Triterpenoid Saponins from the Root Bark of Araliataibaiensis

从太白木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）根皮中首次分离得到四个三萜皂甙，根据理化性质和光谱数据，分别鉴定为齐墩果酸３Ｏ［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸甙（１），ｔａｒａｓａｐｏｎｉｎⅤ（２），３Ｏ｛［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸乙酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（３）和３Ｏ｛［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸丁酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（４）。１为新天然产物，３和４为新化合物，分别命名为太白木皂甙Ⅵ（ｔａｉｂａｉｅｎｏｓｉｄｅⅥ）、太白木皂甙Ⅶ（ｔａｉｂａｉｅｎｏｓｉｄｅⅦ）和太白木皂甙Ⅷ（ｔａｉｂａｉｅｎｏｓｉｄｅⅧ）。     

太白木忽木根皮中三萜皂甙成分研究

从太白木忽木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）根皮中首次分离到四个三萜皂甙，根据理化性质和光谱数据，分别鉴定为齐墩果酸３Ｏ［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸甙（１），ｔａｒａｓａｐｏｎｉｎＶ（２），３Ｏ｛βＤ吡喃木糖（１→２）［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸乙酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（３）和３Ｏ｛βＤ吡喃木糖（１→２）［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸丁酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（４）。１为新天然产物，３和４为新化合物，分别命名为太白木忽木皂甙ＶＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩ）、太白木忽木皂甙ＶＩＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩＩ）和太白木忽木皂甙ＶＩＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩＩ）。     

Chemical Constituents of the Fruit of Licium barbarum L.

从宁夏枸杞（ＬｉｃｉｕｍｂａｒｂａｒｕｍＬ．）的果实（枸杞子）中分离得到１３个化合物，经光谱等方法鉴定其结构为８个长链脂肪酸（１～８），对羟基桂皮酸（ｐｃｏｕｍａｒｉｃａｃｉｄ，９），胡萝卜甙（ｄａｕｃｏｓｔｅｒｏｌ，１０），β谷甾醇（βｓｉｔｏｓｔｅｒｏｌ，１１），甜菜碱（ｂｅｔａｉｎｅ，１２），莨菪亭（ｓｃｏｐｏｌｅｔｉｎ，１３）。其中化合物１～１０为首次从枸杞子中得到     

A Novel Angular Furanocoumarin Isolated from Cnidium monnieri Fruit

从辽宁新民产蛇床Ｃｎｉｄｉｕｍｍｏｎｎｉｅｒｉ果实中分离鉴定出８个化合物，分别为２′乙酰白芷素（２′ａｃｅｔｙｌａｎｇｅｌｉｃｉｎ，８）、欧山芹素（ｏｒｏｓｅｌｏｎｅ，１）、β谷甾醇（βｓｉｔｏｓｔｅｒｏｌ，２）、哥伦比亚内酯（ｃｏｌｕｍｂｉａｎａｄｉｎ，３）、佛手柑内酯（ｂｅｒｇａｐｔｅｎ，４）、Ｏ乙酰基哥伦比亚甙元（Ｏａｃｅｔｙｌｃｏｌｕｍｂｉａｎｅｔｉｎ，５）、Ｏ乙酰异蛇床素（ｃｎｉｆｏｒｉｎＡ，６）和爱得尔庭（ｅｄｕｌｔｉｎ，７）。其中化合物８为一新化合物，化合物１系首次从该植物中分得。     

