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Acetylcholinesterase liquid crystal biosensor for identification of ache inhibitors by a reactivator

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Science China Chemistry 2014年第11期57卷 1589-1595页

作者： DING HuaZhi LIAO ShuZhen XIAO FuBing SHEN GuoLi YU RuQin WU ZhaoYang State Key Laboratory of Chemo/Biosensing and Chemometrics College of Chemistry and Chemical Engineering Hunan University

An improved acetylcholinesterase liquid crystal(LC) biosensor has been developed for the identification of organophosphates(OPs) by using a reactivator. When the acetylcholinesterases(aches) inhibited by different kinds of OPs are reactived by a reactivator, the catalytic activity of aches can be recovered with different activation efficiency because of the different phosphorylation structures formed in the inhibited aches. Accordingly, the reactived aches can catalyze the hydrolysis of acetylthiocholine to generate thiocholine product in different degrees, which will result in different catalytic growth of AuNPs and further form distinct orientational response of LCs. Based on such a reactivation mechanism, the ache LC biosensor with a simple, rapid and visual procedure achieves an obvious identification of three OPs pesticides, methamidophos, trichlorfon and paraoxon, by using a pralidoxime reactivator.

关键词： ache liquid crystal organophosphates reactivator pralidoxime identification

Bis(9)-(−)-Meptazinol,a novel dual-binding ache inhibitor,rescues cognitive deficits and pathological changes in APP/PS1 transgenic mice

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Translational Neurodegeneration 2018年第1期7卷 201-211页

作者： Yuhuan Shi Wanying Huang Yu Wang Rui Zhang Lina Hou Jianrong Xu Zhuibai Qiu Qiong Xie Hongzhuan Chen Yongfang Zhang Hao Wang Department of Pharmacology and Chemical Biology Institute of Medical SciencesShanghai JiaoTong University School of MedicineShanghai 200025People’s Republic of China Department of Medicinal Chemistry School of PharmacyFudan UniversityShanghaiPeople’s Republic of China

Background:Alzheimer’s disease(AD)is a progressive and irreversible neurodegenerative brain disorder,which is the most common form of *** efforts have been made to find effective and safe treatment against *** inhibitors(acheIs)have been widely used for the treatment of mild to moderate *** this study,we investigated the effect of Bis(9)-(−)-Meptazinol(B9M),a novel potential dual-binding acetylcholinesterase(ache)inhibitor,on learning and memory abilities,as well as the underlying mechanism in the APP/PS1 mouse model of ***:B9M(0.1μg/kg,0.3μg/kg,and 1μg/kg)was administered by subcutaneous injection into eight-month-old APP/PS1 transgenic mice for four *** water maze,nest-building and novel object recognition were used to examine learning and memory ability.Aβ levels and Aβplaque were evaluated by ELISA and ***:Our results showed that chronic treatment with B9M significantly improved the cognitive function of APP/PS1 transgenic mice in the Morris water maze test,nest-building test and novel object recognition ***,B9M improved cognitive deficits in APP/PS1 mice by a mechanism that may be associated with its inhibition of the ache activity,Aβ plaque burden,levels of Aβ and the consequent activation of astrocytes and microglia in the brain of APP/PS1 transgenic *** of important,the most effective dose of B9M in the present study is 1μg/kg,which is one thousand of the dosage of Donepezil acted as the control ***,B9M reduced Aβ plaque burden better than ***:These results indicate that B9M appears to have potential as an effective ache inhibitor for the treatment of AD with symptom-relieving and disease-modifying properties.

关键词： Bis(9)-(−)-Meptazinol ache inhibitor Alzheimer’s disease

Studies on Structure-Activity Relationship of Nonquaternary ache Reactivators

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Chinese Science Bulletin 1993年第6期38卷 527-528页

作者：焦克芳宋鸿锵卜志洁 Institute of Pharmacology and Toxicology Beijing 100850 PRC

A series of dialkylaminoalkyl thioesters of α-keto thiohydroximic acid （4-RC6H4-COC·（NOH）-S-（CH2）n-NR′R″） as acetylcholinesterase （ache） reactivators in vitro were reported, whose correlations between oxime acid（α-keto thiohydromate acid） dissociation constants （pKa）, Hammett values（σp） and rate of ache reactivation were discussed by Bedford etal. They were considered as nonquaternary ache reactivators based on the classical reactivative theory by the authors.

