• Ocean and Polar Research
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• v.39 no.1
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• pp.45-49
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• 2017

During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

• Journal of Oriental Neuropsychiatry
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• v.13 no.1
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• pp.79-115
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• 2002

This research investigates the effect of the Crataegus pinnatifida BGE. var. major N.E. BR(CPVM) on Alzheimer's disease. Specifically, the effects of the DYHT extract on (1) $IL-1{\beta}$, IL-6, amyloid precursor proteins(APP), acetylcholinesterase(AChE), and glial fibrillary acidic protein(GFAP) mRNA of PC-12 cells treated with CTI05; (2) the AChE activity and the APP production of PC-12 cell treated with CT105; (3) the behavior; and (4) expression of $IL-1{\beta}$, $TNF-{\alpha}$, reactive oxygen species(ROS), nitrite oxide(NO); and (5) the infarction area of the hippocampus, and brain tissue injury in Alzheimer's diseased mice induced with CT105 were investigated. The results are as follow. 1. The CPVM extract suppressed the expression of $IL-1{\beta}$, IL-6, APP, AChE, and GFAP mRNA in PC-12 cells treated with CT105. 2. The CPVM extract suppressed the AChE activity and the production of APP significantly in PC-12 cells treated with CT105. 3. The CPVM extract group showed a significant inhibitory effect on the memory deficit for the mice with Alzheimer's disease induced by CT105 in the Morris water maze experiment. 4. The CPVM extract suppressed the over-expression of $IL-1{\beta}$, $TNF-{\alpha}$, ROS and NO in the mice with Alzheimer's disease induced by CT105. 5. The CPVM extract reduced the infarction area of hippocampus, and controlled the injury of brain tissue in the mice with Alzheimer's disease induced by CT105. These results suggest that the CPVM extract may be effective for the 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 Microbiology and Biotechnology
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• v.28 no.5
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• pp.679-687
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• 2018

Korean red pine (Pinus densiflora) is one of the major Pinus species in Korea. Red pine bark is removed prior to the chipping process in the wood industry and discarded as waste. However, red pine bark contains a considerable amount of naturally occurring phenolics, including flavonoids, and therefore may have a variety of biological effects. In this study, we investigated if Korean red pine bark extract (KRPBE) could protect neuronal PC-12 cells from oxidative stress and inhibit cholinesterase activity. Analysis of reversed-phase high-performance liquid chromatography results revealed four phenolics in KRPBE: vanillin, protocatechuic acid, catechin, and taxifolin. The total phenolic and flavonoid contents of KRPBE were 397.9 mg gallic acid equivalents/g dry weight (DW) and 248.7 mg catechin equivalents/g DW, respectively. The antioxidant capacities of KRPBE measured using ABTS, DPPH, and ORAC assays were 697.3, 521.8, and 2,627.7 mg vitamin C equivalents/g DW, respectively. KRPBE and its identified phenolics protected against $H_2O_2$-induced oxidative cell death in a dose-dependent manner. Acetylcholinesterase and butyrylcholinesterase, which degrade the neurotransmitter acetylcholine to terminate neurotransmission in synaptic clefts, were inhibited by treatment with KRPBE and its identified phenolics. Taken together, these results suggest that KRPBE and its constituent antioxidative phenolics are potent neuroprotective agents that can maintain cell viability under oxidative stress and inhibit cholinesterase activity.

• The Korean Journal of Food And Nutrition
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• v.24 no.2
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• pp.153-158
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• 2011

This study was performed to develop new anti-obesity agents from medicinal plants for functional food industry. We prepared lipase inhibitor-containing ethanol extracts from Desmodium oxyphyllu DC. and its nutritional characteristics, stability of temperature and pH and physiological functionalities were investigated. Crude lipid content and curde protein content of ethanol extract from Desmodium oxyphyllum DC. were 26.5% and 5.7%, respectively and its asparagine content was 4,860 mg/100 g, dry basis. The ethanol extracts were also stable from pH 3.0 to pH 9.0 and below $80^{\circ}C$. The ethanol extract were showed high lipase inhibitory activity of 74.2% and acetylcholinesterase inhibitory activity of 68.4%.

• The Journal of Korean Medicine
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• v.29 no.5
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• pp.67-76
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• 2008

Objectives : Amnesia is theloss or impairment of memory, caused by physical injury, disease, drugs, or emotional trauma. Recently, the average life span is increasing, while at the same time, the incidence of dementia-like diseases in conjunction with amnesia are also increasing. Therefore learning and memory are very important issues in modern society. Ancient Korean physicians used several herbs to treat dementia and these herbal effects were described in Korean herbal books. Among them are some reports on several cognitive-enhancing herbs which have since been shown to improve dementia in recent pharmacological studies, such as Panax ginseng; however, the facilitatory effects of many Korean cognitive-enhancing herbs on learning and memory are limited. Learning and memory are essential requirements for every living organism in order to cope with environmental demands; cholinergic systems are known to be involved in learning and memory. Methods : In this study, the effects of Acori graminei rhizoma (AGR, 石菖蒲) on learning and memory were investigated by Morris water maze, eight-arm radial maze, and the effects on the central cholinergic system of rats injected with scopolamine. Results : In the water maze, the experimental animals were trained to find a platform in a fixed position for 6 days and then received a 60 sec probe trial in which the platform was removed from the pool on the 7th day. In the eight-arm radial maze, the animals were tested four times per day for 6 days. Scopolamine impaired performance of the maze tests and reduced activity of acetylcholinesterase (AchE) in the hippocampus, which is a marker for the central cholinergic system. There were significant reversals from the scopolamine-induced deficits on learning and memory in these tests, through daily administrations of AGR (100 mg/kg, p.o.) over 14 consecutive days. These treatments also reduced the loss of cholinergic activity in the hippocampus induced by scopolamine. Conclusions : These results demonstrated that AGR ameliorated learning and memory deficits by affecting the central acetylcholine system.

