• Title/Summary/Keyword: 에스테라제

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Inhibitory Effects of Extract of Rosae Rugosae Flos on the Acetylcholinesterase, β-secretase, and β-amyloid Aggregation (매괴화(玫瑰花) 추출물의 아세틸콜린에스테라제, 베타 시크리타제 및 베타 아밀로이드 응집에 대한 저해효과)

  • Kim, Hyo Shin;Kim, Ju Eun;Leem, Jae-Yoon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.30 no.1
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    • pp.33-39
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    • 2016
  • Alzheimer's disease(AD), one of the most common forms of dementia, is characterized pathologically by the presence of intracellular neurofibrillary tangles and deposition of β-amyloid(Aβ) peptides of 40-42 residues. Aβ has been believed to be neurotoxic and now is also considered to have a role on the mechanism of memory dysfunction. Only a few acetylcholinesterase(AChE) inhibitors have been developed for treatment of AD, although the numbers of patients are rapidly increasing within aging society. Here, we show that ethanol extract of Rosae Rugosae Flos(RR) or its butanol fraction reduce the enzyme activity of AChE and BACE1(β-site APP cleaving enzyme 1). Furthermore, We found that RR inhibits Aβ aggregation and removes Aβ aggregates by Transmission electron microscopy(TEM). In addition, RR reduces the free radical of 2, 2-diphenyl-1-picrylhydrazyl(DPPH). We suggest that Rosae Rugosae Flos may be useful as a herbal medicine to treat AD.

The Acetylcholinesterase Inhibitory Activity of the EtOH Extract of Chaenomelis Fructus and its effects on the Metabolism of Amyloid Precursor Protein in Neuroblastoma Cells (모과 에탄올 추출물의 아세틸콜린에스테라제 저해활성과 신경세포에서 아밀로이드 전구단백질의 대사에 미치는 영향)

  • Kim, Ju Eun;Jo, Youn Jeong;Leem, Jae Yoon
    • Korean Journal of Pharmacognosy
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    • v.46 no.4
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    • pp.327-333
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    • 2015
  • Alzheimer's disease (AD) is a progressive neurodegenerative disorder symptomatically characterized by impairment in memory and cognitive abilities. AD is characterized pathologically by the deposition of ${\beta}$-amyloid ($A{\beta}$) peptides of 40-42 residues, which are generated by processing of amyloid precursor protein (APP). $A{\beta}$ has been believed to be neurotoxic and now is also considered to have a role on the mechanism of memory dysfunction. In this study, we tested that EtOH extract of the fruits of Chaenomeles sinensis Koehne (CSE) affects on the processing of APP from the APPswe over-expressing Neuro2a cell line. We found that CSE increased over 2 folds of the $sAPP{\alpha}$ secretion level, a metabolite of ${\alpha}$-secretase. We showed that CSE reduced the secretion level of $A{\beta}42$ and $A{\beta}40$ by down regulation of ${\beta}$-secretase (BACE) without cytotoxicity. Furthermore, we found that CSE inhibited BACE and acetylcholinesterase activity in vitro. We suggest that Chaenomelis Fructus may be an useful source to develop a herbal medicine for AD.

Composition and Anti-cholinesterase Activity of the Essential Oil Obtained from Korean Elsholtzia ciliata (한국산 향유로부터 얻은 정유의 조성과 콜린에스테라제 억제활성)

  • Song, Byong-Min;Choi, Jae Sue;Park, Hee-Juhn
    • Korean Journal of Pharmacognosy
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    • v.47 no.3
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    • pp.226-231
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    • 2016
  • The present GC-MS analysis elucidated the composition of the essential oil obtained from the herb of Elsholtzia ciliata(Lamiaceae). Overall, the content of monoterpenes was higher than that of sesquiterpenes. Monoterpenes rich in this oil were carvone (peak area, 26.180%), camphor (2.304%), borneol (9.974%), dihydrocarveol (3.296%), ${\alpha}$-citral (=geranial, 4.025%), geranic acid (2.961%), while sesquiterpenes occupying relatively higher percentage were ${\alpha}$-humulene (0.918%), (-)-spathulenol (0.974%), ${\alpha}$-caryophyllene oxide (2.014%), globulol (1.362%), ${\beta}$-caryophyllene oxide (0.750%). The components characterizing this oil were 1-octen-3-ol, acetophenone, and butylated hydroxytoluene. The $IC_{50}$ of this oil on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were $42.37{\mu}g/ml$ and $121.34{\mu}g/ml$, respectively, suggesting that the essential oil of E. ciliata may be active on the memory loss of patients suffering from Alzheimer's disease.

