乙酰胆碱酯酶分子生物学研究进展

乙酰胆碱酯酶是一种在神经传导中起关键作用的酶。它对有机磷农药十分敏感，可作为生物传感器监测环境中有机磷农药的含量。因此对乙酰胆碱酯酶的分子生物学研究是十分必要的。文章介绍了乙酰胆碱酯酶的分子形式、三维结构、基因结构，变构乙酰胆碱酯酶与抗药性的关系以及乙酰胆碱酯酶分子领域应用等方面的研究进展，并对乙酰胆碱酯酶的进一步研究提出了展望。     

γ-氨基丁酸抑制剂的研究进展

当前关于抑制神经活性的杀虫剂的研究主要集中在四种靶标类杀虫剂:电压敏感的钠通道(针对滴滴涕和菊酯类农药)、乙酰胆碱酯酶(针对有机磷和氨基甲酸酯类农药)、乙酰胆碱酯酶受体(针对硝基甲基烯及其类似物)和γ-氨基丁酸(GABA)—门控氯离子通道。对前     

利用植物酯酶快速检测有机磷农药残留的研究进展

植物酯酶与动物乙酰胆碱酯酶一样可以有效地检测有机磷农药残留，介绍了利用植物酯酶快速检测有机磷农药残留的原理、酶源的选择、使用的优缺点以及存在的问题和解决的方法。     

环境样品中有机磷农药测定方法研究进展

在有机氯农药被禁用后，有机磷农药的应用急剧增加，成为农业生产领域使用最广泛的杀虫剂。有机磷农药可抑制乙酰胆碱酯酶，对生态安全和人体健康都会产生严重毒害作用。近年来，随着有机磷农药中毒与污染事件的频繁发生，其检测新方法、新技术研究已成为环境科学领域的研究热点。通过对2012～2022年相关文献的检索、归纳、整理，分析、评述了有机磷农药环境残留的主要检测分析方法，包括样品前处理、有机磷提取与测定方法，从环境介质角度，比较、分析了各种检测方法、技术的优缺点和适用性，同时展望了有机磷农药检测技术的发展趋势。     

聚乙二醇基氯硝柳胺衍生物体外抑制钉螺乙酰胆碱酯酶活性的研究

为研究聚乙二醇基氯硝柳胺衍生物体外抑制钉螺乙酰胆碱酯酶的活性,测定了氯硝柳胺衍生物抑制钉螺乙酰胆碱酯酶的半数抑制浓度IC50.结果表明:随着氯硝柳胺衍生物浓度的增加,对乙酰胆碱酯酶活性的抑制作用逐渐增强;随着聚乙二醇基链长的增加,药物对乙酰胆碱酯酶抑制活性依次减弱.     

在食品质量安全保护法中有关拟除虫菊酯类杀虫剂的作用机制的阐述

1996年,食品质量安全保护法通过后,美国环境保护署(EPA)发布了评价相同作用机制的农药暴露的指南.有机磷和氨基甲酸酯类杀虫剂作为常用农药应独立评价,虽然它们都能抑制乙酰胆碱酯酶,但机制不同.正因为如此,对于累积暴露评估的每类农药,意味着每种有机磷或氨基甲酸酯类农药的暴露都要累加起来,甲胺磷暴露被归于有机磷类农药,杀线威暴露被归为氨基甲酸酯类农药.     

山东农药残毒快速检测仪获国家专利

由山东京蓬生物药业股份有限公司与中国农业大学的专家合作，历时3年研制开发的农药残毒快速检测仪，以及与其配套的试剂乙酰胆碱酯酶和酶片，显色片日前获国家专利。该检测仪采用酶抑制法检测有机磷及氨基甲酸酯类农药残留，运用固态可变光及样液脱色去杂技术，     