• Journal of Physiology & Pathology in Korean Medicine
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• v.36 no.1
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• pp.11-17
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• 2022

In this study, we investigated the effects of Ginseng Radix (G), Rehmanniae Radix (R), and Fermented red-ginseng extracts (FRG) on cognitive function in scopolamine-induced memory-impaired mice. We measured the effects of G, R, and FRG on the improvement of memory and cognition via behavior analysis. In addition, we measured the acetylcholinesterase (AChE) activity in the hippocampus of each group of mice. The expression of β-amyloid, Tau, and BDNF in the brain tissues were observed through immunohistochemical staining. Ginseng Radix (G) and Fermented red-ginseng (FRG) have effectively improved cognitive function in the water maze test. Ginseng Radix (G), Rehmanniae Radix (R), and Fermented red-ginseng (FRG) have improved the willingness of mice to explore the new environment, as confirmed by Y maze test. In addition, immunohistochemical staining revealed that Ginseng Radix (G) decreased the expression of β-amyloid and Tau in the hippocampus. In addition, fermented red-ginseng (FRG) increased the expression of BDNF. Ginseng Radix (G), Rehmanniae Radix (R), and Fermented red-ginseng (FRG) have decreased the concentration of acetylcholinesterase in the hippocampus as compared with the control group of mice. In conclusion, Ginseng Radix (G), Rehmanniae Radix (R), and Fermented red-ginseng (FRG) are considered to have the potential for development as candidate drugs to control the progression of Alzheimer's disease (AD).

• Applied Biological Chemistry
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• v.46 no.4
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• pp.353-360
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• 2003

For the simple rapid bioassay of organophosphorus and carbamate pesticide residues, a mass-production system of acetycholinesterase (AChE, EC 3.1.1.7, MAChE) using baculovirus and insect cell culture was constructed. The cDNA for AChE was synthesized from Drosophila melanogaster in Halla Mountain, the lipid anchor tail was removed by PCR and was used for the site-directed mutagenesis of three amino acid residues (E107Y, F368L, L408F). The mutated cDNA was inserted into the baculovirus vector and expressed in insect cells. Maximum cell growth and enzyme activity were reached when the cells $(2{\times}10^6\;cell/ml)$ were infected four times at four-day-intervals. His-tag containing MAChE was purified using Ni-NTA column and used for characterization. The activity was maintained under various pHs (3-10) and temperatures $(20-50^{\circ}C)$ under experimental conditions. As an extraction solution for pesticides, methanol is more effective than ethanol. Against major organophosphate and carbamate pesticides, the MAChE showed better sensitivity than AChE and AChE from housefly (Taiwan).

• Journal of Applied Biological Chemistry
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• v.60 no.3
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• pp.271-277
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• 2017

Ethyl formate has been used for the control of insect pests by fumigation. However, there were not many reports to show its target site of fumigant toxicity on insect pests since its first use in the agricultural industry. In the present study, we showed the presumable target sites of ethyl formate fumigation in insect pests using Myzus persicae nymphs. After ethyl formate fumigation, the nymphs of this species were collected and the changes at the biochemical and molecular level were determined. The activity of cytochrome c oxidase (COX) was approximately two-fold higher after ethyl formate fumigation. In addition, the expression levels of acetylcholinesterase (AChE) decreased gradually with increasing ethyl formate concentration. These two findings suggested that COX and AChE might be the major target sites of ethyl formate fumigation. In addition to these results, the analysis of lipid content using MALDI-TOF MS/MS identified 9 phospholipids differently generated 2-fold higher in the ethyl formate-treated nymphs than that in the control nymphs, thereby leading to changes in cell membrane composition in M. persicae nymphs. Therefore, the ethyl formate fumigation caused lethal effects on M. persicae nymphs by changing COX activity, AChE gene expression, and phospholipid production.

• Korean Journal of Medicinal Crop Science
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• v.24 no.5
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• pp.375-385
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• 2016

Background: The study was conducted to elucidate the extraction conditions under which white ginseng has cognition-improving efficacy. Methods and Results: Extracts from white ginseng under different solvent and temperature conditions were analyzed for ginsenoside content and inhibitory effect on N-methyl-D-aspartate (NMDA) receptor and acetylcholinesterase. The total ginsenoside contents and amounts of ginsenoside Rb1 plus ginsenoside Rg1 from the 1st extracts (prepared with EtOH/$H_2O$ as solvent) were higher than those from the 2nd extracts (extracted with $H_2O$ after the 1st EtOH/$H_2O$ extraction). The contents in the 1st and 2nd extracts produced at $80^{\circ}C$ were also higher than those obtained at $50^{\circ}C$. Samples from the 1st extraction at $80^{\circ}C$ indicated higher inhibitory activities on NMDA receptors-whose excessive activation is thought to mediate the calcium-dependent neurotoxicity associated with several neurodegenerative diseases-than those from the 2nd extraction. Among the samples prepared at varying temperatures, the extract prepared at $50^{\circ}C$ showed the highest suppression activity on NMDA receptors. Note, however, that the extracts from the 2nd extraction at $50^{\circ}C$ inhibited acetylcholinesterase-whose inhibition could be a therapeutic strategy for neurodegenerative diseases with cognitive deficits and memory malfunction-more effectively than those from the 1st extraction. Conclusions: To enhance the cognition-improving activity of white ginseng extract, it is suggested that the extracts be utilized after being combined the 1st extracts (made with EtOH/$H_2O$ solvent) and the 2nd extracts (prepared with $H_2O$) at low temperature.