• 한국환경과학회지
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• 제7권1호
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• pp.52-56
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• 1998

The effects of organophosphorus and carbamate pesticides were examined inhibition of the acetylcholinesterase activity in the chicken brain with enzyme-inhibition methods. The acetylcholinesterase activity in chicken brain determined by the Ellman method was 167 mmol/min/g protein. The optimum pH of acetycholinesterase was 8.2. $pl_{50}$ of acetycholinesterase by some organophosphorus were 3.80M of phosphorodlthioate, 4.04M of phosphorothioate, 6.33M of phosphate, and 6.60M of phosphrothiolate. pluto of acetycholinesterase by some carbamates were 5.1 OM of XMC, 5. 90M of carbofuran, 6.16M of isoprocarb, 6.30M of carbaryl, 6.47M of BPMC, and 6.77M of propoxur. pluto of carbamates selected was similar to that of phosphorothioate and phosphate organophosphates.

• BMB Reports
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• 제28권4호
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• pp.290-292
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• 1995

Existence of a binding site for choline esters with an acyl chain of various sizes was examined by comparing the inhibitory potency of the respective compound. In contrast to acetylcholine, which showed a pure competitive pattern of inhibition, choline esters with an acyl chain of a long size ($C{\geq}5$) expressed a mixed type of inhibition. Binding of choline esters containing a long chain ($C_7-C_{12}$) to the hydrophobic region in the active site is deduced from a linear relationship between the $K_{iE}$ value and the size of acyl moiety, and a good hydrophobicity relationship. In addition, the non-competitive component in the inhibition of acetylcholinesterase seems to be due to the interaction of choline esters with both the hydrophobic site and the trimethylammonium-binding site in the active center of the acetylated acetylcholinesterase.

• 생약학회지
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• 제38권4호
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• pp.308-311
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• 2007

Inhibition of acetylcholinesterase and amyloid beta(1-42) peptide is good drug targets for Alzheimer's disease therapeutics. Among the twenty enthusiasm reducing herbals, the 70% methanol extracts (1 mg/ml) of Moutan Radicis Cortex and Forsythiae Fructus showed 91.5% and 85.3% about acethylcholinesterase inhibition, respectively. The extracts (1 mg/ml) of Coptidis Rhizoma and Paeoniae Radix Rubra showed more than 85% inhibition rate against amyloid beta (1-42) peptide aggregation. The neuroprotective effect of the extracts (1 mg/ml) of Moutan Radicis Cortex, Forsythiae Fructus and Paeoniae Radix Rubra showed 90.0%, 87.4% and 85.1% to compare with amyloid beta (1-42) peptide treated cells (IMR-32), respectively. Three herbs, Moutan Radicis Cortex, Forsythiae Fructus and Paeoniae Radix Rubra are promising candidates from natural products for development of Alzheimer's disease therapeutics.

• 한국미생물·생명공학회지
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• 제28권6호
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• pp.322-328
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• 2000

To screen agent for the treat-ment of Alzhimers Disease several strains of bacteria producing acetylcholinesterase inhibitor ware isolated from soil. Strain 960903 showed strong acetylcholinesteras inhibitory activity and low butyrylcholinesterse inhibitory activity. The strain 960903 was identified as Pseudomonas sp. Acetylcholinesterase inhibitor ws highly achieved in fermentation medium containing soluble starch 3.0%, glycerol 1.0%, pharmamedia 0.5%, KCI 0.3%, $CaCO_3$ 0.2%, MgS $O_4$..$7H_2$O 0.05%, $KH_2$$PO_4$ 0.05%(pH6.5) at $30^{\circ}C$ for 4 days. Acetylcholinesterase inhibitor was purified by Diaion WA-30($OH^{-}$) column charomatography and cellulose column chromatography. Acetylcholinesterase inhibi-tor showd the maximum wavelength at 205 nm and was soluble in water, acetic acid, ethanol, methanol and dime-thyl sulfoxide. The concentration of 50% inhibition($IC_{50}$) of inhibitor against acetylcholinesterase was 25$\mu\textrm{g}$/ml. The inhibitor was inactivated on heating ar $100^{\circ}C$ fro 15 min and more stable in acidic region than alkaline region.n.

• BMB Reports
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• 제37권3호
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• pp.330-338
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• 2004

Different types of cardiotoxin (I-V and n) were isolated and purified from the venom of the Taiwan cobra (Naja naja atra). The effects of these cardiotoxins were studied on membrane-bound acetylcholinesterase, which was isolated from a sheep's brain cortex. The results showed that cardiotoxins I-III, V, and n activated the enzyme by modification of substrate inhibition, but cardiotoxin IV's reaction was different. The inhibition and activation of acetylcholinesterase were linked to the functions of the hydrophobicity index, presence of a cationic cluster, and the accessible arginine residue. Our results indicate that Cardiotoxins have neither a cationic cluster nor an arginine residue in their surface area of loop I; therefore, in contrast to fasciculin, cardiotoxins are attached by loop II to the peripheral site of the enzyme. As a result, fasciculin seems to stabilize nonfunctional conformation, but cardiotoxins seem to stabilize the functional conformation of the enzyme. Based on our experimental and theoretical findings, similar secondary and tertiary structures of cardiotoxins and fasciculin seem to have an opposite function once they interact with acetylcholinesterase.

