格列齐特中亚硝酸盐的电化学测定法

目的：建立用高效液相-电化学(ECD)检测法测定格列齐特中亚硝酸盐(NO2^-)的残留量。方法：阳离子色谱柱，以醋酸盐缓冲液(pH为4．3)为流动相，流速1．0mL／min。结果：线性范围0．04～0．8μg，r=0．9995，重复性试验RSD=1．4％(n=5)。回收率为99．2％，RSD=1．7％(n=9)。结论：方法灵敏，简便，结果准确。     

2型糖尿病患者呼气冷凝液中总硝酸盐的变化

目的观察2型糖尿病患者呼气冷凝液（exhaled breath condansate,EBC）中总硝酸盐（一氧化氮代谢物）的改变,为诊断2型糖尿病肺损害提供新方法。方法本实验选择16例2型糖尿病患者和20例健康非吸烟者;用Rtube收集器收集EBC,用分光光度法检测EBC中总硝酸盐（nitrite／nitrate,NO2^-／NO3^-）,同时检测并记录肺功能。结果2型糖尿病患者呼出气冷凝液总NO2^-／NO3^-水平增高（P〈0．05）;2型糖尿病与对照组之间肺功能FEV1％预计值比较有统计学意义（P〈0．05）、肺弥散（DLCO）％预计值与对照组之间比较有统计学意义（P〈0．01）。结论总NO2^-／NO3^-在2型糖尿病肺损害的发病中起重要作用,对不同时期2型糖尿病EBC中的NO2^-、NO2^-／NO3^-的水平变化,尚需进一步研究。     

RP—HPLC法同时测定鸡冠花中槲皮素、木犀草素和山奈酚的含量

目的建立鸡冠花中槲皮素、木犀草素和山柰酚的含量测定方法。方法反相高效液相色谱法，色谱柱ZORBAX SB-C18（150mm×4．6mm，5μm）；检测波长360nm；甲醇-0．2%磷酸（45：55）为流动相；柱温30℃；流速1．0mL·min^-1。结果槲皮素、木犀草素和山柰酚的回归曲线分别为：Y=1504．412X＋9．9756，Y=1991．745X＋8．6051，Y=567．591X＋2．5397，它们分别在5．5×10^-2～19．3×10^-2mg·L^-1，4．6×10^-2～16．1×10^-2mg·L，12．6×10^-2～43．9×10^-2mg·L^-1范围内线性关系良好，相关系数r=0．99992～0．99998，加样回收率分别为94．68％，91．03％和103．08％，RSD分别为0．35％，1．01％和0．55％。样品分别含槲皮素、木犀草素和山柰酚0．176，0．262和0．105mg·g^-1。结论方法简便可行，重复性好，数据及结果可靠。     

永停法测定盐酸丁卡因注射液及滴眼液含量的商榷

目的：探讨《中国医院制剂规范》中盐酸丁卡因注射液及其滴眼液含量测定方法的准确性，并进行方法改进。方法：采用永停法。将极化电压调至100mV，门限值调至80％，灵敏度调至l0^-8A。结果：按改进后的方法测定，盐酸丁卡因注射液及其滴眼液平均回收率分别为99．38％(RSD=0．77％，n=6)，99．05％(RSD=0．89％，n=4)。结论：改进后的含量测定方法准确度高，重现性好，可用于测定这两种制剂中盐酸丁卡因的含量。     

L-精氨酸和氨基胍对内毒素致肺损伤大鼠的影响

目的：观察L-精氨酸和氨基胍对内毒素（LPS）致肺损伤大鼠的影响，探讨其减轻肺损伤的机制。方法：将35只成年大鼠随机平均分为对照组（Con组）、LPS1组、LPS＋L-精氨酸处理组（L—Arg组）、LPS＋氨基胍处理组（AG组）、LPS＋复合L-精氨酸和氨基胍处理1组（AA1组）。在注射LPS后240分钟开胸采集标本，检测肺组织NF—κB活性；测定血清中NO2^-／NO3^-浓度和肺血管通透性。另将22只大鼠分为LPS2组（n=11）和复合L-精氨酸和氨基胍处理2组（AA2组，n=11），观察大鼠5天内存活率，并对大鼠肺进行病理分析。结果：LPS1组肺组织NF—κB活性、血中NO2^2-／NO3^-浓度较Con组明显升高（P〈0．05）；肺血管通透指数上升（P〈0．05）。L-Arg组和AA1组肺组织NF-κB活性和血中NO2^-／NO3^-浓度以及肺的通透指数均较LPS1组明显下降（P〈0．05）。但AG组肺组织NF-κB活性较LPS1组变化不明显（P〉0．05）。AA2组与LPS2组大鼠病死率分别为18．2％和45．5％，两组比较元显著差异（P〉0．05），但AA2组存活大鼠肺的病理损害程度比LPS2组轻。结论：L-精氨酸能明显抑制LPS诱导大鼠肺NF—κB活性，氨基胍不影响该活性，而复合用药可明显减轻内毒素所致肺损伤的病理改变。     

