葛根正丁醇部位的化学成分研究

目的 研究葛根正丁醇萃取物的化学成分.方法 采用聚酰胺柱色谱、反相ODS柱色谱、凝胶柱色谱、制备液相色谱等方法进行分离纯化,根据化合物的理化性质及波谱数据鉴定其结构.结果 分离鉴定了12个化合物,分别为葛酚苷元A(1)、葛酚苷元B(2)、染料木素(3)、3′-甲氧基葛根素(4)、3′-羟基葛根素(5)、葛根素芹糖苷(6)、葛根素木糖苷(7)、大豆苷元(8)、大豆素7,4′-二葡萄糖苷(9)、大豆苷(10)、葛根素(11)、胡萝卜苷(12).结论 其中化合物1、2为首次从葛属植物中分离得到.     

葛根化学成分研究

摘要：目的:研究葛根化学成分。方法:通过大孔树脂、MCI柱以及制备型HPLC进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果:分离纯化得到23个化合物,分别为美佛辛-4’-O-葡萄糖苷(1)、3’-羟基葛根素芹菜糖苷(2)、大豆苷元-4’-葡萄糖苷(3)、葛根素芹菜糖苷(4)、大豆苷元-4’,7-二葡萄糖苷(5)、葛根素-6’’-O-木糖苷(6)、3’-羟基葛根素(7)、3’-甲氧基葛根素(8)、tuberosin(9)、毛蕊异黄酮苷(10)、葛根苷B(11)、葛根苷A(12)、3’-甲氧基大豆苷(13)、染料木素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷(14)、染料木苷(15)、刺芒柄花素(16)、formononetin-8-C-β-D-apiofuranosyl-(1→6)-O-β-Dglucopyranoside(17)、(+)-puerol B-2"-O-glucoside (18)、印度黄檀苷(19)、3’-甲氧基大豆苷元(20)、puerol B(21)、染料木素(22)、hydroxytuberosone(23)。结论:其中化合物10为首次从葛根中分离得到,研究结果丰富了葛根的化学成分。     

蒙古黄芪化学成分研究

目的研究蒙古黄芪的化学成分。方法采用硅胶柱色谱、凝胶柱色谱方法进行分离纯化,利用波谱分析法结合理化性质确定化合物结构。结果从蒙古黄芪的乙酸乙酯和正丁醇萃取部分中共分离得到14个化合物,分别鉴定为(6aR,11R)-9,10-二甲氧基紫檀烷-3-O-β-D-葡萄糖苷(1),(3R)-2′-羟基-3′,4′-二甲氧基异黄烷-7-O-β-D-葡萄糖苷(2),5′-羟基-3′-甲氧基异黄酮-7-O-β-D-葡萄糖苷(3),芒柄花苷(4),(6aR,11R)-3-羟基-9,10-二甲氧基紫檀烷(5),(3R)-7,2′-二羟基-3′,4′-二甲氧基异黄烷(6),5′,7-二羟基-3′-甲氧基异黄酮(7),芒柄花素(8),黄芪甲苷(9),黄芪皂苷II(10),蔗糖(11),腺嘌呤核苷(12),十六烷酸单甘油酯(13),十六烷酸(14)。结论化合物5,7,11～14为首次从黄芪属植物中分离得到,化合物6为首次从蒙古黄芪中分离得到。     

棉团铁线莲黄酮类成分研究

目的研究棉团铁线莲Clematis hexapetalaPall.的干燥根及根茎的化学成分。方法利用溶剂提取,硅胶柱色谱和高效液相色谱等手段进行分离、纯化,根据理化性质和波谱数据进行结构鉴定。结果分离鉴定了12个黄酮类化合物,分别为3,5,6,7,8,3′,4′-七甲氧基黄酮(1),nobiletin(2),liquiritigenin(3),橙皮素(4),柚皮素(5),7,4′-二羟基-二氢黄酮-7-O-β-D-葡萄糖苷(6),5,7,4′-三羟基-3′-甲氧基黄酮醇-7-O-α-L-鼠李糖(1→6)-β-D-葡萄糖苷(7),6-hydroxybiochainA(8),芒柄花素(9),大豆素(10),染料木素(11),鸢尾苷(12)。结论以上化合物均为首次从该植物中分离得到。     

高山大戟化学成分的研究

目的对藏药高山大戟的化学成分进行研究。方法利用各种柱色谱对其成分进行分离纯化,通过波谱解析进行结构鉴定。结果从中分离得到15个化合物,分别鉴定为:正二十八烷醇(1),十七烷酸甘油酯(2),正二十六烷醇(3),β-谷甾醇(4),β-胡萝卜苷(5),正十八烷醇(6),豆甾醇(7),芹菜素(8),没食子酸(9),荭草苷(10),槲皮素-4'-O-D-半乳糖(11),甘露醇(12),蔗糖(13),槲皮素-4′-O-β-吡喃葡萄糖苷(14)和木犀草素-5-O-β-D-葡萄糖苷(15)。结论所有化合物均为首次从该种植物中分离得到。     

