• 대한약리학회지
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• 제6권1호
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• pp.45-55
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• 1970

It is well known that the uterine contractility is affected by sexual hormone. In this experiment, the authors attempted to study the influences of testosterone and estrogen or the uterine contractility to oxytocics. The contractile sensitivity of the excised uterine muscle of non-castrated and castrated rabbits with testosterone and estrogen 24 hours before experiment is observed respectively. And the cholinesterase activity and electrolytes (Na, K, Ca and Mg) in the uterine muscle are measured in order to study the relationship with contractile sensitivity and those changes. The results obtained were summarized as follows: 1. The contractile effect of spareng on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was markedly increased in small dose, but that of rabbits pretreated with testosterone was significantly increased in large dose, comparing with that of the control group. In castrated rabbits, the contractile sensitivity of the uterine muscle to spareng was significantly increased by pretreatment with estrogen in large dose but it was markedly decreased by pretreatment with testosterone in small dose. 2. The contractile effect of quinine on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was significantly decreased but that of castrated rabbits pretreated with both estrogen and testosterone were markedly increased comparing with that of the control group. 3. The cholinesterase activity in the uterine muscle of non-castrated rabbits was significantly increased by pretreatment with small dose of estrogen or large dose of testosterone, but that of castrated rabbits was markedly decreased by pretreatment with large dose of estrogen. 4. Na and K contents in the uterine muscle of non-castrated rabbits were markedly increased by pretreatment with both estrogen and testosterone, but that of castrated rabbits was significantly increased by pretreatment with small dose of estrogen. 5. Ca content in uterine muscle of non-castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone but increased by pretreatment of testosterone. In castrated rabbits, Ca content was significantly decreased by pretreatment with both estrogen and testosterone. 6. Mg content in the uterine muscle of non-castrated rabbits was markedly increased by pretreatment with estrogen and small dose of testosterone, but that of castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone.

• 농촌의학ㆍ지역보건
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• 제19권2호
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• pp.107-118
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• 1994

Health effects of pesticide among vinylhouse workers in Sangjoo County, Kyungpook Province were assessed by measuring cholinesterase, glutathion reductase, and methemoglobin. Activities of cholinesterases among vinylhouse workers and general farmers were 3.89U and 3.98U in serum and 5.29U and 5.50U in red blood cells, respectively. While levels of methemoglobin between vinylhouse workers(0.16%) and general farmers(0.17%) were very similar, glutathione reductase among vinylhouse workers were 8% lower than that of general farmers. Inhibition of RBC cholinesterase among vinylhouse workers was two times greater than general farmers, suggesting a greater exposure of vinylhouse workers to the organophosphate pesticides. Methemoglobin level among vinylhouse workers with more than or equal to 10 vinylhouse units was 13% higher than that of the workers with less than 10 units. Vinylhouse workers using protective gears during pesticide spray showed higher level of reduced glutathione and lower level of methemoglobin, as compared to the non-users. This indicates that protective gears play an important role against pesticide exposure. Vinylhouse workers practicing good personal hygiene showed a higher level of reduced glutathione, as compared to those with poor personal hygiene, indicating that personal hygiene is also an important factor in reducing pesticide exposure. The present study represents a first attempt to analyze cholinesterase, methemoglobin and glutathione reductase activities among the vinylhouse workers. While neither vinylhouse workers nor general farmers showed abnormal findings among biochemical parameters used in the present study, increased level of methemoglobin and decrease of glutathione reductase activity among vinylhouse workers suggest that these workers have been subject to a higher exposure of pesticide than general farmers.

• 대한예방의학회:학술대회논문집
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• 대한예방의학회 1995년도 제47차 추계 학술대회 연제집
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• pp.303-304
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• 1995

• 생약학회지
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• 제43권2호
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• pp.122-126
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• 2012

The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

• Bulletin of the Korean Chemical Society
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• 제28권2호
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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.

• 한국식품영양과학회지
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• 제29권2호
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• pp.193-197
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• 2000

The effects of black soybena extracts on enzymes activies of rat were evaluated in present study. Eighty-four male Sprague-Dawley rats weighing 100$\pm$10g were divided into twelve groups which consisted of black soybean extract, Pb and Cd solution, and black soybean extract plus Pb or Cd soln groups. The weight gain was increased in black soybean extracts and Pb soln solution group but decreased in Cd soln solution group. The results obtained form the experiment were as follows: Glutamate pyruvate trasaminase (GPT) and glutamate oxaloacetate oxaloacetate transaminase (GOT) activities were not significantly different among experimental groups. The lactate dehydrogenase (LDH) activities of black soybean extract administered groups were decreased than those of Pb and Cd solution group. Black soybean group increased cholinesterase (ChEase) activity as compared to administration of Pb and Cd soln group.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.206.2-206.2
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• 2003

