泰山野生丹参与种植丹参根、茎、叶中三种有效成分含量的分析比较

选用乙醇超声提取法提取丹参酮ⅡA，选用氨水超声提取法提取丹参素和原儿茶醛，用HLPC法测定泰山野生紫花丹参、种植紫花丹参和白花丹参中的丹参素、原儿茶醛、丹参酮ⅡA三种有效成分含量，并进行分析比较。结果表明野生紫花丹参、种植紫花丹参和白花丹参根中均含有丰富的有效成分；丹参叶中丹参素含量较高；丹参茎中三种有效成分含量较低。研究表明泰山三种丹参中有效成分含量无明显差异，丹参叶含丰富的丹参素和原儿茶醛，提示丹参叶也具有一定的药用价值。     

紫花丹参不同部位铅、汞、砷等元素的含量测定

目的:测定分析泰山紫花丹参不同部位铅、汞、砷等元素的含量.方法:用电感耦舍等离子发射光谱法和双通道原子荧光光谱法分别测定泰山紫花丹参根、茎、叶3个部位铅、汞、砷等元素的含量.结果:紫花丹参根中铅元素含量略微超标.根、茎和叶中的汞、砷含量均在行业标准范围内.结论:根据泰山紫花丹参不同部位铅、汞和砷含量的测定结果,建议紫花丹参应种植在环境中铅、汞、砷等元素含量低的地域.     

同种种苗异地栽培丹参质量比较研究

目的 对同种丹参种苗在不同地区栽培的丹参质量进行分析评价.方法 根据2015年版药典方法,采用高效液相色谱法(HPLC),对同种种苗异地栽培丹参的根、须根及地上部分茎、叶、花、花托6个部位的丹酚酸B、丹参酮类(丹参酮ⅡA、隐丹参酮、丹参酮I)进行含量测定.结果 同种种苗的含山栽培丹参中两类成分含量均略高于太和栽培丹参,丹参酮类在不同部位分布的含量为根>须根>花托>茎>叶>花,丹酚酸B则为根>须根>花>茎>花托>叶,丹参不同部位含量有较大差异,其中根和须根的含量均高于药典标准.结论 异地栽培的丹参脂溶性成分差异有统计学意义,含山产栽培丹参优于太和产;异地栽培的丹参水溶性成分丹参含量无差异;该实验为指导优质产区种苗的扩大种植提供参考依据.     

紫花丹参不同部位微量元素含量的分析比较

目的分析比较紫花丹参不同部位微量元素含量。方法用电感耦合等离子发射光谱法分别测定紫花丹参根、茎、叶、花4个部位17种微量元素的含量,对不同部位微量元素含量进行分析比较。结果紫花丹参根中镁元素含量最高,茎中钡和锶含量高,叶中硼和铜含量高,而花中铁元素含量分别是根、茎、叶的2.5、4和10倍,另外,花中的钛、锰、镍、钒、锡、铅、钴、铬、镉、锂、锌等11种微量元素含量也均高于其它3个部位。结论从微量元素角度分析,丹参的花也具有一定的药用价值。     

超高效液相色谱法对丹参不同部位化学成分的研究

目的 对丹参(叶、茎、花、根)不同部位中的可利用化学成分进行含量测定与分析。方法 采用超高效液相色谱——二极管阵列检测器(UPLC-PDA)法对丹参(叶、茎、花、根)中酚酸类、黄酮类成分的含量进行分析评价。结果 丹参中不同部位中丹酚酸类、黄酮类含量差异较大,丹参地上部分(叶、茎、花)中除了含有大量丹酚酸类成分外,相对根而言,还富含以芦丁为主的黄酮类成分,叶、茎、花中分别含有芦丁的质量分数为3.53、0.56、0.66 mg·g-1。结论 丹参叶、茎、花中含有大量的丹参酚酸类、黄酮类等资源性化学成分,对丹参资源利用效率提升以及扩大丹参新药源具有重要科学意义和开发前景。     

GC-MS法分析白花丹参不同部位挥发性成分

目的:研究白花丹参不同部位挥发油化学成分并进行比较。方法:采用水蒸气蒸馏法提取白花丹参根、茎、叶及花的挥发油,应用气相色谱-质谱(GC-MS)联用技术对各部位挥发油进行分析,利用面积归一化法分别计算各成分的相对质量分数。结果:从白花丹参根、茎、叶、花的挥发油中分别鉴定了39、33、21、28种成分。白花丹参根、茎、叶、花挥发油中主要化学成分差别很大,除大根香叶烯D为共有,且在茎、叶、花中相对质量分数都较高外,其它主要成分均不同。结论:本试验结果可为白花丹参的进一步开发利用提供依据。     

HPLC测定薏苡中薏苡素的含量

目的 测定非种仁部位(根、茎和叶)及不同产地、不同采收期的薏苡中薏苡素的含量,并评价品质,寻找新的药用部位.方法 采用HPLC法,以Diamonsil(R)C18为色谱柱,乙腈-水(50:50)为流动相,流速1 ml·min-1,柱温25℃,检测波长232 nm.结果 薏苡素的含量为根>叶>茎;不同产地中,根、茎中薏苡素的含量均以云南大度岗为最高,分别为16.1155、5.6659 mg·g-1;叶中的薏苡素含量以陕西汉中汉台区为最高,为10.6258 mg·g-1;6～11月采收的薏苡素的含量呈下降趋势.结论 该方法操作简便,定量准确,重复性好.建议可以薏苡根、茎、叶入药,不在花果期(7～10月)采收.     

四产地丹参主要成分的含量测定与分析

目的:测定不同产地丹参的主要化学成分及其含量.方法:采用95%～50%乙醇-水的综合工艺流程提纯丹参的脂溶性和水溶性成分,并用薄层双波长扫描法检测丹参酮ⅡA、丹参素、原儿茶醛的含量.结果:经常规对照检测,各产地丹参的脂溶性成分丹参酮ⅡA、水溶性成分丹参素的含量有显著差异,但水溶性原儿茶醛的含量差异不明显.结论:该测定结果可为临床及科研选用丹参提供参考.     

不同产地丹参药材中丹参酮Ⅱ_A的含量比较

目的 测定并比较西藏、四川等5个不同产地的丹参中丹参酮ⅡA的含量。方法 采用HPLC法测定。结果 丹参酮 ⅡA的含量在0.098％-0.913％之间。结论 西藏产丹参中丹参酮ⅡA的含量较高。HPLC法测定快速、灵敏度高。     

丹参茎、叶中丹酚酸B的HPLC法比较分析

目的:建立丹参茎、叶中丹酚酸B的HPLC测定方法,比较不同品种、不同产地、不同采收期丹参茎、叶中丹酚酸B的含量,为进一步合理开发利用丹参茎、叶资源提供理论依据。方法:采用phenomenexC18柱(250mm×4.6 mm,5μm);流动相为甲醇-乙腈-0.25%磷酸溶液(30:10:60);流速为1.0 mL/min;检测波长为286 nm。结果:建立了一个较好的分离和检测条件。工作曲线在(0.488~8.54μg)范围内呈良好的线性关系;平均加样回收率为98.17%。结论:该方法成功用于丹参茎、叶中丹酚酸B的含量测定。不同品种之间丹酚酸B的含量存在差异,其中紫花丹参含量较高。然而对同品种丹参茎叶来说,以泗水产的紫花丹参含量较高,并且8月份采集的含量最高。     

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.

     

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。