• Journal of Ginseng Research
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• v.35 no.4
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• pp.421-428
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• 2011

This study evaluated cholineresterase inhibitory activity of Korean white ginseng extract (WGE), red ginseng extract (RGE), and black ginseng extract (BGE) and the cholinergic effect on scopolamine (SCOP)-induced amnesic mice. WGE, RGE, and BGE inhibited acetylcholineserase (AChE), as well as butyrylcholineserase (BuChE) in a concentration-dependent manner. BGE presented strong inhibition of AChE with an $IC_{50}$ value of 1.72 mg/mL, followed by WGE (5.89 mg/mL), RGE (6.30 mg/mL), respectively. The inhibitory activity of the three ginseng extracts on BuChE showed similar values among the groups. To better understand the mechanisms of the possible effect of ginseng extract on the cholinergic function, this study assessed the expression of the cholinergic markers of choline acetyltransferase (ChAT) and AChE using western blot and RT-PCR analysis in the brains of amnesic mice. Treatment with ginseng extracts led to inhibition of AChE expression and, the activation of ChAT expression in the hippocampus and the cerebral cortex of amnesic mice as induced by SCOP. The results suggest that ginseng extracts including BGE, appear to modulate the metabolism of acetylchoine (ACh), which would greatly increase synaptic ACh levels and most potently revert SCOP-induced amnesia.

• Korean Journal of Environmental Agriculture
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• v.6 no.2
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• pp.77-83
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• 1987

Present study was carried out to elucidate the effect of phorate (0,0-dietyl S-ethylthiomethyl phosphorodithioate), an organophosphorus insecticide on the acetylcholinesterase(AChE) and cholinesterase(ChE) activity in the chicken brain and plasma. The inhibitory effect of phorate and its metabolites on AChE and ChE activity was also increased in the order of phorate (p=S,S)$(p=S,SO_2)<phoratoxon$ (p=O,S)$(P=O,SO_2)$. Acute oral $LD_{50}$ of phorate was 1.02mg/kg. After oral administration of phorate, the activity of plasma ChE was inhibited more rapidly then that of brain AChE, whereas recovery of plasma ChE activity was more rapid than that of brain AChE activity.

• Bulletin of the Korean Chemical Society
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• v.28 no.2
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• pp.225-228
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• 2007

Lipoic acid (LA) is a multifunctional antioxidant against a variety of ROS. Nitrone acts as free radical spin trap and exhibits neuroprotective activity. Thus, LA-nitrone derivatives (6, 7, 8, and 9) were synthesized and screened as an antioxidant and inhibitors for cholinesterases. Even though the antioxidant effect of LA-nitrone derivatives was not improved, they turned out to be effective inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in μM range.

• Journal of The Korean Society of Clinical Toxicology
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• v.6 no.1
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• pp.32-36
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• 2008

Purpose: The major complication of acute organophosphate (OP) poisoning is respiratory failure as a result of cholinergic toxicity. Many clinicians find it difficult to predict the optimal time to initiate mechanical ventilation (MV) weaning, and as a result have tended to provide a prolonged ventilator support period. The purpose of this study is to determine any clinical predictors based on patients characteristics and laboratory findings to assist in the optimal timing of mechanical ventilator weaning. Methods: We reviewed medical and intensive care records of 44 patients with acute OP poisoning who required mechanical ventilation admitted to medical intensive care unit between July 1998 and June 2007. Patient information regarding the poisoning, clinical data and demographic features, APACHE II score, laboratory data, and serial cholinesterase (chE) levels were collected. Base on the time period of MV, the patients were divided into two groups: early group (wean time < 7 days, n = 28) and delayed group (${\geq}$ 7 days, n = 16). Patients were assessed for any clinical characteristics and predictors associated with the MV weaning period. Results: During the study period, 44 patients were enrolled in this study. We obtained the sensitivity and specificity values of predictors in the late weaning group. APACHE II score and a reciprocal convert of hypoxic index but specificity (83.8%) is only APACHE II score. Also, the chE concentration (rho = -0.517, p = 0.026) and APACHE II score (rho = 0.827, p < 0.001) correlated with a longer mechanical ventilation duration. Conclusion: In patients with acute OP poisoning who required mechanical ventilation, the APACHE II scoring system on a point scale of less than 17 and decrements in cholinesterase levels on 1-3 days were good predictors of delayed MV weaning.

• Bulletin of the Korean Chemical Society
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• v.32 no.8
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• pp.2593-2598
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• 2011

Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE ($IC_{50}=2.3{\pm}0.3{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a hyperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is $2.32{\pm}0.15{\mu}M$.