• 동의신경정신과학회지
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• 제14권1호
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• pp.59-74
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• 2003

Alzheimer's disease(AD) is a progressive neurodegenerative disease, which is pathologically characterized by neuritic plaques and neurofibrillary tangles associated with the acetylcholinesterase, apolipoprotein E and butylcholinesterase, and by mutations in the presenilin genes PS1 and PS2, and amyloid precursor proteins (APP) overexpression. The present research is to examine the inhibition effect of CPRT on PS-1, PS-2 and APP overexpression by detected to Western blotting. To verify the Effects of CPRT on cognitive deficits further, we tested it on the scopolamine-induced amnesia model of the mice using the Morris water maze tests, and there was ameliorative effects of memory impairment as a protection to scopolamine. CPRT only partially blocked the increase in blood serum level of acetylcholinesterase and Uric acid induced by scopolamine, whereas blood glucose level was shown to attenuate the amnesia induced by scopolamine and inreased extracellular serum level compared with only scopolamine injection. In conclusion, studies of CPRT that has been known as anti-choline and inhibition ablilities of APP overexpression, this could also be used further as a important research data for a preventive and promising symptomatic treatment for Alzheimer's disease.

• 동의신경정신과학회지
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• 제11권1호
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• pp.19-36
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• 2000

Alzheimer's disease (AD) is progressive neurodegenerative disease, which is pathologically characterized by neuritic plaques and neurofibrillary tangles associated with the acetylcholinesterase, apolipoprotein E and butylcholinesterase, and by mutations in the presenilin genes PS1 and PS2, and amyloid precursor proteins (APPs) overexpression. The present research is to examine the inhibition effect of KBT on PS1, PS2 and APPs overexpression by detected to Western blotting. To verify the Effects of KBT on cognitive deficits further, we tested it on the scopolamine (1 mg/kg)-induced amnesia model of the mice using the Morris water maze tests, and there was ameliorative effects of memory impairment as a protection to scopolamine. KBT only partially blocked the increase in blood serum level of acetylcholinesterase and Uric acid induced by scopolamine, whereas blood glucose level was shown to attenuate the amnesia induced by scopolamine and inreased extracellular serum level compared with only scopolamine injection. In conclusion, studies of KBT that has been know as anti-choline and inhibition ablilities of APPs overexpression, this could also be used further as a important research data for a preventive and promising symptomatic treatment for Alzheimer's disease.

• 한국식품저장유통학회지
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• 제23권2호
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• pp.239-245
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• 2016

본 연구는 선행 연구된 삼채뿌리의 뛰어난 영양성을 토대로 기능성 식품소재로의 이용가능성을 확인하고 활용도를 높이고자 국내산 및 미얀마산 삼채뿌리의 항산화 및 생리활성을 측정하였다. 삼채뿌리의 총 폴리페놀과 총 플라보노이드 함량은 국내산 삼채뿌리가 각각 5.27 mgGAE/g, 0.35 mgQE/g, 미얀마산 삼채뿌리가 각각 4.80 mgGAE/g, 0.24 mgQE/g으로 국내산 삼채뿌리가 더 높은 함량을 나타냈다. 삼채뿌리의 항산화력을 측정한 결과 DPPH 라디칼 소거능은 미얀마산이 더 높은 활성을 보였지만, ABTS 라디칼 소거능과 $Fe^{2+}$ 킬레이팅 활성, 환원력은 국내산이 더 높은 활성을 보였다. ${\alpha}-Glucosidase$ 저해활성은 국내산의 저해활성이 미얀마산 삼채뿌리의 저해활성보다 더 높았으며 대조구인 acarbose에 비해서도 우수한 저해활성을 보였다. Acetylcholinesterase 저해 활성을 측정한 결과, 50 mg/mL 농도에서 국내산 삼채뿌리가 51.44%로 44.33%의 저해활성을 보인 미얀마산 삼채뿌리보다 더 높은 저해활성을 보였다. 본 연구를 통해 삼채뿌리 특히 국내산 삼채뿌리는 높은 항산화 활성, ${\alpha}-glucosidase$ 및 acetylcholinesterase 저해 활성을 보여 혈당조절제, 치매예방 및 개선제로써의 활용가능성이 큰 것으로 확인되었으며, 이로써 기능성 식품소재로의 활용이 증가될 것으로 판단된다. 하지만 향후 국내산 삼채의 우수성을 검증하기 위하여 여러 지역에서 재배된 삼채의 기능성 분석이 필요할 것으로 판단된다.

• 생약학회지
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• 제33권3호통권130호
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• pp.211-218
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• 2002

The methanol extracts of 340 kinds of Korean medicinal herbs were examined in vitro for the inhibitory effect on the acetylcholinesterase (AChE, E.C. 3.1.1.7) from electric eel using acetylthiocholine as a substrate. Among tested, the extracts of Coptidis Rhizoma, Phellodendri Cortex, Evodiae Fructus, Myrrha, Arecae Semen and Piperis nigri Fructus were found to exhibit a significant inhibition upon the acetylcholinesterase in a dose dependent manner, respectively.

• 산업식품공학
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• 제15권4호
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• pp.289-296
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• 2011

Twenty four fractions by solvent extraction and/or acid precipitation from fruit body and culture broth of Inonotus obliquus were prepared, and their inhibitory effect against acetylcholinesterase (AChE) was investigated. Among these fractions, acid (1 M HCl) precipitates from cell-free culture broth and fruit body exhibited the highest inhibitory effect on AChE in vitro. Acid precipitates inhibited AChE activity in a concentration-dependant manner and $IC_{50}$ values of both acid precipitates were 0.53 mg/mL. The inhibition pattern was general non-competitive inhibition. The energetic parameters were also determined by dual substrate/temperature design. Both acid precipitates increased the values of Ea, ${\Delta}H,/;{\Delta}G$ and ${\Delta}H^{\ast}$ decreasing the value of ${\Delta}S$ for AChE. The results implied that the acid precipitates from I. obliquus increased the thermodynamic barrier, leading to the breakdown of ES complex and the formation of products as inhibitory mechanism.