• 한국동물위생학회지
• /
• 제14권1호
• /
• pp.71-77
• /
• 1991

Parathion is widely used in agriculture, but it is highly toxic and now clear that parathion behaves like a cholinergic drug by inhibiting the enzyme cholinesterase. In order to know acute toxicity and the changes of cholinesterase activity according to time lapsed in Sprague-Dawley rats injected single with half dose to LD$_{50}$ of parathion, cholinesterase activities in serum, spinal cord, whole brain and median lethal dose between sex difference were investigated. The results obtained were summerized as follows ; 1. 4LD_{50}$ values of parathion given intraperitoneally to male and female rats were 10.5mg / kg(95% confidence limits, 6.6-16.8mg/ kg) and 3.3mg/ kg(95% confidence limits, 1.9-5.6mg/ kg). 2. The inhibition rate of cholinesterase activities in serum of parathion-injected rats according to time lapsed were peakly decreased to 35.4%(male) and 32.4%(female) after 1 hour in comparison to control group, but cholinesterase activities were completely recovered after 48 hours. 3. The inhibition rate of cholinesterase activities in spinal cord of parathion-injected rats according to time lapsed were peakly decreased to 31.1% (male) and 36.3% (female) after 30 minutes in comparison to control group, but cholinesterase activities were completely recovered after 48 hours. 4. The inhibition rate of cholinesterase activities in whole brain of parathion -injected rats according to time lapsed were peakly decreased to 32.2%(male) and 42.6%(female) after 1 hour in comparison to control group, but cholinesterase activities were completely recovered after 48 hours.s.

• 한국환경과학회지
• /
• 제11권4호
• /
• pp.391-397
• /
• 2002

Carbamate 농약에 대한 cholinesterase(ChE)활성저해 관계를 규명 하고자 in vivo와 in vitro 실험을 하였다. ChE의 최적 pH는 8.0이었다. 병아리 혈장의 ChE 활성은 기질로 acetylcholin를 사용할 경우 24.6 $\mu$mol/min/g protein이었다. in vivo에서 BPMC을 0.32 mg/kg 경구 투여한 15분 후에 ChE 활성이 60%까지 저해되었으며 그 후 12시간 후에 97% 까지 회복이 일어났다. in vitro에서 효소 활성이 50%로 저해되는데 필요한 농도인 I$_{50}$이 Phenyl N-methylcarbamate계에 XMC는 329 $\mu\textrm{g}$/$\ell$였고, metolcarb은 214 $\mu\textrm{g}$/$\ell$였다. BPMC는 111 $\mu\textrm{g}$/$\ell$, propoxur는 107 $\mu\textrm{g}$/$\ell$, isoprocarb는 104 $\mu\textrm{g}$/$\ell$이었다. Aromatic N-methylcarbamate계에 속하는 carbaryl의 I$_{50}$은 280 $\mu\textrm{g}$/$\ell$이었고, carbofuran 114 $\mu\textrm{g}$/$\ell$이었다.이었다.

• 한국동물위생학회지
• /
• 제15권1호
• /
• pp.58-66
• /
• 1992

The insecticide p-nitropheny diethyl thiophospate is alse known by the symbol E.605 and a legion of trade names including “parathion”. The insecticide is widely used in agriculture, but it is highly toxic and now clear that parathion behaves like a cholinergic drug by inhibiting the enzyme cholinesterase. In order to know acute toxicity and the changes of glucose concentrations and activity according to time lapsed in female mice given orally single with the half dose to $LD_{50}$ of parathion, glucose contents and cholinesterase activities in serum as well as cholinesterase activities in whole brain and spinal cord were investigated, otherwise median lethal dose ($LD_{50}$) of parathion given orally against female mice was determined. The results obtained were summerized as follows ; 1. $LD_{50}$ value of parathion given orally to female mice was 7.1mg/kg(95% confidence limits, 3.8-13.1mg/kg) 2. The inhibition rate of cholinesterase activities in serum of parathion-administrated mice according to time lapsed were peakly decreased to 61% after 30 minutes in comparison to control group, but activities were completely recovered after 48 hours. 3. The inhibition rate of cholinesterase activities in whole brain of parathion-administrated mice according to time lapsed were peakly decreased to 49% after 2 hours in completely recovered after 24 hours. 4. The inhibition rate of cholinesterase activities in spinal cord of parathion-administrated mice according to time lapsed were peakly decreased to 57% after 2 hours in comparison to control group, but activities were completely recovered after 48 hours. 5. The changes of glucose contents in serum of parathion-administrated mice according to time lapsed and in directly after death due to parathion poisoning were no significantly difference.

