反相HPIC法测定血清布洛芬含量

本文以消炎痛为内标，用反相ＨＰＩＣ测定血清中的布洛芬。色谱柱为ＹＷＧＣ（１８）（１０μｍ）２００ｍｍ×５ｍｍ。流动相为甲醇－２０ｍｍｏｌ／Ｌ。磷酸二氢钾缓冲液（７０：３０，ｐＨ３．８）。流速为１ｍｌ／ｍｉｎ。检测波长为２２５ｎｍ。色谱柱柱温为５０℃。布洛芬和内标的保留时间分别为７．２和５．２ｍｉｎ。布洛芬的检测限为２ｎｇ（Ｓ／Ｎ≥４：１）。血清样品的预处理采用１：１的乙腈沉淀蛋白后直接进样。血清布洛芬浓度在０．５～６４μｇ／ｍｌ范围呈线性关系（ｒ＝０．９９９６）。天内天间精密度分别为１．６％～３．９％和２．１％～５．０％。     

高效毛细管电泳测定盐酸小檗碱脂质体包封率

目的：建立一个快速、简便且经济的盐酸小檗碱脂质体包封率测定方法。方法：采用高效毛细管电泳法，分析条件为，石英毛细管，７０ｃｍ×７５μｍｉｄ；温度，２０℃，运行缓冲液，１０ｍｍｏｌ／Ｌ磷酸氢二钠（０１ｍｏｌ／Ｌ氢氧化钠调至ｐＨ１０８１）；运行电压，３０ｋｖ；检测波长，２５４ｎｍ。结果：线性范围１００～５０００ｍｇ／Ｌ，ｒ＝０９９８９，平均回收率９８７％（ｎ＝５），ＲＳＤ＝３５１％，薄膜分散法的包封率（１９５±２３）％远高于乙醇注入法的包封率（８３±３７）％。结论：本法适用于盐酸小檗碱脂质体包封率测定     

盐酸多柔比星的高效毛细管电泳法分析

用高效毛细管电泳法测定盐酸多柔比星的含量。考察不同试验条件下盐酸多柔比星的胶束动电毛细管电泳行为。选择５０ｍｍｏｌ／Ｌ十二烷基硫酸钠，５０ｍｍｏｌ／Ｌ硼 溶液（ｐＨ８．７）含１０％乙腈为运行缓冲液，以β－萘磺酸钠为内标，于２３１ｎｍ波长处测定。在０．１７～０．８５ｇ／Ｌ的范围内呈良好的线性关系，ｒ＝０．９９９４，重现性实验ＲＳＤ为２．５％（ｎ＝５）。     

硫酸长春地辛的高效毛细管电泳分析

目的：用高效毛细管电泳法测定硫酸长春地辛的含量。考察不同试验条件下硫酸长春地辛的胶束动电毛细管电泳行为。方法：选择５ｍｍｏｌ·Ｌ－１十二烷基硫酸钠、５０ｍｍｏｌ·Ｌ－１硼砂溶液（ｐＨ７７）为运行缓冲液,毛细管有效长度是５０ｃｍ（ＩＤ７５μｍ）,以烟酰胺为内标,于２６０ｎｍ波长处测定。结果：在５８～５８０μｇ·ｍＬ－１浓度范围内呈良好线性,平均回收率达１００１％,ＲＳＤ为１８％（ｎ＝５）。     

盐酸利多卡因胶浆胶束电动毛细管电泳法测定

采用高效毛细管电泳法测定盐酸利多卡因胶浆含量。以烟酰胺为内标,５０ｍｍｏｌ／Ｌ硼酸盐缓冲液（ｐＨ８．６,含２５ｍｍｏｌ／Ｌ ＳＤＳ）为运行缓冲液,工作电压为２０ｋＶ,在０．０５～０．０６ｍｇ／ｍｌ浓度范围内线性关系良好,ｒ＝０．９９９７,平均回收率为１００．８％,ＲＳＤ为１．５％。     

反相高效液相色谱法测定阿霉素的血药浓度

本文采用反相ＨＰＬＣ法测定阿霉素的血药浓度，血浆样品用甲醇－氯仿（１：４）在ｐＨ９．０的条件下提取后进样，５ｍｍｏｌ／Ｌ磷酸－异丙醇－甲醇－乙腈（４５：３５：１０：１０，ｐＨ２．９）为流动相，荧光检测器λｅｘ＝４５０ｎｍ，λｅｍ＝５３０ｎｍ。最低检测浓度１０ｎｇ／ｍｌ，线性范围在３０－１５００ｎｇ／ｍｌ内ｒ＝０。９９８７，日内ＲＳＤ为１．５％－２．４％，日间ＲＳＤ为１．８％－３．７％。并对７例肺癌     

