兵豆中一新脑酰胺糖甙

从兵豆（Lens culinaris Medic.)种子乙醇提取物中分离到8个化合物,通过理化鉴定与波谱分析测定所分离出化合物的分子结构,分别鉴定为β－谷甾醇（1）,β－谷甾醇棕榈酸酯（Ⅱ）,胡萝卜甙（Ⅲ）,棕榈酸（Ⅳ）,9,10－二羟基硬脂酸（V）,乙基－α-D－葡萄糖甙（VI）,3－O－甲基－D－手机醇（Ⅶ）和兵豆甙（Ⅷ）,所有化合物均是首次从该植物中分离得到,其中Ⅷ为一新脑酰胺糖甙,命名兵豆甙。     

莲子心中黄酮类物质的提取和鉴定

目的 阐述了莲子心中两种黄酮甙的提取和鉴定.方法 通过用各种色谱法从莲子心甲醇提取液分离纯化得到2个化合物,并应用核磁共振技术对获得的化学成分进行化合物结构鉴定.结果 分离并鉴定了2个化合物,分别为未犀草素-8-C-β-D-葡萄糖甙和木犀草素-6-C-β-D-葡萄糖甙.结论 分离到的2个黄酮类化合物均为碳甙黄酮[0].     

铁扫帚化学成分研究

目的研究铁扫帚的化学成分。方法采用反复柱色谱方法进行分离，利用化合物的光谱学数据结合理化性质鉴定化合物的结构。结果分离并鉴定8个化合物：β-谷甾醇（Ⅰ）、正二十八烷醇（Ⅱ）、水杨酸（Ⅲ）、香草酸（Ⅳ）、山柰酚（Ⅴ）、桷皮素（Ⅵ）、山柰酚-3-O-β-D-葡萄糖苷（Ⅶ）、胡萝卜苷（Ⅷ）。结论化合物Ⅱ～Ⅷ为首次从该种植物中分离得到。     

土贝母化学成分的分离与鉴定

目的研究中药土贝母的化学成分.方法用硅胶、Sephadex LH-20柱色谱法进行分离纯化,通过理化性质及光谱数据,结合化学反应确定化合物的结构.结果分离得到7个化合物,分别鉴定为β-谷甾醇(Ⅰ)、胡萝卜苷(Ⅱ)、胡萝卜苷棕榈酸酯(Ⅲ)、β-谷甾醇棕榈酸酯(Ⅳ)、5-羟甲基糠醛(Ⅴ)、麦芽酚(Ⅵ)、正丁基-β-D-吡喃果糖苷(Ⅶ).结论除化合物Ⅵ外,其他化合物均为首次从该植物中分离得到.     

裸花紫珠的化学成分研究

目的研究裸花紫珠的化学成分。方法应用各种柱层析方法分离纯化,运用光谱数据解析鉴定化合物结构。结果分离鉴定了11个化合物,分别为：2α,3α,24-三羟基-齐墩果烷-12-烯-28-酸（Ⅰ）,2α,3β,24-三羟基-齐墩果烷-12-烯-28-酸（Ⅱ）,2α,3β,19α-三羟基-齐墩果烷-12-烯-28-O-β-D-葡萄糖苷（Ⅲ）,2α,3α,19α,23-四羟基-齐墩果烷-12-烯-28-O-β-D-葡萄糖苷（Ⅳ）,岳桦素（Ⅴ）,芹菜素（Ⅵ）,木犀草素（Ⅶ）,无梗五加苷B（Ⅷ）,aurantiamide acetate（Ⅸ）,β-谷甾醇（Ⅹ）,β-胡萝卜苷（Ⅺ）。结论化合物Ⅱ～Ⅳ,Ⅷ和Ⅸ为首次从紫珠属植物中分离得到,化合物Ⅰ和Ⅴ为从裸花紫珠中首次分得。     