Effects of Cholinesterase Inhibitors on Neuronal Injuries in Primary Cultured Rat Cortical Cells (배양한 대뇌피질세포에서 유발한 신경손상에 대한 콜린에스테라제 억제제의 영향)

  • 독고향;이광헌;조정숙
    • YAKHAK HOEJI
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    • v.46 no.3
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    • pp.185-191
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    • 2002
  • Alzheimer's disease (AD) involves neuronal degeneration with impaired cholinergic transmission, particularly in areas of the brain associated with learning and memory. Several cholinesterase inhibitors are widely prescribed to ameliorate the cognitive deficits in AD patients. In an attempt to examine if tacrine and donepezil, two well-known cholinesterase inhibitors, exhibit additional pharmacological actions in primary cultured rat cortical cells, we investigated the effects on neuronal injuries induced by glutamate or N-methyl-D-aspartate (NMDA), $\beta$-amyloid fragment ( $A_{{beta}25-35)}$), and various oxidative insults. Both tacrine and donepezil did not significantly inhibit the excitotoxic neuronal damage induced by glutamate. However, tacrine inhibited the toxicity induced by NMDA in a concentration-dependent fashion. In addition, tacrine significantly inhibited the $A_{{beta}25-35)}$-induced neuronal injury at the concentration of 50 $\mu$M. In contrast, donepezil did not reduce the NMDA- nor $A_{{beta}25-35)}$-induced neuronal injury. Tacrine and donepezil had no effects on oxidative neuronal injuries in cultures nor on lipid peroxidation in vitro. These results suggest that, in addition to its anticholinesterase activity, the neuroprotective effects by tacrine against the NMDA- and $A_{{beta}25-35)$-induced toxicity may be beneficial for the treatment of AD. In contrast, the potent and selective inhibition of central acetylcholinesterase appears to be the major action mechanism of donepezil.

Airborne Chlorpyrifos Concentrations and RBC Cholinesterase Activity of Workers in Its Formulation Workplace (클로르피리포스 제조업장의 기중 농도와 작업자의 적혈구 콜린에스테라제 활성도)

  • Han, Don-Hee
    • Journal of Korean Society of Occupational and Environmental Hygiene
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    • v.22 no.2
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    • pp.91-99
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    • 2012
  • Airborne chlorpyrifos concentrations in formulation workplaces have not been determined in Korea. The aim of the study was to evaluate chlorpyrifos concentrations of air in a formulation workplace and recognize the RBC cholinesterase activities for the formulation workers. 30 air samples (personal or area sampling) were collected and bood samples from 10 workers were collected for RBC chlorinesterase (RBC AChE) activity in a factory on May 2008. Air samples were collected by the National Institute for Occupational Safety and Health (NIOSH) method and were analyzed by GC-MS. Airborne chlorpyrifos concentrations ranged from 0.003 to $12.90mg/m^3$ and geometric mean (GM) was $0.15\;mg/m^3.$ Compared to Korean Occupational Exposure Limit (KOEL) of 0.1 (2011) or $0.2\;mg/m^3$ (2008), at 95% confidence, airborne concentrations exceeded the KOEL 69.7% or 56.1% of the time or less, indicating that this concentration level was unacceptable according to exposure assessment using a LogNorm2$^{(R)}$. Since the workers were continually at work on the organophosphate or carbamate pesticides formulation, individual baseline for RBC AChE activity was not determined. As the results of comparison with reference average value of RBC AChE activity, it was found that a worker was below 70% RBC AChE activity and five workers were abnormal.

Urinalysis: The Usefulness and Limitations of Urine Dipstick Testing (요검사: 요시험지봉 검사의 유용성과 한계)

  • Han, Tae Hee
    • Childhood Kidney Diseases
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    • v.17 no.2
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    • pp.42-48
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    • 2013
  • The urinalysis is an essential part of the diagnostic work-up for kidney disease and other renal system disorders. The dipstick test allows rapid and simultaneous chemical analyses of urine, including factors such as pH, specific gravity, protein, glucose, ketones, occult blood, bilirubin, urobilinogen, nitrite, and leukocyte-esterase. The chemical reactions on dipstick are complicated and can be affected by oxidizing, reducing, and discoloring substances in the urine. Therefore, false positive and false negative results are common in dipstick testing. To obtain reliable results with the dipstick, it is necessary to collect urine cleanly and examine the urine carefully. It is mandatory to clearly understand the principles of dipstick testing to evaluate abnormal findings. If the urine dipstick results suggest hematuria, proteinuria, or urinary tract infection, microscopy of the urine should be performed to confirm the findings.

Acetylcholinesterase Inhibitory and Antioxidant Properties of Aster yomena Extract (쑥부쟁이 추출물의 아세틸콜린에스테라제 저해 및 항산화 활성)

  • Bae, Jong-Sup;Kim, Tae-Hoon
    • The Korea Journal of Herbology
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    • v.24 no.4
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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.

