• 제목/요약/키워드: Acetylcholinesterase activity

검색결과 337건 처리시간 0.023초

두견화(杜鵑花)가 Alzheimer's Disease 병태(病態) 모델에 미치는 영향(影響) (The Effects of Rhododendron simsii Planch(RSP) on the Alzheimer's Disease Model)

  • 장진실;이상룡;정인철
    • 동의신경정신과학회지
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    • 제17권2호
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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.

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총명탕(聰明湯)과 산사총명탕(山査聰明湯)이 Alzheimer's Disease 병태(病態) 모델에 미치는 영향(影響) (The Effects of ChongMyungTang(CMT) and SanSaChongMyungTang(SCMT) on the Alzheimer's Disease Model)

  • 하수영;정인철;이상룡
    • 동의신경정신과학회지
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    • 제17권1호
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    • pp.59-78
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    • 2006
  • Objective : This research investigates the effect of the CMT and SCMT on Alzheimer's disease. Methods : The effects of the CMT and SCMT on (1) amyloid precursor proteins(APP), acetylcholinesterase(AChE) mRNA of PC-12 cells treated with CT-105; (2) the AChE activity and the APP production of PC-12 cell treated with CT-105; (3) the behavior; (4) expression of $IL-1{\beta}$, $TNF-{\alpha}$, MDA; (5) the infarction area of the hippocampus in Alzheimer's disease mice induced with CT105 & ${\beta}A$ were investigated Rresults : 1. The CMT and SCMT suppressed the expression of APP, AChE mRNA in PC-12 cells treated with CT-105 2. The CMT and SCMT suppressed the AChE activity, and the production of APP significantly in PC-12 cells treated with CT-105. 3. For the CMT and SCMT group a significant inhibitory effect on the memory deficit was shown for the mice with Alzheimer's disease induced by ${\beta}A$ in the Morris water maze experiment, which measured stop-through latency, and distance movement-through latency 4. The CMT and SCMT suppressed the over-expression of $IL-1{\beta}$, $TNF-{\alpha}$, MDA in the mice with Alzheimer's disease induced by ${\beta}A$. 5. The CMT and SCMT reduced the infarction area of hippocampus with Alzheimer's disease induced by ${\beta}A$. Conclusions : These results suggest that the CMT and SCMT may be effective for the prevention and treatment of Alzheimer's disease. Investigation into the clinical use of the CMT and SCMT for Alzheimer's disease is suggested for future research.

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머루전초, 독활전초, 감초 혼합추출물의 Amyloid β Protein (25-35) 유발 신경 독성에 대한 억제효과 (Inhibitory Effect of an Ethanol Extract Mixture of Vitis amurensis, Aralia cordata, and Glycyrrhizae radix on Amyloid β Protein (25-35)-Induced Neurotoxicity)

  • 장지연;성연희
    • 한국약용작물학회지
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    • 제22권2호
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    • pp.105-112
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    • 2014
  • The present study investigated an ethanol extract (SSB) of a mixture of three medicinal plants of Vitis amurensis, Aralia cordata, and Glycyrrhizae radix for possible neuroprotective effects on neurotoxicity induced by Amyloid ${\beta}$ protein ($A{\beta}$) (25-35) in cultured rat cortical neurons and antidementia activity in mice. Exposure of cultured cortical neurons to $15{\mu}M$ $A{\beta}$ (25-35) for 36 h induced neuronal apoptotic death. At $1-30{\mu}g/m{\ell}$, SSB inhibited neuronal death, elevation of intracellular calcium concentration ($[Ca^{2+}]_i$), and generation of reactive oxygen species (ROS) induced by $A{\beta}$ (25-35) in cultured cortical neurons. Memory impairment and increase of acetylcholinesterase activity induced by intracerebroventricular injection of mice with 16 nmol $A{\beta}$ (25-35) was inhibited by chronic treatment with SSB (25, 50 and 100 mg/kg, p.o., for 8 days). From these results, it is suggested that antidementia effect of SSB is due to its neuroprotective effect against $A{\beta}$ (25-35)-induced neurotoxicity and that SSB may have a therapeutic role in preventing the progression of Alzheimer's disease.

