三胶颗粒质量标准研究

目的建立三胶颗粒的质量标准.方法采用TLC法定性鉴别了当归、女贞子、黄芪、陈皮;用HPLC法测定制剂中橙皮苷的含量.结果制剂样品中橙皮苷的平均含量为1.69 mg·g-1,平均回收率为100.41%,RSD=1.36%(n=5).结论该方法简单、准确,能有效控制制剂质量.     

排石止痛合剂质量标准的研究

目的制定排石止痛合剂的质量标准.方法用TLC法鉴别制剂中延胡索、木香、大黄;用HPLC法测定芍药苷的含量.结果TLC色谱中能明显地检出延胡索、木香、大黄;HPLC法测定,芍药苷在0.8～26.0 μg·mL-1线性良好,r=0.999 6(n=6),平均回收率为99.64%,RSD为0.29%.结论定性、定量方法简便、准确,专属性强,能有效控制排石合剂的质量.     

温中止泻丸质量标准研究

目的建立温中止泻丸的质量标准。方法采用薄层色谱法对处方中丁香、木香进行定性鉴别;用HPLC法测定橙皮苷含量。结果在TLC定性鉴别中丁香酚、去氢木香内酯分离度好,专属性强;橙皮苷0.00592~7.40μg范围内,线性关系良好,相关系数r=0.9999(n=5);平均加样回收率为97.70%,RSD为1.59%(n=9)。结论该方法简便、准确,重复性好,可作为温中止泻丸的质量控制方法。     

平安丸的质量标准研究

目的:建立平安丸的质量标准。方法:采用薄层色谱(TLC)法对平安丸中的青皮、陈皮、枳实、肉豆蔻、木香、延胡索进行定性鉴别;采用高效液相色谱法测定处方中橙皮苷的含量。结果:TLC斑点清晰、分离度好;橙皮苷进样量在0.1～1.1μg(r=0.9999)范围内与峰面积积分值呈良好线性关系,平均回收率为99.48%,RSD=0.62%(n=6)。结论:所建标准可用于平安丸的质量控制。     

正气片质量标准研究

目的：建立正气片的质量标准。方法：采用TLC法鉴别正气片中的木香、甘草和厚朴,并用HPLC法对橙皮苷进行定量分析。结果：TLC法可以鉴别出木香、甘草和厚朴。HPLC检测橙皮苷的线性范围为0.05～0.75μg,线性方程为Y=1190.2X＋0.7771,r=0.9999。该方法回收率为（99.81±2.15）%（n=9）,精密度、重复性和稳定性良好。结论：本研究建立的方法专属性强,重现性好,准确、可靠,可有效控制正气片的质量。     

七味散质量标准的研究

目的:建立七味散的质量标准.方法:采用TLC对方中佛手、肉桂、木香、筚茇进行鉴别;采用RP-HPLC对制剂中胡椒碱的含量进行测定.结果:TLC法能检出佛手、肉桂、木香和筚茇;平均回收率为97.0%,RSD=1.8%(n=6).结论:方法快速、简便,适合该制剂的质量控制.     

沉香化滞丸质量标准研究

目的:建立沉香化滞丸的质量标准。方法:采用薄层色谱(TLC)法对制剂中的木香、香附、山楂、大黄、厚朴、牵牛子进行定性鉴别;采用高效液相色谱法测定制剂中橙皮苷的含量。结果:TLC显色清晰且阴性对照无干扰。橙皮苷的检测浓度在0.0242～0.4832mg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9994);平均回收率为102.5%,RSD=2.0%(n=6)。结论:所建标准可用于沉香化滞丸的质量控制。     

更年灵胶囊质量标准研究

目的:提高更年灵胶囊的质量标准,更有效控制其质量.方法:采用TLC法对处方中的女贞子进行定性鉴别;用HPLC法测定淫羊藿苷的含量.结果:用TLC能检出女贞子;淫羊藿苷在0.0868～1.6275μg范围内呈良好的线性关系,r=0.99995,平均回收率97.27%,RSD为1.98%.结论:方法简便,准确,重现性好,能有效控制该制剂质量.     

木香顺气丸鉴别与含量测定

的研究木香顺气丸的质量标准。方法采用薄层色谱法（TLC）对香附、木香、苍术、陈皮、青皮进行定性鉴别;采用高效液相色谱法（HPLC）测定橙皮苷含量,色谱柱为Diamonsil C18柱,流动相为甲醇 水 醋酸（40：60：0.3）,流速为1.0 mL•min－1,检测波长283 nm,柱温25 ℃。结果采用TLC可鉴别出香附、木香、苍术、陈皮、青皮对应的斑点;采用HPLC测定橙皮苷的含量,橙皮苷在0.180 2～1.802 0 μg范围内有良好的线性关系（r＝0.999 4）,平均回收率为99.0%,RSD为2.3%（n＝9）。结论所建立的质量标准简便可行、重复性好,可用来评价木香顺气丸质量。     

舒肝和胃丸质量标准研究

目的 修订舒肝和胃丸的质量控制方法。方法 采用TLC法对木香、佛手和陈皮药材进行鉴别;采用HPLC法同时测定去甲异波尔定、芍药内酯苷、芍药苷、1,2,3,4,6-O-五没食子酰葡萄糖与橙皮苷5种成分的含量。结果 木香、佛手和陈皮药材的TLC鉴别方法简单可行;去甲异波尔定、芍药内酯苷、芍药苷、1,2,3,4,6-O-五没食子酰葡萄糖与橙皮苷5种成分与其他色谱峰得到良好的分离,平均回收率分别为98.44%、100.99%、99.04%、100.15%和101.61%;RSD分别为1.84%、1.86%、1.82%、1.98%、1.82%。结论 该方法简便、准确,重现性好,可用于控制该产品质量。     

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.     

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.     

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.     

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.