• Title/Summary/Keyword: AchE

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Acetycholinesterase Inhibiting Effect and Free Radical Scavenging Effect of Soybean(Glycine max) and Yak-Kong(Rhynchosia nolubilis) (대두와 약콩의 Acetylcholinesterase 활성 억제효과와 항산화 효과)

  • 강순아;한진아
    • Journal of the East Asian Society of Dietary Life
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    • v.14 no.1
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    • pp.64-69
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    • 2004
  • The deficiency of the neurotransmitter acetylcholine(ACh) is responsible for the initiation of Alzheimer's disease. In addition, there is a simple evidence that oxidative stress significantly increases in persons with Parkinson's disease compared to age-matched healthy persons. Therefore, the objective of the study was to investigate the neurodegeneration inhibitory effect of soybean(Glycine Max) and Yak-Kong(Rhynchosia Nolubilis) by measuring the degree of inhibiting Acetylcholinesterase (AChE) catabolizing the ACh and the free radical scavenger effect in vitro. AChE was measured by the minor modified Ellman assay. Free radical scavenging activity was measured using l-diphenyl-2-picrylhydrazyl (DPPH). First, the MeOH extracts of Soybean and Yak-Kong showed the AChE inhibiting activity of 62.0$\pm$2.43% and 65.0$\pm$3.29% at the 5 mg/$m\ell$ concentration. The 50% inhibitory concentration ($IC_{50}$/) of AChE was 1.96 and 1.31 mg/$m\ell$ in the MeOH extracts of soybean and Yak-Kong. Second, the MeOH extracts of soybean and Yak-Kong showed the free radical scavenger activity of 23.1$\pm$4.26% and 80.7$\pm$4.61% at the 5 mg/$m\ell$. IC50 of free radical scavenger activity in Soybean and Yak-Kong was 13.00 and 1.41 mg/$m\ell$ in MeOH extracts and was 5.95 and 2.74 mg/$m\ell$ in hot-water extracts, respectively. In this study, the extracts of Soybean and Yak-Kong showed powerful effects in the AChE inhibition and free radical scavenging. The extracts of Soybean and Yak-Kong were expected to prevent the many neurodegenerative diseases.

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Acetylcholinesterase-based Biosensor for Detection of Residual Organophosphates and Carbamates Insecticides (유기인계 및 카바메이트계 농약을 측정할 수 있는 바이오 센서의 개발)

  • Kim, Young-Mee;Kim, Jin-Young;Cho, Moon-Jae;Chang Kong-Man;Hyun, Hae-Nam;Cho, Somi K.
    • Applied Biological Chemistry
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    • v.49 no.4
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    • pp.315-321
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    • 2006
  • Inhibitors of acetylcholinesterase(AchE), such as organophosphates and carbamates, interfere the action of AchE in nerve and may lead to a severe impairment of nerve functions or even death. Therefore, insect AchE is the biological target of predominant insecticides used in agriculture. Biosensors are sensitive and can be used as dispoisable sensors for environmental control. In recent years, the use of AchEs in biosensor technology has gained enormous attention, in particular with respect to insecticide detection. The principle of biosensors using AchE as a biological recognition element is based on the inhibition the catalytic activity by the agents to be detected. We here present a strip-type biosensor based on AchE inhibition. In this study, acetylcholinesterase and PVA-SbQ(polyvinyl alcohol functionalized with methyl pyridinium methyl sulfate) were co-immobilized on immobilone-P membranes. Immobilization of the enzymes showed a stability in 6 months without activity loss in $4^{\circ}C$ storage. Enzymes immobilized on surfaces of membrane responded to organophosphates and carbamate more sensitivitive than enzyme in solution. Organophosphates and carbamates concentrations could be detected by entrapped and surface immobilized enzymes, in 5 min. For chlorpyrifos, carbofuran, cabaryl, and methidathion, the detection limits of AChE-strip were similar to that of HPLC/GC method.