关键词： ache dissociation constants Bedford ache salts substituted heterocyclic Phenyl diethyl

EFFECT OF ELECTROACUPUNCTURE ON ACH CONTENT AND ache ACTIVITY IN THE SPINAL GANGLIA OF RAT

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针刺研究 1989年第Z1期 182-183页

作者： Zhang Yuwen Zhang Nana Qian Hui Liu Xiaochun Guan Xinmin Research Department of Acupuncture Analgesia Mechanism Tong-ji Medical University

The present exneriment war carried out for the observations on changes ofACh content and ache activity in spinal ganglia after dorsal rhiztomy andelectroacupuncture by means of physiological and biochemical methods andaimed at investigations into relationship between peripheral and acupunctureinformation transmitted through primary afferent. The results indicate:1. It was proved that ACh exists in spinal *** average value of ACh content measured bioassaily is 0.424±0.109ngper mg of humid tissue. The data is normal distribution.

关键词： ache ACH EFFECT OF ELECTROACUPUNCTURE ON ACH CONTENT AND ache ACTIVITY IN THE SPINAL GANGLIA OF RAT

不同温度条件下呋喃丹对赤子爱胜蚓体内蛋白含量以及SOD和ache活性的影响

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生态与农村环境学报 2007年第1期23卷 57-62页

作者：孙维林玉锁胡玲南京农业大学资源与环境学院江苏南京210095 国家环境保护总局南京环境科学研究所/国家环境保护农药环境评价与污染控制重点实验室江苏南京210042 江苏省环境监测中心江苏南京210000

采用滤纸法研究不同温度下呋喃丹对赤子爱胜蚓(E isenia foetida)死亡率、体内蛋白含量以及超氧化物歧化酶(SOD)和乙酰胆碱酯酶(ache)活性的影响。研究发现,10℃下,蚯蚓体内蛋白含量在30 mg.L-1呋喃丹处理时略有升高,而后随时间和浓度... 详细信息

采用滤纸法研究不同温度下呋喃丹对赤子爱胜蚓(E isenia foetida)死亡率、体内蛋白含量以及超氧化物歧化酶(SOD)和乙酰胆碱酯酶(ache)活性的影响。研究发现,10℃下,蚯蚓体内蛋白含量在30 mg.L-1呋喃丹处理时略有升高,而后随时间和浓度的升高,蛋白含量则随之降低;各浓度处理组的SOD活性值基本上高于对照组,48和72 h的SOD活性比24 h时平均提高220%和148%。时间和浓度对蛋白含量和SOD活性的影响达到极显著(Pache活性都具有明显抑制作用,ache活性在处理时段内的最高降低率为90%。结果表明:温度对蚯蚓死亡率、蛋白含量以及SOD和ache活性影响显著,ache可以作为一个稳定的生物监测指标用于评价农药对土壤环境的污染影响。

关键词：呋喃丹赤子爱胜蚓温度蛋白质 SOD ache

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镉对罗非鱼脑ache及组织中代谢酶的影响

浙江大学学报（农业与生命科学版） 2004年第6期30卷 673-678页

作者：惠天朝王家刚朱荫湄陈晓明陆永干浙江大学动物医学系浙江杭州310029 浙江大学环境科学系浙江杭州310029 杭州市畜牧兽医总站浙江杭州310020

将尼罗罗非鱼分别在含0.5mg/LCd和5.0mg/LCd的水环境中染毒28d,对其脑乙酰胆碱脂酶(ache)及鳃、肝脏和心脏中的乳酸脱氢酶(LDH)、丙氨酸氨基转移酶(ALT)和天门冬氨酸氨基转移酶(AST)分别进行测定.结果表明,高浓度或长期的低浓度镉污染... 详细信息

将尼罗罗非鱼分别在含0.5mg/LCd和5.0mg/LCd的水环境中染毒28d,对其脑乙酰胆碱脂酶(ache)及鳃、肝脏和心脏中的乳酸脱氢酶(LDH)、丙氨酸氨基转移酶(ALT)和天门冬氨酸氨基转移酶(AST)分别进行测定.结果表明,高浓度或长期的低浓度镉污染可抑制脑ache的活性.高镉组中LDH在三个组织中都极显著下降,下降的程度依次为:肝脏>心脏>鳃,而在低镉组中LDH在后期显著升高;肝、心及鳃中ALT和AST在两组中匀显著下降,其中ALT下降程度依次为肝>心>鳃;AST依次为心>肝>鳃.可见,高浓度镉可引起鱼的神经机能紊乱和能量代谢障碍;使鱼的组织细胞受到不同程度的损害,其中对肝脏细胞的损害最为严重,其次是心脏和鳃.

关键词：镉罗非鱼 ache 酶

ache deficiency or inhibition decreases apoptosis and p53expression and protects renal function after ischemia/reperfusion

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AChE deficiency or inhibition decreases apoptosis and p53exp...

