夏枯草中苯丙素和三萜的分离和鉴定

从夏枯草中用色谱法分离得到1个新的苯丙素类化合物1和5个已知的三萜类化合物2－6,经波谱法和化学法鉴定为3,4,α-三羟基苯丙素丁酯（1）,2α,3α,24－三羟基乌苏－12,20（30）－二烯－28－酸（2）、2α,3α,24－三羟基齐墩果－12－烯－28－酸（3）、2α,3α,24－羟基乌苏－12－烯－28－酸（4）、2α,3β－二羟基齐墩果－12－烯－28－酸（5）和2α,3β－二羟基乌苏－12－烯－28－酸（6）,5个三萜类化合物均为首次从夏枯草中分离得到。     

2,5-二苄氧基苯甲酸的制备

以乙醇为溶剂，KI为催化剂，用苄基氯对活泼试剂2，5－二羟基苯甲酸进行羟基保护得到2，5－二苄氧基苯甲酸，收率64％。     

连翘中一个新木脂素单糖甙

从连翘果实中分离得到了五个单体化合物，根据理化性质和光谱分析鉴定为：对－羟基苯乙酸[p-hydroxyphenyl acetic acid](1),( )松脂素－β-D－葡萄糖甙[( )pinoresinol-β-D-glucoside]（2），（＋）表松脂素－4－β-D-葡萄糖甙[( )epipinoresinol-4-β-D-glucoside]（3），（＋）松脂素单甲基醚－β-D-葡萄糖甙[( )pinoresinol mono methyl ether-β-D-glucoside]（4），连翘甙[phillyrin](5)。其中3未见文献报告，1－4为首次从连翘中分离得到的已知成分。     

黄海葵附生真菌Penicillium Sp.化学成分的研究（I）

从黄海葵[Anthopleura xanthogrammica (Berkly]附生真菌Penicillium sp.的发酵液中首次分离到4个化合物,分别鉴定为：对羟基苯乙醇（I）,（Z）N－[2,-(4,羟基苯基）乙烯基]甲酰胺（II）;（E）N－（2,（4－羟基苯基）乙烯基]甲酰胺（III）,邻苯二甲酸二异丁基酯（IV）,其中化合物（III）为首次从天然界分离得到,它们的化学结构经理化数据和波谱分析,结合文献报道数据照得以确定。     

葎草乙酸乙酯部位化学成分研究

从葎草[Humulus scandens（Lour.）Merr.]全草80%乙醇提取物乙酸乙酯萃取部位分离得到11个化合物,分别鉴定为：蒙花苷（1）,5,4′-二羟基-3,7-二甲氧基-6-甲基黄酮（2）,内消旋二氢愈创木脂酸（3）,β-蜕皮甾酮（4）,24（S）-5α-lanost-9（11）-ene-3β,24,25-triol（5）,积雪草酸（6）,对羟基苯甲酸（7）,反式桂皮酸（8）,松柏醛（9）,芥子醛（10）,尿嘧啶（11）。其中化合物1~5和7~11为首次从葎草属植物中分离得到,化合物6为首次从该种植物中分离得到。     

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。     

平叶酸藤子果实化学成分研究

摘要：目的:研究平叶酸藤子果实的化学成分。方法:采用硅胶柱色谱、凝胶柱色谱、重结晶、高效制备液相色谱法等现代分离方法和技术对平叶酸藤子果实乙酸乙酯部位化学成分进行分离纯化,并根据理化性质和波谱数据进行结构鉴定。结果:从平叶酸藤子果实中分离得到6个化合物,分别鉴定为柠檬酸三甲酯（1）、香草酸（2）、5-羟甲基糠醛（3）、1,5-二甲基柠檬酸酯（4）、1,6-二甲基-5-乙基柠檬酸酯（5）、3,4-二羟基苯甲酸（6）。结论:化合物1～6均为首次从平叶酸藤子中分离得到。     

白茅根化学成分研究

从白茅（Imperata cylindrica Beauv.var.major(Nees)C.E.Hubb.)的根茎中分离得到两种化合物，根据理化性质及波谱分析分别鉴定为α－联苯双酯（1）和4，7－二甲氧基－5－甲基香豆素（2）。这两个化合物均为首次从该属植物中分得。α－联苯双酯具有显著的保肝作用。     

(4R,5S)-4-甲基-3,5-二羟基己酸特丁酯的化学-生物合成

以2－甲基－3－羰基丁酸乙酯为原料，以面包酵母为生物催化剂，采用化学－生物法合成了光学纯（4R,5S)-5-羟基－3－羰基－4－甲基己酸（99．2％ee)。     

天然产物(E)-白黎芦醇的全合成

从价廉易得的3，5－二羟基苯甲酸为原料，通过甲基化、肼化、氧化反应得到中间体3，5－二甲基苯甲醛，与对甲氧基苄磷酸酯经Witting-Horner缩合反应得到单一反应的3，4‘,5－三甲氧基芪，最后用BBr3/CH2Cl2脱去甲基保护基，合成目标产物（-)-白黎芦醇，总收率为35．7％。     

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.