• 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 $18.9\;{\mu}g$.

• 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 Korea Journal of Herbology
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• v.22 no.4
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• pp.51-58
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• 2007

Objectives : Investigation of the memory and cognitive enhancing effect of HT008-1 in scopolamine induced amnesia mice. Methods : At 60 min before acquisition trials, HT008-1 (30, 100, 300 mg/kg p.o.) was administered, and 30 min later, mice were injected with scopolamin (1.0 mg/kg, i.p.). In the passive avoidance test, acquisition trials were carried out 30 min after a single scopolamine treatment. Retention trials were carried out 24h after acquisition trials. Y-maze test was carried out 30 min after a single scopolamine treatment. Spontaneous alternation behavior during an 8-min session was recorded. Inhibitory effects of HT008-1 (0.01, 0.1, 1.0 mg/ml) on AChE activity was measured. Result : HT008-1 ameliorated scopolamine-induced learning impairments and spatial cognitive function in passive avoidance and Y-maze test, respectively. Moreover HT008-1 showed a significant inhibitory effect on AChE activity. Discussion: This study presented that eMultiherb mixture HT008-1 enhanced learning memory and spatial cognitive function in scopolamine-induced amnesia mice. These results suggest that the effect of HT008-1 may be dependent on the inhibition of AChE activity.

• Natural Product Sciences
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• v.25 no.2
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• pp.115-121
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• 2019

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl($1{\rightarrow}6$)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.

• Mycobiology
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• v.37 no.3
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• pp.203-206
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• 2009

To develop new antidementia nutraceuticals, a potent acetylcholinesterase (AChE)-inhibiting extract was screened from various extracts of nutritional mushrooms and lichens nutritional and its physicochemical properties were investigated. Among the several extracts tested, methanol extracts of Umbilicaria esculenta fruiting body showed the highest AChE inhibitory activity of 22.4%. U. esculenta AChE inhibitor was maximally extracted when fruiting bodies were treated with 80% methanol at $40^{\circ}C$ for 18 h. The methanol extracts contained 18.9% crude lipid, 18.8% crude protein, and 11.6% total sugar. In addition, they contained 444 mg/g glutamic acid, 44 mg/g histidine, and 41 mg/g aspartic acid. The methanol extracts were soluble in a solution of methanol and 20% dimethylsulfoxide, insoluble in n-hexane, chloroform, and water, and were stable at $20{\sim}60^{\circ}C$ and pH $1.0{\sim}5.0$ for 1 h.

• Archives of Pharmacal Research
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• v.27 no.1
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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.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.1
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• pp.130-138
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• 2005

This experiment was designed to investigate the effect of Phellodendron amurense(PLDA) on the Alzheimer's disease. The effects of PLDA extract on $IL-1{\beta}$, IL-6, amyloid precursor proteins(APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ and AChE activity of PC-12 cell lysate treated by $A{\beta}$ plus $rIL-1{\beta}$ and behavior of memory deficit mice induced by scopolamine and mice glucose, uric acid, AChE activity of memory deficit rats induced by scopolamine were investigated, respectively. PLDA extract suppressed $IL-1{\beta}$, IL-6, APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ ; AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$. PLDA extract increased glucose, decreased uric acid and AChE significantly in the serum of the memory deficit rats induced by scopolamine. PLDA extract group showed significantly inhibitory effect on the memory deficit of mice induced by scopolamine in the experiment of Morris water maze. According to the above results, it is suggested that PLDA extract might be usefully applied for prevention and treatment of Alzheimer's disease.

• Journal of Oriental Neuropsychiatry
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• v.18 no.1
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• pp.63-78
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• 2007

Objective : This experiment was designed to investigate the effect of Thalictrum foetidum(TFD) on the Alzheimer's disease. Method : The effects of TFD on amyloid precursor proteins(APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by amyloid ${\beta}$ $protein(A{\beta})$ and $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA of THP-l cell treated by lipopolysaccharide(LPS), AChE activity of PC-12 cell lysate treated by $A{\beta}$ and behavior of the memory deficit mice induced by scopolamine, and glucose, AChE in serum of the memory deficit mice induced by scopolamine were investigated, respectively. Results : The results were summarized as follows ; 1. TFD suppressed APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$. 2. TFD suppressed $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA in THP-l cell treated by LPS 3.. TFD suppressed AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$. 4. TFD increased glucose and decreased AChE significantly in the serum of the memory deficit mice induced by scopolamine. 5. TFD group showed significantly inhibitory effect on the scopolamine-induced impairment of learning and memory in the experiment of Morris water maze. Conclusion : According to the above results, it is suggested that TFD might be usefully applied for prevention and treatment of Alzheimer's disease.

• Journal of Oriental Neuropsychiatry
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• v.17 no.2
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• pp.75-89
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• 2006

Objective : This experiment was designed to investigate the effect of Rhododendron simsii Planch(RSP) on the Alzheimer's disease. Method : The effects of RSP on amyloid precursor proteins(APP), acetylcholinesterase (AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by amyloid ${\beta}$ protein$(A{\beta})$ and $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA of THP-1 cell treated by lipopolysaccharide(LPS), AChE activity of PC-12 cell lysate treated by $A{\beta}$ and behavior of the memory deficit mice induced by scopolamine, and glucose, AChE in serum of the memory deficit mice induced by scopolamine were investigated, respectively. Result : 1. RSP suppressed APP, AChE, GFAP mRNA in PC-12 celt treated by $A{\beta}$. 2. RSP suppressed $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA in THP-1 cell treated by LPS. 3. RSP suppressed AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$. 4. RSP increased glucose and decreased AChE significantly in the serum of the memory deficit mice induced by scopolamine. 5. RSP group showed significantly inhibitory effect on the scopolamine-induced impairment of teaming and. memory in the experiment of Morris water maze. Conclusion : According to the above results, it is suggested that RSP might be usefully applied for prevention and treatment of Alzheimer's disease and memory deficit symptom.

• Journal of Oriental Neuropsychiatry
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• v.15 no.1
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• pp.87-99
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• 2004

This experiment was designed to investigate the effect of Coptis japonica Makino(CJM) on the Alzheimer's disease. The effects of CJM extract on $IL-1{\beta}$, IL-6, amyloid precursor proteins (APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ and AChE activity of PC-12 cell lysate treated by $A{\beta}$ plus $rIL-1{\beta}$ and behavior of memory deficit rats induced by scopolamine and mice glucose, uric acid, AChE activity of memory deficit rats induced by scopolamine were investigated, respectively. The results were summarized as follows ; 1. CJM extract suppressed $IL-1{\beta}$, IL-6 mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 2. CJM extract suppressed APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 3. CJM extract suppressed AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 4. CJM extract group showed significantly inhibitory effect on the memory deficit of mice induced by scopolamine in the experiment of Morris water maze. 5. CJM extract increased glucose, decreased uric acid and AChE significantly in the serum of the memory deficit rats induced by scopolamine. According to the above results, it is suggested that CJM extract might be usefully applied for prevention and treatment of Alzheimer's disease and memory deficit symptom.