MTDLs Design on ache （Acetylcholinesterase） and β-Secretase （BACE-1）： 3D-QSAR and Molecular Docking Studies

第三届细胞结构与功能的信号基础研讨会

作者：张学军中国科学院上海生命科学学院生物化学与细胞生物学研究所

We recently reported that the expression of thesynaptic form of acetylcholinesterase(ache) is inducedduring apoptosis in various cell types in vitro. Here,we provide evidence to confirm that ache is expressed during ischemia-reperfusion(I/R)-induced apoptosis in *** I/R is a major cause of acute renal failure(ARF),resulting in injury and the eventual death of renal cells due to a combination of apoptosis and *** achedeficient mice and ache inhibitors,we investigated whether ache deficiency or inhibition can protect against apoptosis caused by I/R in a murine kidney *** clamping of renal pedicles for 90 min followed by reperfusion for 24 h caused significant renal dysfunction and *** genetic ache deficiency and chemical inhibition of ache(provided by huperzine A,tacrine and donepezil) significantly reduced the biochemical and histological evidence of renal dysfunction following I/*** of caspases-8,-9,-12,and -3 in vivo wereprevented and associated with reduced levels of cell apoptosis and cell death.A further investigation also confirmed that ache deficiency down-regulated p53 induction and phosphorylation at serine-15,and decreased the Bax/ Bcl-2 ratio during I/*** conclusion,our study demonstrates that ache may be a pro-apoptotic factor and the inhibition of ache reduces renal I/R *** findings suggest that ache inhibitors may represent a therapeutic strategy for protection against ischemic acute renal failure.

关键词： Apoptosis ache p53

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Journal of Pharmacy and Pharmacology 2015年第10期3卷 489-501页

作者： Jiancheng Shi Wentong Tu Jiarong Sheng Chusheng Huang College of Chemistry and Material Sciences Guangxi Teachers Education University Nanning 530001 China

To find promising new multitargeted AD （Alzheimer＇s disease） inhibitors, the 3D-QSAR （three-dimensional quantitative structure-activity relationship） model for 32 AD inhibitors was established by using the CoMFA （comparative molecular field analysis） and CoMSIA （comparative molecular similarity index analysis） methods. Results showed that the CoMFA and CoMSIA models were constructed successfully with a good cross-validated coefficient （q2） and a non-cross-validated coefficient （R2）, and the binding modes obtained by molecular docking were in agreement with the 3D-QSAR results, which suggests that the present 3D-QSAR model has good predictive capability to guide the design and structural modification of novel multitargeted AD inhibitors. Meanwhile, we found that one side of inhibitory molecule should be small group so that it would be conductive to enter the gorge to interact with the catalytic active sites of ache （acetylcholinesterase）, and the other side of inhibitory molecule should be large group so that it would be favorable for interaction with the peripheral anionic site of ache. Furthermore, based on the 3D-QSAR model and the binding modes of ache and [3-secretase （BACE-1）, the designed molecules could both act on dual binding sites of ache （catalytic and peripheral sites） and dual targets （ache and BACE-1）. We hope that our results could provide hints for the design of new multitargeted AD derivatives with more potency and selective activity.

关键词： 3D-QSAR molecular docking ache BACE-1 MTDLs.

两种温度条件下杀虫单对赤子爱胜蚓蛋白含量SOD和ache活性的影响

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农业环境科学学报 2007年第5期26卷 1816-1821页

作者：孙维邰托娅林玉锁国家环境保护总局南京环境科学研究所国家环境保护农药环境评价与污染控制重点实验室

为评价土壤的农药污染程度,选用杀虫剂杀虫单对赤子爱胜蚓(Eiseniafoetida)进行染毒试验,采用滤纸法研究两种温度下农药污染对赤子爱胜蚓的毒理和其体内蛋白含量、超氧化物歧化酶(SOD)和乙酰胆碱酯酶(ache)酶活力的影响。结果发现,杀虫... 详细信息

为评价土壤的农药污染程度,选用杀虫剂杀虫单对赤子爱胜蚓(Eiseniafoetida)进行染毒试验,采用滤纸法研究两种温度下农药污染对赤子爱胜蚓的毒理和其体内蛋白含量、超氧化物歧化酶(SOD)和乙酰胆碱酯酶(ache)酶活力的影响。结果发现,杀虫单单一作用时,在10℃和20℃两种温度下,蚯蚓死亡率分别为20%和30%;随杀虫单浓度的增大,蚯蚓体内蛋白含量出现不同程度的升高;SOD活性随农药浓度的升高整体表现为下降趋势,其降低率分别为32.2%和21.2%,但规律不很明显;时间和浓度对SOD的影响达到极显著(Pache活力的抑制作用不明显,这与该农药是较弱的胆碱酯酶抑制剂有关,且随暴露时间的延长,ache活力表现出一定的恢复现象。试验结果表明,温度对蚯蚓死亡率及蛋白含量、SOD、ache酶的活性有一定影响,可通过对比两种温度下的蚯蚓体内酶活性的大小来进行生物监测和环境影响评价。

关键词：杀虫单赤子爱胜蚓温度蛋白含量 SOD ache