新疆鼠尾草中酚酸类化学成分的研究

目的 研究新疆鼠尾草的酚酸类化学成分.方法 采用多种柱色谱技术对化合物进行分离纯化,根据理化数据及波谱数据鉴定化合物的结构.结果 从新疆鼠尾草中分离得到7个化合物,分别鉴定为:丹参素(Ⅰ)、丹参素甲酯(Ⅱ)、原儿茶醛(Ⅲ)、原儿茶酸(Ⅳ)、咖啡酸(Ⅴ)、迷迭香酸(Ⅵ)、丹酚酸K(Ⅶ).结论 化合物Ⅰ、Ⅱ、Ⅲ、Ⅳ、Ⅴ为首次从新疆鼠尾草中分离得到.     

掌叶大黄新鲜叶柄的化学成分研究

目的 研究掌叶大黄Rheum palmatum L.新鲜叶柄的化学成分。方法 采用正相硅胶柱色谱、半制备高效液相色谱、重结晶等方法进行分离和纯化,采用核磁共振波谱方法鉴定结构。结果 从掌叶大黄新鲜叶柄汁的乙酸乙酯及正丁醇萃取部位共分离纯化得到了7个化合物,分别鉴定为：β-谷甾醇(Ⅰ)、大黄素(Ⅱ)、丁二酸(Ⅲ)、原儿茶酸甲酯(Ⅳ)、原儿茶酸(Ⅴ)、槲皮素(Ⅵ)和2-羟基-丁二酸-1-甲酯(Ⅶ)。结论 化合物Ⅲ、Ⅳ、Ⅶ均为首次从掌叶大黄中分离得到;化合物Ⅳ、Ⅶ为首次从大黄属植物中分离得到。     

弯锥香茶菜地下根茎的化学成分研究

目的 研究弯锥香茶菜Isodon loxothyrsa地下根茎的化学成分.方法 采用硅胶柱层析、RP-18、Sephadex LH-20等进行分离纯化,通过波谱法进行结构鉴定.结果 从弯锥香茶菜的地下根茎70％丙酮提取物的乙酸乙酯部位中分得10个化合物,分别鉴定为齐墩果酸(Ⅰ)、蒲公英甾醇(Ⅱ)、β-谷甾醇(Ⅲ)、棕榈酸(Ⅳ)、6,12,15-三羟基-5,8,11,13-松香四烯-7-酮(Ⅴ)、咖啡酸甲酯(Ⅵ)、胡萝卜苷(Ⅶ)、迷迭香酸甲酯(Ⅷ)、2α-羟基乌索酸(Ⅸ)、3-(3',4-二羟基苯基)-(2R)-乳酸甲酯(Ⅹ).结论 所有的化合物均是首次从该植物中分离得到.     

黄荆子亲脂性化学成分研究

目的研究马鞭草科牡荆属植物黄荆果实亲脂性化学成分。方法采用硅胶柱层析法、ODS柱层析法、Sephadex LH-20柱层析等分离方法对黄荆子亲脂性化学成分进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果分离得到7个单体化合物,分别为abietatrien-3β-ol(Ⅰ)、vitexifolin C(Ⅱ)、phytol(Ⅲ)、obtusalin(Ⅳ)、L-芝麻脂素(Ⅴ)、邻苯二甲酸二丁酯(Ⅵ)、β-谷甾醇(Ⅶ)。结论化合物为Ⅰ,Ⅱ,Ⅲ首次从该植物中分离得到。     

毛脉酸模内生真菌RGT-S11菌丝体化学成分研究

研究毛脉酸模(Rumex gmelini Turcz.)内生真菌RGT-S11菌丝中的化学成分。运用溶剂萃取、硅胶柱色谱、ODS反相柱色谱、Sephadex LH-20柱色谱、制备液相等方法进行分离纯化,根据理化性质、NMR数据鉴定化合物的结构。结果:分离得到7个单体化合物:苯甲酸(Ⅰ),棕榈酸(Ⅱ),麦角甾-5,7,22-三烯-3β-醇(Ⅲ),油酸(Ⅳ),腺苷(Ⅴ),鸟苷(Ⅵ),没食子酸(Ⅶ)。以上化合物均为首次从内生真菌RGT-S11菌丝中分离得到。     

玄参的化学成分研究

目的研究中药玄参(Scrophularia ninpoensis Hemsl.)的化学成分。方法利用乙酸乙酯萃取、硅胶柱色谱,Sephadex LH-20柱色谱,制备薄层色谱等方法对化合物进行分离和纯化,并通过波谱手段对分离得到的化合物进行鉴定。结果从玄参的乙酸乙酯萃取部位中分离得到6个化合物:eucalyptolic acid(Ⅰ),buergerisides A1(Ⅱ),原儿茶酸(Ⅲ),五-羟甲基糠醛(Ⅳ),肉桂酸(Ⅴ),β-谷甾醇(Ⅵ)。结论化合物Ⅰ,Ⅱ,Ⅲ为首次从该植物中分离得到。     

狗脊化学成分的研究

[目的]通过对狗脊Cibotium barometz(L.)J.Sm．根茎中化学成分的分离鉴定，为其进一步开发利用提供依据。[方法]采用硅胶柱层析和Sephadex LH-20柱层析分离化合物，并通过理化数据和波谱数据确定其结构。[结果]共分离并鉴定了9个化合物，即：棕榈酸(Ⅰ)、肛谷甾醇(Ⅱ)、棕榈酸单甘酯(Ⅲ)、胡萝卜苷(Ⅳ)、咖啡酸(Ⅴ)、原儿茶酸(Ⅵ)、原儿茶醛(Ⅶ)、正丁基-β-D-吡喃果糖苷(Ⅷ)和葡萄糖(Ⅸ)。[结论]化合物Ⅲ、Ⅶ、Ⅷ、Ⅸ为首次从该属植物中分离得到。     

白花牛角瓜茎的化学成分研究

目的研究白花牛角瓜茎的化学成分。方法通过反复硅胶柱色谱分离,sephadex LH-20及重结晶等方法进行分离纯化,根据波谱数据结合理化性质鉴定化合物结构。结果从白花牛角瓜的茎中分离得到5个化合物,其结构分别鉴定为蒲公英甾醇乙酸酯(Ⅰ),蒲公英甾醇(Ⅱ),6β-羟基-豆甾-4-烯-3-酮(Ⅲ),过氧麦角甾醇(Ⅳ)和吲哚-3-甲酸(Ⅴ)。结论化合物Ⅳ和Ⅴ为首次从该植物中分离得到。     

丹参注射液成份研究

丹参注射液具有治疗心血管系统疾病和肝脏疾病的作用。本文报道从丹参注射液中分离得到8个单体化合物,其中7个经鉴定为:丹参酮-1(Ⅰ)、隐丹参酮(Ⅱ)、异阿魏酸(Ⅲ)、原儿茶醛(Ⅳ)、琥珀酸(Ⅴ)、迷迭香酸(Ⅵ)和丹酚酸 A(Ⅶ)。     

金果榄化学成分的研究

目的对金果榄的化学成分进行研究。方法应用硅胶、MCI、Sephadex LH-20、RP-18柱色谱进行分离、纯化,根据理化常数和光谱分析鉴定结构。结果从青牛胆中分离出5个化合物,分别鉴定为:巴马亭(Ⅰ),胡萝卜苷(Ⅱ),巴马士宾(Ⅲ),β-谷甾醇(Ⅳ),1-四氢巴马亭(Ⅴ)。结论其中化合物V为首次从该植物中分离得到。     

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.     

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.     

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.