毛枝卷柏黄酮类成分的研究

目的对毛枝卷柏黄酮类化学成分进行系统研究。方法采用正相硅胶柱、Sephadex LH-20柱色谱以及半制备高效液相色谱等分离纯化方法,根据化合物的理化性质和光谱方法鉴定其结构。结果从毛枝卷柏70%乙醇提取物中分离得到5个化合物,分别鉴定为:4'-甲氧基穗花杉双黄酮(1)、穗花杉双黄酮(2)、7,4',7',4'-四甲氧基穗花杉双黄酮(3)、橡胶树双黄酮(4)和2,6,8-三甲基-5,7-二羟基色原酮(5)。结论化合物1~5均首次从毛枝卷柏中分离得到。     

卷柏化学成分研究

目的研究卷柏中的化学成分。方法利用色谱法对卷柏75%乙醇提取物中的化学成分进行分离。利用核磁共振、红外等方法对分离得到的单体化合物进行结构鉴定。结果从卷柏中分离得到6个化合物,分别是橡胶树双黄酮(1)、selaginellin(2)、selaginellin A(3)、穗花衫双黄酮(4)、十八烷酸(5)、β-谷甾醇(6)。结论其中化合物2为首次从卷柏中分离得到。     

江南卷柏中双黄酮类化学成分研究

目的 研究江南卷柏中的双黄酮类成分.方法 利用色谱法对江南卷柏75％醇提部分的化学成分进行系统分离纯化,利用理化性质及核磁共振图谱等手段对分离得到的单体化合物进行结构鉴定.结果 从江南卷柏中分离得到了5个化合物,分别为穗花杉双黄酮( ametoflavone,1),罗巴斯塔双黄酮-4 ’-甲醚(4’-O-methylrobustaflavone,2),穗花杉双黄酮-4 ’甲醚(4'-O-methylametoflavone,3),穗花杉双黄酮-7-甲醚(7-O-methylametoflavone,4),7,4'-二甲氧基穗花杉双黄酮(7,4 ’-di- O-methylametoflavone,5).结论 其中化合物4为首次从江南卷柏中分离得到.     

藏药香柏的化学成分研究

目的 研究香柏Sabina pingii(Cheng ex Ferre)var.wilsonii(Rehd.)Cheng et L.K.Fu枝叶的化学成分.方法 运用多种层析分离方法进行分离纯化,采用化学及光谱方法进行结构鉴定.结果 分离得到了6个化合物,并鉴定了其中4种,分别为海波拉亭-7-O-β-D-吡喃木糖苷(Ⅰ)、南方贝壳杉双黄酮(Ⅱ)、伞形花内酯(Ⅲ)和β-谷甾醇(Ⅳ).结论 化合物Ⅰ～Ⅳ均为首次从该种植物中分离得到.     

胡柚皮中化学成分的研究

目的:对胡柚皮中黄酮类成分进行研究.方法:采用硅胶柱色谱分离及重结晶的方法从胡柚皮中分离化合物,并根据理化性质和波谱数据进行化合物的结构鉴定.结果:分离并鉴定了五个黄酮类化合物,分别为:5-羟基-6,7,8,3',4'-五甲氧基黄酮(Ⅰ),5,6,7,8,4'-五甲氧基黄酮(Ⅱ),5,6,7,8,3',4'-六甲氧基黄酮(Ⅲ),5,6,7,3',4'-五甲氧基黄酮(Ⅳ),5-羟基-3,6,7,8,3',4'-六甲氧基黄酮(Ⅴ),结论:从该植物中分离鉴定了五个黄酮类化合物.     