• Fisheries and Aquatic Sciences
• /
• 제17권4호
• /
• pp.421-425
• /
• 2014

The antioxidant and cholinesterase inhibitory activities of the acetone and dichloromethane ($CH_2Cl_2$) extracts of the by-products (heads, shells, and tails) of Pandalus borealis, Pandalus hypsinotus, and Pandalopsis japonica belonging to the family Pandalidae were investigated and their bioactivities were compared. The antioxidant and cholinesterase inhibitory activities of the organic solvent extracts of three shrimp by-products were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis[3-ethylbenzothiazoline-6-sulfonic acid] ($ABTS^+$) radical scavenging activities, reducing power and xanthine oxidase (XO) inhibitory activity assays and Ellman's colorimetric method. The extracts of P. hypsinotus exhibited the highest antioxidant and cholinesterase inhibitory activities. The acetone extracts showed more potent activities toward antioxidant and cholinesterase inhibition compared with the $CH_2Cl_2$ extracts. Furthermore, the total carotenoid contents of the acetone extracts were higher than those of the $CH_2Cl_2$ extracts. Thus, the carotenoid contents may affect antioxidant and cholinesterase inhibition. Our results suggest that the shrimp by-products could act as a nutraceutical agent to prevent oxidative stress and Alzheimer's disease.

• 농약과학회지
• /
• 제5권1호
• /
• pp.12-18
• /
• 2001

유기인계 농약에 대한 cholinesterase(ChE)활성저해 관계를 규명 하고자 in vivo와 in vitro 실험을 하였다. 병아리 혈장의 ChE 활성은 $23{\mu}mol$/min/g protein이었다. in vivo에서 terbufos의 투여량을 $LD_{50}$의 0.2배(0.362 mg/kg)와 0.5배(0.905 mg/kg)로 투여하였을 경우, 투여 15분 후에 ChE 활성이 각각 36%와 96%까지 저해되었으며 그 후 회복이 일어난다. in vitro에서 유기인계의 P에 S가 결합된 P=S구조의 phosphorodithioate와 phosphorothioate의 Ki는 $74{\sim}322\;mole^{-1}min^{-1}$로 낮았다. 그러나 P에 S가 산화되어 O가 결합된 P=O구조의 phosphate와 phosphorothiolate의 Ki는 $13898{\sim}79610\;mole^{-1}min^{-1}$로 높았다. 따라서 P=S가 P=O로 산화됨으로서 ChE의 저해도가 커져서 독성이 강해짐을 확인하였다. phosphorodithioate와 phosphorothioate형의 $pI_{50}$값은 $21{\sim}102 mg/L(ppm)$ 이었다. 그러나 phosphate와 phosphorothiolate형의 $pI_{50}$값은 $0.519{\sim}0.071$ mg/L(ppm)이었다. 즉 ChE을 이용한 enzyme-inhibition(EI)법을 유기인계 농약의 정성적 검출에 이용한다면, P=O구조인 phosphate와 phosphorothiolate형은 1ppm이하 즉 ppb단위까지 정성적 검출이 가능하다.

• 한국응용곤충학회지
• /
• 제10권1호
• /
• pp.13-22
• /
• 1971

이 실험은 이화명나방 월동 유충에 대한 유기인 살출제의 in vitro에 있어서의 ChE저해력과 약제의 화학 구조와의 관계, in vivo에 있어서의 국소 시용법에 의한, 살충제의 독성과 화학 子조와의 관계, 특히 ChE 저해력과 살충력(독성)과의 관계를 비교 연구할 목적으로 실험하였으며 그 결과를 다음과 같이 요약할 수 있다. 1, Phosphate compounds는 thiophosphate compounds보다 in vitro에 있어서의 ChE 저해력은 강하다고 할 수 있으나 in vivo에 있어서의 독성은 비례적으로 반드시 강하다고 할 수 없다. 2. Alcoxy 즉 diethoxy는 dimethoxy보다 ChE 저해력과 독성이 비례적으로 반드시 강하다고 할 수 없다. 3. $(RO)_2PO(S)X$ 부분에 있어서 이 X부분이 달라짐에 따르는 ChE 저해력과 살충력에 대해서는 약제에 따라서 각각 다르게 나타나므로 언급할 수 없다. 4. ChE 저력이 강한 약제는 살충력도 비례적으로 강하다고 할 수 없다. 그러나 화학 구조상 안정성이고 실용 농약인 Ethylparathion, Malathion, Let aycid, EPN, Sumithion 및 Diazinon 등에서 고찰할 때 반드시 비례적인 것은 아니나 어느 정도의 파행 관계가 있지 않은가 추찰된다.