莶脂溶性成分的研究

从莶（ＳｉｅｇｅｓｂｅｃｋｉａｏｒｉｅｎｔａｌｉｓＬ）的地上部分，分离出八个化合物，其中Ｉ和Ｉ根据理化性质和光谱数据确定其结构为ｅｎｔ１７ａｃｅｔｏｘｙ１８ｉｓｏｂｕｔｙｒｙｌｏｘｙ１６（α）ｋａｕｒａｎ１９ｏｉｃａｃｉｄ（Ｉ）和ｅｎｔ１７ｅｔｈｏｘｙ１６（α）ｋａｕｒａｎ１９ｏｉｃａｃｉｄ（ＩＩ），均为新化合物，分别被命名为莶酯酸（ｓｉｅｇｅｓｅｓｔｅｒｉｃａｃｉｄ，Ｉ）和莶醚酸（ｓｉｅｇｅｓｅｔｈｅｒｉｃａｃｉｄ，Ｉ）。其余化合物分别鉴定为腺梗莶萜醇酸（ｅｎｔ１６β，１７ｄｉｈｙｄｒｏｘｙｋａｕｒａｎ１９ｏｉｃａｃｉｄ，ＩＩ），奇任醇（ｋｉｒｅｎｏｌ，ＩＶ，β谷甾醇葡萄糖甙（βｓｉｔｏｓｔｅｒｏｌｇｌｕｃｏｓｉｄｅ，Ｖ），二十一醇（ｈｅｎｅｉｃｏｓａｎｏｌ，ＶＩ），花生酸甲酯（ｍｅｔｈｙｌａｒａｃｈｉｄａｔｅ，ＶＩＩ）和β谷甾醇（βｓｉｔｏｓｔｅｒｏｌ，ＶＩＩ）。除奇任醇和β谷甾醇外，均为首次从该植物中分得。     

太白木根皮的齐墩果酸皂甙

从太白木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）根皮中首次分离到５个齐墩果酸皂甙，根据理化性质和光谱数据，分别鉴定为木皂甙Ａ（１），３Ｏ［αＬ呋喃阿拉伯糖（１→４）βＤ吡喃葡萄糖醛酸丁酯］齐墩果酸２８ＯβＤ吡喃葡萄糖甙（２），３Ｏ［αＬ呋喃阿拉伯糖（１→４）βＤ吡喃葡萄糖醛酸乙酯］齐墩果酸２８ＯβＤ吡喃葡萄糖甙（３），屏边三七甙Ｒ２（４）和３Ｏ｛βＤ吡喃葡萄糖（１→３）［αＬ呋喃阿拉伯糖（１→４）］βＤ吡喃葡萄糖醛酸乙酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（５）。２，３和５为新化合物，分别命名为太白木皂甙Ｉ（ｔａｉｂａｉｅｎｏｓｉｄｅＩ）、太白木皂甙Ｉ（ｔａｉｂａｉｅｎｏｓｉｄｅＩ）和太白木皂甙ＩＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＩＩ）。     

耳草属植物的化学研究I.黄毛耳草中环烯醚萜甙的分离和鉴定

从中药黄毛耳草（Ｈｅｄｙｏｔｉｓｃｈｒｙｓｏｔｒｉｃｈａ）中分离鉴定出１０个环烯醚萜类化合物，其中８个已知物为：车叶草甙（ａｓｐｅｒｕｌｏｓｉｄｅ，１），鸡屎藤甙甲酯（ｓｃａｎｄｏｓｉｄｅｍｅｔｈｙｌｅｓｔｅｒ，２），车叶草酸（ａｓｐｅｒｕｌｏｓｉｄｉｃａｃｉｄ，３），去乙酰车叶草酸（ｄｅａｃｅｔｙｌａｓｐｅｒｕｌｏｓｉｄｉｃａｃｉｄ，４），马钱子素（ｌｏｇａｎｉｎ，５），去乙酰车叶草甙（ｄｅａｃｅｔｙｌａｓｐｅｒｕｌｏｓｉｄｅ，６），乙酰鸡屎藤甙甲酯（ａｃｅｔｙｌｓｃａｎｄｏｓｉｄｅｍｅｔｈｙｌｅｓｔｅｒ，７），６β羟基京尼平（６βｈｙｄｒｏｘｙｇｅｎｉｐｉｎ，８）；２个新化合物命名为耳草甙（ｈｅｄｙｏｓｉｄｅ，９），６′乙酰车叶草甙（６′ａｃｅｔｙｌａｓｐｅｒｕｌｏｓｉｄｅ，１０）。除车叶草甙外均为首次从该植物得到，６β羟基京尼平为首次从天然界发现     

