夏枯草的药用研究概述

夏枯草具有降血压、降血糖、抗肿瘤等药理作用,主要化学成分是三萜类,甾体类,黄酮类,苯丙素类等。夏枯草化学成分及药理作用研究较多,但化学成分研究主要集中在脂溶性成分的分离与分析方面,对夏枯草真正发挥药理作用的水溶性成分研究尚少,活性研究主要集中在粗提物方面,对夏枯草主要药理作用的作用机制、靶点和环节研究较少。应加强夏枯草水溶性化学成分、有效部位和有效单体、作用机制研究,为该药材的进一步应用开发提供依据。通过查阅国内外科技文献、书籍,对夏枯草药用植物的化学成分和药理作用的有关方面进行分析和归纳,综述夏枯草药用植物的化学成分和药理作用的有关研究进展。     

大血藤化学成分提取方法和药理作用的研究进展

目的：综述中药大血藤的化学成分提取方法及药理作用情况。方法对国内大血藤的化学成分、药理作用方面的文献进行总结。结果大血藤主要化学成分有酚酸类、蒽醌类、黄酮类、总皂苷、鞣质类等;药理作用有抗菌、抗病毒、消炎、抗肿瘤等。结论大血藤中化学成分的提取与测定方法较成熟、临床应用广泛,具有很好的应用前景。     

白术内酯类成分及其药理作用研究进展

目的:为白术的深入研究提供参考。方法:查阅国内、外文献,对白术化学成分和药理作用研究进展进行综述。结果:白术内酯类化学成分的研究主要集中在白术内酯Ⅰ、Ⅱ、Ⅲ上,而药理作用主要涉及对胃肠运动、离体子宫、炎症、肿瘤的影响等。结论:应进一步加强白术水溶性化学成分及药理作用的研究。     

文冠果化学成分及药理作用研究进展

目的对文冠果 (XanthocerassorbifoliaBunge )化学成分及药理作用研究进展进行综述。 方法按照化学成分和药理作用类型进行分类综述。结果与结论文冠果中主要含有三萜皂苷、黄酮、香豆素等类型成分 ,并且具有抗炎、抑制HIV 1蛋白酶、改善学习记忆功能等药理活性     

苍耳属植物化学成分及药理作用研究进展

目的对菊科苍耳属(XanthiumL.)植物的化学成分及药理作用作一综述。方法按照化合物的结构类型对苍耳属植物的化学成分进行分类综述,并且对其主要的生物活性进行总结。结果苍耳属植物中含有的化学成分主要有倍半萜内酯类、水溶性苷类、挥发油等化合物,它们具有抗菌、抗氧化、抗肿瘤、抗炎镇痛等药理作用。结论为苍耳属植物的进一步研究提供了依据。     

田基黄成分及药理应用研究进展

田基黄植物全草中主要化学成分为黄酮类、口山酮类、间苯三酚类等化合物,具有保肝护肝、退黄、抗菌、抗病毒、抗氧化以及抗肿瘤等药理作用。在检索国内外相关文献的基础上,对田基黄植物化学成分和药理作用以及临床应用进行了综述。     

大青属常见药用植物的研究进展

综述近年来国内外对大青属植物的化学成分与药理作用的研究,大青属植物中含有的化学成分主要为甾醇类、黄酮类、挥发性成分等;其药理作用主要有抗炎、抗氧化、抗肿瘤、治疗高血压等。     

文冠果的化学成分和药理作用研究进展

目的:为文冠果的深入研究和应用提供参考。方法:系统查阅国内、外文献并进行整理和归纳,对文冠果的化学成分和药理作用研究进展进行综述。结果与结论:文冠果中含有多种类型化学成分,主要有黄酮类、三萜皂苷类、甾类、香豆素类等,并具有抗炎、抗肿瘤、抑制人类免疫缺陷病毒蛋白酶、改善学习记忆功能、抑菌、抗氧化等多方面的药理作用。进一步深入开展文冠果化学成分和药理作用的研究,对全方位综合利用文冠果这一植物资源具有重要意义。     

马鞍树属植物化学成分及药理作用研究进展

目的对豆科马鞍树属(Maackia)植物的化学成分及药理作用作一综述。方法检索归纳相关文献26篇。按照化合物的结构类型对马鞍树属植物的化学成分进行分类综述,并且对其主要的生物活性进行总结。结果马鞍树属植物中含有的化学成分主要有黄酮类、生物碱类、艹氐类等化合物,它们具有抗氧化、抗辐射、抗肿瘤等药理作用。结论为马鞍树属植物的进一步的研究提供了依据。     

臭牡丹化学成分和药理作用的研究进展

对近年来国内外臭牡丹的化学成分与药理作用的研究进展作一概述,臭牡丹中含有的化学成分主要为甾醇类、萜类、过氧化物、挥发性成分等;其药理作用主要有局部麻醉、镇痛、抗肿瘤等。有必要对臭牡丹作进一步的研究。     

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。