酶生物传感器测定农药实验条件的探索

有机磷农药对乙酰胆碱酯酶具有较强的抑制性,利用乙酰胆碱酯酶生物传感器,测定有机磷农药,采用玻碳电极为工作电极,在不同pH值的磷酸缓冲溶液、硼砂盐酸缓冲溶液中进行实验研究。最合适的工作电位区间为0～0.5 V;选用0.1 mL浓度为0.05 mol/L的硼酸（pH=7.0）溶液作底液;底液、底物、酶片依次加入的-△I比较大,信号电流较稳定。     

沙棘叶提取物的体外抗氧化及乙酰胆碱酯酶抑制能力

以沙棘叶为原料,以DPPH?清除能力、总还原力为指标,评估沙棘叶提取物的体外抗氧化活性,并以沙棘叶提取物对乙酰胆碱酯酶的抑制能力为指标,考察其成为乙酰胆碱酯酶抑制剂的潜力。研究结果表明：5种不同乙醇体积分数的（40%、50%、60%、70%、80%）沙棘叶提取物均有较好的抗氧化活性与对乙酰胆碱酯酶抑制能力。以60%乙醇提取的沙棘叶提取物的DPPH?清除率、总还原力及乙酰胆碱酯酶抑制能力最强,分别为（85.80±1.39）%,3.06±0.18,（97.14±0.809）%,可作为抗氧化剂与乙酰胆碱酯酶抑制剂。筛选后的沙棘叶提取物对乙酰胆碱酯酶有较强的抑制能力,半数抑制质量浓度（IC50）值为（1.086±0.144）mg/mL,并且根据酶的抑制动力学分析得出对乙酰胆碱酯酶是竞争性大于非竞争性的混合可逆抑制类型。AutoDock分子对接结果也表明,沙棘叶活性成分与乙酰胆碱酯酶具有一定的对接亲和力。剂效相关性分析表明沙棘叶提取物的抗氧化、酶抑制活性与功能成分之间均存在良好的正相关性（P<0.05）,沙棘叶提取物中起主要抗氧化与酶抑制作用的成分为多酚类化合物.     

利用AChE活性作生物标记监测水环境污染的研究进展

本文综述了乙酰胆碱酯酶 (AChE)受抑制的机理、抑制剂的种类、抑制恢复情况等的研究状况。资料表明 ,除了有机磷农药和氨基甲酸酯农药外 ,还有其它的物质如表面活性剂、重金属离子、复杂化合物等均能抑制AChE活性。因此 ,基于AChE抑制来监测水环境污染 ,需在合适的条件下谨慎应用 ,必要时应采用多指标联合评价或辅以化学监测方法加以综合判断     

商品化酶抑制-比色法农残速测试剂盒对农药的敏感性测定

探讨商品化的酶抑制-比色法农残速测试剂盒对50种农药的敏感性测定.使用商品化的酶抑制.比色法试剂盒对嘧啶磷等40种有机磷和10种氨基甲酸酯类农药残留进行5个浓度水平的测定;对有3个浓度水平的抑制率大于0的农药,用抑制率和农药浓度的常用对数进行线性拟合,得出相关系数和抑制率方程,并据此计算IC10和IC50,通过IC10...     

Co-Treatment of Copper Oxide Nanoparticle and Carbofuran Enhances Cardiotoxicity in Zebrafish Embryos

The use of chemicals to boost food production increases as human consumption also increases. The insectidal, nematicidal and acaricidal chemical carbofuran (CAF), is among the highly toxic carbamate pesticide used today. Alongside, copper oxide nanoparticles (CuO) are also used as pesticides due to their broad-spectrum antimicrobial activity. The overuse of these pesticides may lead to leaching into the aquatic environments and could potentially cause adverse effects to aquatic animals. The aim of this study is to assess the effects of carbofuran and copper oxide nanoparticles into the cardiovascular system of zebrafish and unveil the mechanism behind them. We found that a combination of copper oxide nanoparticle and carbofuran increases cardiac edema in zebrafish larvae and disturbs cardiac rhythm of zebrafish. Furthermore, molecular docking data show that carbofuran inhibits acetylcholinesterase (AChE) activity in silico, thus leading to impair cardiac rhythms. Overall, our data suggest that copper oxide nanoparticle and carbofuran combinations work synergistically to enhance toxicity on the cardiovascular performance of zebrafish larvae.     