가상 검색 및 시험관 시험을 이용한 총명탕 중 주성분들에 대한 약물작용 및 대사 예측 (In silico Prediction and In vitro Screening of Biological Activities and Pharmacokinetics for the Major Compounds in Chong Myung Tang)

  • 권영이
    • 약학회지
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    • 제51권6호
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    • pp.463-468
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    • 2007
  • Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

New ecological health assessment approaches of an urban stream using molecular and physiological level biomarkers and bioindicators

  • Kim, Ja-Hyun;Yeom, Dong-Hyuk;Kim, Joon-Ha;An, Kwang-Guk
    • Animal cells and systems
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    • 제16권4호
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    • pp.329-336
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    • 2012
  • This study evaluated ecological health, using various biomarkers and bioindicators, of pale chub (Zacco platypus) as a sentinel species, in Daejeon Stream, South Korea, during AprilMay 2011. The biomarkers and bioindicators were compared among three sites of control: Reference ($C_z$), transition ($T_z$), and the urban zones ($U_z$); and the 7-Ethoxyresorufin-O-deethylase (EROD) activity, DNA damage, acetylcholinesterase (AChE) activity, and vitellogenin (VTG) concentrations were more significantly increased in the $U_z$ than in the $C_z$. Also, physiological markers such as condition factor, liver somatic index, visceral somatic index, and gonad somatic index were significantly increased in the $U_z$ than in the $C_z$. For the health assessments, three categorized parameters of blood chemistry, molecular biomarkers, and physiological bioindicators were standardized and calculated as a star-plot, representing values of Integrated Health Response (IHR). Values of IHR had more significant (P<0.05) increases in the $U_z$ than any other zones, indicating an impairment of ecological health by organic matter, nutrients (N, P), and toxic chemicals. This study is based on low levels of biological organization approach of molecular and physiological biomarkers and bioindicators, so further study of high-levels of biological organization approach such as community and population is required for overall range of health assessments. The approach of IHR values, however, may be useful in providing early warning of future impacts on ecological health.

Scopolamine 유발 기억력 손상 마우스 모델에서 목향(木香)의 기억력 개선 및 항산화 효과 (Aucklandiae Radix Ameliorates Scopolamine-induced Memory Impairment in Mice)

  • 박나은;한다영;김상호;정대규
    • 동의신경정신과학회지
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    • 제28권2호
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    • pp.123-136
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    • 2017
  • Objectives: The objective of this study is to investigate the anti-amnesic effects of AR, Aucklandiae Radix, ground powder on scopolamine (Sco)-induced memory impairment in mice (C57BL/6) through its favorable acetylcholine (ACh) and acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expression, and antioxidant effect. Methods: Six groups, a total of 20 intact or 100 Sco treated mice, were selected based on their body weights and were used in this study. Half of the mice in each group were used for the passive avoidance task test and the measurements of hippocampus ACh content, AChE activity and ChAT mRNA expression. The remaining half of the mice in each group were used for the Morris water maze test and cerebral antioxidant defense system measurement. Results: Marked decreases in step-through latency times in the passive avoidance task test and increases in escape latency times in the Morris water maze test were observed with decreases in the hippocampus ACh content and ChAT mRNA expression, and increases in the hippocampal AChE activities, as a result of Sco intraperitoneal treatment, in the present study. In addition, destruction of the cerebral cortex antioxidant defense systems was observed in Sco control mice as compared with intact vehicle control mice. However, 28 days of continuous oral pre-treatment with AR ground powder at doses of 400, 200 and 100 mg/kg markedly and dose-dependently inhibited the Sco treatment-related amnesia. Conclusions: The results prove that oral administration of AR ground powder reduces Sco-induced memory impairment. This is because it can preserve ACh, related to ChAT mRNA expression, cause AChE inhibition, and activate the cerebral antioxidant defense system.

Chromenone Derivatives as Monoamine Oxidase Inhibitors from Marine-Derived MAR4 Clade Streptomyces sp. CNQ-031

  • Oh, Jong Min;Lee, Chaeyoung;Nam, Sang-Jip;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • 제31권7호
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    • pp.1022-1027
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    • 2021
  • Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC50) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC50 of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The Ki value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the Ki values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

Scopolamine 유발 건망증 마우스 모델에서 육미지황탕(六味地黃湯)의 기억력 개선 및 항산화 효과 (Anti-amnesic Effect and Antioxidant Defense Systems of Yukmijihwang-tang on Scopolamine-induced Memory Impairment in Mice)

  • 서영민;한다영;김상호;정대규
    • 동의신경정신과학회지
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    • 제29권4호
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    • pp.207-221
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    • 2018
  • Objectives: The objective of this study was to observe the anti-amnesic effects of Yukmijihwang-tang (YMJHT), on the scopolamine (Sco)-induced memory impairment in C57BL/6 mice through its favorable acetylcholine (ACh). Also, to observe acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expressions, and antioxidant effect. Methods: Six groups, with a total of 20 normal and 100 Sco treated mice were selected based on their body weights after 1 week of acclimatization, were used in this study as follows. Half of the mice in each group were used for passive avoidance task tests and hippocampus ACh content, AChE activity and ChAT mRNA expression measurement, and the remaining half in each group used for Morris water maze test and measurement of cerebral antioxidant defense system. Results: Amnesia due to AChE activations and destroyed cerebral cortex antioxidant defense systems were markedly and dose-dependently inhibited after 28 days of continuous oral pre-treatment with YMJHT 400, 200 and 100 mg/kg, respectively. The overall effects of YMJHT 400 mg/kg were similar to those of tacrine 10 mg/kg. Conclusions: Based on the results, it was established that oral administration of YMJHT favorably alleviates Sco-induced memory impairment, through preservation of ACh, mediated by up-regulation of ChAT mRNA expressions and related AChE inhibition and augmentation of cerebral antioxidant defense system, at least in a condition of this experiment. The overall effects of YMJHT 400 mg/kg were similar to those of tacrine 10 mg/kg.

