二氯化锰慢性染毒对大鼠脏器和血液元素含量的影响

用ＭｎＣｌ２水溶液通过气管和腹腔二条途径对Ｗｉｓｔａｒ大鼠染毒，气管染毒４个月，总量达（７４．４９～１８．５９）×１０－６，腹腔染毒４个月，总量达（１１４５．２６～５７２，４）×１０－６．采用原子吸收光谱法，测定了大鼠肝、脾、肺、肾、脑和血液中锰、钙、镁元素的含量．结果：脑、肺组织中锰元素含量显著高于对照组（Ｐ＜０．０５和Ｐ＜０．０１），脾脏钙元素和血液镁元素含量显著低于对照组（Ｐ＜０．０５和Ｐ＜０．０１）．提示：慢性锰中毒对脏器与血液中元素含量的影响不可忽视．     

健骨胶囊中微量元素对实验大鼠股骨的影响

通过对健骨胶囊及实验大鼠股骨中的微量元素铜、锌、铁、锰的分析，阐述了健骨胶囊中微量元素对实验大鼠股骨中的微量元素铜、锌、铁、锰的影响以及骨质疏松症的改善，具有重要的营养学、药理功效学作用。     

胆碱酯酶荧光探针的研究进展

作为生物体中一类重要的糖蛋白水解酶,胆碱酯酶主要有乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)两种同工酶.它们分布在大脑、血液和其他组织中,广泛参与人和动物体内的多种生理代谢过程.因此,胆碱酯酶在神经生物学、药学、临床医学和毒理学等研究领域发挥着重要的作用.胆碱酯酶的活性分析对于药物发现以及相关疾病的诊断和治疗具有重要的指导意义.本文简要评述了胆碱酯酶荧光探针的研究进展,包括抑制剂型探针、底物型探针以及整合纳米技术等所建立的荧光定量分析方法.     

新生儿肺炎血中元素含量的变化

对５０例新生儿肺炎患儿和５０例正常新生儿进行了全血中元素锌、铁、钙、镁、铜、锰含量的对比观察，结果发现新生儿肺炎患儿血液中锌、铁、钙、镁４种元素均显著低于正常新生儿，血铜、锰与正常组无显著性差异．提示新生儿肺炎患儿血锌、铁、钙、镁的代谢方面均存在一定缺陷，认为新生儿肺炎患儿合理补充微量元素，对治病有益处。     

健康猕猴血液和毛发微量元素含量的正常值测定和差异比较

对猕猴(Macaca mulatta)血液和毛发的镁、锰、钼、镍、铅、铬、镉、锌、铁、铜、钙等11种元素的含量，用电感耦合高频等离子体发射光谱仪进行了测定．给出了各个元素在血液和毛发中的平均含量值和变动范围．指出毛发中的微量元素含量一般较血液为高，且变动较小．与人体内含量比较，猴毛发的Cu、Mo、CA、Ni的含量与人发接近；猴血液的Zn、Fe、Ca、Mn、Ca亦与人的接近．对猴血液微量元素含量随年龄、体重、性别变化及血液含量和毛发含量的相关关系进行了统计学检验．通过对测定值的比较分析，认为尽管动物体内的微量元素含量随种类、环境、个体差异变化较大，就群体平均含量而言，仍存在着相似的变化规律。本文的测定结果对了解猕猴对微量元素的需要提供了初步依据．     

急性镉中毒大鼠致死时重要器官镉的分布

分别通过静脉和呼吸道急性镉染毒，探讨了急性镉中毒大鼠致死时，血液，心、肝、肾、脑、肺的镉分布。８０只Ｗｉｓｔａｒ大鼠分为对照组和染毒组，氯化镉进行急性染毒，在心肌收缩功能降低为染毒前的５０％及心跳停止时，取器官标本，用原子吸收分光光度计测定镉含量。实验结果提示，急性镉中毒时，血液、心脏的镉含量早期升高缓慢，后期升高较快，肝脏镉含量呈线性快速升高；而肾脏镉含量经呼吸道染毒时与肝脏类似，经静脉染毒时，     

