多酶片的四酶活力测定

对不同厂家生产的１４批多酶片中的４种酶的活力进行质量考察，结果表明多酶片的质量存在严重问题，互相互间存在着显著性差异。     

胰酶酶活力测定方法分析

胰酶系从猪、牛、羊等动物的胰脏提取的多种酶混合物,临床上主用于消化不良、食欲不振及胰腺分泌疾病引起的消化障碍等疾病。根据１９９５年版《中国药典》,其质量指标是以胰蛋白酶、胰淀粉酶及胰脂肪酶的活力指标来衡量的,这几种酶的测定方法较复杂,实验要求较高,现对测定方法进行分析。１胰蛋白酶１．１测定原理：胰蛋白酶可催化酪蛋白水解生成不被三氯醋酸所沉淀的、肽、陈及氨基酸等,其中酪氨酸、色氨酸和苯丙氨酸在２７５ｎｍ处有最大吸收。药典中的测定方法以酪蛋白为底物（１．５％）,用硼酸盐缓冲液稀释配成相应浓度,采用Ｃ…     

从生产胰岛素的胰渣中制备胰酶、胰蛋白酶及糜蛋白酶

目的 从中性乙醇提取胰岛素后的残渣中提取制备高活性的胰酶,并从中分离纯化出胰蛋白酶(T)、糜蛋白酶(CT).方法 在胰渣中加入活化剂活化后,用PEG-6000沉淀、丙酮脱脂干燥得到胰酶;胰酶经CM-纤维素纯化得到胰糜蛋白酶混合制剂,再经CM-sepharose FF层析分离得胰蛋白酶和糜蛋白酶.结果 胰酶回收率为12.1％,胰蛋白酶、胰脂肪酶、胰淀粉酶的活性分别为5.40、39.72、76.72 U·mg-1,3种酶的活性比例达1∶7.4∶14.2.胰蛋白酶、糜蛋白酶的效价分别为2505、1003 U·mg-1;相对于胰酶,二者的活性回收分别为48.93％、61.73％.结论 从胰渣中制得的胰酶活性较高(约9倍于《中国药典》2010年版中的标准);制得的T及CT的活力也达到《中国药典》2010年版中的标准.     

高活力胰酶的生产

将酶激活剂及稳定剂用于高活力胰酶生产.酶活力为蛋白酶4.5ku/g,淀粉酶70ku/g,脂肪酶35ku/g.胰酶总收率为7.9～1O.8%.     

高活力胰酶制备工艺的研究

本文报告了高活力胰酶的简易制备方法。本法用稀醇提取,加适量保护剂与激活剂,将酶原激活,获高活力胰酶。按干品计算,每克胰酶粉的酶活力平均含胰蛋白酶为281,000个单位、胰淀粉酶为37,400个单位、胰脂肪酶为18,300个单位;炽烧残渣为4.59％;干燥失重为3.97％;收率为10.47％;脂肪含量小于20毫克。本法工艺简单、稳定、生产周期短、易推广。     

胰酶及多酶片中胰蛋白酶活力测定项下的去蛋白方法的探讨

胰酶及多酶片是常用的治疗消化不良的药物 ,其中胰蛋白酶活力测定项下的除去蛋白质的方法在中国药典 1995年版未作具体规定 ,生产胰酶和多酶片的厂家所采用的方法不尽相同 ,大致有 :定性滤纸过滤法 (Ａ) ,定量滤纸过滤法 (Ｂ) ,离心沉淀法 (10 0 0×ｇ) (Ｃ)和三号垂熔漏斗过滤法(Ｄ)。我们用以上方法对胰酶和多酶片中的胰蛋白酶的活力进行了测定 ,以观察不同的除去蛋白方法对酶活力的影响。1　仪器与试药ＵＶ - 2 6 0紫外可见分光光度计 ,日本岛津 ;80- 2型离心沉淀器 ,上海手术器械厂 ;ＨＨ·Ｓ电热恒温水浴锅 ,江苏医疗器械厂 ;Ｌ -酪氨…     