忍冬叶的化学成分

目的研究忍冬(Lonicera japonica Thunb.)叶中的化学成分。方法采用反复硅胶柱色谱法、Sephadex LH-20柱色谱法等进行分离纯化,并通过理化常数测定和波谱分析鉴定了其化学结构。结果从忍冬叶的体积分数为75%的乙醇溶液提取物中分离得到4个化合物,并鉴定其结构为:似梨木双黄酮-7-O-β-D-吡喃葡萄糖苷(ochnaflavone,1)、似梨木双黄酮(ochnaflavone7-O-β-D-gluco-pyranoside,2)、次大风子素(hydnocarpin,3)、忍冬苷(lonicerin,4)。结论化合物2为一新化合物,化合物3,4为首次从该植物叶中分离得到。     

卷柏的化学成分

目的研究卷柏[Selaginella tamariscina(Beauv.)Spring]的化学成分。方法采用硅胶柱色谱、ODS柱色谱、制备型HPLC等手段进行分离纯化,并利用波谱学方法鉴定化合物的结构。结果从卷柏乙醇提取物中分离得到13个化合物,分别鉴定为3β-羟基-7α-甲氧基-24β-乙基-胆甾-5-烯(1)、胆甾醇(2)、β-谷甾醇(3)、海棠果酸(4)、白桦脂酸(5)、5,4′-二羟基-7-甲氧基黄酮(6)、3-methoxychrysazin(7)、穗花杉双黄酮(8)、异柳杉双黄酮(9)、香草酸(10)、对甲氧基苯甲醛(11)、对羟基苯甲酸(12)、胡萝卜苷(13)。结论化合物1-2、4-7、10、13为本属植物中首次分离得到的化合物。     

栽培曼地亚红豆杉针叶化学成分的分离与鉴定

目的对栽培于我国辽宁本溪的曼地亚红豆杉(Taxus media)针叶的化学成分进行研究。方法采用大孔树脂、硅胶柱色谱、ODS柱色谱、凝胶柱色谱及MDS柱色谱等方法进行分离纯化,通过NMR数据分析鉴定化学结构。结果从曼地亚红豆杉针叶的乙醇提取物中分离得到8个化合物,分别鉴定为二萜类化合物:紫杉宁(taxinine,1)、东北红豆杉素(taxacin,2)、紫杉欧吉酚(taxa-gifine,3)、2-去乙酰氧基紫杉宁J(2-deacetoxytzxinine J,4)、东北红豆杉素I5-O-桂皮酰基三乙酸酯(5-O-cinnamoyltaxacin I triacetate,5);黄酮类化合物:芹菜素(apigenin,6)、银杏双黄酮(ginkget-in,7)、金松双黄酮(sciadopitysin,8)。结论化合物2、5、7、8为首次从栽培曼地亚红豆杉针叶中分离得到。     

298红厚壳属植物Calophyllum panciflorum中具抗肿瘤促进作用的新双黄酮类化合物

作者曾从红厚壳属植物 C.panciflorumA.C.Smith(藤黄科)中分得新的双苯并呋喃化合物 calophyfuran 和两个新咄酮化合物pancixanthone A 和 B。在继续研究中从该植物茎皮的乙醇提取物中分到一个新双黄酮化合物 pancibiflavonol(1)和6个已知的双黄酮化合物。作者报道了化合物1的分离和鉴     

半枝莲的化学成分

目的对黄芩属植物半枝莲(Scutellaria barbataD.Don)的抗肿瘤活性部位(氯仿萃取物和正丁醇萃取物)的化学成分进行分离、鉴定。方法用体积分数为70%的乙醇加热回流提取干燥药材,经石油醚、氯仿、正丁醇分步萃取,利用反复硅胶柱色谱、聚酰胺柱色谱、Sephadex LH 20凝胶柱色谱进行分离、纯化,根据理化性质和核磁共振氢谱、碳谱数据对所得化合物进行结构鉴定。结果得到8个化合物,分别鉴定为对羟基苯甲醛(1)、3,4二羟基苯甲酸(2)、对羟基苯乙酮(3)、5,7,4′三羟基8甲氧基黄酮(4)、5,7,4′三羟基6甲氧基黄酮(5)、5,7,4′三羟基黄酮(6)、5,4′二羟基6,7,3′,5′四甲氧基黄酮(7)、5羟基4′甲氧基黄酮7OαL鼠李糖基(1→6)βD吡喃葡萄糖苷(8)。结论化合物7、8为半枝莲中首次分离得到。     

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.