木桔根中的两个新香豆素成分

从木桔（Aegle marmelos Corr.）的根中分离出21个化合物，根据理化常数及波谱分析分别鉴定为：β－谷甾醇十五酸酯（β－sitosteryl pentadecanoate,1)，4－甲氧基－1－甲基－2－喹诺酮（4－methoxy-1-methyl-2-quinolone,2），酸橙皮油素(aurapten,3），4－谷甾烯－3－酮（4－sitosten-3-one，4），蛇麻脂醇（lupeol,5），前胡内酯（imperatorin,6），花椒毒素(xanthotoxin,7），白鲜碱（dicatmnine,8），（＋）－环氧酸橙皮油素（（＋）－epoxyaurapten,9），β－谷甾醇（β-sitosterol,10），崖椒碱（γ-fagarine,11),茵芋碱（skimmianine,12），木桔醛（marminal,13),6,7-二甲氧基香豆素（scoparone 14），7′－O－甲基木桔素（7′－O－methylmarmin,15），伞形花内酯（umbelliferone,16），东莨菪素（scopoletin,17），前胡醇(decursinol,18），异紫花前胡内酯（marmesin,19），木桔素(marmin,20），花椒喹诺酮（integriquinolone,21），其中，木桔醛和7′－甲基木桔素是新的天然产物。     

虹开堇菜的有效成分

首次报道了自堇菜科植物早开堇菜（Viola prionantha Beg.）全草中分离到三个香豆素类化合物。根据理化性质与光谱数据（IR.MS.^1HNMR.^13CNMR.2DNMR）推定，化合物Ⅲ的结构为6－羟基，7－[(6′-O－乙酰基－β－D－葡萄糖基）－O－]香豆素[6-hydroxy,7-[(6′-O-acetyl-β-D-glucopyranosyl)-oxy-]-coumarin]是新化合物，命名为早开堇菜甙（prionanthoside)。化合物Ⅰ、Ⅱ分别为已知化合物七叶内酯（esculetin）和菊苣甙(cichoriin）。     

走马芹中香豆素成分的研究

自走马芹根中分离出八种香豆素化合物(Ⅰ～Ⅷ),经鉴定为异佛手柑内酯(Ⅰ)、茴芹内酯(Ⅱ)、甲氧基欧芹素(Ⅲ)、佛手柑内酯(Ⅳ)、异茴芹内酯(Ⅴ)和牛防风素(Ⅵ)。4′-羟基-二氢欧山芹醇(Ⅶ)和香豆素化合物(Ⅷ)是新化合物,后者命名为走马芹内酯(moellendorffiline)。从走马芹叶和种子中均分离到六种香豆素化合物(Ⅰ～Ⅵ)。     

山蒟化学成分研究(Ⅱ)

从胡椒科植物山蒟(Piper hancei Maxim)中分得两个新木脂素成分(Ⅰ,Ⅱ)及三个生物碱(Ⅲ,Ⅳ,Ⅴ)。Ⅰ经光谱(IR,UV,MS,~1HNMR,~(13)CNMR,APT-~(13)SCNMR,2 D-HNMR)分析等证明其结构为rel-(7 S,8 S,1′R,3′S,4′R)-1′烯丙基-7-(3,4-二甲氧基苯基)-4′-羟基-5′-甲氧基-8-甲基-2′-氧双环[3.2.1]辛-5′-烯,为新结构,命名为山蒟醇(hancinol)。经光谱鉴定Ⅱ为burchellin,Ⅲ,Ⅳ,Ⅴ分别为风藤酰胺(futoamide)、荜拨明宁碱(piperlonguminine)和N-异丁基-反-2-反～4-癸二烯酰胺。后四种均首次从该植物中得到。     

山蒟化学成分研究(Ⅱ)

从胡椒科植物山蒟(Piper hancei Maxim)中分得两个新木脂素成分(Ⅰ,Ⅱ)及三个生物碱(Ⅲ,Ⅳ,Ⅴ)。Ⅰ经光谱(IR,UV,MS,¹HNMR,¹³CNMR,APT-¹³SCNMR,2 D-HNMR)分析等证明其结构为rel-(7 S,8 S,1′R,3′S,4′R)-1′烯丙基-7-(3,4-二甲氧基苯基)-4′-羟基-5′-甲氧基-8-甲基-2′-氧双环[3.2.1]辛-5′-烯,为新结构,命名为山蒟醇(hancinol)。经光谱鉴定Ⅱ为burchellin,Ⅲ,Ⅳ,Ⅴ分别为风藤酰胺(futoamide)、荜拨明宁碱(piperlonguminine)和N-异丁基-反-2-反～4-癸二烯酰胺。后四种均首次从该植物中得到。     