新型他克林-丁苯酞杂合物作为多靶点胆碱酯酶抑制剂的设计合成及活性评价（英文）

设计合成并评价了一系列他克林-丁苯酞杂合物作为多功能胆碱酯酶(ChE)抑制剂治疗阿尔茨海默病的活性.结果表明,他克林-丁苯酞杂合物对两种胆碱酯酶均表现出抑制活性.其中3-丁基-6-((7-((1,2,3,4-四氢吖啶-9-基)氨基)庚基)氧基)异苯并呋喃-1(3H)-酮(10b)显示出最优的乙酰胆碱酯酶(AChE,IC50=38.65nmol·L-1)抑制活性,高于他克林(IC50=200.70 nmol·L-1)约5倍. 3-丁基-6-((8-((6-氯-1,2,3,4-四氢吖啶-9-基)氨基)庚基)氧基)异苯并呋喃-1(3H)-酮(10g)显示出最好的丁酰胆碱酯酶(BuChE,IC50=33.69nmol·L-1)抑制活性,其值与他克林(IC50=27.12nmol·L-1)相似,高于多奈哌齐(IC50=7530nmol·L-1)约220倍.在大鼠海马体神经元细胞Aβ诱导损伤模型中,测试化合物对大鼠海马神经元细胞(Rat hippocampal neurons)中ROS水平的影响,结果显示,大多数化合物均能对Aβ1-42诱导的大鼠海马体神经元细胞分泌的ROS产生抑制作用.     

微量元素锰在临床医学中的应用

介绍了锰在临床医学中的应用，主要内容包括，锰的生理意义，作用机制，营养意义，毒性，锰制剂，影响锰的生物利用率的因素等。     

湖南省湘潭锰矿596名儿童发锰含量的调查报告

对湖南湘潭锰矿地区空气、水质、土壤和食物中标元素浓缩状态进行调查，同时对锰区１～１４岁儿童共５９６例发锰含量作了调查研究．以求得锰工业区儿童发锰含量的本底值．以便进一步探讨锰污染对人体健康的影响．检测结果：湘潭锰矿儿童发锰上限１５．８４×１０－６～１６．２４×１０－６，高于国内正常发锰上限的０．６５７倍，高于湖南医科大学附二院儿童发锰正常值的３．８６倍．锰区降尘比国家规定高４．８５倍，土壤比非锰区高９．７４倍，大米比非锰区高０．７５倍，井水、池塘水分别高于国家标准５８．６倍和１１．５倍，大气高于国家规定０．６倍．表明湘潭锰矿地区锰元素高度浓缩状况（污染状况）．儿重发锰测定结果与该地区环境中的锰含量成正相关．发锰可作为锰浓缩地区的指示器，为环保、公卫工作提供科学依据。鉴于该矿从事锰作业２５年者出现严重的锰中毒脑病．从而提示体内锰过多可引起脑功能障碍，与儿童智力精神的影响相关．正在进一步探讨高浓度的锰对正在生长发育中的儿童潜在影响和远期危害．     

高硒情况下维生素E对老龄大鼠血清中抗氧化作用的影响

研究了高Se或高维生素E下，老龄大鼠体内抗氧化活性的变化以及高Se下维生素E对其体内抗氧化水平的影响。将十二月龄Wistar大鼠32只随机分成4组：（1）正常饲料组；（2）高Se饲料组；（3）高维生素E饲料组；（4）高Se高维生素E饲料组。饲至十周末，处死大鼠，按试剂盒要求取其血液制成血清测GSH－Px,SOD活性，MDA含量。结果表明，高Se或高维生素E下饲养下的大鼠与对照组比较，血清中GSH－Px活性升高（P＜0．05）。SOD活性未见改变，MDA含量分别减少50％和56％，有显著差异（P＜0．01）；维生素E与高Se合用与高Se组比较能进一步同GSH－Px,SOD活性（P＜0．01）。结论：高Se会升高老龄大鼠的抗氧化活性，而与维生素E合用更加升高老龄大鼠血液中抗氧化活性。     

