用二维核磁共振法研究肿足蕨碱的结构

从金星蕨科植物山东肿足蕨Hypodematium sinense Iwatsuki的全草分得一种新化合物，通过^1H-^1H COSY谱，^1H-^13C COSY谱和远程^1H-^13C COSY谱确定其结构是一种具有苯基取代苯并氮杂环辛四烯新型骨架的生物碱，命名为肿足蕨碱Hypodematine(Ⅰ）。     

连翘中苯乙醇甙类化合物

从连翘果实中分离了三种苯乙醇甙类化合物，calceolarioside A(1),plantainoside A(2)和forsythoside A(3），用光谱方法鉴定了它们的结构。1和2系首次从本属植物中分离得到，通过^1H－^1H COSY和^13C-^1H COSY对3的氢信号与碳信号进行正确归属，补充文献的不足，3能显著促进Con A诱导的淋巴细胞转化，提示其具有增强免疫作用，该活性未见报导。     

苯并硫氮杂(艹卓)类化合物的研究进展

在寻找先导化合物的过程中，苯并硫氮杂革类化合物占有非常重要的位置。按照结构类型，苯并硫氮杂革类主要包括1，3-、1,4-、4，1-和1，5-苯并硫氮杂革四大类。它们可以作用于许多不同家族的靶点，显示出了广泛的生物学活性。在苯并硫氮杂革类化合物中，1，5-苯并硫氮杂革类化合物的生物学活性最为广泛，可以作为钙离子通道拮抗剂、某些蛋白激酶的抑制剂、一些G蛋白偶联受体的拮抗剂以及缓激肽激动剂等。作者对苯并硫氮杂革类化合物的研究进展进行了综述。     

微生物来源白细胞介素1受体拮抗剂的研究Ⅱ．链霉菌660代谢产物的化学研究

从活性链霉菌660的发酵液中,经溶媒萃取,硅胶制备薄层层析及ODS等分离得到化合物4和化合物6,通过理化性质研究和UV、IR、MS、^1H-NMR、^13C-NMR、DEPT、^1H-^1H COSY、^1H-^13C COSY、HMBC等光谱分析确定化合物4为N－乙酰基酪胺（N-acetyltyramine),化合物6为3－丙基－7－甲基－六氢吡咯[1,2-a]并吡嗪－1,4－二酮（3－propyl-7-methyl-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione)。并对其活性进行研究。     

Assignments of ^1H and ^13C NMR Signals of Mogroside IVa

Aim To investigate the structure of mogroside IVa isolated from traditional Chinese medicine fructus momordicae [fruits of Siraitia grosvenori (Swingle) C. Jeffery] and summarize the NMR characteristics of the structure. Methods Cormnon extraction, separafion and purification methods were used. Various NMR techniques including ^1H NMR,^13C NMR, DEPT, ^1H-^1H COSY, HSQC, HMBC, NOESY and molecular model simulated by comtmter were used to elucidate the structure. Results ^1H and ^13C NMR signals of mogroside IVa were assigned, and spectroscopic basis was obtained for identification of such type of compounds. Conclusion 1D and 2D NMR techniques including ^1H-^1H COSY, HSQC, HMBC, NOESY spectra are powerful tools for structure analysis. The structure determined by NMR methods is identical with energy minimized conformation simulated by computer.     

2D NMR Studies on the Benzodiheteropine and its Cycloaddition Products

苯并硫氮杂卓是一类具有镇静作用的合成药物，对精神病，心脏病及高血压等疾病有一定疗效。为了深入探讨其结构与药效关系，应用１Ｈ１ＨＣＯＳＹ，１３Ｃ１ＨＣＯＳＹ和ＮＯＥＳＹ等２ＤＮＭＲ技术对苯并硫氮杂卓１及其环加成产物２～５进行了研究，对其１Ｈ、１３ＣＮＭＲ化学位移进行了指定，并分析讨论了化合物１～５的结构特征及苯并硫氮七元杂环呈船式构象的特点，各相关质子间的偶合常数也与讨论结果相符     

迭鞘石斛的化学成分研究

自兰科石斛属（Dendrobium）植物迭鞘石斛Dendrobium chryseum Rolfe中分得5个化合物，根据UV、IR、^1H NMR及^13C NMR确定其为β－谷甾醇，2，6－二甲氧基苯醌，鼓槌联苄，毛兰菲及鼓槌石斛素。这五种化合物均首次从该植物中分得。     

Naphtho-[2,3-b]pyrandiones类抗生素SP-1的分离与结构研究

在利用化学筛选法获得新染料类抗生素研究中，从产生菌Z-2002中，应用硅胶柱层析、薄层层析、凝胶柱层析及重结晶，分离纯化得到化合物SP-1，该化合物分子式为C14H12O6，分子量为276。SP-1与浓硫酸反应．呈鲜红色，对金黄色葡萄球菌209P有明显的抑制作用。通过UV、IR、EI．MS、HR．MS、^1h-NMR、^13C-NMR、DEPT、^1H-^1H COSY ^13C^1H COSY、HMBC、比旋光度等光谱学数据分析，确定了SP-1的结构。证明该化合物与（＋）-Cryptosporin一致并首次利用2D核磁共振数据明确了（＋）-Cryptosporin结构中各个^1H、^13C信号的归属。     

非那雄胺的核磁共振谱研究

利用NMR、IR、UV和MS等技术研究T5α-还原酶抑制剂非那雄胺分子结构的波谱学特征。结合DEPT谱、^H-^1H COSY、^33C^1H HETCOSY等方法对非那雄胺的氢谱和碳谱进行了归属。     

假轮枝链霉菌Streptomyces pseudoverticillus生产的Elaiophylin类新细胞周

通过波谱及X－线晶体结构分析，将从假轮枝链霉菌Streptomyces pseudouerticillus发酵物中分得的3个elaiophylin类化合物分别鉴定为elaiophyin(1)．11-O-monomethylelaiophyin(2)和efomycinG(3)，并利用DNMR技术对比合物1－3的^1H及^13C－NMR进行了详细解析，为今后该类新化合物的结构研究提供了有用的．详尽的NMR研究数据。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.