健脾补肾颗粒的质量标准研究

目的 建立健脾补肾颗粒的质量标准。方法 采用薄层色谱法（TLC）鉴别制剂中黄芪、丹参、党参、陈皮和白芍五味药材。用高效液相色谱法（HPLC）测定白芍中芍药苷的含量：色谱柱：Agilent Eclipse Plus C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：乙腈-0.1%磷酸水溶液梯度洗脱;流速：1.0 ml/min;柱温：25℃;检测波长：230 nm。结果 5种药材的TLC图谱斑点清晰,无阴性对照干扰;芍药苷在8.676~277.632 μg/ml范围内线性关系良好,（r=0.999 9）。结论 该法操作简单、重复性好,能够有效控制健脾补肾颗粒的质量。     

桃红通脉颗粒质量标准提高研究

目的 提高桃红通脉颗粒的质量标准。方法 采用薄层色谱（TLC）法对赤芍、地黄、甘草进行薄层鉴别,以及采用高效液相色谱法对主药桃仁的有效成分苦杏仁苷进行鉴别;采用高效液相色谱法测定芍药苷的含量,色谱柱为Agilent HC-C₁₈柱（250 mm×4.6 mm,5 μm）,流动相为乙腈-水（13：87）,流速为1.0 ml/min,柱温为30℃,检测波长为230 nm。结果 赤芍、地黄、甘草的TLC图均斑点清晰,阴性无干扰;芍药苷在1.79~57.28 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为99.99%,RSD为2.05%（n=9）。结论 提高桃红通脉颗粒质量标准后,鉴别方法重现性更好,优化了芍药苷的含量测定方法,增强了成品质量的可控性。     

医院制剂感冒颗粒质量标准研究

目的 建立医院制剂感冒颗粒的质量标准。方法 采用薄层色谱法（TLC）对黄芩、黄柏、柴胡进行薄层鉴别;采用高效液相色谱法（HPLC）测定黄芩苷的含量,色谱柱为Agilent HC-C₁₈（250 mm×4.6 mm,5 μm）,流动相为甲醇-0.2%磷酸（43：57）,流速为1.0 ml/min,柱温30℃,检测波长为280 nm。结果 黄芩、黄柏、柴胡的薄层色谱图均斑点清晰,阴性无干扰;黄芩苷在1.81~72.40 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为98.55%,RSD为1.91%（n=9）。结论 本研究建立的鉴别方法重现性更好,确定了黄芩苷的含量测定方法,增强了该制剂质量的可控性。     

复方生化颗粒的定性鉴别和含量测定研究

目的 提高复方生化颗粒的质量标准。方法 采用薄层色谱（TLC）法对处方中的甘草、丹参进行定性鉴别;采用高效液相色谱（HPLC）法鉴别苦杏仁苷;采用HPLC法测定处方中的丹酚酸B含量,色谱柱为Agilent HC-C₁₈（4.6 mm×250 mm,5 μm）,流动相为乙腈-0.1%磷酸（23：77）,流速为1.0 ml/min,检测波长为286 nm,柱温为30 ℃。结果 TLC斑点清晰,分离度较好,专属性强,阴性对照无干扰;HPLC法定性鉴别更加准确、可靠与客观;丹酚酸B在1.56~49.92 μg/ml范围内浓度与峰面积呈良好的线性关系（r=0.999 9）,平均回收率为100.07%,RSD为1.61%（n=9）。结论 建立的方法准确、可靠,重复性好,可用于复方生化颗粒的质量控制。     

康咳灵合剂质量标准研究

目的 建立康咳灵合剂的质量标准。方法 采用薄层色谱法（TLC）对矮地茶、百部进行定性鉴别;采用高效液相色谱法（HPLC）测定岩白菜素的含量。色谱柱为Lichrospher C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：甲醇-水（20：80）;检测波长：275 nm;柱温：30℃;流速：1 ml/min。结果 TLC法能准确鉴别矮地茶和百部,斑点清晰;岩白菜素在0.064 8~0.648 μg（r=0.9998）范围内线性关系良好,平均回收率100.24%（RSD为1.9%,n=6）。结论 本实验建立的方法简便、专属性高、重复性好,结果准确可靠,可用于康咳灵合剂的质量控制。     