Acetylcholinesterase Inhibition and Behavioral Changes of Crucian carp (Carassius auratus) Exposed to the Waterborne Parathion (Parathion에 노출된 붕어(Carassius auratus)의 Acetylcholinesterase 억제와 행동변화)

  • Cho, Kyu-Seok;Park, Jong-Ho;Lee, Won-Ho;Kang, Ju-Chan
    • Journal of Korean Society on Water Environment
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    • v.22 no.2
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    • pp.364-369
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    • 2006
  • The investigation of the Acetylcholinesterase (AChE) activity in tissues (brain, eye, muscle and serum) of crucian carp (Carassius auratus) exposed to the waterborne parathion was carried out for application as biomarker of organophosphate pesticides. The AChE activities were significantly inhibited in the experimental organs of C. auratus treated ${\geq}63{\mu}g/L$ of concentrations of parathion. The AChE activity of C. auratus was significantly reduced in response to brain (79.1~92.4%), eye (76.0~91.5%), muscle (89.7~97.6%) and serum (68.9~78.0%) after 30 days exposure. No significant mortality occurred during the experiment duration but behavioral changes occurred in the carp after exposure to the parathion were erratic swimming and convulsions. The anomaly in the carp exposed to parathion were observed in the form of scoliosis. The use of AChE activity and other adverse responses of the carp might be use as a reliable monitoring tool to detect parathion in aquatic ecosystem which might produce significant population changes.

Physicochemical Characteristics of Antidementia Acetylcholinesterase Inhibitor-containing Methanol Extract from Sorghum bicolor and Industrial Application (항치매성 Acetylcholinesterase저해물질을 함유하고 있는 수수 메탄올 추출물의 특성 및 산업적 응용)

  • Song, Jung-Eun;Lee, Jong-Soo
    • The Journal of Natural Sciences
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    • v.19 no.1
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    • pp.45-55
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    • 2008
  • Alzheimer's disease is charaterized by the acetylcholine depletion, amyloid b-protein aggregation and neurofibrillary tangles. The prevention of the breakdown of acetylcholine by acetylcholinesterase (AChE) inhibitor has the best clinically therapeutic efficacy for Alzheimer's disease patients. To develop new antidementia alternative drugs or nutraceuticals, methanol extracts of Sorghum bicolor was screened from various extracts of cereals and legumes as a potent AChE inhibitor-containing extract in previous paper. In this paper, physicochemical properties of the methanol extracts was investigated. The methanol extracts was soluble by water, methanol and DMSO and had 215 nm and 282nm of maximum absorption spectra. It was also stable at 20-$100^{\circ}C$ and pH 2.0-10.0 for 1 hr. Test product was prepared by using methanol extracts from Sorghum bicolor and changes of its quality during storge at $20^{\circ}C$ and $40^{\circ}C$ were investigated. It was very stable for 8 weeks at $40^{\circ}C$.

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Biruloquinone, an Acetylcholinesterase Inhibitor Produced by Lichen-Forming Fungus Cladonia macilenta

  • Luo, Heng;Li, Changtian;Kim, Jin Cheol;Liu, Yanpeng;Jung, Jae Sung;Koh, Young Jin;Hur, Jae-Seoun
    • Journal of Microbiology and Biotechnology
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    • v.23 no.2
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    • pp.161-166
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    • 2013
  • At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.

Study on Biochemical Pollutant Markers for Diagnosis of Marine Pollution III. Changes in Cholinesterase Activity of Flounder(Paralichthys olivaceus)in the Yellow Sea (해양오염의 진단을 위한 생화학적 오염지표에 관한 연구 III. 황해산 넙치(Paralichthys olivaceus)의 콜린에스테라아제 활성의 변화)

