• YAKHAK HOEJI
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• v.46 no.3
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• pp.185-191
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• 2002

Alzheimer's disease (AD) involves neuronal degeneration with impaired cholinergic transmission, particularly in areas of the brain associated with learning and memory. Several cholinesterase inhibitors are widely prescribed to ameliorate the cognitive deficits in AD patients. In an attempt to examine if tacrine and donepezil, two well-known cholinesterase inhibitors, exhibit additional pharmacological actions in primary cultured rat cortical cells, we investigated the effects on neuronal injuries induced by glutamate or N-methyl-D-aspartate (NMDA), $\beta$-amyloid fragment ( $A_{{beta}25-35)}$), and various oxidative insults. Both tacrine and donepezil did not significantly inhibit the excitotoxic neuronal damage induced by glutamate. However, tacrine inhibited the toxicity induced by NMDA in a concentration-dependent fashion. In addition, tacrine significantly inhibited the $A_{{beta}25-35)}$-induced neuronal injury at the concentration of 50 $\mu$M. In contrast, donepezil did not reduce the NMDA- nor $A_{{beta}25-35)}$-induced neuronal injury. Tacrine and donepezil had no effects on oxidative neuronal injuries in cultures nor on lipid peroxidation in vitro. These results suggest that, in addition to its anticholinesterase activity, the neuroprotective effects by tacrine against the NMDA- and $A_{{beta}25-35)$-induced toxicity may be beneficial for the treatment of AD. In contrast, the potent and selective inhibition of central acetylcholinesterase appears to be the major action mechanism of donepezil.

• Mycobiology
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• v.44 no.4
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• pp.291-301
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• 2016

Culinary mushroom Pleurotus pulmonarius has been popular in Asian countries. In this study, the anti-oxidant, cholinesterase, and inflammation inhibitory activities of methanol extract (ME) of fruiting bodies of P. pulmonarius were evaluted. The 1,1-diphenyl-2-picryl-hydrazy free radical scavenging activity of ME at 2.0 mg/mL was comparable to that of butylated hydroxytoluene, the standard reference. The ME exhibited significantly higher hydroxyl radical scavenging activity than butylated hydroxytoluene. ME showed slightly lower but moderate inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase than galantamine, a standard AChE inhibitor. It also exhibited protective effect against cytotoxicity to PC-12 cells induced by glutamate ($10{\sim}100{\mu}g/mL$), inhibitory effect on nitric oxide (NO) production and inducible nitric oxide synthase protein expression in lipopolysaccharide-stimulated RAW 264.7 macrophages, and carrageenan-induced paw edema in a rat model. High-performance liquid chromatography analysis revealed the ME of P. pulmonarius contained at least 10 phenolic compounds and some of them were identified by the comparison with known standard phenolics. Taken together, our results demonstrate that fruiting bodies of P. pulmonarius possess antioxidant, anti-cholinesterase, and inflammation inhibitory activities.

• Journal of Preventive Medicine and Public Health
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• v.16 no.1
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• pp.51-58
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• 1983

This study was carried out to obtain the basic data for the preverition of chronic poisonig by organic phosphate pesticides. 6 sprayers who participated in the summer pest control programs of Jeonju city were chosen as the subjects in this study. Pesticides which were spread in the period of study are DDVP (1.09%), dursban (1.8%) and dibrom (1.9%). And from May 16, 1983 to Aug. 22, 1983, plasma cholinesterase activity, hematological and biochemical parameters were measured with several physical examinations for each sprayers and controls. Major findings are as following; 1. Before pesticides were sprayed, plasma cholinesterase were $7.32{\pm}1.76{\mu}M/20{\mu}l/hr$. in sprayers and $7.13{\pm}1.39{\mu}M/20{\mu}l/hr$. in the control group (p>0.05). 2. At 60th day of spraying, plasma cholinesterase activity of sprayers was $6.78{\pm}2.01{\mu}M/20{\mu}l/hr$. which is significantly decreased from the pre-exposed value (p<0.01), but plasma cholinesterease activity in the control group was not changed. 3. The specific findings which suggested to organophosphorous poisoning were not found through the period of study. 4. Hematological and bichemical parameters were not sigricantly changed in the both groups.

• Journal of Pharmacopuncture
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• v.22 no.4
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• pp.231-238
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• 2019

Objectives: Alzheimer's disease (AD), an overwhelming neurodegenerative disease, has deleterious effects on the brain that consequently causes memory loss and language impairment. This study was intended to investigate the neuroprotective activity of the two essential oils (EOs) from Iranian Pistacia khinjuk (PK) leaves and Allium sativum (AS) cloves against β-Amyloid 25-35 (Aβ25-35) induced elevation of cholinesterase enzymes in AD. Methods: The EOs of PK (PKEO) and AS (ASEO) were prepared and analyzed in terms of extraction yield, phenolic content, and cholinergic markers in vitro. Moreover, both were administered orally to adult male Wistar rats at concentrations of 1, 2, and 3%. The inhibitory potential of PKEO and ASEO was compared with Donepezil (0.75 mg/kg) against the high activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Results: PKEO reached an inhibition rate of 83.6% and 81.4% against AChE and BChE, respectively. ASEO had lower anti-cholinesterase activity (65.4% and 31.5% for the inhibition AChE and BChE). PKEO was found to have more phenolic content than ASEO. A significantly positive correlation was observed between the total phenolics and anti-cholinesterase potential. In rats, both EOs decreased the enzyme activity in a concentration-dependent manner. As compared with Donepezil, the significant difference in the AChE and BChE inhibition occurred as rats were treated with PKEO 3% (p < 0.05). Conclusion: It could be concluded that PKEO and ASEO are potent inhibitors of AChE and BChE in rats that hold promise to be used for the treatment of AD.