• Applied Biological Chemistry
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• v.29 no.3
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• pp.324-330
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• 1986

The responses of brain acetylcholinesterase(Ach-E) and plasma cholinesterase (Ch-E) activities were studied in chicknes given oral doses of Terbufos(S-tert-butyl thiomethyl 0,0-diethyl phosphorodithioate), an organophosphorus insecticide. The acute oral $LD_{50}$ of terbufos was 1.82mg/kg. The activity of plasma Ch-E was inhibited more rapidly than that of brain Ach-E, whereas recovery of plasma Ch-E activity was more rapid than that of brain Ach-E. Recovery of brain Ach-E and plasma Ch-E was followed the model $Y=a+b(log_{10}X)$. Brain Ach-E activity and plasma Ch-E were inhibited 83% and 94%, respectively, at 60min after administered oral $LD_{50}$. Brain Ach-E and plasma Ch-E was inhibited in vitro by Terbufos

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.259.3-260
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• 2003

Alzheimer's disease(AD) is the most common cause of senile dementia in elderly people and the causes of AD are currently not fully understood. However, AD is generally understood to be associated with reduced levels of acetylcholine in the brain as cholinergic neurons are lost and cholinergic neurotransmission declines. There are growing evidences that two types of cholinesterase(ChE), i.e., acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) both play important roles in the regulation of acetylcholine level in brain and thus may have a crucial role in the development and progression of AD. (omitted)

• Bulletin of the Korean Chemical Society
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• v.34 no.4
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• pp.1025-1029
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• 2013

In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between ${\alpha}$-lipoic acid (ALA) and polyphenols (PPs) connected with neutral 2-(2-aminoethoxy)ethanol linker (linker-1) showed new biological activity such as butyrylcholinesterase (BuChE) inhibition. In order to increase the binding affinity of the hybrid compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)ethanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The $IC_{50}$ values of the linker-2 hybrid molecules for BuChE inhibition were lower than those of linker-1 hybrid molecules (except 9-2) and they also had the same great selectivity for BuChE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl caffeic acid (10-2, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.44{\pm}0.24{\mu}M$). A kinetic study using 7-2 showed that it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is $4.3{\pm}0.09{\mu}M$.

• Journal of Society of Preventive Korean Medicine
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• v.4 no.2
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• pp.285-293
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• 2000

Objectives: We have accomplished a clinical research about counteracting the pesticides intoxication using oriental medical method and treatment. And we observed the preventive effect of Gamdu-tang(甘豆湯) to intoxication of Organophosphorus Insecticides. Material and Methods: The subjects were 8 volunteers who were healthy and not taking medications. we observed change of cholinesterase(ChE) activity in serum of them after exposed to pesticides Results and Conclusions : In this study of the preventive effects of Gamdu-tang(甘豆湯) on the intoxication of Organophosphate Insecticides, we evaluated that the decreasing value of ChE activity after spraying insecticides of Gamdu-tang medication group was smaller than non-medication group, but it was less significant(P>0.05 P<0.1). We had a difficult to gather participant in this study, so it's necessary for us to get together more larger group in the next study.

• Korean Journal of Plant Resources
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• v.31 no.5
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• pp.433-452
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• 2018

This study was conducted to select candidates from plant resources for the purpose of improving or treating Alzheimer's disease, a type of dementia. One hundred and eighty-four plant extracts at a final concentration of $100{\mu}g/ml$ were screened to determine their capacity to inhibit acetylcholinesterase (AChE) by in vitro assay. From this AChE assay, seven plant extracts - including methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark), methanol ext. of Nelumbo nucifera Gaertn (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), ethanol ext. of Cinnamomum cassia Blume(bark) and ethanol ext. of Carthamus tinctorius L. (fruit) - showed effective inhibition activity ranging from 18.7% to 63.1%. The selected extracts were testified their inhibition activities on AChE and BuChE (butyrylcholinesterase) at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the AChE assay, five extracts including methanol ext. of Nelumbo nucifera Gaertn. (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark) showed inhibition activity of 15.0%~73.5%, 19.5%~63.5%, 81.6%~58.5%, 69.9%~80.5%, and 54.8%~78.3%, respectively, at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the BuChE assay, the extracts of Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS (flower), and Coptis chinensis (rhizome) showed inhibitory capacities of 58.9~81.6%, 45.8%~72.4%, and 33.1%~55.4% at concentrations of 25, 50, 100, $200{\mu}g/ml$, respectively. In conclusion, it is suggested that Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS, Coptis chinensis (rhizome) and Phellaodendron amurense Rupr. (bark) could be selected as candidate materials for improving or treating Alzheimer's disease on the basis of further study.