• Archives of Pharmacal Research
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• 제27권1호
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• pp.53-56
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• 2004

In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$/ values of compounds 1 and 2 were 33.6 (79 $\muM$) and 10.0 (52 $\muM$) $\mu$g/mL, respectively.

• 생약학회지
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• 제23권2호
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• pp.106-114
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• 1992

The acute toxicity and the effect of steam distillate obtained from several plant mixtures (G-3) on the reactivation of brain, lung, and blood acetylcholinesterase (AChE) activity, and recovery from other toxic symptoms following intoxication by organophosphate pesticides were investigated in mice and mudfish. Administration of G-3 $(50{\sim}100\;ml/kg,\;i.p.)$ immediately or 30 min prior to Diazinon or Sumithion treatments, respectively, resulted in a significant reactivation of AChE activity in brain, lung, and blood, their potencies being almost equipotent to those of 2-PAM, one of well-known antidotes. G-3 itself exhibited almost no acute toxicity even at the highest dose employed, and without effect on the inhibition of hepatic drug metabolism function following organophosphate administrations. G-3 showed a significant diminution of the death rate in mudfish as well as in mice intoxicated by Diazinon.

• 생약학회지
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• 제34권1호통권132호
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• pp.14-17
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• 2003

In the course of screening Korean natural plants for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the leaves of Securinega suffruticosa showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of dihydrosecurinine, as a active principle. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$ value of dihydrosecurinine was $18.9\;{\mu}g$.

• 한국응용곤충학회지
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• 제43권4호
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• pp.317-322
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• 2004

배추좀나방의 발육단계별 indoxacarb의 살충활성, 침투이행성 및 잔효성을 조사하였고, esterase, acetylcholinesterase, glutathione S-transferase 등의 효소활성에 미치는 영향을 검토하였다. 배추좀나방 유충에 대해서 높은 살충효과를 나타내었으나, 알과 번데기에 대해서는 살충율이 $10\%$이하이었다. 엽면침투이행성과 근부침투이행성의 효과는 없었으며, 잔효성은 10일째까지 $80\%$의 살충효과를 유지하였다. Indoxacarb는 esterase와 glutathione S-transferase의 활성은 저해하지 않았지만 acetylcholinesterase의 활성을 저해하였다.

• 동의신경정신과학회지
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• 제19권2호
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• pp.65-75
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• 2008

Objective : This experiment was designed to investigate the effect of the KBHT and PMCMT extract on protecting microglia and inhibiting acetylcholinesterase and oxidants. Method : The effects of the KBHT and PMCMT extract on cell death of BV2 microglial cell line treated by ${\gamma}$ ; expression of NO, ROS in BV2 microglial cell line treated by lipopolysaccharide(LPS) ; AChE activity in PC-12 cell treated by NGF were investigated, respectively. Result : The KBHT and PMCMT extract significantly increased cell viability in BV2 microglial cell line treated with ${\gamma}$. The KBHT and PMCMT extract suppressed the NO and ROS production in BV2 microglial cell line treated by LPS. The KBHT and PMCMT extract groups also showed inhibition of AChE activity in PC-12 cell line. Conclusion : According to the above result, it is suggested that the KBHT and PMCMT extract might be usefully applied for prevention and treatment of Alzheimer' s disease.

• 동의생리병리학회지
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• 제22권5호
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• pp.1276-1282
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• 2008

This experiment was designed to investigate the effect of the ODTCMT and DDTCMT extract on protecting microglia and inhibiting acetylcholinesterase and oxidants. The effects of the ODTCMT and DDTCMT extract on cell death of BV2 microglial cell line treated by $IFN-{\gamma}$ ; expression of NO, ROS in BV2 microglial cell line treated by lipopolysaccharide (LPS) ; AChE activity in PC-12 cell treated by NGF were investigated, respectively. The ODTCMT and DDTCMT extract significantly increased cell viability in BV2 microglial cell line treated with $IFN-\nu$. The ODTCMT and DDTCMT extract suppressed the NO and RDS production in BV2 microglial cell line treated by LPS. The ODTCMT and DDTCMT extract groups also showed inhibition of AChE activity in PC-12 cell line. According to the above result, it is suggested that the ODTCMT and DDTCMT extract might be usefully applied for prevention and treatment of Alzheimer's disease. OnDam-TanghapChongMyoung-Tang (ODTCMT), DoDam-TanghapChongMyoung-Tang (DDTCMT), Microglia, acetylcholinesterase, ROS

• 동의생리병리학회지
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• 제22권1호
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• pp.120-125
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• 2008

This experiment was designed to investigate the effect of the CBD and SJT extract on protecting microglia and inhibiting acetylcholinesterase and oxidants. The effects of the CBD and SJT extract on cell death of BV2 microglial cell line treated by $IFN-{\gamma}$ ; expression of NO, ROS in BV2 microglial cell line treated by lipopolysaccharide(LPS) ; AChE activity in PC-12 cell treated by NGF were investigated, respectively. The CBD and SJT extract significantly increased cell viability in BV2 microglial cell line treated with $IFN-{\gamma}$. The CBD and SJT extract suppressed the NO and ROS production in BV2 microglial cell line treated by LPS. The CBD and SJT extract groups also showed inhibition of AChE activity in PC-12 cell line. According to the above result, it is suggested that the CBD and SJT extract might be usefully applied for prevention and treatment of Alzheimer's disease.

• 약학회지
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• 제51권6호
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• pp.409-414
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• 2007

Acetylcholinesterase (AChE) plays a role in the progression of Alzheimer's disease (AD). In this study, we examined the improving effect of L-theanine, a major amino acid in Japanese green tea (Camellia sinensis) on the scopolamine (1 mg/kg/mouse)-induced memory dysfunction in mice. Treatment with L-theanine (2, 4 mg/kg/mouse p.o.) in the drinking water for 7 days reversed the scopolamine-induced latency time and distance in the water maze test, latency time in the passive avoidance test, and inhibited AChE activity. This study suggests that L-theanine may be a useful agent for prevention of progression of AD.

• 한국약용작물학회지
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• 제17권6호
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• pp.434-438
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• 2009

For the development of a new antidementia functional food or alternative drug using agricultural products, Job's tears (Coix lachrymajobi L.), which shows high acetylcholinesterase (AChE) inhibitory activity (55.1%) was selected and the extraction conditions of AChE inhibitor were optimized. AChE inhibitor of Job's tears was maximally extracted when it was treated with 60% methanol at $40^{\circ}C$ for 6 h. The AChE inhibitor of the methanol extracts was partially purified by systematic solvent extraction, thin layer chromatography, silica gel chromatography and reverse-phase HPLC and the partial purified AChE inhibitor with inhibitory activity ($IC_{50}$) of $0.608\;{\mu}g$ was obtained. The partial purified AChE inhibitor was soluble in methanol and hexane, and insoluble in water. Its maximum absorption spectra was 230 nm and also it was stable in the range of $30^{\circ}C$ and $70^{\circ}C$ and pH 4.0-8.0 for 1 h.

• 약학회지
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• 제38권5호
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• pp.511-515
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• 1994

We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.