胰激肽释放酶生产新工艺研究

在得到胰酶和弹性蛋白酶的同时,用国产T离子交换树脂吸附分离胰激肽释放酶,再经除盐后用离子交换纤维素(DEAE——Cellulose)精制,平均可得胰激肽释放酶4.52万u/kg胰脏,比活为25.07u/mg。     

关于胰酶中的胰蛋白酶效价测定的探讨

目的:改进、提高《中国药典》标准,提高胰酶标准的科学性和可操作性。方法:对《中国药典》与BP、USP、EP收载的胰酶中胰蛋白酶效价测定标准的差异作比较。结果:《中国药典》标准的叙述太简单,不便于操作,BP、USP、EP标准的描述详细、清晰,EP最为严谨。结论:应修订完善《中国药典》。     

离子交换色谱法制备高纯度胰激肽原酶

目的建立高纯度胰激肽原酶的纯化工艺。方法通过离子交换色谱法一步纯化胰激肽原酶粗品。结果纯化得到的胰激肽原酶效价(活力)达到2 37～2 6 8U/mg ,比活在30 0U/mg蛋白质以上,活性回收率在75 %以上。结论该纯化方法简单、高效     

Correlation between low/high affinity ratios for 5-HT(1A) receptors and intrinsic activity

G protein-coupled receptors exist in G protein-coupled and -uncoupled forms that exhibit high and low affinity for agonists, respectively. Consequently, affinity differences of a compound for the high vs. the low affinity state of a receptor have been used to estimate its intrinsic activity at that receptor. We examined the affinity of a series of compounds for 5-hydroxytryptamine(1A) (5-HT(1A)) receptor sites labeled with 0.2 nM [3H](+/-)-8-hydroxy-2-(di-n-propylamino)tetralin ([3H]8-OH-DPAT) (high affinity), or with 0.25 nM [3H]4-(2'-methoxy-)-phenyl-1-[2'-(N-2"-pyridyl)-p-fluorobenzamido] eth yl-piperazine ([3H]p-MPPF) in the presence of 100 microM guanylylimidodiphosphate (Gpp(NH)p) (low affinity) in rat hippocampal membranes. For a variety of 5-HT(1A) receptor ligands, the low/high affinity ratio (ranging from 110 for 5-HT to 0.12 for spiperone) was in good agreement with their reported intrinsic activity. Positive rank correlations were found between low/high affinity ratios and intrinsic activities (E(max) values) reported in the literature. The high efficacy 5-HT(1A) receptor agonists, 1[2-(4-fluorobenzoylamino)ethyl]-4-(7-methoxynaphtyl)piperaz ine (S-14506) and dihydroergotamine, however, had similar, high affinity for both G protein-coupled and -uncoupled forms of the receptor. The Hill coefficients for both compounds were markedly higher than 1.0, suggesting that positive cooperativity could be responsible for the unexpected results. The 5-HT(1A) receptor agonist activity of dihydroergotamine and S-14506, assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation, was blocked completely by pertussis toxin, reinforcing the suggested involvement of an inhibitory G protein in their effects. Taken together, the results suggest that, although the low/high affinity ratio of a ligand for 5-HT(1A) receptors generally covaries with its intrinsic activity, dihydroergotamine and S-14506 may interact with 5-HT(1A) receptors in a manner different from that of other 5-HT(1A) receptor agonists. Their effects, however, appear to be G(i) protein-dependent.     

产黄青霉简单高效遗传转化法——电激转化法

目的 研究产黄青霉(P.chrysogenum)电激转化方法,建立产黄青霉快速、高效的遗传转化方法.方法 应用美国Bio-Rad电转仪,将外源DNA转化入产黄青霉菌丝中,研究了菌丝培养时间、电场强度、DNA类型等对遗传转化的影响.结果菌丝培养24h,处于旺盛生长阶段,电场强度为6000V/cm,电阻200Ω,电容20μF,环状质粒DNA较线状能获得转化效率稍高,1μg DNA获得的克隆数可达500个.结论 应用电激转化方法对产黄青霉进行遗传转化属首次报道,特别是可直接将目的片段与T-DNA相融合,转化入产黄青霉中,该方法操作简单,快速高效.     