万年蒿化学成分研究

<正> 从抗肝炎草药万年蒿(Artemisia sacrorum Ledeb)地上部分的水煎液中,分离到28个化合物,经理化常数测定,化学合成,光谱分析,分别鉴定为:7个香豆素类:香豆素Ⅰ,东莨菪内酯Ⅱ,异东莨菪内酯Ⅲ,异秦皮定Ⅳ,七叶内酯Ⅴ,5-甲氧基-7,8-次甲二氧基香豆素Ⅵ,8-甲氧基-6,7-次甲二氧基香豆素Ⅶ;3个倍半萜类化合物:去乙酰氧母菊内酯Ⅷ,Ridentin Ⅸ,万年蒿氯内酯Ⅹ;6个贝壳杉烷型二萜类化合物:3α,16α,17-三羟基贝壳     

忍冬花蕾化学成分研究

目的：对忍冬花蕾化学成分进行研究，寻找抗菌活性化合物。方法：采用溶剂分配法，硅胶柱层析进行成分提取、分离。运用UV，IR，MS，^1H-NMR,^13C-NMR及标准品对照等。结合文献对比确定其结构，并进行抗菌活性药理实验。结果：从忍冬花蕾中分离得到11个化合物，分别是木犀草素（Ⅰ），5－羟基－7，3′，4′，5′－四甲氧基黄酮（Ⅱ）、5－羟基－7，3′，4′－三甲氧基黄酮（Ⅲ），5－羟基－7，4′－二甲基氧基黄酮（Ⅳ）、槲皮素（Ⅴ）、忍冬苷（Ⅵ）、5，7，3′，4′－四羟基黄酮醇－3－O－β-D－葡萄糖苷（Ⅶ）、3－O-[α-L－鼠李吡喃糖苷（1→2）－α－L－阿拉伯吡喃糖基]－28－O-[β-D-葡萄吡喃糖基（1→6）－β-D－葡萄吡喃糖基]齐墩果酸（Ⅷ）、绿原酸（Ⅸ）、胡萝卜苷（Ⅹ）、蔗糖（Ⅺ）。结论：化合物Ⅳ为首次从该属植物中发现，化合物Ⅴ，Ⅵ、Ⅷ和Ⅹ为首次从该植物的花蕾中发现，一些化合物显示较强的抗菌活性。     

万年蒿化学成分的研究

继前报作者又从蒿属植物万年蒿中（氯仿萃取部分，醋酸乙酯萃取部分和经大孔树脂乙醇洗脱部分）分得七个化合物。经理化学数测定，光谱分析鉴定化合物Ⅰ为东莨菪内酯，化合物Ⅱ为异秦皮定，化合物Ⅲ为琥珀酸，化合物Ⅳ为ｓｕｇｅｒｇｏｓｉｄ，化合物Ⅴ为万年蒿甙Ｃ，化合物Ⅵ为邻羟基桂皮酸酯甙和化合物Ⅶ为６－甲氧基－香豆素－７－羟基樱草甙，后者为首次从该属植物中分得的已知化合物。     

白花前胡中的香豆素类成分

从中药白花前胡（ＰｅｕｃｅｄａｎｕｍｐｒａｅｒｕｐｔｏｒｕｍＤｕｎｎ）根中分离得到６个化合物,经理化常数和波谱特征分别鉴定为Ｐｄ Ⅱ（Ⅰ）、顺式 ３′,４′ 二千里光酰基 ３′,４′ 二氢邪蒿内酯（Ⅱ）、ｉｓｏｂｏｃ ｃｏｎｉｎ（Ⅲ）、ａｅｇｅｌｉｎｏｌ（Ⅳ）、（－） 反式凯林内酯（Ⅴ）和伞形花内酯（Ⅵ）．化合物（Ⅲ）和（Ⅳ）为从前胡属植物首次分离得到,（Ⅱ）为从白花前胡中首次分离得到     

万年蒿化学成分的研究

继前报作者又从蒿属植物万年蒿中（氯仿萃取部分，醋酸乙酯萃取部分和经大孔树脂乙醇洗脱部分）分得七个化合物．经理化常数测定，光谱分析鉴定化合物Ⅰ为东莨菪内酯（ｓｃｏｐｏ－ｌｅｔｉｎ），化合物Ⅱ为异秦皮定（ｉｓｏｆｒａｘｉｄｉｎ），化合物Ⅲ为琥珀酸（ｓｕｃｃｉｎｉｃａｃｉｄ），化合物Ⅳ为ｓｕｇｅｒｅ－ｏｓｉｄ，化合物Ⅴ为万年蒿甙Ｃ（ｓａｃｒｏｓｉｄｅｃ），化合物Ⅵ为邻羟基桂皮酸酯甙（ｏ－ｈｙｄｒｏｘｙ－ｃｉｎｎａｍｏｙｌ－β－Ｄ－ｇｌｕｃｏｐｙｒａｎｏｓｉｄｅ）和化合物Ⅶ为６－甲氧基－香豆素－７－羟基樱草甙（６－ｍｅｔｈｏｘｙ－ｃｏｕｍａｒｉｎ－７－ｈｙｄｒｏ－ｘｙｌｐｒｉｍｅｖｅｒａｓｉｄｅ），后者为首次从该属植物中分得的已知化合物．     

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.

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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.     

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.     

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.