  • Choi, Jin-Ho;Kim, Dong-Woo;Moon, Young-Sil;Park, Chung-Kil;Yang, Dong-Beom
    • Journal of Life Science
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    • v.7 no.1
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    • pp.17-23
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    • 1997
  • This study was designed as a part of efforts to investigate the biochemical pollutant markers for diagnosis of maine pollutions by changes in cholinesterase activity of the flounder (Paralichthys olivaceus)in Yellow Sea of Korea. Acetylcholinesterase (AChE) activities in brain and muscle of cultured flounders in Yellow Sea were remarkably lower (40-50% and 40-55%, respectively)than those of wild flounder in Pohang (control) of East Sea, but AChE activities in brain and muscle of wild flounders in Yellow Sea were significantly lower(15-40% and 25-35%, respectively)than those of wild flounder in Pohang of East Sea. Butyrylcholinesterase(BChE) activities in barin and muscle of cultured flounders in Yellow Sea were remarkably lower(70-75% and 65-75%, respectively) than those of wild flounder in Pohang of East Sea, but BChE activities in barin and muscle of wild flounders in Yellow Sea were significantly lower (15-40%and 25-35%, respectively)than those of wild flounder in Pohang of East Sea. Lactate dehydrogenase (LDH) activities in serum of cultured flounders in Yellow Sea were significantly 10-50% higher than those of wild flounder in Pohang of East Sea, but LDH activities in serum of wild flounders in Yellow Sea were significantly 20-25% higher than those of wild flounder in Pohang of East Sea. It suggests that AChE and BChE activities in brain and muscle of cultured and wild flounders of Yellow Sea may be used as the most effective mean in a biochemical markers for diagnosis of pollutant effects by organophosphorus pesticides.

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Characteristics of Resistance to Chlorpyrifos in Diamondback-moth (Plutella xylostella L.) (Chlorpyrifos 저항성 배추좀나방(Plutella xylostella L.)의 살충제 저항성 특성)

  • Kim, Kyung-Ju;Kim, Sung-Su;Kim, Song-Mun;Hur, Jang-Hyun
    • The Korean Journal of Pesticide Science
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    • v.7 no.4
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    • pp.288-295
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    • 2003
  • To determine the mechanism of the resistance to organophosphorus insecticide, chlorpyrifos, in diamondback-moth (Plutella xylostella L.), activities of esterases, glutathione-S-transferase (GST) and AChE insensitivity which were known for causing factor of resistance were measured. Also, the relationship between AChE insensitivity and the resistant ratio was investigated to inquiry the cross-resistance. The resistant ratio of chlorpyrifos-resistant strain (CRS) of diamondback-moth at the 6th generation was developed 160 fold compared to susceptible strain (SS) one. Activity of GST that are extracted from CRS was 1.7-fold higher than that from SS. However, activity of total esterases from CRS was similar to that from SS. In AChE insensitivity test, CRS was 11.8-fold less sensitive than that from SS. CRS was ranged from 17.6 to 33.6-fold less sensitive than SS to other insecticides having same target site with chlorpyrifos such as dichlorvos, dimethylvinphos and carbofuran. Insensitivity of AChE to phenthoate-oxon, however, was 1.7-fold. Resistance of CRS was 82-fold, 47-fold and 42-fold higher than SS to dichlorvos, dimethylvinphos and carbofuran, respectively, but 2.3-fold to phenthoate and then we could identify that the resistance development of insecticide might have a lot of difference among the chemicals with the same target site. The relationship between the AChE insensitivity and the resistant ratio was significantly correlated$(r=0.9951^{**},\;p^{(0.01)}$. This result indicates that AChE insensitivity was associated with insecticide resistance. Overall, these results suggest that insensitivity of AChE was an important factors to chlorpyrifos resistance in diamondback-moth, and the slightly increased activity of GST may also have contributed to that.

Diagnostic Strategy Using Barium Enema and Rectal Suction Biopsy with Acetylcholinesterase Histochemistry in Neonates with Suspious Hirschsprung's Disease (신생아 Hirschsprung's Disease에서 Barium Enema와 Acetylcholinesterase 조직화검사법을 이용한 진단적 접근)