香苏胃痛胶囊质量标准研究

目的 建立香苏胃痛胶囊的质量标准。方法 采用薄层色谱（TLC）法定性鉴别处方中甘草、延胡索、茯苓、香附;采用HPLC法测定延胡索乙素的含量。色谱柱为Welchrom C₁₈（4.6 mm×250 mm,5 μm）;以乙腈-0.1%磷酸（三乙胺调pH 6.0）（40∶60）为流动相;检测波长为280 nm;柱温：30℃;流速：1 ml/min。结果 薄层定性鉴别斑点清晰,分离效果良好,专属性强;延胡索乙素在1~80 μg/ml范围内与峰面积呈良好的线性关系（r=0.999 9）。平均加样回收率为99.1%,RSD为1.28%（n=6）。结论 本方法结果准确、操作简单,专属性和重复性良好,可作为该制剂的质量控制标准。     

清热败毒颗粒剂的质量标准研究

目的 建立清热败毒颗粒剂的质量标准。方法 采用薄层色谱法（TLC）鉴别处方中的板蓝根、连翘、紫花地丁和甘草,采用高效液相色谱法（HPLC）测定绿原酸的含量,色谱柱为Agilent ZORBAX SB-C₁₈柱（4.6 mm×250 mm,5 μm）;流动相为乙腈（A）与含0.2%甲酸的水溶液（B）,梯度洗脱：0~12 min,11%~12%A;流速：1.0 ml/min;柱温：30 ℃;检测波长：327 nm;进样量：20 μl。结果 薄层鉴别色谱中特征斑点明显,专属性强。绿原酸在6.19~396.00 μg/ml浓度范围内呈良好线性关系,其回归方程为Y=60.239 4X+9.096 3（r>0.999 9）,回收率为99.66%（RSD=2.82%）。结论 该法简便、稳定可靠、重复性好,为控制清热败毒颗粒的质量标准提供了可借鉴的依据。     

复方虎杖酊的质量标准研究

目的 建立复方虎杖酊的质量控制标准。方法 采用薄层色谱法对复方虎杖酊中虎杖、蜂房和冰片进行定性鉴别;采用HPLC法测定虎杖中虎杖苷的含量,色谱柱为Agilent Eclipse XDB-C₁₈柱（4.6 mm×250 mm,5 μm）,流动相：乙腈-水（23：77）,检测波长306 nm,流速1.0 ml/min,柱温40℃。结果 复方虎杖酊中虎杖、蜂房和冰片的薄层色谱图斑点明显,阴性对照无干扰;虎杖苷的定量测定在8.25~66.0 μg/ml范围内与峰面积呈良好的线性关系（r=0.999 9）,平均回收率为100.1%,RSD为0.2%。结论 本实验建立的方法快速简便,准确可靠,可作为该制剂的质量控制方法。     

复方黑参颗粒质量标准研究

目的 建立复方黑参颗粒的质量标准。方法 采用TLC法对复方黑参颗粒中玄参和射干进行定性鉴别,应用HPLC法同时测定肉桂酸、射干苷和次野鸢尾黄素的含量,色谱柱为Kromasil C₁₈柱（150 mm×4.6 mm,5 μm）,流动相为乙腈（A）-0.1%磷酸（B）水溶液,进行梯度洗脱;柱温30℃,检测波长270 nm;流速1.0 ml/min。结果 采用TLC法对玄参和射干进行定性鉴别具有良好的专属性,阴性对照无干扰。肉桂酸、射干苷、次野鸢尾黄素分别在16.22~113.57 μg/ml（r=0.999 8）、48.19~337.34 μg/ml（r=0.999 8）、16.40~114.80 μg/ml（r=0.999 9）范围内与峰面积呈良好的线性关系,平均加样回收率分别为99.23%、98.82%、99.17%。结论 本实验建立的方法快速、简便、重复性好,可用于复方黑参颗粒的质量标准控制。     

三藤口服液的质量标准研究

目的 建立三藤口服液的质量标准。方法 采用薄层色谱法鉴别处方中的大血藤和鸡血藤,采用HPLC法测定绿原酸的含量,色谱柱为Agilent Zorbax SB-C₁₈柱（4.6 mm×250 mm,5 μm）;流动相为乙腈-水（0.1%甲酸）（9∶91,v/v）等度洗脱;流速：1.0 ml/min;柱温：30 ℃;检测波长：330 nm;进样量：20 μl。结果 薄层鉴别色谱中特征斑点明显,专属性强。绿原酸在2.70~202.50 μg/ml浓度范围内线性关系良好,其回归方程为Y = 60.14X－6.37（r>0.999 9）。结论 该法简便、稳定可靠、重复性好,能够较好地控制三藤口服液的质量。     

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.

     

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.     

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.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。