石墨炉原子吸收分光光度法测定大鼠血浆和尿液中的赛特铂

目的建立大鼠血浆和尿液中赛特铂含量测定的无火焰石墨炉原子吸收分光光度法。方法采用岛津AA-670原子吸收分光光度仪及GFA-4A石墨炉,上海电光KY-1铂空心阴极灯,检测波长265.9 nm,测定大鼠血浆和尿液中的赛特铂含量。血尿样品用Triton X-100稀释,进样50μL。结果在浓度范围0.25 mg·L^-1-10.0 mg·L^-1内,样品峰面积与浓度呈良好线性关系,相关系数r²分别为血浆0.9952,尿液0.9878;加样回收率为血浆89%～112%,尿液82%～100%。结论方法简便可靠,适于生物样本中的赛特铂含量测定和动物药动学研究。     

石墨炉原子吸收法测定血浆顺铂含量

目的建立测定血浆中顺铂含量的方法。方法将血浆在1 000 r·min 1离心10 min后，取上清液，采用石墨炉原子吸收分光光度法测定顺铂的含量。结果人血浆中顺铂的回收率为94.7%～103.70%。结论该方法为一种可信度较高、操作性较强的血浆顺铂的测定方法。     

口服抗肿瘤药赛特铂在大鼠的药动学

目的 :观察口服抗肿瘤药赛特铂(satraplatin)在大鼠的药动学。方法 :石墨炉原子吸收分光法测定体内赛特铂的总铂浓度。结果 :剂量为 5 0mg·kg- 1和 10 0mg·kg- 1时 ,主要药动学参数分别为 :T12 β(4 3±s 34)h和 (5 8± 38)h ,Tmax(5 .0± 2 .0 )h和 (6 .0± 1.0 )h ,Cmax(12 .6± 2 .5 )mg·L- 1和 (13.4± 1.5 )mg·L- 1,AUC0 ∞(4 2 2± 12 0 )mg·h·L- 1和 (70 2± 118)mg·h·L- 1。组织分布以肝、肾最高。 4 8h后药物排出已基本完成 ,主要经粪便排出 ,约 5 5 % ,尿排出小于 6 % ,2 4h胆中排出0 .2 3%。结论 :赛特铂的药时曲线为口服一级吸收2室模型。     

石墨炉原子吸收光谱法测定药用玻璃中锑浸出量

目的：建立石墨炉原子吸收光谱法测定药用玻璃中锑浸出量的方法。方法：采用石墨炉原子吸收分光光度法,加入基体改进剂,测定标准溶液和供试液锑含量。结果：锑在0～100 g·L-1 浓度范围内呈良好的线性关系,r =0.9998;锑的检出限为1.38g·L-1;平均回收率为97.48%;样品测定结果为5.038/g·L-1。结论：该法经方法学验证可用于药用玻璃中锑浸出量的测定。     

石墨炉原子吸收法用于奥沙利铂脂质体大鼠的药动学

目的建立一种石墨炉原子吸收分析方法测定奥沙利铂脂质体大鼠静脉注射给药后的血药浓度,并考察其药动学行为。方法采用微波消解法对血浆样品进行前处理,使用石墨炉原子吸收光谱仪对药物浓度进行测定。大鼠分别尾静脉注射给药8 mg·kg~(-1)的奥沙利铂脂质体和注射剂,不同时间取血,分离获得血浆样品,利用所建立的方法测定血浆中奥沙利铂的浓度,计算药动学参数,考察其药动学行为。结果本方法可以准确、精密测定大鼠血浆中奥沙利铂的药物浓度,线性为0.52～187.25 mg·L~(-1),日内和日间变异系数均小于15%,最低定量限为0.327 mg·L~(-1)。奥沙利铂脂质体主要药动学参数:ρ_(max)为(120.64±18.42)mg·L~(-1),t_(1/2)为(11.61±5.22)h,V为(396.56±228.54)mL·kg~(-1),Cl为(24.07±9.43)mL·h~(-1)·kg~(-1),AUC_(0-24)为(311.38±93.29)mg·L~(-1)·h。结论该方法可以用于奥沙利铂脂质体大鼠药动学的研究,满足体内分析方法要求。与市售注射剂相比,奥沙利铂脂质体最大血药浓度与药时曲线下面积均显著提高,消除半衰期延长,显著改善了对应注射剂的体内药动学行为。     