凤丫蕨化学成分研究

目的研究风丫蕨Coniogramme japonica的化学成分。方法采用色谱法进行分离,根据理化性质和波谱数据鉴定化合物的结构。结果分离得到14个化合物,分别鉴定为onitisin（1）、1,3-双棕榈酸甘油酯（2）、5α,8α-过氧麦角甾-6,22E-二烯-3β-醇（3）、β-谷甾醇棕榈酸酯（4）、棕榈酸（5）、硬脂酸（6）、豆甾-4-烯-3β,6β-二醇（7）、芹菜素（8）、β-谷甾醇（9）、β-胡萝卜苷（10）、葡萄糖（11）、9S,12S,13S—trihydroxy-10-octadecenoic acid（12）、胡萝卜苷棕榈酸酯（13）、4-oxododecanedioic acid（14）。结论化合物1～3、5～8和11—14均是首次从凤丫蕨中得到。     

狗脊化学成分的研究

[目的]通过对狗脊Cibotium barometz(L.)J.Sm．根茎中化学成分的分离鉴定，为其进一步开发利用提供依据。[方法]采用硅胶柱层析和Sephadex LH-20柱层析分离化合物，并通过理化数据和波谱数据确定其结构。[结果]共分离并鉴定了9个化合物，即：棕榈酸(Ⅰ)、肛谷甾醇(Ⅱ)、棕榈酸单甘酯(Ⅲ)、胡萝卜苷(Ⅳ)、咖啡酸(Ⅴ)、原儿茶酸(Ⅵ)、原儿茶醛(Ⅶ)、正丁基-β-D-吡喃果糖苷(Ⅷ)和葡萄糖(Ⅸ)。[结论]化合物Ⅲ、Ⅶ、Ⅷ、Ⅸ为首次从该属植物中分离得到。     

知母化学成分的研究

从知母根茎乙醇提取物中分离得到20个化合物，采用光谱法和化学方法鉴定其中15个化合物的结构；分别为二十九烷醇（Ⅰ）、二十八烷酸混合物（Ⅱ）、β-谷甾醇（Ⅲ）、胡萝卜甙（Ⅳ）、菝葜皂甙元（Ⅴ）、马尔可皂甙元（Ⅵ）、知母皂甙AⅢ（Ⅶ）、知母皂甙BⅠ（Ⅷ）、知母皂甙BⅢ（Ⅸ）、2，6，4＇-三羟基-4-甲氧基苯酰酮（Ⅹ）、宝藿甙Ⅰ（Ⅺ）、淫羊藿甙-Ⅰ（Ⅻ）、芒果甙（ⅩⅢ）、7-O-萄葡糖基芒果甙（ⅩⅣ）、知母双糖（ⅩⅤ）．其中化合物Ⅷ为新的天然产物，化合物Ⅰ，Ⅺ，Ⅻ，ⅩⅣ为首次从知母中分得的已知化合物．     

西南獐牙菜化学成分的研究

从西南獐牙菜的全植物中分离出五个化合物,其中四个分别被鉴定为β-谷甾醇(Ⅶ),齐墩果酸(Ⅵ),1,3,7,8-四羟基咄酮(Ⅴ)和山楂酸(Ⅱ)。另一化合物系新的三萜酸糖酯甙,命名为獐牙菜皂甙(swericinctoside,Ⅰ),其结构为2α,3β-二羟基齐墩果-12-烯-28-羧酸-28-O-β-D-葡萄吡喃糖基-(1-6)-β-D-葡萄吡喃糖基-(1-2)-β-D-葡萄吡喃糖甙。     

板蓝根提取物化学成分研究（I）

利用反复硅胶柱色谱对板蓝根中的化学成分进行分离纯化，共得到7个化合物，分别鉴定为：腺苷（adenosine，1）、棕榈酸（2）、棕榈酸α，α’-双甘油酯（3）、棕榈酸．单甘油酯（4）、青黛酮（qingdainone，5）、靛玉红（indirubin，6）、β-谷甾醇（7）。其中化合物3、4为首次从该属中分离得到。     

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.

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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.