Scopolamine 유발 기억력 손상 마우스 모델에서 분심기음의 항산화 및 기억력 감퇴 억제 효과 (Anti-amnesic and Antioxidant Effect of Bunsimgieum (Fenxinqiyin) on Scopolamine-Induced Memory Impairment in Mice)

  • 한다영;유옥철;김상호;정대규
    • 동의신경정신과학회지
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    • 제30권3호
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    • pp.221-235
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    • 2019
  • Objectives: The purpose of this study was to confirm the anti-amnesic effects of Bunsimgieum (BSGE) through its favorable acetylcholine (ACh) and, acetylcholinesterase (AChE) activity, choline acetyltransferase (ChAT) mRNA expressions, and antioxidant effect on scopolamine (Sco)-induced memory impairment in C57BL/6 mice. Methods: Six groups, a total of 20 intact or 100 Sco-induced mice were used in this study, based on their body weight. Half of each group underwent passive avoidance tests and the measurement of hippocampus AChE activity, ACh content, and ChAT mRNA expression, The remaining half of each group underwent a Morris water-maze test and antioxidant defense system measurement as well. Results: Significant reductions in the step-through latency times from the passive avoidance test and reductions in the escape latency times from the Morris water-maze test were observed with increases of hippocampal AChE activities and, reductions in ACh contents and ChAT mRNA expression in hippocampus, as a result of Sco intraperitoneal treatment, in this study. Additionally, the increases in cerebral cortical MDA levels and, reductions in GSH contents, SOD activities, and CAT activities were demonstrated in the Sco control mice compared with the intact vehicle control mice, respectively. However, 28 days of consecutive oral pre-treatment of BSGE hot water extracts of 400, 200, and 100 mg/kg, respectively, markedly and dose-dependently inhibited Sco treatment-related amnesia. Conclusions: The results demonstrate that the oral administration of BSGE hot water extracts reduces Sco-induced memory impairment, through preserving ACh, related to ChAT mRNA expressions, causes AChE inhibition, and enhances the cerebral antioxidant defense system.

Actinidia arguta Sprout as a Natural Antioxidant: Ameliorating Effect on Lipopolysaccharide-Induced Cognitive Impairment

  • Kang, Jeong Eun;Park, Seon Kyeong;Kang, Jin Yong;Kim, Jong Min;Kwon, Bong Seok;Park, Sang Hyun;Lee, Chang Jun;Yoo, Seul Ki;Heo, Ho Jin
    • Journal of Microbiology and Biotechnology
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    • 제31권1호
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    • pp.51-62
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    • 2021
  • Here, we investigated the prebiotic and antioxidant effects of Actinidia arguta sprout water extract (AASWE) on lipopolysaccharide (LPS)-induced cognitive deficit mice. AASWE increased viable cell count, titratable acidity, and acetic acid production in Lactobacillus reuteri strain and showed a cytoprotective effect on LPS-induced inflammation in HT-29 cells. We assessed the behavior of LPS-induced cognitive deficit mice using Y-maze, passive avoidance and Morris water maze tests and found that administration of AASWE significantly improved learning and memory function. The AASWE group showed antioxidant activity through downregulation of malondialdehyde levels and upregulation of superoxide dismutase levels in brain tissue. In addition, the AASWE group exhibited activation of the cholinergic system with decreased acetylcholinesterase activity in brain tissue. Furthermore, AASWE effectively downregulated inflammatory mediators such as phosphorylated-JNK, phosphorylated-NF-κB, TNF-α and interleukin-6. The major bioactive compounds of AASWE were identified as quercetin-3-O-arabinopyranosyl(1→2)-rhamnopyranosyl(1→6)-glucopyranose, quercetin-3-O-apiosyl(1 → 2)-galactoside, rutin, and 3-caffeoylquinic acid. Based on these results, we suggest that AASWE not only increases the growth of beneficial bacteria in the intestines, but also shows an ameliorating effect on LPS-induced cognitive impairment.