• 한국물환경학회지
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• 제22권2호
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• pp.364-369
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• 2006

파라치온에 노출된 붕어의 뇌, 안구, 근육 및 혈청의 AChE 활성 변화를 조사한 결과 파라치온 $63{\mu}g/L$ 농도 이상에서 유의하게 감소하는 경향을 보였다. 실험종료 시 AChE 활성은 뇌에서 79.1~92.4%, 안구에서 76.0~91.5%, 근육에서 89.7~97.6% 및 혈청에서 68.9~78.0% 감소하였다. 실험기간동안 유의한 생존율 변화는 관찰되지 않았으나, 유영이상 및 경련을 보였다. 또한 파라치온에 노출된 붕어의 형태변화는 척추측만(scoliosis)이 관찰되었는데 이러한 변화는 파라치온 $190{\mu}g/L$ 농도는 15%, $380{\mu}g/L$에서는 75%로 관찰되었다. 따라서 붕어의 AChE 활성과 그 밖의 행동 및 형태적 특성은 자연수계에서 파라치온 오염을 추정할 수 있는 생물학적 모니터닝 도구로 활용할 수 있다.

• BMB Reports
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• 제31권3호
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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.

• 한국식품영양과학회지
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• 제41권10호
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• pp.1395-1401
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• 2012

생강과 식물의 인지기능 관련 활성을 검토하고 종류와 산지에 따른 차이를 비교하기 위하여, 시중에서 많이 사용되고 고품질로 알려져 있는 국산 생강과 울금, 미얀마산 울금과 인도산 강황의 항산화 효과, GABA 함량, 활성성분 분석, 그리고 AChE 억제 활성을 측정하였다. 미얀마산 울금 에탄올추출물에서 총 폴리페놀(98 ${\mu}g/mg$), curcumin(97.1 ${\mu}g/mg$), GABA 함량(1.31 ${\mu}g/mg$)이 가장 높았으며, DPPH, ABTS 라디칼 소거능 및 AChE 저해능도 비교적 높게 나타났다. 한편, 인도산 강황 추출물도 미얀마산 울금과 비슷한 항산화 효과와 AChE 저해 효과가 나타났으나, curcumin (12.2 ${\mu}g/mg$)과 GABA(0.04 ${\mu}g/mg$) 함량은 매우 낮게 나타났다. 국산 생강과 울금 추출물의 경우 총 폴리페놀 함량은 비슷하였으나(39.7~42.5 ${\mu}g/mg$) 6-gingerol, 6-shogaol 등의 진저롤류를 함유하고 있는 생강 추출물에서 울금보다 높은 라디칼 소거능, 특히 강한 ABTS 라디칼 소거능을 나타내었으며, AChE 저해능은 두 추출물 모두 매우 낮은 것으로 나타났다. 국내산 2가지 추출물의 GABA 함량(약 1.11 ${\mu}g/mg$)은 미얀마산 울금과 비슷한 정도로 높게 검출되어 라디칼 소거능과 AChE 억제능은 GABA 함량과는 상관성이 없었다. 따라서 본 실험에 사용한 4가지 생강과 식물 추출물의 AChE 억제능은 총 폴리페놀 함량과 밀접한 관계가 있으며, curcumin 함량, 라디칼 소거능 및 GABA 함량과는 직접적인 상관관계가 없는 것으로 나타났다. 이상의 결과와 같이, 미얀마산 울금은 나머지 추출물과 비교하여 높은 항산화 활성과 curcumin 및 GABA 함량, 그리고 비교적 높은 AChE 저해활성을 갖는 강력한 인지능 개선 소재로 활용될 수 있을것으로 사료된다.

• 한국식품영양학회지
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• 제31권2호
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• pp.213-219
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• 2018

This study was performed to determine the optimal time of harvest for ramie leaves with the two varieties (Seocheon Seobang and Seoncheon Baekpi) by comparison of physiological activity and physicochemical characteristics. The crude protein, minerals, ascorbic acid, folate, chlorophyll, ACE inhibitory activity and AChE inhibitory activity were determined. The amount of crude protein in ramie leaf, which was collected in Seocheon-gun, Chungcheongnam-do, grew up steadily from early May to September. The content of calcium in was higher in Baekpi than in Seobang. Seobang displayed its highest value of 3,569.90 mg% in September, while Baekpi displayed its highest value of 3,163.84 mg% in October. Although, folate and vitamin C contents in the two varieties were slightly different, they were higher as the growth date grew in October. The highest value of chlorophyll content was observed in October, which was later in the vegetative state. ACE inhibitory activity and AChE inhibitory activity appeared to be higher in Baekpi than in Seobang. Between June and August, ACE inhibitory activity was highest in Baekpi variety.

• 대한약침학회지
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• 제22권4호
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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.