土茯苓中2个新化学成分

采用大孔树脂柱色谱、硅胶柱色谱、凝胶色谱及半制备液相色谱分离技术,对土茯苓Smilax glabra Roxb.乙酸乙酯部位化学成分进行了系统的分离纯化。结合分离单体化合物的理化性质,通过MS、NMR和CD等波谱数据鉴定其结构。从土茯苓乙酸乙酯部位中分离得到20个化合物,包括10个黄酮(1、3～11)、8个酚类(2、12～18)和2个呋喃衍生物(19、20),分别鉴定为土茯苓苷A (1)、土茯苓酮A (2)、5-羟基-3′,4′,7-三甲氧基二氢黄酮(3)、柚皮素(4)、槲皮素7-O-α-L-鼠李糖苷(5)、新落新妇苷(6)、新异落新妇苷(7)、异落新妇苷(8)、圣草素-7-O-β-D-吡喃葡萄糖苷(9)、柚皮素-7-O-α-L-鼠李糖苷(10)、山柰酚3-O-[4′′′′′-O-乙酰基-α-L-鼠李糖基-(1→6)]-[β-D-吡喃葡萄糖基-(1→2)]-β-D-吡喃葡萄糖苷(11)、5-羟基麦芽酚(12)、3,4,5-三甲氧基苯基-1-O-β-D-吡喃葡萄糖苷(13)、2-(3′,4′-二羟基苯基)-1,3-苯骈二氧戊环-5-甲醛(14)、kompasinol A (15)、ica...     

蒲葵子化学成分研究

目的 研究蒲葵子Livistona chinesis的化学成分.方法 应用多种色谱技术进行分离纯化,根据化合物的理化性质和波谱数据鉴定化合物的结构.结果 从蒲葵子的70％乙醇提取物中分离得到15个化合物,分别鉴定为:苜蓿素(1),棕榈酸(2),油酸(3),十六碳酸乙酯(4),亚油酸乙酯(5),十六烯酸乙酯(6),菜油甾醇(7),胆甾醇-3-O-β-D-葡萄糖苷(8),荭草苷(9),异荭草苷(10),牡荆素(11),异牡荆素(12),异鼠李素-3-O-β-葡萄糖苷(13),谷甾醇(14),豆甾醇(15).结论 化合物4、6、8～13为首次从蒲葵子中分离得到,9、11、12为首次从棕榈科植物中分离得到.     

金银忍冬叶的化学成分研究

目的 研究金银忍冬叶Lonicera macckii (Rupr.) Maxim.的化学成分.方法 采用硅胶柱色谱、Sephadex LH-2柱色谱、重结晶等方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构.结果 从金银忍冬叶中分离鉴定了12个化合物,分别为山柰酚(1)、芹菜素(2)、金丝桃苷(3)、芹菜素-7-O-β-D-吡喃葡萄糖苷(4)、金圣草素-4′-O-β-D-葡萄糖苷(5)、木犀草素-7-O-β-D-吡喃葡萄糖苷(6)、裂环马钱素酸(7)、獐牙菜苷(8)、3,5-O-二咖啡酰基奎宁酸甲酯(9)、齐墩果酸(10),胡萝卜苷(11)、β-谷甾醇(12).结论 化合物1～6、8～12为首次从该植物中分离得到,化合物5为首次从该属植物中分离得到.     

赤胫散的化学成分研究

目的研究赤胫散的化学成分。方法利用多种色谱方法对赤胫散进行系统的化学成分研究,应用波谱学技术和理化常数对照等方法鉴定其结构。结果从赤胫散干燥根分离鉴定12个化合物:没食子酸(1);3,3′-二甲基鞣花酸(2);3,3′,4′-三甲基鞣花酸(3);3,3′-二甲基鞣花酸-4′-O-β-D-葡萄糖苷(4);3-甲基鞣花酸-4′-O-α-L-吡喃鼠李糖苷(5);3,3′-二甲基鞣花酸-4′-O-(6″-没食子酰基)-β-D-葡萄糖苷(6);短叶苏木酚(7);短叶苏木酚酸乙酯(8);短叶苏木酚酸(9);二十四烷酸(10);β-谷甾醇(11);β-胡萝卜苷(12)。结论化合物5,7,8,9,10和11为首次从该植物中分离得到。     

西红花花瓣化学成分研究

采用硅胶、制备HPLC等柱色谱方法对鸢尾科植物西红花(Crocus sativus L.)花瓣的化学成分进行分离,通过NMR、MS等波谱技术鉴定化合物结构,分离鉴定了9个化合物,分别为:苯乙醇-O-β-D-吡喃葡萄糖苷(1),苄醇-1-O-[6′-O-(S)-3′′-羟基-3′′-甲基戊二酸单酯]-β-D-吡喃葡萄糖苷(2),苯乙醇-1-O-[6′-O-(S)-3′′-羟基-3′′-甲基戊二酸单酯]-β-D-吡喃葡萄糖苷(3),4-羟基苯甲酸-4-O-α-L-吡喃鼠李糖-1-O-β-D-吡喃葡萄糖酯苷(4),4-羟基苯甲酸-4-O-β-D-吡喃葡萄糖苷(5),菠甾醇-3-O-β-D-吡喃葡萄糖苷(6),山柰酚(7),山柰酚-3-O-β-D-吡喃葡萄糖苷(8),山柰酚-7-O-β-D-吡喃葡萄糖苷(9).其中,化合物4为新化合物,化合物1～3,5～6均为首次从该植物中分离得到.体外活性初步评价了化合物1～9对皮质酮诱导PC12细胞损伤的保护作用,化合物2～5具有中等神经保护作用.     

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.     

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.     

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.