• The Korea Journal of Herbology
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• v.22 no.1
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• pp.7-12
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• 2007

Objectives : In Alzheimer's disease(AD), free radical oxidative stress caused by amyloid beta-peptide may lead to DNA damage, neuronal dysfunction, neurotoxicity and cell death, Hwangryunhaedok-tang(HHT) is traditionally used for the treatment of pyrogenetic diseases. To develop a new anti-AD drug from natural herb, HHT was selected and extracted in this study. Methods : The antioxidant activities of HHT water extract powder were examined by hydroxyl radical-induced DNA strand nicking assay, and antioxidative enzymes expression assay in H4IIE cell. In addition, HHT was examined for the inhibitory effect on the acetylcholinesterase(AChE) using by Ellman's coupled assay. Results: The HHT exhibit DNA protective effect in the hydroxyl radical-induced DNA Strand nicking assay, mRNA expression of superoxide dismutase and glutathione peroxidase were recovered at a normal level by HHT treatment in H4IIE cell. Furthermore, water extract of HHT showed inhibitory effect on AChE activity. Conclusion : These results suggest that HHT may be effective in delaying and preventing AD progression related to the free radical-induced DNA damage and AChE activity.

• The Korean Journal of Mycology
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• v.47 no.4
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• pp.337-346
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• 2019

To develop a new antidementia acetycholinesterase (AChE) inhibitor from edible mushrooms, the inhibitory effects on AChE of water and ethanol extracts from various edible mushrooms were measured. Among the tested compounds, 70% ethanol extracts from Tremella fuciformis showed the highest AChE inhibitory activity, at 25.3% (IC₅₀: 9.9 mg). Water extracts from the fruiting body of Pleurotus ostreatus (Heuktari) showed AChE inhibitory activity of 20.2% (IC₅₀: 12.4 mg). However, the yield (40.8%) from Pleurotus ostreatus (Heuktari) was higher than that from Tremella fuciformis (5.0%). Therefore, we selected Pleurotus ostreatus (Heuktari) as the most promising candidate for a mushroom containing anti-dementia AChE inhibitors. The AChE inhibitor from Pleurotus ostreatus (Heuktari) was optimally extracted when its fruiting body was treated with water for 6 h at 30℃. The anti-dementia effects of the partially purified AChE inhibitor from Pleurotus ostreatus (Heuktari) were observed in PC12 nerve cells.

• 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.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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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 $18.9\;{\mu}g$.

• Korean Journal of Medicinal Crop Science
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• v.17 no.6
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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.

• Korean Journal of Food Science and Technology
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• v.36 no.6
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• pp.1026-1031
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• 2004

Acetylcholinesterase inhibitory activity and protective effect against cytotoxicity of PC 12 cell induced by beta-amyloid protein and glutamate were examined in perilla seed methanol extract and its solvent fractions. Methanol extract of perilla seed showed dose-dependent acetylcholinesterase inhibitory activity, with n-butanol fraction showing strongest activity. Perilla seed methanol extract also decreased glutamate- and ${\beta}-amyloid$ protein $(A{\beta})-induced$ cytotoxicities of PC 12 cells dose-dependently. Formation of TBARS induced by $FeSO_{4^-}H_2O_2$ in rat brain was significantly reduced by perilla seed methanol extract, with strongest protective activity formation of TBARS shown in n-butanol fraction. Results suggest perilla seed methanol extract may attenuate actylcholinesterase activity and cytotoxicity induced by glutamate and ${\beta}-amyloid$ protein through suppression of oxidative stress.

• Journal of Life Science
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• v.23 no.12
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• pp.1525-1531
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• 2013

Baegilju is a famous traditional Korean wine made over the course of 100 days. The physiological functionalities of Baegilju were evaluated using different tests. The spectrophotometric method was used to determine the total concentration of polyphenolics and flavonoids and DPPH and ABTS radicals. A nitrite scavenging assay was used to evaluate antioxidant activity. The fibrin plate method was used for fibrinolysis and to evaluate angiotensin I converting enzyme (ACE) inhibitory activity; finally, the colorimetric determination method was used to evaluate acetylcholinesterase (AChE) inhibitory activity. The total polyphenolic content of non-sterilized Baegilju and sterilized Baegilju were 391.59 ${\mu}g$ and 401.33 ${\mu}g$ tannic acid equivalents/ml, respectively; and the flavonoids contents were 284.75 ${\mu}g$ and 308.35 ${\mu}g$ quercetin equivalents/ml, respectively. Baegilju exhibited more excellent antioxidant activities (DPPH and ABTS radicals, nitrite scavenging activity) than did Cheongju. In addition, the fibrinolytic activity and AChE inhibitory activity were found to be higher in Baegilju than they were in Cheongju. The ACE inhibitory activity of non-sterilized Baegilju, sterilized Baegilju, and Cheongju were 23.62%, 19.99%, and 38.91%, respectively. Therefore, these results suggest that Baegilju has potential as an antioxidant agent and anti-thrombosis agent.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, 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.

• YAKHAK HOEJI
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• v.55 no.6
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• pp.473-477
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• 2011

Alzheimer's disease (AD), one of the most common forms of dementia, is a progressive neurodegenerative disorder symptomatically characterized by the decline in memory and cognitive abilities. To date, the successful therapeutic strategy to treat AD is to maintain the levels of acetylcholine (ACh) by inhibiting acetylcholinesterase (AChE) to lead five drugs in clinical use. In this study, several coumarin derivatives were designed based on the lead structure of scopoletin and evaluated for their AChE inhibitory activities.