• Environmental Analysis Health and Toxicology
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• v.2 no.1_2
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• pp.17-24
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• 1987

Changes in cholinesterase (ChE) activity, electrophoretic pattern of ChE and histopathologic state on the mice serum, brain and liver by administration of organophos-phorous insecticides were studied. The mice ChE activities on serum, brain and liver decreased by increasing of concentration and time both administration of malathion and DDVP, whereas on serum and brain the activities of the 7 days after administration decreased, and then presented the gradually slight recovery in course of time. The ChE on serum and liver showed many isozyme bands by polyacrylamide gel electrophoresis but several on brain. And isozyme bands disappeared and diffused by administration of organophosphorous insecticides and development of time. The mice liver with administration group of malathion on histopathologic test showed midzonal necrosis between central vein and portal area, and with administration group of DDVP mainly presented portal necrosis on location of potal area.

• YAKHAK HOEJI
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• v.39 no.4
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• pp.450-460
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• 1995

The acute toxicity of fthalide in rat was studied in vivo by the observations of the changes in hematogram, serological parameters, content of cytochrome p-450, activities of NADPH-cytochrom c reductase, glucose-6-phosphatase, and the contents of cholinesterase and carboxylesterase in liver. Fthabde is a practically non-toxic substance(LD50 is 3.86g/kg), but rats were intoxicated with fthabde at a oral dose of 100 mg/kg for 12 days. WBC were significantly decreased and activities of ALT and LDH, on the cotrary, the content of glucose in serum were slightly increased. Cytochrome p-450 and lipid peroxide in liver were significantly increased in the fthalide-intoxicated rats. The longer administration of fthalide showed further increase of carboxylesterase activity in liver and serum, but decrease of activities of glucose-6-phosphatase and cholinesterase in liver and serum. These results show that fthatide can induce the hepatocellular injury and neurotoxicity.

• Proceedings of the Korean Society of Veterinary Clinics Conference
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• 2009.10a
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• pp.207-207
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• 2009

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.3 no.1
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• pp.62-67
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• 1993

This study aims at investigating the relationships between the urinary mercury concentration and blood zinc-protoportphyrin, serum cholinestrase activity, making 149 workers exposed to mercury vapor and 68 workers who were not exposed to mercury among the workers in a flurorescent lamp manufactureing factory an object of this investigation. The results are as follows ; 1. In an exposed group the number of those whose urinary mercury concentration showed over $100{\mu}g/l$ was 21 persons (14.3%) among 147 workers. The average urinary mercury concentration was $52.1{\pm}46.1{\mu}g/l$($1.8-361.2{\mu}g/l$), which proved to be higher than the average concentration in a control group. 2. In an exposed group, the average concentration of blood zinc-protoporphyrin was $27.8{\pm}12.5{\mu}g/dl$($12.2-101.5{\mu}g/dl$), which proved to be somewhat higher than the average concentration in a control group. But it did not show a significant difference. 3. In an exposed group, the average concentration of serum cholinesterase activity showed $1936.7{\pm}341.0IU/l$(1,120,0-2,8750IU/l), which proved to be lower than the average concentration in a control group. 4. The relational coefficient between urinary mercury concentration and blool zinc-protoporphyrin, serum cholinesterase activity of the whole workers exposed to mercury showed little difference. While the relational coefficient between the urinary mercury concentration and blood zinc-protoporphyrin of the workers whose urinary mercury concentration showed over $100{\mu}g/l$ was relatively high, which was 0.62.

• Journal of The Korean Society of Clinical Toxicology
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• v.4 no.2
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• pp.113-121
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• 2006

Purpose: Previous studies have reported that plasma cholinesterase (AchE) concentration can serve as a useful prognostic parameter in cases of acute organophosphate (OP) poisoning. However, there has been considerable disagreement regarding the degree of its prognostic value. Earlier cross-sectional and one- time point studies were plagued with methodologic flaws, making it difficult to interpret their results. The purpose of this study was to clarify the prognostic value of time-variable cholinesterase levels and their relationship with clinical outcomes in OP poisoning. Methods: We reviewed medical and intensive care records of patients with acute OP poisoning admitted to our emergency department between March 1998 and Sep 2006. We collected patient information regarding poisoning, clinical, and demographic features. Patients were assessed for clinical outcomes and AchE concentrations on days 1, 2, 3, 5, and 7 and on the final day. Results: During the study period, 58 patients were enrolled in this study. There was a statistically significant difference in the AchE differentials on 1-3 days for patients requiring mechanical ventilation and for patients with mild poisoning (p<0.05). Also, the decrease in the log AchE concentration correlated with longer durations of mechanical ventilation (r=-0.411, p=0.002). Conclusion: In severe OP poising, measurements of time-variable AchE concentrations can be helpful in the prediction of mortality, the development of intermediate syndrome, and duration of mechanical ventilation.

• Bulletin of the Korean Chemical Society
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• v.35 no.6
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• pp.1681-1686
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• 2014

A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.