Rats selectively bred for high and low swim-test activity show differential responses to dopaminergic drugs

Rationale: Selective breeding of Sprague-Dawley rats has been used to generate a line of animals with very low swim-test activity (SwLo) in an attempt to model certain characteristics of depression. For comparison with the SwLo animals, a line bred for high swim-test activity (SwHi) and a non-selectively bred line (SwNS) have been generated. Previous studies using these lines suggested an inverse relationship between dopamine (DA) function in the brain and inactivity in the swim test. Objectives: The current experiments investigated the possibility that SwLo and SwHi rats show differences in central DA processes, as suggested by responsiveness to DA agonists. Results: The increase in ambulation produced by d-amphetamine (0.25– 1.0 mg/kg) was largest in SwHi rats and smallest in SwLo rats, with SwNS rats showing an intermediate response. Amphetamine levels in plasma and brain tissue were similar in SwHi and SwLo rats, indicating that pharmacokinetic differences were not responsible for the behavioral differences. Repeated amphetamine administration produced enhancement in the ambulation-increasing effects of this drug (i.e., sensitization), with significant enhancement seen in all three lines. Apomorphine in doses that stimulate postsynaptic receptors (0.25– 4.0 mg/kg) produced mainly increased sniffing behaviors in SwHi and SwNS rats and oral behaviors in SwLo rats, suggesting that the lines differ in proportions of D1, D2, and D3 postsynaptic receptors. Conclusions: The findings suggest that DA function differs in lines of rats selectively bred for differences in swim behavior, a feature that may make these lines useful for studying certain depressive symptoms that might be related to DA function. Received: 26 September 1998 / Final version: 28 May 1999     

一种检测药物镇痛作用和局部麻醉作用的简便方法

４－氨基吡啶（４－ＡＰ）２．６ｍｍｏｌ·Ｌ－１０．０２ｍＬｓｃ于小鼠颈背部可引起用后足爪搔抓注射部位的反应．以４－ＡＰｓｃ后５ｍｉｎ内发生搔抓鼠数为指标，观察不同药物对它的抑制作用．麻醉性镇痛药吗啡，哌替啶和芬太尼能明显抑制这一反应；弱镇痛药罗通定，安乃近，水杨酸钠和非镇痛药无效．局部麻醉药普鲁卡因，利多卡因或丁卡因与４－ＡＰ混合ｓｃ也可取消搔抓反应．结果表明这一方法可用于检测麻醉性镇痛药的镇痛作用和局麻药的局部麻醉作用．     

Brain aldehyde dehydrogenase activity in rat strains with high and low ethanol preferences

The activity of aldehyde dehydrogenase in subcellular fractions of whole brain homogenates from the AA and ANA rat strains developed respectively for high and low ethanol preferences has been studied. No significant strain or sex differences between naive AA and ANA rats were found. In ethanol-experienced rats some strain and sex differences were found, the most consistent being higher enzyme activity in AA females than in males both with aliphatic and aromatic aldehyde substrates. However, contrary to previous findings no relation between brain aldehyde dehydrogenase activity and drinking behavior was found in the AA and ANA rat strains.     

Effects of low and high doses of acetylsalicylic acid on penicillin-induced epileptiform activity

Background

The most common headache associated with epilepsy occurs after seizure activity and is called a postictal headache. Therefore, the objective of this study was to investigate the effects of low and high doses acetylsalicylic acid (aspirin) on a penicillin-induced experimental epilepsy model.

A method for preparing sodium acrylate‐d3, a useful and stable precursor for deuterated acrylic monomers

A convenient and economical method for converting propiolic acid to sodium acrylate‐d₃ is described. Successive D/H exchange of the alkyne proton of sodium propiolate (prepared from propiolic acid) using D₂O affords sodium propiolate‐d having up to 99 at.% D. Sodium propiolate‐d can be partially reduced to sodium acrylate‐d₃ with 90% conversion and 89% yield using D₂ and the Lindlar catalyst, with control of reaction parameters to maximize conversion while minimizing over‐reduction. Copyright © 2011 John Wiley & Sons, Ltd.