A New Phenylethanoid Glucoside from Buddleia officinalis

从密蒙花（Ｂｕｄｄｌｅｉａｏｆｆｉｃｉｎａｌｉｓ）中分离得到一个新苯乙醇甙，通过波谱分析，确定新化合物结构为β（３′，４′二羟基，６′Ｎ吡啶盐酸盐基苯基）乙基ＯαＬ吡喃鼠李糖基（１→３）βＤ（４″Ｏ咖啡酰基）呋喃葡萄糖甙，命名其为密蒙花新甙Ｂ。     

Studies on the Constituents of Aerial Parts of Scutellaria planipes

首次从木根黄芩地上部分分离出１３个化合物。经理化常数和光谱分析分别鉴定为异甘草甙元（ｉｓｏｌｉｑｕｉｒｉｔｉｇｅｎｉｎ），蓟黄素（ｃｉｒｓｉｍａｒｉｔｉｎ），汉黄芩素（ｗｏｇｏｎｉｎ），芹菜素（ａｐｉｇｅｎｉｎ），粘毛黄芩素Ⅲ（ｖｉｓｃｉｄｕｌｉｎⅢ），紫丁香甙（ｓｙｒｉｎｇｉｎ），白杨素６ＣβＤ葡萄糖８ＣαＬ阿拉伯糖甙（６ＣβＤｇｌｕｃｏｓｙｌ８ＣαＬａｒａｂｉｎｏｓｙｌｃｈｒｙｓｉｎ），白杨素６ＣαＬ阿拉伯糖８ＣβＤ葡萄糖甙（６ＣαＬａｒａｂｉｎｏｓｙｌ８ＣβＤｇｌｕｃｏｓｙｌｃｈｒｙｓｉｎ），黄芩甙（ｂａｉｃａｌｉｎ），汉黄芩甙（ｗｏｇｏｎｉｎ７ＯβＤｇｌｕｃｕｒｏｎｉｄｅ），白杨素７ＯβＤ葡萄糖醛酸甙（ｃｈｒｙｓｉｎ７ＯβＤｇｌｕｃｕｒｏｎｉｄｅ）和两个苯乙醇甙（ａｃｔｅｏｓｉｄｅ和ｍａｒｔｙｎｏｓｉｄｅ）。其中异甘草甙元，蓟黄素和紫丁香甙均为首次从黄芩属植物中分离得到。     

蛇毒中鞣花酸类及三萜类成分研究

自蛇毒（ＤｕｃｈｅｓｎｅａｉｎｄｉｃａＦｏｃｋ）全草中分离出６个化合物，其中，２个为新化合物，分别命名为蛇莓甙Ａ（ｄｕｃｈｅｓｉｄｅＡ）和蛇莓甙Ｂ（ｄｕｃｈｅｓｉｄｅＢ），经化学及光谱（ＵＶ，１Ｒ，１ＨＮＭＲ，１３ＣＮＭＲ，ＮＯＥＤＳ和ＭＳ）分析确定，蛇莓甙Ａ的结构为３＇－Ｏ－甲基－鞣花酸－４－Ｏ－β－Ｄ－吡喃木糖甙（Ⅰ），蛇莓甙Ｂ的结构为３＇－Ｏ－甲基－鞣花酸－４－Ｏ－α－Ｌ－呋喃阿拉伯糖甙（Ⅱ）。另外４个化合物为已知三萜类化合物：３β－羟基－乌苏烷－１２－烯－２８－羧酸（Ⅲ），２α，３β，１９α－三羟基－乌苏烷－１２－烯－２８－羧酸（Ⅳ），２α，３β，１９α－三羟基－乌苏烷－１２－烯－２８－羧酸－２８－Ｏ－β－Ｄ－吡喃葡萄糖甙（Ⅴ），２α，３α，１９α－三羟基－乌苏烷－１２－烯－２８－羧酸－２８－Ｏ－β－Ｄ－吡喃葡萄糖甙（Ⅵ）。其中化合物Ⅳ，Ⅴ和Ⅵ为首次从该属植物中分离得到。     

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.

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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.