络合分光光度法测定卡铂抗肿瘤膜剂含量

目的 建立络合分光光度法测定膜剂中卡铂含量的方法.方法 用蒸馏水提取膜剂中卡铂,与等体积1mol·L-1 SbCL2 的 1mol·L-1盐酸溶液反应后,用络合分光光度法测定反应液吸收度,检测波长为395 nm.结果 反应液中卡铂浓度于7.67～46.00 μg·mL-1之间与其吸收度有良好线性关系,r=0.9993;平均回收率=100.3%,RSD=2.3%(n=6).结论 该方法简便、快速、准确,适于测定膜剂中卡铂含量及质量控制使用.     

顺铂在大鼠体内血药浓度测定方法学研究

目的 建立大鼠血浆中铂含量测定的方法学,探讨顺铂经静脉注射给药后在大鼠体内的药动学过程。方法 采用浓硝酸消解法,石墨炉原子吸收法GFAAS测定血浆中铂含量。结果 第一步干燥温度100 ℃,时间20 s,第二步干燥温度150 ℃,时间30 s;灰化温度1 500 ℃,时间30 s,升温速率150 ℃·s^-1;原子化温度为2 700 ℃,净化温度2 800 ℃下,此法测定铂标准曲线方程为：A=0.002 49C+0.007 2,相关系数为R²=0.999 7;检出限为1.93 ng·mL^-1。结论 石墨炉原子吸收法测定血浆中铂含量的方法准确可靠,简便易行。     

改良原子吸收光谱法测定组织中载顺铂磁性纳米药物中的顺铂含量

目的建立改良组织消化和原子吸收光谱测定组织中铂浓度的方法。方法应用岛津原子吸收光谱系统,条件:AA-6300型原子吸收分光光度计、GFA-Ex7i石墨炉、ASC-6100自动进样器、铂元素空心阴极灯,含载顺铂磁性纳米药物的组织烘干后经硝酸和双氧水水浴消化后直接采用原子吸收光谱仪在265.9nm处测定。结果各不同组织顺铂线性范围均是54～283.5μg.L-1,相关系数r均大于0.999,日内变异系数均小于5%,日间变异系数均小于10%。结论采用改良原子吸收光谱法可高效、准确的检测湿化消化法处理的组织样本中铂元素的含量,该改良方法适用于顺铂药物动力学的研究。     

高效液相色谱法测定赛特铂胶囊含量

目的:建立赛特铂胶囊含量测定的高效液相色谱法。方法:色谱柱为北京迪马 Diamonsil~(TM)C_(18)(250mm×4.6mm,5μm)柱,流动相为甲醇-水-2%醋酸(50:35:15),检测波长260 nm。结果:在浓度范围6～200 mg·L~(-1)内,赛特铂峰面积与浓度呈良好线性关系(r=0.9999),样品加样回收率(n=5)为98.2%,RSD为1.1%。结论:方法简便可靠,能够满足赛特铂胶囊的含量测定要求。     

决明子富钒培育研究

目的:探讨决明子生芽、决明子耐钒和富钒能力.方法:用不同浓度的偏钒酸钠水溶液培育决明子芽,用石墨炉原子吸收分光光度计测定富钒决明子芽的钒含量.结果:决明子对偏钒酸钠有较强的耐受力,能够耐受的最大偏钒酸钠浓度是1200 mg·L-1.结论:当培养液中偏钒酸钠浓度为800 mg·L-1时,决明子芽中钒含量最高.     

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.

---

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.