• 동의신경정신과학회지
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• 제28권2호
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• pp.123-136
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• 2017

Objectives: The objective of this study is to investigate the anti-amnesic effects of AR, Aucklandiae Radix, ground powder on scopolamine (Sco)-induced memory impairment in mice (C57BL/6) through its favorable acetylcholine (ACh) and acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expression, and antioxidant effect. Methods: Six groups, a total of 20 intact or 100 Sco treated mice, were selected based on their body weights and were used in this study. Half of the mice in each group were used for the passive avoidance task test and the measurements of hippocampus ACh content, AChE activity and ChAT mRNA expression. The remaining half of the mice in each group were used for the Morris water maze test and cerebral antioxidant defense system measurement. Results: Marked decreases in step-through latency times in the passive avoidance task test and increases in escape latency times in the Morris water maze test were observed with decreases in the hippocampus ACh content and ChAT mRNA expression, and increases in the hippocampal AChE activities, as a result of Sco intraperitoneal treatment, in the present study. In addition, destruction of the cerebral cortex antioxidant defense systems was observed in Sco control mice as compared with intact vehicle control mice. However, 28 days of continuous oral pre-treatment with AR ground powder at doses of 400, 200 and 100 mg/kg markedly and dose-dependently inhibited the Sco treatment-related amnesia. Conclusions: The results prove that oral administration of AR ground powder reduces Sco-induced memory impairment. This is because it can preserve ACh, related to ChAT mRNA expression, cause AChE inhibition, and activate the cerebral antioxidant defense system.

• 동의신경정신과학회지
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• 제30권3호
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• pp.221-235
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• 2019

Objectives: The purpose of this study was to confirm the anti-amnesic effects of Bunsimgieum (BSGE) through its favorable acetylcholine (ACh) and, acetylcholinesterase (AChE) activity, choline acetyltransferase (ChAT) mRNA expressions, and antioxidant effect on scopolamine (Sco)-induced memory impairment in C57BL/6 mice. Methods: Six groups, a total of 20 intact or 100 Sco-induced mice were used in this study, based on their body weight. Half of each group underwent passive avoidance tests and the measurement of hippocampus AChE activity, ACh content, and ChAT mRNA expression, The remaining half of each group underwent a Morris water-maze test and antioxidant defense system measurement as well. Results: Significant reductions in the step-through latency times from the passive avoidance test and reductions in the escape latency times from the Morris water-maze test were observed with increases of hippocampal AChE activities and, reductions in ACh contents and ChAT mRNA expression in hippocampus, as a result of Sco intraperitoneal treatment, in this study. Additionally, the increases in cerebral cortical MDA levels and, reductions in GSH contents, SOD activities, and CAT activities were demonstrated in the Sco control mice compared with the intact vehicle control mice, respectively. However, 28 days of consecutive oral pre-treatment of BSGE hot water extracts of 400, 200, and 100 mg/kg, respectively, markedly and dose-dependently inhibited Sco treatment-related amnesia. Conclusions: The results demonstrate that the oral administration of BSGE hot water extracts reduces Sco-induced memory impairment, through preserving ACh, related to ChAT mRNA expressions, causes AChE inhibition, and enhances the cerebral antioxidant defense system.

• 생약학회지
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• 제47권3호
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• pp.287-294
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• 2016

Acetylcholinesterase (AChE) activation and amyloid-${\beta}$ ($A{\beta}$) aggregation are major biological markers of Alzheimer's disease. In the present study, we evaluated the inhibitory effects of 50 kinds of herbal formulas on AChE activity and $A{\beta}$ aggregation. Among them, Hwanglyeonhaedok-tang, Cheonwangbosim-dan, Makmundong-tang, and Gamisoyo-san had a potent effects on the inhbition of AChE activity. Sosiho-tang, Samsoeum, Cheonsimyeunjaeum, and Bunsimgieum exerted to have the inhibitory activity on $A{\beta}$ aggregation. In addition, these 8 herbal formulas showed the 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, indicating their antioxidant activities.

• Archives of Pharmacal Research
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• 제19권6호
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• pp.520-528
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• 1996

The involvement of the cyclic AMP (cAMP) effector system in the release of endogenous dopamine and acetylcholine from the rat neostriatum was assessed. Forskolin, an activator of adenylate cyclase, was used to enhance cAMP production, and the consequence of this enhancement on the spontaneous and potassium stimulated release of dopamine and acetylcholine was evaluated. Neostriatal slices were prepared from Fischer 344 rats and after a preincubation period the release of each endogenous neurotransmitter was measured from the same slice preparation. To measure acetylcholine release the slice acetylcholinesterase (AChE) activity was inhibited with physostigmine, but the release from slices with intact AChE activity was also determined (choline, instead of acetylcholine was detected in the medium). Under both conditions forskolin induced a significant dose-dependent increase in the potassium-evoked release of dopamine. In the same tissue preparations the release of neither acetylcholine (AChE inhibited) nor choline (AChE intact) was affected by forskolin. The results indicate that the CAMP second messenger system might be involved in neuronal mechanisms that enhance neostriatal dopamine release, but stimulation of this second messenger by forskolin does not further enhance neostriatal acetylcholine release.

• 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.