高效液相色谱法测定人血浆中比索洛尔浓度

本文采用高效液相色谱（ＨＰＬＣ）内标法测定血浆中比索洛尔浓度。色谱柱为ＴＭＳ（７μｍ，０．４６ｃｍ×１５ｃｍ）；流动相为乙腈－磷酸二氢胺（１ｍｏｌ／Ｌ，ｐＨ４）－水（１８：５：７７），荧光检测波长２７５／３０５ｎｍ（Ｅｘ／Ｅｍ）。血浆样品经碱化二氯甲烷提取，催醒胺作内标。方法线性范围为２～５０ｎｇ／ｍｌ；检测下限２ｎｇ／ｍｌ；在５、１５和５０ｎｇ／ｍｌ３种浓度平均回收率为（８８．１±６．２）％；日内日间ＲＳＤ均小于８．０％。     

高糖增强兔血管平滑肌细胞对内皮素-1的增殖反应性(英文)

观察高糖对内皮素－１（ＥＴ－１）促兔主动脉血管平滑肌细胞（ＶＳＭＣ）增殖的影响．方法： ＶＳＭＣ分别培养于含正常葡萄糖、高糖或高渗（５．５，２５，葡萄糖 ５．５＋甘露醇 １９．５ ｍｍｏｌ·Ｌ－１）的培养基中［３Ｈ］胸腺嘧啶掺入法检测ＤＮＡ合成速率，蛋白质印迹法检测磷酸化 ｐ４４／４２ ＭＡＰＫ的表达．结果：在 １０至 １０－８ｍｏｌ·Ｌ－１浓度范围内， ＥＴ－１以浓度依赖方式增加 ＶＳＭＣ的［３Ｈ］胸腺嘧啶掺入及磷酸化ｐ４４／４２ ＭＡＰＫ的表达，从 １０－１１到 １０－８ｍｏｌ·Ｌ－１，培养于高糖的 ＶＳＭＣ对相同浓度 ＥＴ－１的增殖反应性高于正常糖或高渗培养条件下的ＶＳＭＣ（Ｐ＜ ０．０５，或 Ｐ＜ ０．０１），而在后两种条件下，ＶＳＭＣ对ＥＴ－１的增殖反应无显著差别．同样，在高糖条件下，ＥＴ－１诱导的ＶＳＭＣ磷酸化ｐ４４／４２ＭＡＰＫ的表达较正常糖和高渗ＶＳＭＣ增加 ６０％－６５％结论：高糖增强ＶＳＭＣ对ＥＴ－１的增殖反应性，可能与磷酸化的 ｐ４４／４２ ＭＡＰＫ高表达有关     

高效毛细管电泳法同时测定4种喹诺酮类药物

用高效毛细管电泳法分离测定４种喹诺酮类药物，盐酸洛美沙星，依诺沙星，盐酸环丙沙星，氧氟沙星，用５０ｍｍｏｌ／Ｌ硼砂－磷酸盐缓冲液（ｐＨ８．５）运行电压１８ｋＶ２１４ｎｍ检测，压差法进样１０ｃｍ，１０ｓ，以咖啡因为内标定量，线性范围分别为：氧氟沙星和盐酸环丙沙星２０～１００ｍｇ／Ｌ，依诺沙星２４～１２０ｍｇ／Ｌ盐酸洛美沙星２０．８～１０４ｍｇ／Ｌ。峰面积之比与样品浓度线性回归，ｒ〉０．９９９５，最低     

注射用氨曲南高效液相色谱法含量测定

用高效液相色谱法，Ｃ１８柱，含５ｍｍｏｌ／Ｌ辛烷磺酸钠和２０ｍｍｏｌ／Ｌ磷酸二氢钾的水－甲醇（体积比８０２０，ｐＨ２．５）为流动相，检测波长２０６ｎｍ，同时测定氨曲南和Ｌ－精氨酸的含量。在５０～４００μｇ／ｍｌ浓度范围内，浓度与峰面积线性关系良好，ｒ分别为１．００００和０．９９９９。重复进样相对标准差分别为０．２２％（ｎ＝８）和０．２６％（ｎ＝８）。含量测定结果与ＵＳＰ２３版方法所得结果相符     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.