云芝的化学成分

目的研究云芝的化学成分。方法用色谱学方法进行分离纯化,以波谱学方法进行结构解析。结果从云芝中分离并鉴定了八个化合物,分别为： 麦角甾-7,22-二烯-3β-棕榈酸酯（1）,麦角甾-7,22-二烯-3β-醇（2）,白桦脂酸（3）,4-羟基苯甲酸（4）,3-甲氧基-4-羟基苯甲酸（5）,3,5-二甲氧基-4-羟基苯甲酸（6）,2-呋喃酸（7）和烟酸（8）。结论八个化合物均为首次从云芝中分离得到。     

板栗种皮化学成分的分离与鉴定

目的更好地开发利用板栗(Castanea mollissimaBlume)的药用资源。方法采用硅胶柱色谱、凝胶柱色谱、氧化铝柱色谱和重结晶等方法对板栗种皮的体积分数为75%的乙醇提取物进行分离;通过NMR谱和薄层色谱等方法对分离得到的化合物进行结构鉴定。结果分离得到8个化合物,分别鉴定为对羟基苯甲酸(p-hydroxy benzoic acid,1)、原儿茶酸(protocatechuic acid,2)、没食子酸(gallic acid,3)、香草酸(vanillic acid,4)、东莨菪内酯(scopoletin,5)、豆甾-4-烯-6β-羟基-3-酮(stigmast-4-en-6β-ol-3-one,6)、豆甾-4-烯-3,6-二酮(stigmast-4-en-3,6-dione,7)、豆甾烷-3β,6α-二醇(stigmastane-3β,6α-diol,8)。结论化合物7、8为首次从栗属植物中分离得到。     

海燕化学成分研究

目的：研究海燕的化学成分。方法：采用多种层析方法分离海燕乙醇提取物,根据理化性质和光谱数据分析鉴定化合物的结构。结果：分离鉴定了7个化合物,分别为：3-十八烷氧基-1,2丙二醇（1）,3β-羟基-胆甾-7烯（2）,asterosaponin P1（3）,5α-胆甾烷-3β,4β,6α,7α,8β,15β,16β,26-八醇（4）,5α-胆甾烷-3β,6α,7α,8β,15α,16β,26-七醇（5）,色氨酸（6）,苯丙氨酸（7）。结论：化合物1、2为首次从海燕中分离得到,化合物4为首次从中国海域的海燕中分离得到。     

药用红树植物老鼠簕(Acanthus ilicifolius)乙醇提取物的化学成分研究

目的探讨老鼠簕的化学成分。方法将老鼠簕全株粉碎后,用95%乙醇浸提3次,合并浓缩,浸膏的石油醚部位经反复硅胶柱层析分离,结合波谱学数据鉴定化合物结构。结果从石油醚部位分离得到8个化合物,分别为β-谷甾醇(Ⅰ)、豆甾醇(Ⅱ)、正十六烷酸(Ⅲ)、正二十八烷酸(Ⅳ)、4,22-二烯-3-酮豆甾烷(stig-masta-4,22-dien-3-one)(Ⅴ)、4-烯-3-酮豆甾烷(stigmast-4-en-3-one)(Ⅵ)、5,22-二烯-7-酮-3β-羟基豆甾烷(3β-hydroxystigmasta-5,22-dien-7-one)(Ⅶ)、2-唑啉酮(2-benzoxazolinone)(Ⅷ)。结论其中Ⅴ,Ⅵ,Ⅶ为首次从该植物中分离得到。     

滇藏荨麻根中化学成分的分离与鉴定

目的研究荨麻属植物滇藏荨麻的化学成分。方法运用硅胶柱色谱、薄层色谱、制备薄层色谱S、ephadex LH-20柱色谱等方法进行分离纯化,通过理化性质和1H-NMR1、3C-NMR、EI-MS等数据以及与对照品对照等方法进行结构鉴定。结果从滇藏荨麻根分离得到10个化合物,分别鉴定为:豆甾-4-烯-3-酮(1)、4-羟基反式桂皮酸(2)、4-羟基苯甲醛(3)、4-甲氧基苯甲酸(4)、4-羟基苯甲酸(5)、己二酸(6)、二十四烷酸甲酯(7)、2-羟基二十四烷酸甲酯(8)、胡萝卜苷(9)、β-谷甾醇(10)。结论化合物1~10均为首次从滇藏荨麻中分离得到,其中化合物4、6~8为首次从荨麻属植物中分离得到。     

洋紫荆中化学成分的分离与鉴定

目的研究洋紫荆中的化学成分.方法采用硅胶、聚酰胺、Sephedex LH-20柱色谱分离纯化,理化常数和谱学方法鉴定结构.结果 分离得到7个化合物和1个混合物,鉴定为friedelin(1)、24(R)-9,19-cyclolanost-3-one-24,25-diol(2)和24(S)-9,19-cyclolanost-3-one-24,25-diol(3)的混合物、豆甾烷-3-酮(4)、豆甾烷-4-烯-3-酮(5)、豆甾烷-3β-醇-6-酮(6)、豆甾烷-5-烯-3β-醇-7-酮(7)、β-谷甾醇(8)、大黄素甲醚(9).结论 化合物2和3的混合物、5、7、9为首次从该属植物中分离得到.     