四(4-磺酸基苯基)卟啉锰钠盐-NO配合物的合成及NO释放效能和 生物学活性研究

合成、表征了一种新型的NO供体化合物meso-5,10,15,20-四(4-磺酸基苯基)卟啉锰钠盐—NO配合物(TPPSNa-Mn-NO), 并初步研究其药理学作用. 采用重氮化偶合反应检测TPPSNa-Mn-NO体外NO的释放效果. 观察TPPSNa-Mn-NO对家兔离体胸主动脉环的舒张作用和对于大鼠收缩压、舒张压及心率的影响. TPPSNa-Mn-NO的体外NO释放效率约为70.86%, 该化合物可以使30 mmol•L－1甲氧胺引起家兔离体胸主动脉收缩的量效关系曲线非平行右移, 最大反应(Emax)压降低约30.2%, 静脉给药后实验组大鼠血压第5 min时开始下降, 并持续缓慢降低, 给药后30 min下降幅度达最大, 而后缓慢回升, 给药后120 min时接近用药前水平且仍低于用药前水平. 药物对大鼠心率无显著影响. TPPSNa-Mn-NO具有缓慢持久降压的药理作用, 且不影响其他重要的生命指标, 有望成为长效降压药理想的候选化合物.     

A lab-on-a-chip for detection of nerve agent sarin in blood

Sarin (C(4)H(10)FO(2)P,O-isopropyl methylphosphonofluoridate) is a colourless, odourless and highly toxic phosphonate that acts as a cholinesterase inhibitor and disrupts neuromuscular transmission. Sarin and related phosphonates are chemical warfare agents, and there is a possibility of their application in a military or terrorist attack. This paper reports a lab-on-a-chip device for detecting a trace amount of sarin in a small volume of blood. The device should allow early detection of sarin exposure during medical triage to differentiate between those requiring medical treatment from mass psychogenic illness cases. The device is based on continuous-flow microfluidics with sequential stages for lysis of whole blood, regeneration of free nerve agent from its complex with blood cholinesterase, protein precipitation, filtration, enzyme-assisted reaction and optical detection. Whole blood was first mixed with a nerve gas regeneration agent, followed by a protein precipitation step. Subsequently, the lysed product was filtered on the chip in two steps to remove particulates and fluoride ions. The filtered blood sample was then tested for trace levels of regenerated sarin using immobilised cholinesterase on the chip. Activity of immobilised cholinesterase was monitored by the enzyme-assisted reaction of a substrate and reaction of the end-product with a chromophore. Resultant changes in chromophore-induced absorbance were recorded on the chip using a Z-shaped optical window. Loss of enzyme activity obtained prior and after passage of the treated blood sample, as shown by a decrease in recorded absorbance values, indicates the presence of either free or regenerated sarin in the blood sample. The device was fabricated in PMMA (polymethylmethacrylate) using CO(2)-laser micromachining. This paper reports the testing results of the different stages, as well as the whole device with all stages in the required assay sequence. The results demonstrate the potential use of a field-deployable hand-held device for point-of-care triage of suspected nerve agent casualties.     

A comparison of three methods for cholinesterase analysis

Three methods of cholinesterase analysis in blood are compared: the ΔpH (modified Michel method), pH Stat, and radiometric methods. The ΔpH method was determined to be the best choice for routine laboratory screeening for organophosphate exposure. The methods all agree within experimental variation. The radiometric method uses a thin-layer chromatography (TLC) separation of acetate (¹⁴C) activity from acetylcholine (¹⁴C) activity with direct β counting or scintillation counting to determine the concentration of acetate activity. The methods were compared on freeze-dried human blood and on experimentally carbamate-inhibited mouse blood. The radiometric analysis may be performed using as little as 5 μl of blood. The radiometric method may enhance the ability to detect sublethal exposure to cholinesterase inhibitors. It should be of particular use where sampling size is of greatest importance.     

Amperometrisches Verfahren zur Bestimmung der Aktivit?t von Cholinesterasen und Nachweis der Inhibitoren dieser Enzyme

Summary An electrochemical procedure based on the anodic oxidation of thiocholine iodide for the determination of the activity of cholinesterase both in serum and in the red blood cells is described. Using electronic differentiation of the current time curve the enzyme activity is directly available. The values obtained agree very well with the established method. Furthermore, both reversible and irreversible inhibitors of the cholinesterase have been quantified by using standardized serum samples.     

