• Archives of Pharmacal Research
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• v.25 no.6
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• pp.817-819
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• 2002

In the course of screening Korean natural products for acetylcholinesterase (AChE) inhibitory activity, it was found that a methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) showed significant inhibitory effects on AChE. Corynoline isolated from this plant inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$ value of corynoline was $30.6{\;}{\mu}M$. The AChE inhibitory activity of corynoline was reversible and noncompetitive.

• The Korean Journal of Mycology
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• v.44 no.4
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• pp.314-317
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• 2016

To develop a new anti-dementia acetylcholinesterase (AChE) inhibitor from edible mushrooms, AChE inhibitory activities were determined on water and ethanol extracts of various edible mushrooms from oriental medicine markets and agriculture markets. As a result, the 70% ethanol extract from Pholiota adiposa fruiting body had the highest AChE inhibitory activity of 30.6, and its water extract also had an AChE inhibitory activity of 23.8%. Therefore, we finally selected P. adiposa as a potent anti-dementia AChE inhibitor-containing mushroom. The AChE inhibitor of P. adiposa was maximally extracted when its fruiting body was treated with water for 3hr at $70^{\circ}C$ and 70% ethanol for 12 hr at $70^{\circ}C$, respectively.

• The Korea Journal of Herbology
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• v.24 no.4
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• pp.121-126
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• 2009

Objectives : To evaluate the radical scavenging and acetylcholinesterase (AChE) inhibitory activities of the ethylacetate (EtOAc)-soluble portion of a methanolic extract of Aster yomena, three different assay systems were performed. Methods : The antioxidant activity of A. yomena extract was tested as its capacity to scavenging free radicals of DPPH and $ABTS^+$, which has been widely used to evaluate the antioxidant activity of natural products from plant sources. AChE inhibitory activity was tested against mouse brain AChE by spectrophotometric method of Ellman using ELISA microplate reader. Results : The methanolic extract of A. yomena was fractionated and the EtOAc-soluble portion showed significant AChE inhibitory and free radical scavenging effects. Also the EtOAc-soluble portion revealed the highest phenolic contents as compared to the other extracts. Conclusions : These results indicate that phenolic compounds may be important constituents that give rise to the anti-AChE and antioxidative activities of A. yomena extract. Further phytochemical studies on this plant, for nutraceutical or pharmaceutical application, are warranted.

• Archives of Pharmacal Research
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• v.26 no.9
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• pp.735-738
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• 2003

The methanolic extract of the twigs of Celtis chinensis was found to show inhibitory activity on acetylcholinesterase (AChE), an enzyme that plays a role in the metabolic hydrolysis of ACh. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of N-p-coumaroyl tyramine. as an inhibitor on AChE. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_50$ value of trans-N-p-coumaroyl tyramine was 34.5 $\mu$g/mL (122 $\mu$M).

• CELLMED
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• v.2 no.2
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• pp.19.1-19.6
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• 2012

$Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

• The Korean Journal of Food And Nutrition
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• v.31 no.2
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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.

• 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.

• Journal of Oriental Neuropsychiatry
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• v.17 no.1
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• pp.1-16
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• 2006

Objective: An water extract of the Hwang-Ryun-Chung-Sim-Um (HRC) was assessed to determine the mechanisms of its antioxidant activity. In addition, the HRC was examined in vitro for the inhibitory effect on the acetylcholinesterse (AChE). Methods: The HRC exhibited a concentration-treatment; scavenging ${\alpha},{\alpha}-diphenyl-{\beta}-picrylhydrazyl$ (DPPH) radical, linoleic acid oxidation in a thiocyanate assay system, hydroxyl radical-induced DNA nicking. We investigated mRNA levels such as catalase activity, superoxide-dismutase and glutathione peroxidase. The water extract of HRC showed inhibitory effect on AChE activity. Result: The HRC extract showed dose-dependent free radical scavenging activity, including DPPH radicals and hydroxyl radicals, using different system. The HRC was also found to be effective in protecting plasmid DNA against the strand breakage induced by Hydroxyl radicals in Fenton's reaction mixture. Futhermore, catalase mRNA expression levels increased, but SOD1 and MnSOD was not expressed. HRC in a various concentration-dependent decreased AChE mRNA levels and inhibitory effect showed AChE. Conclusion: According to the above results, it is supposed that HRC is applicable to the Dementia-type of Alzheimer clinically.

• 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.

• Korean Journal of Pharmacognosy
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• v.47 no.3
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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.