• 대한본초학회지
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• 제22권1호
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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.

• 한국균학회지
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• 제47권4호
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• pp.337-346
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• 2019

본 연구에서는 버섯으로부터 항치매성 건강소재를 개발하고자 주요 식용 및 약용 버섯들의 물과 에탄올 추출물들을 제조한 후 이들의 수율과 acetylcholinesterase 저해활성을 측정하여 우수 버섯을 선발하였다. 또한 선발된 우수버섯에 함유되어있는 항치매성 acetylcholinesterase 저해 물질의 추출 최적조건을 검토하였고, 이 저해물질을 부분정제한 후 PC12 신경세포사 저해 활성을 측정하여 항치매 효능을 검증하였다. 시료 버섯들의 물 추출물과 70% 에탄올 추출물을 각각 제조하여 이들의 acetylcholinesterase 저해 활성을 측정한 결과 물 추출물의 수율이 40%로 높고 acetylcholinesterase 저해 활성도 20.2% (IC₅₀: 12.4 mg)로 우수한 흑타리버섯을 acetylcholinesterase 저해물질을 함유한 우수 버섯으로 최종 선발하였다. 흑타리버섯 자실체중의 항치매성 acetylcholinesterase 저해물질의 추출 최적 조건은 흑타리버섯 분말을 1:30으로 증류수에 현탁 시킨 후 30℃에서 6시간 추출하는 조건이었다. 흑타리버섯 자실체의 항치매성 acetylcholinesterase 저해물질을 한외여과와 gel 여과 등으로 부분정제한 후 신경세포 PC12의 세포치사 억제에 미치는 영향을 조사한 결과 부분정제 물질을 50 ㎍/mL 처리했을 때 세포치사율이 17.0%로 낮아져서 흑타리버섯 부분정제물이 치매 진행과정을 억제하거나 지연시키는 효과를 보이는 것으로 사료된다.

• 셀메드
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• 제2권2호
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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.

• 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 $18.9\;{\mu}g$.

• 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.

• 한국식품과학회지
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• 제36권6호
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• pp.1026-1031
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• 2004

들깨 메탄올 추출물이 acetylcholinesterase(AChE)의 활성 및 PC 12 cell 세포사멸에 미치는 영향을 검토하였다. AChE에 대한 억제환성은 들깨 메탄을 추출물의 농도가 높을수록 유의적으로 높았으며 추출물의 분획물 중에서는 n-butanol층이 가장 높은 억제율을 나타내었다. L-glutamate 또는 ${\beta}-amyloid$ protein $(A{\beta})$으로 유도된 PC 12 cell에 대한 세포사멸 억제효과도 추출물의 농도가 높을수록 유의적으로 증가하였다. 또한 rat brain에 $FeSO_{4^-}H_2O_2$로 산화적 스트레스를 유발시켜 추출물의 TBARS 생성 억제활성을 조사한 결과 들깨 메탄을 추출물은 농도가 높아질수록 산화적 스트레스에 대한 억제활성이 증가하였으며 분획물 중에서는 n-butanol층에서 가장 높은 억제활성을 나타내었다. 이상의 결과들로 미루어 볼 때 들깨 메탄을 추출물은 AChE 활성을 억제하고 glutamate 또는 $A{\beta}$에 의하여 유도된 PC12 cell의 세포사멸을 억제하며 이러한 효과는 들깨 메탄을 추출물의 항산화력에 기인할 수도 있을 것으로 사료되었다.

• 생명과학회지
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• 제23권12호
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• pp.1525-1531
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• 2013

백일주는 찹쌀, 백미, 누룩, 재래종 국화꽃, 오미자, 진달래, 솔잎 및 물을 넣고 100일간 발효 숙성시킨 전통주이다. 본 연구에서 백일주의 생리활성을 알아보기 위하여 총 폴리페놀과 플라보노이드 함량, 항산화 활성(DPPH 라디칼, ABTS 라디칼, 아질산염 소거활성), 혈전용해활성, angiotensisn 전환효소 저해활성 및 acetylcholinesterase 저해활성을 평가하였다. 살균 처리되지 않은 백일주와 살균 처리된 백일주의 총 폴리페놀 함량은 391.59와 401.33 ${\mu}g$ tannic acid equivalents/ml이었고, 총 플라보노이드 함량은 284.75와 308.35 ${\mu}g$ quercetin equivalents/ml이었다. 백일주의 항산화 활성(DPPH 라디칼, ABTS 라디칼, 아질산염 소거활성)은 청주 보다 우수한 것으로 나타났다. 또한 백일주의 혈전용해활성과 acetylcholinesterase 저해활성도 청주에 비해 우수한 것으로 나타났다. 반면에 angiotensin 전환효소 저해활성을 측정한 결과 살균 처리되지 않은 백일주는 23.62%, 살균 처리된 백일주는 19.99%, 청주는 38.91%로 청주가 가장 높은 것으로 나타났다. 따라서 본 연구 결과는 백일주가 항산화 효과와 혈전용해 활성이 있음을 시사하고 있다.

• Archives of Pharmacal Research
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• 제25권6호
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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.

• 대한본초학회지
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• 제24권4호
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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.

• 약학회지
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• 제55권6호
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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.