补血中药对贫血大鼠体内微量元素分布的影响

补血中药可以明显地改善慢性失血性贫血大鼠的缺铁贫血状态。用ＩＣＰ－ＡＥＳ法测定了饱料、中药及大鼠体内微量元素含量,结果显示,补血中药含铁量比饲料中的铁含量还略低,服药贫血大鼠体内脾、肝等贮铁库中的铁含量显著降低。提示补血中药对贫血的治疗作用。主要是通过积极调动、利用体内铁库的贮量和直接对造血干细胞的造血刺激作用的实现的。由于贫血大体内铁库贮量已近耗竭,所以积极而适当地补充铁剂及锰、镍、钒等元素也是     

The use of Metomega Chrome Blue BBL as a metal indicator and its application for the determination of calcium and magnesium in serum

Summary Metomega Chrome Blue BBL was used as a metal indicator for the detection and titration of calcium, magnesium, manganese, nickel and manganese. A displacement reaction was described for the titration of cadmium using Mn-EDTA. A stepwise titration was conducted for the direct titration of both calcium and magnesium in blood serum.Fenugreek mucilage was used as a media for increasing the sensitivity limits of detection of barium, cadmium, cerous, calcium, copper, cobalt, magnesium, manganese, nickel, lead and zinc.     

血清胆碱酯酶水平在脓毒症患者诊断中的应用价值分析

目的分析脓毒症患者胆碱酯酶含量及其与降钙素原的相关性,为早期诊断脓毒症提供一个新的初筛检测敏感性指标。方法选择60例脓毒症患者为观察组,另选择同期非脓毒症患者60例作为对照组,测定两组患者血清胆碱酯酶活性,且测定观察组PCT含量,分析PCT与胆碱酯酶的相关性。结果观察组胆碱酯酶含量明显高于对照组,差异有统计学意义(P0.05);胆碱酯酶与降钙素原呈现一定线性相关,相关性曲线为:y=2 325.23 x+239 882.3(r=0.843)。结论血清胆碱酯酶结果与降钙素原呈现一定线性关系,可考虑用于早期评估脓毒症及预后情况。     

New developments of conductometric measurements in analytical biochemistry

A recently described conductometric device with precise temperature regulation is used. For determination of cholinesterase activities, different substrates were studied; with regard to the enzyme activities present in serum or in whole blood, butyrylcholine was selected for the serum assay and propionylcholine for whole blood assay. Ethanol was determined by using alcohol and aldehyde dehydrogenases with measurement of the conductance changes, mainly from the appearance of acetate ions. In the kinetic method, the relationship between the rate of conductance variation and ethanol concentration was linear in the range 0–0.2 mM.     

基于UFLC-MS/分子模拟计算的吴茱萸醇提取物中胆碱酯酶抑制剂筛选

采用超高速液相色谱-质谱(UFLC-MS)研究了吴茱萸醇提取物中入血小分子化合物的体内药代动力学过程.同时对UFLC-MS生物样品分析方法进行包括特异性、线性、精密度、准确度、稳定性、基质效应和回收率等考察,结果表明,该方法稳定可靠,且醇提取物中10个生物碱类化合物均被胃肠道快速吸收,并且多数化合物血药浓度在1～2 h左右达到峰值.将吸收入血的10个生物碱类化合物与乙酰胆碱酯酶和丁酰胆碱脂酶进行柔性分子对接及构效关系分析,发现其中活性最高的为去氢吴茱萸碱、吴茱萸碱、吴茱萸次碱和吴茱萸酰胺Ⅰ4个吲哚型生物碱,它们与乙酰胆碱酯酶的对接打分均在-46. 02 k J/mol以下;与丁酰胆碱脂酶对接打分均在-41. 84 k J/mol以下.吴茱萸碱、吴茱萸次碱、去氢吴茱萸碱和吴茱萸酰胺可能是以乙酰胆碱酯酶和丁酰胆碱脂酶为靶点的胆碱酯酶抑制剂前体化合物.     

Synthesis of lupinine esters and their interaction with cholinesterases

A number of lupinine esters of carboxylic acids and their hydrochlorides and methiodides have been synthesized. It has been shown that these compounds are reversible inhibitors of human blood erythrocyte acetylcholinesterase and horse blood serum butyryl cholinesterase. Noncompetitive inhibitors of these enzymes have been found among the compounds synthesized.A. S. Sadykov Institute of Bioorganic Chemistry, Academy of Sciences of the Uzbek SSR, Tashkent. Translated from Khimiya Prirodnykh Soedinenii, No. 1, pp. 75–79, January–February, 1990.