多裂委陵菜化学成分研究

目的研究多裂委陵菜的化学成分.方法应用色谱技术分离纯化,应用波谱技术确定化合物的结构.结果从多裂委陵菜中分离鉴定了4个化合物,分别为腺苷(1)、芹菜素-6-C-阿拉伯吡喃糖基-8-C-葡萄吡喃糖苷(2)、芹菜素-7-O-β-D-葡萄糖醛酸苷(3)、木犀草素-7-O-β-D-葡萄糖醛酸苷(4).结论 4个化合物均为首次从委陵菜属中得到.     

江南卷柏中的黄酮碳苷类成分研究

目的:研究江南卷柏中的黄酮碳苷类成分。方法:采用溶剂提取、聚酰胺柱色谱、SehpadexLH-20柱色谱分离纯化,通过理化性质和波谱分析鉴定结构,并对化合物Ⅰ进行活性测试。结果:从江南卷柏正丁醇部位得到4种黄酮碳苷,鉴定其中3种,分别为芹菜素-6,8-二-C-β-D-吡喃葡萄糖苷(Ⅰ)、芹菜素-6-C-β-D-吡喃葡萄糖-8-C-β-D-吡喃木糖苷(Ⅱ)和芹菜素-6-C-β-D-吡喃木糖-8-C-β-D-吡喃葡萄糖苷(Ⅲ)。化合物Ⅰ能浓度依赖性地抑制结肠癌细胞环氧化酶-2mRNA的表达。结论:化合物Ⅰ为首次从江南卷柏中分离得到,Ⅱ、Ⅲ为首次从卷柏属中得到。     

风轮菜中黄酮苷类化合物的结构鉴定

从风轮菜全草的乙醇提取物中分离并鉴定了3个黄酮苷类人工产物,分别为芹菜素-7-氧-β-D-吡喃葡萄糖醛酸丁酯（1）、木犀草素-7-氧-β-D-吡喃葡萄糖醛酸丁酯（2）和柚皮素-7-氧-β-D-吡喃葡萄糖醛酸丁酯（3）。其中化合物3为新化合物。     

北葶苈子中黄酮苷类成分的分离与鉴定

目的对北葶苈子的黄酮苷类成分进行研究,为该植物资源开发利用提供依据。方法综合应用大孔吸附树脂、硅胶、Sephadex LH-20和ODS等柱色谱以及HPLC制备法对北葶苈子化合物进行分离纯化,利用理化性质与核磁共振波谱数据鉴定化合物的结构。结果从体积分数为50%的北葶苈子乙醇溶液提取物中分离鉴定了7个单体成分,分别为芹菜素-7-O-β-D-吡喃葡萄糖醛酸苷(apigenin-7-O-β-D-pyranglycuronide,1)、木犀草素-7-O-β-D-葡萄糖醛酸苷(luteolin-7-O-β-D-glycuronide,2)、(+)-4'-O-methylcatechin-7-O-β-D-glucopyranoside,3)、山奈酚-3-O-β-D-葡萄糖醛酸苷(kaempferol-3-O-β-D-glycuronide,4)、山奈酚-3-O-β-D-葡萄糖(1→2)-β-D-葡萄糖苷(kaempferol-3-O-β-D-glucosyl(1→2)-β-D-glucoside,5)、山奈酚-3-O-β-D-吡喃葡萄糖基(1→2)-β-D-吡喃葡萄糖基7-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl-7-O-β-D-glucopyranoside,6)及kaempferol 2G-glucosylgentiobioside(7)。结论在对北葶苈子的化学成分进行研究的过程中,分离鉴定了7个黄酮苷类化合物。化合物1~7均为首次从独行菜属中分离得到,并首次对化合物7的核磁数据进行报道。     

青钱柳水溶性成分的研究

目的:研究青钱柳的水溶性成分。方法:利用反相色谱的方法分离纯化,根据化合物的化学性质与光谱数据鉴定结构。结果:青钱柳的70%乙醇提取物中分得7个化合物,确定其结构分别为山奈酚-3-O-β-D-吡喃葡萄糖醛酸钠盐(kaempferol-3-O-β-D-glucuronate sodium,Ⅰ)、槲皮素-3-O-β-D-葡萄糖醛酸钠盐(quer- eetin-3-O-β-D-glucuronate sodium,Ⅱ)、杨梅素-3-Oβ-D-葡萄糖醛酸钠盐(myricetin-3-O-β-D-glucuronate sodi- um,Ⅲ)、2,6-二甲氧基-4-羟基苯酚-1-O-β-D-吡喃葡萄糖苷(2,6-dimethoxy-4-hydroxyphenol-1-O-β-D-gluco- pyranoside,Ⅳ)、色氨酸(tryptophan,Ⅴ)、没食子酸(gallic acid,Ⅵ),苯甲酸(benzoic acid,Ⅶ)。结论:化合物Ⅰ～Ⅵ为首次从该属中分得。     

