was increased compared to control group by experimental group and increased significantly administration by aluminum sulfate solution 500ppm. Cholinesterase (ChE) activity was decreased compared to control group by experimental group.

• Korean Journal of Environmental Agriculture
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• v.7 no.1
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• pp.58-64
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• 1988

The acute oral, intraperitoneal and subacute toxicity of monocrotophos, an insecticide, was studied in albino rats. The acute oral $LD_{50}$ values for female and male rats were 5.0mg/kg and 8.7mg/kg, respectively. Conversely the intraperitoneal $LD_{50}$ values for female and male rats were 4.9mg/kg and 6.0mg/kg, respectively. Plasma cholinesterase (ChE) activity in rats treated with a single dose was the most depressed 4 hours after administration, but returned to normal within 72 hours of administration. Significant depression of body weight gain and food consumption was observed in rats receiving the 3.5mg/kg/day dose level for 28 days as compared with the controls. Additionally plasma ChE activity depression was also observed.

• Archives of Pharmacal Research
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• v.14 no.4
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• pp.330-335
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• 1991

The effects of physostigmine and neostigmine on the parathin induced toxicity were examined in adult female rats. Physostigmine $(100\;{\mu}g/kg,\;ip)$ or neostigmine $(200\;{\mu}g/kg,\;ip)$ inhibited acetylcholinesterase (AChE) and cholinesterase (ChE) activities in blood, brain and lung when the enzyme activity was measured 30 min after the treatment. At the doses of two carbamates equipotent on brain AChE, neostigmine showed greater inhibition on peripheral AChE/ChE. The enzyme activity returned to normal in 120 min following the carbamates except in the lung of rats treated with neostigmine. Carbamates administered 30 min prior to parathion (2 mg/kg) antagonized the inhibition of AChE/ChE by parathion when the enzyme activity was measured 2 hr following parathion. Neostigmine showed greater protective effect on peripheral AChE/ChE. The effect of either carbamate on AChE/ChE was not significant 2 hr beyond the parathion treatment. Carbamates decreased the mortality of rats challenged with a lethal dose of parathion (4 mg/kg, ip) either when treated alone or in combination with atropine (10 mg/kg, ip). Lethal action of paraoxon (1.5 mg/ks ip), the active metabolite of parathion was also decreased by the carbamate treatment indicating that the protection was not mediated by competitive inhibition of metabolic conversion of parathion to paraoxon. The results suggest that carbamylation of the active sites may not be the sole underlying mechanism of protection provided by the carbamates.

• BMB Reports
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• v.31 no.3
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• pp.296-302
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• 1998

A potentiometric flow injection biosensor for the analysis of anti-cholinesterases (anti-ChEs), based on inhibition of enzyme activity, was developed. The sensor system consists of a reactor with acetylcholinesterase (AChE) immobilized on controlled pore glass and a detector with an $H^{+}-selective$ PVC-based membrane electrode. The principle of the analysis is based on the fact that the degree of inhibition of AChE by an anti-ChE is dependent on the concentration of the anti-ChE in contact with AChE. The sensor system was optimized by changing systematically the operating parameters of the sensor to evaluate the effect of the changes on sensor response to ACh. The optimized biosensor was applied to the analysis of paraoxon, an organophosphorus pesticide. Treatment of the inhibited enzyme with pyridine-2-aldoxime fully restored the enzyme activity allowing repeated use of the sensor.