• 대한약침학회지
• /
• 제22권4호
• /
• pp.231-238
• /
• 2019

Objectives: Alzheimer's disease (AD), an overwhelming neurodegenerative disease, has deleterious effects on the brain that consequently causes memory loss and language impairment. This study was intended to investigate the neuroprotective activity of the two essential oils (EOs) from Iranian Pistacia khinjuk (PK) leaves and Allium sativum (AS) cloves against β-Amyloid 25-35 (Aβ25-35) induced elevation of cholinesterase enzymes in AD. Methods: The EOs of PK (PKEO) and AS (ASEO) were prepared and analyzed in terms of extraction yield, phenolic content, and cholinergic markers in vitro. Moreover, both were administered orally to adult male Wistar rats at concentrations of 1, 2, and 3%. The inhibitory potential of PKEO and ASEO was compared with Donepezil (0.75 mg/kg) against the high activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Results: PKEO reached an inhibition rate of 83.6% and 81.4% against AChE and BChE, respectively. ASEO had lower anti-cholinesterase activity (65.4% and 31.5% for the inhibition AChE and BChE). PKEO was found to have more phenolic content than ASEO. A significantly positive correlation was observed between the total phenolics and anti-cholinesterase potential. In rats, both EOs decreased the enzyme activity in a concentration-dependent manner. As compared with Donepezil, the significant difference in the AChE and BChE inhibition occurred as rats were treated with PKEO 3% (p < 0.05). Conclusion: It could be concluded that PKEO and ASEO are potent inhibitors of AChE and BChE in rats that hold promise to be used for the treatment of AD.

• 한국자원식물학회지
• /
• 제31권1호
• /
• pp.10-15
• /
• 2018

황칠나무 잎과 줄기를 분리하여 각각 methanol 추출하여, 계통분획상법에 따라 dichloromethane, ethyl acetate, butanol로 분획하였다. 분획물로 실시한 TLC에서 알칼로이드 성분으로 분리되는 성분을 확인할 수 있었다. 잎과 줄기 모두 ethyl acetate분획물은 $IC_{50}$ $30{\mu}g/m{\ell}$으로 높게 측정 되었으며, ethyl acetate, dichloromethane, butanol분획물 순으로 저해 활성이 높게 나타났다. Acetyl cholinesterase inhibition assay를 실시한 결과 황칠나무 잎과 줄기 모두 dichloromethane, ethyl acetate, butanol 분획물 순으로 저해 활성이 높은 것으로 나타났으며, 가장 높은 활성을 보인 황칠나무 줄기와 잎의 dichloromethane 분획물의 알칼로이드 함량이 상대적으로 높은 것으로 보아 알칼로이드 성분에 의한 것으로 유추 할 수 있으므로, 알칼로이드 성분의 동정 및 성분구조의 규명을 통하여 AChE저해 활성을 이용한 신경관련 질환에 도움을 줄 수 있는 천연물의 개발이 가능할 것으로 사료된다.

• Environmental Analysis Health and Toxicology
• /
• 제7권3_4호
• /
• pp.57-67
• /
• 1992

BPMC (2-Sec-butylphenyl N-methylcarbamate) was treated at the level of 100mg/kg/day in oral administration for 12th days in rat. It was investigated not only that the hematogram and the serological parameters, but also the content of cytochrome P-450, the activity of TBA, glucose-6-phosphatase, cholinesterase and carboxylesterase in rat. The results were as follows: The hematogram was not found any alteration but the value of AST, ALT, LDH and the content of glucose in serum were significantly increased compare with that of control group. The content of cytochrome P-450 in liver was increased significantly on the contrary cytochrome P-450 in kideny and NADPH-cytochrome c reductase in liver and Kidney were not significantly increased. After the final 12th day, the value of TBA and the activity of glucose-6-phosphatase appeared to the tendency of increasement in the liver. The activity of cholinesterase and carboxylesterase both in serum and liver were decreased. Especially the activity of cholinesterase was more significantly decreased. It was conclusion that the function of this insectivide should be due th the inhibition of cholinesterase activity.

• Bulletin of the Korean Chemical Society
• /
• 제35권6호
• /
• pp.1681-1686
• /
• 2014

A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.