5种植物精油对植物病原真菌的抑菌活性

[目的]植物精油用作农药具有对人畜安全、对环境友好、生物活性多样等特点,可克服化学农药的局限性,具有开发潜力。研究5种植物精油对10种重要农作物病原真菌的抑菌活性,以期为其在农药领域的开发利用提供依据。[方法]采用生长速率法测定植物精油对病原菌的抑菌活性。[结果]南丰蜜橘精油和胜红蓟精油对供试病原菌表现出较高的抑制活性,精油体积分数为1 mL/L时,对10种植物病原真菌的抑制率分别为77.27%~100%和63.54%~100%。南丰蜜橘精油和胜红蓟精油对10种植物病原真菌菌丝的EC50值分别为0.2316~0.5653、0.0573~0.1943 mL/L。[结论]南丰蜜橘精油和胜红蓟精油对供试植物病原真菌的抑制活性好,具有开发应用前景。     

Insecticidal Effects of Organotin(IV) Compounds on Plutella Xylostella (L.) Larvae. II. Inhibitory Potencies Against Acetylcholinesterase and Evidence for Synergism in Tests With Bacillus Thuringiensis(BER.) and Malathion

Features of pesticide synergism and acetylcholinesterase (AChE) inhibition (in vitro) were studied using a selected range of organotin compounds against the early 4th instar larvae of a highly resistant strain of the diamondback moth (DBM), Plutella xylostella, a major universal pest of cruciferous vegetables.Fourteen triorganotin compounds were evaluated for their ability to enhance the toxicity of the microbial insecticide, Bacillus thuringiensis (BT) and of the commercial insecticide, Malathion to Plutella xylostella larvae. Supplemental synergism was observed with triphenyl- and tricyclopentyltin hydroxides in combinations with Bacillus thuringiensis. Increased synergism was observed with an increase in the number of cyclopentyl groups on tin in the mixed series, Cyp(n) Ph(3-n) SnX, where X = OH, and 1-(1,2,4-triazolyl). The combination of (p-chlorophenyl)diphenyltin N,N-dimethyldithiocarbamate at LD(10) and LD(25) concentrations with sublethal concentrations of Malathion as well as of tricyclohexyltin methanesulphonate at the 0.01% (w/v) concentration with Malathion exerted strong synergistic effects (supplemental synergism) with toxicity index (T.I) values of 7.2, 19.8 and 10.1, respectively.Studies on the in vitro inhibition of acetylcholinesterase prepared from the DBM larvae showed that while most of the triorganotin Compounds tested were without effect on the enzyme, compounds containing the thiocarbamylacetate or the dithiocarbamylacetate moieties demonstrated appreciable levels of inhibition, being comparable in efficacy to commercial grades of Malathion and Methomyl.     

敌敌畏与马拉硫磷对猪肾细胞PK15增殖抑制分析

[目的]为了研究有机磷化合物在体外对猪肾细胞损伤作用。[方法]选择敌敌畏和马拉硫磷作用猪肾细胞系PK15。MTT比色法测量2种有机磷化合物对细胞抑制作用,荧光染色和DNA ladder法检测它们对PK15的致凋亡作用。同时检测氧化相关因子超氧化物歧化酶(SOD)活性、丙二醛(MDA)含量和PON1基因m RNA水平。[结果]敌敌畏和马拉硫磷抑制PK15细胞的生长呈时间-剂量效应,并能诱导PK15产生较明显的凋亡现象,同时能使细胞中的超氧化物歧化酶活性下降、丙二醛水平上升。[结论]2种有机磷农药可使细胞的抗氧化能力下降,致使细胞中的氧自由基水平上升,可能是有机磷化合物致细胞凋亡、损伤的因素之一。     