空心莲子草中三萜皂苷类化学成分的研究

为了研究苋科植物空心莲子草[Alternanthera philoxeroides(Mart.)Griseb]抗病毒活性的物质基础,对其化学成分进行了研究。本文主要报道从空心莲子草正丁醇部位分离得到的5个三萜皂苷类化合物,经图谱分析,结构分别鉴定为:3-O-β-D-吡喃葡萄糖(1→3)-O-[β-D-吡喃葡萄糖]-齐墩果酸-28-O-β-D-葡萄糖醛酸苷(1)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷(2)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸-28-O-β-D-吡喃葡萄糖苷(竹节参苷Ⅳa,3)、3-O-β-D-吡喃葡萄糖醛酸丁酯-齐墩果酸-28-O-β-D-吡喃葡萄糖苷(4)和3-O-β-D-吡喃葡萄糖醛酸-常春藤皂苷K(尼泊尔常春藤皂苷K,5),其中化合物1为新化合物,化合物4和5为首次从该植物中分离得到。     

鹅绒藤地上部位化学成分研究

目的研究鹅绒藤(Cynanchum chinense R.Br.)地上部位的化学成分。方法采用AB-8大孔树脂柱,硅胶柱色谱,LX2000树脂柱,Sephadex LH-20柱色谱等方法分离纯化;利用核磁共振波谱技术鉴定化合物结构。结果从鹅绒藤地上部位70%乙醇提取物中分离得到9个化合物,分别鉴定为十六烷酸(Ⅰ)、水杨酸(Ⅱ)、β-谷甾醇(Ⅲ)、β-胡萝卜苷(Ⅳ)、芹菜素(Ⅴ)、山奈酚(Ⅵ)、山奈酚-3-O-β-D-吡喃葡萄糖苷(Ⅶ)、小麦黄素(Ⅷ)、小麦黄素-7-O-β-D-葡萄糖醛酸苷(Ⅸ)。结论化合物Ⅴ、Ⅷ、Ⅸ为首次从本属植物中分离得到;化合物Ⅰ、Ⅱ、Ⅴ～Ⅸ为首次从本植物中分离得到。     

益心巴迪然吉布亚颗粒中5种有效成分的含量测定方法及其指纹图谱研究

目的 建立益心巴迪然吉布亚颗粒中5种有效成分的含量测定方法及其指纹图谱.方法 采用高效液相色谱法测定10批(编号S1～S10)益心巴迪然吉布亚颗粒中木犀草素-7-O-β-D-葡萄糖醛酸苷(LG)、芹菜素-7-O-葡萄糖醛酸苷(APG)、迷迭香酸(RA)、香叶木素-7-O-β-D-葡萄糖醛酸苷(DG)、田蓟苷(TL)的含...     

黄花蒿水提物黄酮苷类成分研究

采用HP-20大孔吸附树脂、MCI柱色谱、硅胶柱色谱、中压液相色谱、葡聚糖凝胶Sephadex LH-20柱色谱及制备液相色谱等多种色谱技术,从黄花蒿水提物的正丁醇部位分离得到21个黄酮苷类化合物。根据化合物的理化性质和波谱数据确定了它们的结构,分别为甲氧基万寿菊素-7-O-β-D-吡喃木糖-(1→6)-β-D-吡喃葡萄糖苷(1)、荭草苷(2)、芹菜素-6-C-β-D-吡喃葡萄糖-8-C-β-L-吡喃阿拉伯糖苷(3)、芹菜素-6-C-β-D-吡喃半乳糖-8-C-β-L-吡喃阿拉伯糖苷(4)、芹菜素-6-C-β-L-吡喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(5)、芹菜素-6-C-α-L-呋喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(6)、槲皮素-3-O-β-D-吡喃葡萄糖苷-(1→2)-β-D-吡喃葡萄糖苷(7)、芹菜素-6-C-α-L-吡喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(8)、芹菜素-6,8-二-C-吡喃葡萄糖苷(9)、万寿菊素-7-O-β-D-吡喃葡萄糖苷(10)、木犀草素-6-C-吡喃葡萄糖苷(11)、牡荆素(12)、山柰酚-3-O-β-吡喃半乳糖-(1→2)-β-吡喃葡萄...     

山苦荬保肝活性部位筛选及其化学成分研究

目的:筛选山苦荬保肝活性部位并对其化学成分进行研究。方法:采用系统溶剂法,以70%乙醇对山苦荬药材进行提取,用不同溶剂对所得提取物进行萃取,分别得石油醚、乙酸乙酯、正丁醇部位和剩余水部位。以对乙酰氨基酚诱导人肝细胞HL-7702复制肝损伤细胞模型,采用MTT法检测上述各部位(40μg/mL,均以生药量计)对损伤细胞的保护作用并筛选活性部位。采用硅胶柱、葡聚糖凝胶柱色谱等分离手段对活性部位进行分离纯化,根据理化性质和波谱(氢谱、碳谱)数据鉴定化合物结构。结果:经山苦荬不同萃取部位作用后,各药物组细胞的存活率均较模型组显著升高(P<0.01),其中正丁醇部位和水部位的活性最强(细胞存活率分别为49.3%、52.2%)。从正丁醇部位中共分离并鉴定出6个化合物,分别为苦荬菜木脂素A(Ⅰ)、芹菜素-7-O-β-D-吡喃葡萄糖醛酸苷甲酯(Ⅱ)、木犀草素7-O-β-D-吡喃葡萄糖醛酸苷甲酯(Ⅲ)、木犀草素-7-O-β-D-葡萄糖苷(Ⅳ)、芹菜素-7-O-β-D-葡萄糖苷(Ⅴ)和木犀草素(Ⅵ)。结论:山苦荬正丁醇部位为该药材的保肝活性部位之一,其活性成分以黄酮类化合物为主。     

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.