丁座草的化学成分研究

目的 研究丁座草块茎的化学成分。方法用色谱方法分离丁座草块茎的乙醇提取物。结果 共分离得到8个化合物，根据理化性质及各种光谱技术进行结构鉴定，分别为α-香树素（Ⅰ）、3β-乙酰氧基-熊果-28，13-内酯（11）、3β-乙酰氧基-熊果-11（12）-烯-28，13-内酯（Ⅲ）、3β-乙酰熊果酸（Ⅳ）、3β-乙酰齐墩果酸（V）、β-谷甾醇（Ⅵ）、熊果酸（Ⅶ）、（＋）-松脂素单葡萄糖苷（Ⅷ）。结论 化合物Ⅰ～Ⅲ为首次从该属植物中分离得到。     

梅叶冬青根的化学成分研究

目的研究梅叶冬青根的化学成分。方法采用硅胶柱层析、凝胶柱层析和反相硅胶柱层析等方法分离纯化梅叶冬青根的化学成分,并根据理化性质和波谱数据鉴定化合物的结构。结果从梅叶冬青根的甲醇提取物中分离得到9个化合物,分别鉴定为3β-O-乙酰熊果醇(Ⅰ)、3β-O-乙酰熊果酸(Ⅱ)、泰国树脂酸(Ⅲ)、齐墩果酸(Ⅳ)、咖啡酸(Ⅴ)、乌索酸(Ⅵ)、2α,3β,19α-三羟基乌索-12-烯-23,28-二羧酸(Ⅶ)、β-谷甾醇(Ⅷ)和胡萝卜苷(Ⅸ)。结论化合物Ⅰ～Ⅴ为首次从该植物中分离得到。     

广东紫珠地上部位化学成分研究(Ⅰ)

目的研究广东紫珠的化学成分.方法用硅胶色谱技术分离化学成分,用IR、NMR和MS等方法鉴定化合物.结果得到并鉴定的6个化合物分别为:β-谷甾醇(Ⅰ)、齐墩果酸(Ⅱ)、熊果酸(Ⅲ)、水杨酸(Ⅳ)、丙氨酸(Ⅴ)和琥珀酸(Ⅵ).结论上述化合物均为首次从该植物中分离得到.     

团状雪灵芝的化学成分研究(Ⅰ)

目的 研究石竹科蚤缀属植物团状雪灵芝的化学成分.方法 采用多种色谱法分离纯化单体化合物并鉴定其结构.结果 分离并鉴定出的5个化合物分别为22,23-二氢波甾醇-3-O-β-D-葡萄糖苷(Ⅰ)、β-谷甾醇(Ⅱ)、β-胡萝卜苷(Ⅲ)、22,23-二氢波甾醇(Ⅳ)和22,23-二氢波甾酮(Ⅴ).结论 所有化合物均为首次从该植物中分离得到;化合物Ⅰ为首次从该属植物中分离得到.     

城南细辛化学成分研究(Ⅰ)

目的研究城南细辛的活性化学成分.方法利用柱层析方法分离化合物,理化性质以及光谱方法(UV、IR、NMR、MS)鉴定化合物.结果从城南细辛中离分得3个化合物,鉴定为1-细辛脂素(Ⅰ),1-芝麻脂素(Ⅱ)和β-谷甾醇(Ⅲ).结论化合物Ⅰ、Ⅱ、Ⅲ均为首次从该植物中分离得到.     

留兰香的活性成分(Ⅰ)

目的对唇形科薄荷属植物留兰香(Mentha spicataL.)的活性部位的化学成分进行研究。方法采用硅胶柱色谱等方法进行分离纯化,根据理化性质和光谱数据进行结构鉴定。结果得到4个化合物,分别鉴定为3甲氧基4羟基苯甲酸(3 methoxy 4 hydroxybenzoic acid,Ⅰ)、3,5二甲氧基4羟基苯甲酸(3,5 dimethoxy 4 hydroxybenzoic acid,Ⅱ)、橙皮素7OβD葡萄糖苷(hes-peretin 7OβDglucoside,Ⅲ)、芹菜素7OβD吡喃葡萄糖苷(apigenin 7OβDpyranglucoside,Ⅳ)。结论化合物Ⅰ,Ⅱ为首次从薄荷属植物中分离得到,化合物Ⅲ,Ⅳ为留兰香中首次分离得到。     

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。     

维药睡莲花中的黄酮醇苷类成分分析

目的 对维药睡莲花的黄酮醇苷类成分进行研究.方法采用硅胶、聚酰胺和Sephadex LH-20柱进行分离,利用理化性质和波谱学方法鉴定化合物的结构.结果分得六个黄酮醇苷类化合物,分别为黄芪苷(Ⅰ)、槲皮素3-O-甲基-3'-D-β-D-吡喃木糖苷(Ⅱ)、槲皮素3'-O-β-D-吡喃木糖苷(Ⅲ)、异槲皮苷(Ⅳ)、山萘酚3-O-β-D-芸香糖苷(Ⅴ)、芦丁(Ⅵ).结论 化合物Ⅰ、Ⅳ、Ⅵ为首次从该植物中分离得到,其中化合物Ⅳ为首次从该属植物中分离得到.     

栾树花中香豆素类化合物研究

目的对栾树的花进行化学成分研究。方法采用硅胶、聚酰胺柱层析进行分离纯化,根据理化性质和光谱分析鉴定化合物结构。结果从栾树花三氯甲烷部分中分离得到了3个化合物,经鉴定分别为β-谷甾醇(Ⅰ)、乙酰基伞形花内酯(Ⅱ)和6-苯甲酰基伞形花内酯(6-苯甲酰基-7-羟基香豆素)(Ⅲ)。结论化合物Ⅱ、Ⅲ为香豆素类化合物,是首次从栾树属植物中分离得到;3个化合物均为首次从栾树花中分离得到。     

金刚藤化学成分研究

目的：研究百合科菝葜属植物金刚藤Smilax bockii.的化学成分。方法：采用反复硅胶柱层析进行分离纯化,通过理化常数测定和光谱分析鉴定其化学结构。结果：从金刚藤分离得到了6个黄酮类及有机酸类化合物,分别为芦丁（rutin,Ⅰ）,异台黄杞苷（isoengeletin,Ⅱ）,咖啡酸正丁酯（caffeic acid n-butyl ester,Ⅲ）,正丁基-β-D-吡喃果糖苷（n-butyl-β-D-fructopyranoside,Ⅳ）,3,5-二甲氧基-4-羟基苯甲酸（3,5-dimethoxy-4-hydroxy-benzonic acid,Ⅴ）,原儿茶酸（protocatechuic acid,Ⅵ）。结论：以上化合物均为首次从该植物中分离得到,化合物Ⅰ,Ⅲ,Ⅳ,Ⅵ为首次从本属植物中分离得到。     

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.

---

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.