• Fisheries and Aquatic Sciences
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• v.25 no.2
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• pp.49-63
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• 2022

Anti-cholinesterase (ChE)s are commonly prescribed as the symptomatic treatment of Alzheimer's disease. They are applied to prevent the breakdown of neurotransmitter acetylcholine (ACh) that bind to muscarinic and nicotinic receptors in the synaptic cleft. Seaweeds are one of the richest sources of bioactive compounds for both nutraceuticals and pharmacognosy applications. This study aimed to determine the anti-ChEs activity of Gracilaria manilaensis, one of the red seaweeds notables for its economic importance as food and raw materials for agar production. Methanol extracts (GMM) of G. manilaensis were prepared through maceration, and further purified with column chromatography into a semi-pure fraction. Ellman assay was carried out to determine the anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BuChE) activities of extracts and fractions. Lineweaver-Burk plot analysis was carried out to determine the inhibition kinetic of potent extract and fraction. Major compound(s) from the most potent fraction was determined by liquid chromatography-mass spectrometry (LCMS). GMM and fraction G (GMMG) showed significant inhibitory activity AChE with EC₅₀ of 2.6 mg/mL and 2.3 mg/mL respectively. GMM and GMMG exhibit mixed-inhibition and uncompetitive inhibition respectively against AChE. GMMG possesses neuroprotective compounds such as cynerine A, graveolinine, militarinone A, eplerenone and curumenol. These findings showed a promising insight of G. manilaensis to be served as a nutraceutical for neuronal health care in the future.

• Ocean and Polar Research
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• v.39 no.1
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• pp.45-49
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• 2017

During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

• Korean Journal of Veterinary Research
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• v.15 no.1
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• pp.39-45
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• 1975

The authors believe that farm livestok will be greatly affected by the marked increasing use of organic phosphate. This study was carried out to observe the clinical signs and histopathological changes of mouse, guinea pig, hamster and rabbit that were orally administered with diazinon used usually as agricultural insecticide, and cholinesterase (ChE) activity was histochemically examined in the liver, heart, kidney, adrenal gland, duodenum and salivary gland of these experimental animals administered with diazinon. The results obtained were as follows: 1. Clinical signs such as dullness, severe salivation, ataxia, dyspnea, irregular slight convulsion and inappetance and as the histopathological changes cloudy swelling, congestion and hemorrhage of parenchymal organs, catarrh or local necrsois of the gastrointestinal tract, congestion or hemorrhage of the other organs were observed. Especially, hemorrhage of adrenal glands (rabbit, guinea pig) and pulmonary congestion and hemorrhage were necessarily constant. 2. In the histochemical study, ChE activity appeared intensely in the liver, heart, medulla of adrenal glands and salivary glands (submaxillary and parotid) of control animals, but ChE activity was negative or markedly decreased in experimental animals administered with diazinon. There was no marked difference between the control and experimental animals in ChE activity of the kidney. 3. Histochemical observation of ChE activity was helpful to explain the clinical signs and histopathological changes and was regarded as a diagnostic method for organic phosphate poisoning.

• Toxicological Research
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• v.12 no.2
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• pp.231-236
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• 1996

The toxicity of the mixture of diazinon, toxaphene(TOX) and/or endrin was studied in ICR male mice(18-22 g) by oral intubation, in corn oil, daily for up to 14 days. On day 15, the exposure was discontinued and animals were monitored for an additional period of 7 days for the possible reversibility of the toxicity. The body weight gain decreased with the mixtures, as well as with the individual pesticides, during the 14-day period. TOX and TOX containing mixtures significantly increased the liver/body weight ratio. The serum glutamic pyruvic transaminase level increased at 23~374% in diazinon, TOX, and endrin or their mixture group. The cholinesterase(ChE) activity in the serum and brain was inhibited in the animals of the group of diazinon(5, 10 mg/kg) and diazinon(5 mg/kg) containing mixtures. TOX(40, 80 mg/kg) caused initial inhibitory effects on the serum ChE Day 1. but there is little effects on the brain ChE levels. endrin(5,10 mg/kg) results in significantly elevated levels of the serum ChE, with substantial decreases in the brain ChE activity. TOX and TOX containing mixtures decreased the pentobarbital(60 mg /kg, ip., in saline) induced sleep. The effects produced by this pesticides singly, as well as by their mixtures, appeared to be reversible in nature. The toxic effects exhibited by the mixtures of diazinon(5 mf/kg), TOX(40 mg/kg), and /or endrin(5 mg/kg) were found to be the resultant of the effect showed by their components individually.