Regulation of Haemolymph Juvenile Hormone Esterase Activity in Larvae of the Silkworm, Bombyx mori (누에 유충의 혈림프 유약호르몬 에스테라제 활성의 조절에 관한 연구)

  • 손흥대;강필돈
    • Journal of Sericultural and Entomological Science
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    • v.34 no.1
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    • pp.15-20
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    • 1992
  • Effects of starvation, ligation, refeeding and methoprene treatment in the feeding phase of the fifth instar larvae of Bombyx mori on the regulation of juvenile hormone esterase(JHE) activity were investigated. Starvation and ligation contributed to the reduction of JHE activity, however, JHE levels in starved larvae were slightly higher than in legated larvae. Haemolymph JEH activity of starved larvae was increased by refeeding, and duration of increasing time of JHE activity after starvation was related to duration of starvation. When starved larvae were applied methoprene topically, JHE activity were not changed at day 0 and 1, but were increased by 1.3-1.4 times between day 2 and 5. When ligated larvae were applied methoprene topically, JHE activity was not changed at day 0, but were increased by 1.9-2.3 times between day 1 and 5. These results suggest that head factor, juvenile hormone(JH) and nutrient are major factors in the regulation of JHE in the feeding phase of the fifth instar larvae of Bombyx mori. Especially JHE might be regulated by the co-operative action of head factor and JH. However, head factor plays important role in the early stage, while JH plays important role thereafter.

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Screening of the Acetylcholinesterase Inhibitors from Water Extracts of the Medicinal Plants (한약재 물 추출물의 아세틸콜린에스테라제 활성 억제 검색)

  • Lee Hyung Chul;Hwang Sang-Gu;Lee Young Chan;Kim Dae Gun;Park Young Jun;Kim Tae Eun;Kim Moung Dong;Jeon Byung Hun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.2
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    • pp.215-219
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    • 2002
  • Over the past decade there has been a resurgence of interest in botanical products for their medicinal uses. This present study was designed to screen medicinal plants for the treatment of brain diseases such as Alzheimer's disease or aging. We tested the effects of the water extracts from 41 species medicinal plants on acetylcholinesterase (AChE) inhibition and antioxidant activity in vitro. Among them, Euodia rutaecarpa, Rubus coreanus, Achyranthes japonica, Morus alba, Salvia miltiorrhiza, Liriope platyphylla, and Rheum palmatum showed relatively AChE inhibition potency over 80%. Among the 7 medicinal plants investigated, E. rutaecarpa showed an 25%, 65%, and 93% inhibitions on AChE activity at 2.5, 12.5, and 25 ㎍/㎖ of the extract, respectively and was found to be one of most potent AChE inhibitor. The water extracts from 4 species (E. rutaecarpa, R. coreanus, A. iaponica, and M. alba) were tested on their antioxidant capacities using radical scavenging effect against ABTS/sup ㆍ+/. Among the 4 medicinal plants investigated, both R. coreanus and E. rutaecarpa showed significant antioxidant capacity. Therefore, E. rutaecarpa and R. coreanus are expected to ameliorate the clinical symptoms in Alzheimer's disease due to significant AChE inhibition and radical scavenging effect.

Is it Meaningful to Use the Serum Cholinesterase Level as a Predictive Value in Acute Organophosphate Poisoning? (혈청 콜린에스테라제 활성도를 이용하여 유기인계 농약 음독 환자의 증증도를 예측할 수 있는가?)

  • Lee, Sang-Jin;Jung, Jin-Hee;Jung, Koo-Young
    • Journal of The Korean Society of Clinical Toxicology
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    • v.2 no.2
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    • pp.72-76
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    • 2004
  • Purpose: Dealing patients with organophosphate poisoning, cholinesterase level has been used as a diagnostic and prognostic value. But there are some controversies that the cholinesterase level is significantly related to the severity or prognosis of acute organophosphate poisoning. We evaluated the correlation between initial serum level of cholinesterase and APACHE II score as an index for severity, and we assessed cholinesterase levels for predicting value of weaning from mechanical ventilation. Method: From August 1996 to March 2003, 23 patients with organophosphate poisoning who needed ventilatory care were enrolled. Retrospective review was done for the serum level of cholinesterase, APACHE II score, and the duration of ventilatory care. The percentage of measured serum cholinesterase to median normal value was used to standardize cholinesterase levels from different laboratories. Result: There were tendencies that the lower initial serum of cholinesterase, the higher the APACHE II score (r=0.297) and the longer the duration of mechanical ventilation (r=-0.204), but they were not significant (p=0.264 and p=0.351 respectively). In 9 patients whose serum cholinesterase level were checked at the time of weaning, mean of measured cholinesterase level was $10.3\pm7.60\%$ of normal value. Conclusion: There was no significant relationship between initial level of serum cholinesterase and severity or duration of mechanical ventilation. General health status of patient, amount of ingestion, toxicity of agent should be considered as important factors for severity of poisoning. And the decision of weaning should be based not solely on the cholinesterase level but on the consideration of general and respiratory state of individual patients.

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