• Ocean and Polar Research
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• 제39권1호
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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 ${\beta}-amyloid$.

• 동의신경정신과학회지
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• 제13권1호
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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.

• 동의신경정신과학회지
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• 제18권1호
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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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• 제28권5호
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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.

• 한국식품영양학회지
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• 제24권2호
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• pp.153-158
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• 2011

천연물로부터 lipase 저해물질을 개발하여 기능성 식품 산업에 응용하고자 lipase 저해 활성이 우수하여 전보에서 최종 선발된 도둑놈의 갈고리(Desmodium oxyphyllum DC.) 에탄올 추출물의 영양성분, 온도, pH 안정성과 생리기능성 등을 측정하였다. Lipase 저해물질을 함유한 도둑놈의 갈고리 에탄올 추출물의 지질과 단백질 함량은 각각 26.5%와 5.7%이었고 유리아미노산으로 asparagine과 tryptophan 함량이 각각 4,860 mg/건조중량 100 g, 1,209 mg/건조중량 100 g으로 물 추출물보다 높았다. 또한, 도둑놈 갈고리의 에탄올 추출물은 pH 3.0~9.0, $80^{\circ}C$ 이하에서 비교적 안정하였고, 이에 대한 생리 기능성을 측정한 결과, lipase 저해 활성은 74.2%, 항 치매성 Acetylcholinesterase 저해 활성은 68.4%로 비교적 높은 활성을 나타내었다.

• 대한한의학회지
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• 제29권5호
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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.

• 동의생리병리학회지
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• 제36권1호
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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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• 제46권4호
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• pp.353-360
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• 2003

본 실험에서는 acetylcholinesterase(AChE, EC 3.1.1.7)를 이용한 간이 잔류농약 검사법에 필요한, 유기인계 및 카바메이트계 살충제에 대한 감수성이 증가된 AChE(MAChE)를 baculovirus를 이용하여 대량으로 생산하는 시스템을 구축하고 생산된 효소의 특성을 관찰하였다. 한라산에서 채취한 초파리에서 AChE의 cDNA를 합성한 후 PCR을 이용하여 AChE의 lipid anchor부분을 제거하고 site directed mutagenesis에 의해 E107Y, F368L, L408E의 염기서열을 변화시켜 재조합된 MAChE cDNA를 합성하였고 baculovirus vector에 삽입하여 대량생산을 시도하였다. 대량 증식에 필요한 조건으로 감염횟수가 네 번일 때, 그리고 세포수가 $2{\times}10^6$ cell/ml일 때 세포의 증식과 효소의 활성이 극대화됨을 알 수 있었다. His tag을 붙여 Ni-NTA affinity column을 이용하여 MAChE를 정제하였으며, 정제된 효소는 실험조건하에서는 pH(3-10)와 온도$(20-50^{\circ}C)$의 변화에 영향을 받지 않았다. 농약 추출액으로 methanol을 사용했을 때가 ethanol을 사용할 때 보다 효과적임을 알 수 있었다. 대표적인 유기인계와 카바메이트계 농약에 대한 저해율을 조사한 결과 재조합된 MAChE는 대만의 집파리 및 변형되지 않은 AChE에 비하여 전반적으로 농약에 대한 감수성이 높은 것으로 나타났다.

• Journal of Applied Biological Chemistry
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• 제60권3호
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• pp.271-277
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• 2017

에틸포메이트는 해충을 방제하기 위한 훈증제로서 사용되어 왔다. 그러나 농산업에서 해충을 박멸하기 위하여 사용된 이 물질이 일으키는 훈증독성의 작용점에 대해서는 많은 연구가 수행되지 않았다. 본 연구에서 저자들은 복숭아혹진딧물 약충에 에틸포메이트를 훈증 처리 하였을 때 추측 가능한 작용점들을 제시하였다. 에틸포메이트 훈증 처리 후 복숭아혹진딧물 약충에 대한 생화학 및 분자적 수준에서의 변화를 측정하였다. Cytochrome c oxidase (COX)의 활성은 에틸포메이트 훈증 처리된 복숭아혹진딧물 약충에서 약 2배 이상 증가하였다. Acetylcholinesterase (AChE)의 경우 에틸포메이트의 훈증 처리 농도가 증가됨과 함께 유전자 발현이 감소되었다. 이 두 발견은 COX와 AChE가 주요한 에틸포메이트 훈증독성의 작용점임을 시사하였다. 이 결과들과 함께 MALDI-TOF MS/MS를 이용하여 지질대사체를 분석한 후 2배 이상 증감을 보인 9종 인지질들을 동정하였고 이들이 세포막 조성에 변화를 유발함을 밝혔다. 결론적으로 복숭아혹진딧물 약충에 대한 에틸포메이트의 훈증독성은 COX 활성 변화, AChE 발현 변화, 그리고 인지질의 생성 변화에 기인하였다.

• 한국약용작물학회지
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• 제24권5호
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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.