肾复康胶囊的抗炎作用与NO的关系研究

目的：为探讨肾复康胶囊治疗肾炎的机理，研究肾复康的抗炎作用与NO的关系，方法：应用镉还原柱层析和Griess反应法测定NO的稳定代谢产物NO2^-(NO3^-)。结果：肾复康对正常大鼠血，尿中亚硝酸盐（硝酸盐）[NO2^-(NO3^-)]含量无显著影响；能不同程度地抑制角叉菜胶所 大鼠中足跖肿胀，并显著地降低血清，尿液和炎性足跖组织中NO2^-(NO3^-）含量；使棉球肉芽肿大鼠模型中棉球肉芽肿重量减轻，显著降低血清，尿液和炎症组织中NO2^-(NO3^-)的含量。结论：肾复康对正常大鼠体内NO的产生没有影响；其抗炎（大鼠角叉菜胶性足跖肿胀和棉球肉芽肿）作用与抑制其体内NO水平有关。肾复康抑制体内NO水平可能是与其治疗肾炎有效的可能机制。     

替硝唑注射液质量标准的研究

研究替硝唑注射液的质量标准,用紫外分光光度法测定其含量,在317nm波长处测定吸收度,平均回收率为99．77％,RSD=0．48％(n=5),有关物质NO2^-的浓度控制在4μ/ml以内为宜。     

高效液相色谱法同时测定肤康涂膜剂中水杨酸和酮康唑的含量

目的：建立一种高效液相色谱法测定肤康涂膜剂中水杨酸和酮康唑的含量。方法：采用C18柱，乙腈-甲醇-2％醋酸铵(14：43：43)为流动相，检测波长为235nm，柱温30℃。结果：水杨酸线性范围0．5～2．5mg／mL(r=0．9999)，平均回收率为99．8％，RSD=0．64％(n=9)，酮康唑线性范围0．5～2．5mg／mL(r=0．9999)，平均回收率为100．6％，RSD=0．86％(n=9)。结论：该法简便，灵敏，准确。     

高效液相色谱法测定萜烯树脂中有机溶剂残留量

目的：建立苯、甲苯、苯乙烯在萜烯树脂中残留量的高效液相色谱测定法。方法：采用高效液相色谱法，色谱柱：ZORBAX SB-C18柱（5μm，4．6mm×250mm，Agilent）；流动相：甲醇-水（60：40）；流速：1mL·min^-1；检测波长：261nm；柱温：30℃；进样量：10μL；结果：在考察的浓度范围内呈现良好的线性关系。苯：（10．015～50．075ng，Y=1043．3X-58．3），甲苯：（20．042～501．5ng，Y=1995．8X＋1322．3），苯乙烯：（2．0234～505．85ng，Y=42059.9X-16659．6）；回收率：苯为98．18％，RSD=1．80％，n=6；甲苯为99．12％，RSD=0．77％，n=6；苯乙烯为99．28％，RSD=0．75％，n=6；最低检测限：苯为2×10^-1ppm；甲苯为1×10^-1ppm；苯乙烯为2×10^-2ppm。结论：该法操作简便、准确、灵敏，重现性好，可用于萜烯树脂中苯、甲苯、苯乙烯的残留量检测。     

离子选择性电极法测定卡托普利片含量

目的：建立离子选择性电极法测定卡托普利片含量的新方法。方法：卡托普利结构含有-SH,呈酸性,与碱作用生成RS-硫离子选择性电极对其产生响应。结果：电极响应的电位值与-lg[RS-]符合能斯特方程。能斯特响应范围为1．0×10^-6～1．0×10^-2mol／L（r=0．9998）,平均回收率为99．4％,RSD=0．29％（n=6）。结论：本法设备仪器简单,分析快速,专属性强。     

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.     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.