西瑁岛软珊瑚Sinularia sp. 的化学成分和生物活性研究

摘要：目的 对采自中国南海西瑁岛的软珊瑚Sinularia sp.的化学成分和生物活性进行研究。方法 综合利用薄层色谱、硅胶柱色谱、凝胶柱层析、半制备HPLC等分离手段,结合NMR和MS等波谱数据分析并对比文献数据,对化合物进行分离鉴定;选用A549和HL-60细胞株,采用CCK-8筛选方法,对化合物进行体外细胞毒活性测试。结果 从软珊瑚Sinularia sp.中共分离鉴定了10个甾体化合物,包括8个孕甾烷及其苷类化合物：3β-羟基-5,20-二烯孕甾烷乙酸酯（1）,20-烯-3-酮孕甾烷（2）,1,20-二烯-3-酮孕甾烷（3）,1,4,20-三烯-3-酮孕甾烷（4）,3β-羟基-20-烯孕甾烷（5）,3β-羟基-5,20-二烯孕甾烷（6）,1,4-二烯-3-酮-20α-羟基孕甾烷乙酸酯（7）,3β-羟基-5,20-二烯孕甾烷吡喃岩藻糖苷（8）;1个麦角甾烷类化合物：(22E,24R)-3β,5α,6β-三羟基-7,22-二烯麦角甾烷（9）和1个胆甾烷类化合物：(20S)-1,4-二烯-3,16-二酮-20β-羟基胆甾烷（10）。结论 化合物1～10对A549细胞株均未表现明显的细胞毒活性,但化合物4和7对HL-60细胞株具有中等的细胞毒活性,其IC50值分别为1.61 和 3.26 μmol/L。     

红树植物老鼠簕中的甾醇成分

目的系统研究红树植物老鼠簕Acanthus ilicifolius的化学成分。方法利用硅胶柱色谱、Sephadex LH-20凝胶色谱、HPLC高效液相色谱等方法分离纯化化合物,根据波谱数据和理化常数确定其结构。结果与结论从老鼠簕甲醇提取物的石油醚部位分离鉴定了9个化合物,分别是豆甾-4-烯-3-酮(1),豆甾-4,22-二烯-3-酮(2),麦角甾-4-烯-3-酮(3),豆甾-4-烯-3,6-二酮(4),豆甾-4,22-二烯-3,6-二酮(5),豆甾-4,22-二烯-6β-羟基-3-酮(6),6β-羟基-豆甾-4-烯-3-酮(7),3β-羟基-豆甾-5,22-二烯-7-酮(8),3β-羟基-豆甾-5-烯-7-酮(9)。其中,化合物4～8为首次从该植物中分离得到。体外细胞毒筛选实验表明,化合物2、4和9具有中等的细胞毒活性。     

楝树皮中的四环三萜类化合物

楝科植物楝树（Melia azedarach L.）为中药苦楝皮的基源植物之一。本研究从楝树的干燥树皮中分离鉴定出了8个化合物：其中6个为四环三萜类化合物,分别为meliastatin 3（1）、dubione B（2）、toosendanone A（3）、sendanolactone（4）、melianodiol（5）和1-tigloyl-3,20-diacetyl-11-methoxymeliacarpinin（6）;2个为甾醇类化合物,即豆甾-5-烯-3β,7α-二醇（7）和豆甾-4-烯-3β,6β-二醇（8）。化合物7、8为首次从楝属植物中分离得到,化合物1、2、3为首次从楝树中分离得到,化合物4、5、6为首次从楝树树皮中分离得到。     

藏药尼哇的植物甾醇苷类成分

目的：研究藏药尼哇（鸡蛋参）Codonopsis convolvulacea Kurz.的化学成分。方法：采用柱层析法进行分离,所得产物经光谱分析及化学方法鉴定。结果：分得一植物甾醇苷混合物,由△^7-豆甾烯醇-β-D-6'（二十碳烯酰）-吡喃葡萄糖苷（Ⅰ）;豆甾烷醇-β-D-6'（软脂酰）-吡喃葡萄糖苷（Ⅱ）;△^7-豆甾烯醇-β-D-6'（软脂酰）-吡喃葡萄糖苷（Ⅲ）及α-菠甾醇-β-D-6'（软酯酰）-吡喃葡萄糖苷（β）4种成份组成。结论：四组份均为首次党参属植物中获得。其中,Ⅰ、Ⅱ为新化合物。     

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.

     

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.