Extraction and Enrichment of Pesticides for Analysis using Binary Supercritical Fluid Mixtures

Abstract

To improve the extraction selectivity in analytical supercritical fluid extraction (SFE), binary mixtures of supercritical fluids have been used to selectively produce lipid‐free extracts of trace pesticide residues for chromatographic analysis. Mixtures of nitrogen and HC‐134a have been used in conjunction with carbon dioxide to selectively extract both fortified and incurred residues from a variety of fatty foods using both experimental and commercially‐available extraction instrumentation. Extraction of fortified pesticides in butter fat showed high recoveries for both organo‐chlorine and ‐phosphorus pesticides with recoveries declining for specific pesticide moieties at the 1 ppb spiking level for CO₂/N₂ mixtures. For CO₂ and HC‐134a mixtures, there was poor and little improvement in analyte recovery relative to using neat SC‐CO₂ for fortified organochlorine pesticides in butter fat at the 0.5–5.0 ppm level. However using a CO₂/HC‐134a mixture for organophosphorus pesticides in butter fat improved recoveries (>90%) of the analytes at the 1–3.5 ppm level relative to using neat SC‐CO₂. Excellent recoveries were obtained for incurred organochlorine and ‐phosphorus pesticides from a variety of food products at ppb levels using either CO₂/N₂ or CO₂/HC‐134 mixtures. Results from these and additional experiments suggest that binary fluid mixtures can significantly reduce the need for additional sample cleanup prior to chromatographic analysis, allowing in some cases, direct injection of the extract after dilution into the gas chromatograph.     

Two types of organophosphate pesticides and their combined effects on heterotrophic growth rates in activated sludge process

BACKGROUND: Pesticides are sometimes non‐biodegradable and, moreover, toxic to microorganisms. If pesticides exceed the tolerance of microorganisms, failure of the activated sludge process (ASP) occurs. Therefore the effects of two types of organophosphate pesticides on heterotrophic growth rate constant in sludge from ASP were investigated. Oxygen uptake rate was employed to measure the rate constants. RESULTS: The results indicated that the value of heterotrophic growth rate constant decreased from 3.88 d^?1 to 1.46 d^?1 or by 62% when 0.5 mg L^?1 of glyphosate was added. When adding 0.5 mg L^?1 of malathion, the value of heterotrophic growth rate constant decreased to 1.33 d^?1 or by 66%. The value of heterotrophic growth rate constant decreased to 1.98 d^?1 or by 49% when 0.5 mg L^?1 of pesticide combination (50% for each) was added. CONCLUSIONS: The inhibitory effects of glyphosate and malathion were in good agreement with non‐competitive inhibition kinetics, but pesticide combination did not follow non‐competitive kinetics. The inhibition coefficient values for glyphosate, malathion and their combination were 0.29, 0.29 and 0.58 mg L^?1, respectively. For comparison, linear and exponential types of models were derived by regression. According to non‐competitive kinetics, and linear and exponential models, the inhibitory effects of glyphosate and malathion were almost consistent. Finally, the degree of inhibition was simulated using different types of model. It was found that the toxicity of the two pesticides agreed with the antagonism well. Copyright © 2009 Society of Chemical Industry     

7种杀菌剂对马铃薯早疫病菌室内毒力及田间防效

[方法]采用菌丝生长速率法测定7种杀菌剂对马铃薯早疫病菌的抑制作用。[结果]结果表明:嘧菌酯与苯醚甲环唑混合物(质量比8∶5)对菌丝生长的抑制(EC50值为0.238 mg/L)作用最强,具有明显增效作用,显著高于其他6种杀菌剂;田间药效试验结果表明:4次施药7 d后,32.5%嘧菌酯.苯醚甲环唑SC对马铃薯早疫病的防治效果(95.33%)最为突出,显著高于其他杀菌剂。[结论]7种杀菌剂中嘧菌酯与苯醚甲环唑的混合物对早疫病具有较好的防治效果,可优选用于马铃薯早疫病的防治。