  • Choi, Young-Il;Choi, Soon-Ok;Park, Woo-Hyun
    • Advances in pediatric surgery
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    • v.7 no.2
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    • pp.105-111
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    • 2001
  • To investigate the diagnostic accuracy and applicability of barium enema(BE) and rectal suction biopsy with acetyl cholinesterase(AChE) histochemistry in the diagnosis of neonatal Hirschsprung's disease(HD), we retrospectively reviewed the findings of BE and AChE staining in 96 neonates with suspected HD during a 10-year period from January 1991 to December 2000. Sixty-nine cases of HD(58 males and 11 females) and 27 cases of non-HD are included in this study. In regard to BE, HD was based on definite transitional zone, suspicious HD on reversed rectosigmoid index(RSI <1), and non-HD on normal RSI(RSI>1). The histochemical criterion used for the diagnosis of HD was that of Chow et al(1977), i.e., the presence of many coarse discrete cholinergic nerve fibers in the muscularis mucosae and in the immediately subjacent submucosa regardless of infiltration of cholinergic nerve fibers in the lamina propria. Of 66 neonates with HD who underwent BE, transitional zone was identified in 33 cases(50 %) and reversed RSI in 19 cases(21 %), microcolon in 4 cases and normal finding in 10 cases(15 %) while of 27 neonates with non-HD, there was normal finding in 16 cases and reversed RSI in 9 cases(41 %). Thus diagnostic accuracy based on transitional zone was 64 %. The positive predictive value of reversed RSI for the diagnosis of HD was 68 %. Of 42 neonates with HD who underwent AChE histochemistry, there were 41 AChE-positive reactions and one AChE-negative reaction in a neonate with total colonic aganglionosis, while of 27 cases of non-HD, there were one equivocal AChE-positive reaction and 26 AChE-negative reactions. Thus AChE histochemical study showed a 97 % diagnostic accuracy with a 98 % sensitivity and a 96 % specificity. In conclusion, we believe that BE is valuable as a first diagnostic step since about 80 % of neonates with HD show significant radiologic findings such as a transitional zone or reversed RSI. AChE histochemical study was a more reliable diagnos tic tool showing a 97 % diagnostic accuracy, and is part.

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Isolation of Acetylcholinesterase Inhibitors from the Flowers of Chrysanthemum indicum Linne

  • Lim, Soon-Sung;Han, Sag-Myung;Kim, Sun-Young;Bae, Young-Soo;Kang, Il-Jun
    • Food Science and Biotechnology
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    • v.16 no.2
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    • pp.265-269
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    • 2007
  • There is significant interest in finding new sources of acetylcholinesterase (AChE) inhibitors for use in treating Alzheimer's disease, since only a few AChE inhibitors are available for clinical use, such as galanthamine, physostigmine, and tacrine. The ethanol extract of Chrysanthemum indicum Linne flowers was analyzed and found to markedly decrease AChE activity. Acaciin and $acacetin-7-O-{\beta}-D-galactopyranoside$ were identified as the active compounds responsible for the AChE inhibition by using an activity-guided fractionation strategy. The relationship between structure and activity for five flavonoids (acaciin, $acacetin-7-O-{\beta}-D-galactopyranoside$, luteolin, and two other commercially available flavonoids, i.e., apigenin and acacetin) was also investigated, revealing that the presence of methoxy groups at C-4' in the B ring and a sugar at O-7 in ring A appear to be essential for the inhibition of AChE.

Flow Injection Biosensor for the Detection of Anti-Cholinesterases

  • Chung, Myung-Sun;Lee, Yong-Tae;Lee, Hye-Sung
    • BMB Reports
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    • v.31 no.3
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    • pp.296-302
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    • 1998
  • A potentiometric flow injection biosensor for the analysis of anti-cholinesterases (anti-ChEs), based on inhibition of enzyme activity, was developed. The sensor system consists of a reactor with acetylcholinesterase (AChE) immobilized on controlled pore glass and a detector with an $H^{+}-selective$ PVC-based membrane electrode. The principle of the analysis is based on the fact that the degree of inhibition of AChE by an anti-ChE is dependent on the concentration of the anti-ChE in contact with AChE. The sensor system was optimized by changing systematically the operating parameters of the sensor to evaluate the effect of the changes on sensor response to ACh. The optimized biosensor was applied to the analysis of paraoxon, an organophosphorus pesticide. Treatment of the inhibited enzyme with pyridine-2-aldoxime fully restored the enzyme activity allowing repeated use of the sensor.

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