In continuing search for bioactive compounds from Korean marine algae, we found cholinesterase-inhibitory activity in the methanolic extract of brown alga Sargassum sagamianum. After partitioning between CHCl$_3$ and 30% MeOH, the former layer was purified by a series of ODS flash, silica column, gel-filtration on Sephadex LH-20, and HPLC to give two farnesylacetone derivatives. Their structures were identified by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC$\sub$50/ values of 65.0∼48.0 ${\mu}$M and 34.0∼23.0 ${\mu}$M, respectively. (omitted)

• 대한한의학회지
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• 제25권4호
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• pp.1-7
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• 2004

Objective : This study was designed to examine the effects of orally administered Prunus persica water extract (PPE), which is used as herbal medicine, for treatment of Yu Xue (stasis of blood) and tacrine on the basal concentration of extracellular acetylcholine in the hippocampus of rats. Methods: To investigate the effects of PPE and tacrine on concentration of extracellular acetylcholine in the hippocampus of rats, the microdialysis technique, under the same experimental conditions, was used. And we used male Wistar rats which were 7 weeks of age and 210-290 g. PPE was extracted with boiling water, and the rats were anesthetized with pentobarbital Na. Their skulls were exposed and a hole was drilled for implantation of a microdialysis probe. In order to increase the recovery of acetylcholine, a probe with a long membrane was used. One day after surgery, the microdialysis probe was perfused with Ringer's solution at a flow rate of 1.5 l/min. The acetylcholine concentration in dialysis samples was measured by high-performance liquid chromatography (HPLC) with electrochemical detection. AChE activity was measured using the radiometric method, as described by Sherman. Results : The comparative effects of PPE and tacrine on hippocampal extracellular acetylcholine concentration was that these cholinesterase inhibitors produced dose-dependent increases in the extracellular acetylcholine concentration. And the effect of PPE and tacrine on rat brain AChE activity was that PPE produced maximal inhibition at 1 h after administration, when AChE activity was 44% of the intact level. AChE activity gradually recovered thereafter, and reached 78% of the intact level at 12 h after administration. Conclusion : In this study, PPE has a potent activity and a long-lasting effect on the central cholinergic system, in terms of the basal concentration of extracellular acetylcholine in the hippocampus and the AChE activity in the brain of rats. And oral administration of PPE increased dose-dependently the basal concentration of extracellular acetylcholine in the hippocampus of rats. PPE may be one of the more useful cholinesterase inhibitors for the treatment of Alzheimer's disease.

• Natural Product Sciences
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• 제26권2호
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• pp.165-170
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• 2020

Carica papaya is a medicinal and fruit plant owing biological activities including antioxidant, antiviral, antibacterial and anticancer. The present study aims to investigate the acetyl (AChE) and butyryl (BChE) cholinesterase inhibitory potentials of C. papaya extracts as well as their chemical compositions. The chemical composition of the active extract was identified using a gas chromatography-mass spectrometry (GC-MS). Ellman enzyme inhibition assay showed that the alkaloid-enriched leaf extract of C. papaya possessed significant anti-BChE activity with an enzyme inhibition of 75.9%. GC-MS analysis showed that the alkaloid extract composed mainly the carpaine (64.9%) - a major papaya alkaloid, and some minor constituents such as aliphatic hydrocarbons, terpenes and phenolics. Molecular docking of carpaine revealed that this molecule formed hydrogen bond and hydrophobic interactions with choline binding site and acyl pocket. This study provides some preliminary findings on the potential use of C. papaya leaf as an herbal supplement for the prevention and treatment of Alzheimer's disease.

• 생명과학회지
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• 제9권3호
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• pp.282-288
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• 1999

This study was designed as a part of efforts to investigate the biochemical pollutant markers for diagnosis of marine pollutions by changes in cholinesterase activity of the mussel (Mytilus coruscus) in South Sea of Korea. Acetylcholinesterase (AChE) activities in muscle of cultured mussels in South Sea were remarkably lower (20∼41%, respectively) than those of wild mussel in Pohang(control) of East Sea. Acetylcholine (Ach) activities in muscle of cultured mussels in South Sea were remarkably lower (15∼30%, respectively) than those of wild mussel in Pohang of East Sea. Monoamineoxidase (MAO-B) activities in muscle of cultured mussels in South Sea were significantly 2∼19% higher than those of wild mussel in Pohang of East Sea. It suggests that AChE, ACh and MAO-B activities in muscle of cultured mussels of South Sea may be used as the most effective mean in a biochemical markers for early warning of environmental damages caused by organophosphorus pesticides.