瓜蒌化学成分的分离与鉴定

目的研究葫芦科栝楼属植物栝楼果实体积分数为90%乙醇提取物的正丁醇部分,对其中的化学成分进行分离鉴定。方法利用硅胶柱色谱,凝胶柱色谱(Sephadex LH-20),反相中低压柱色谱,制备高效液相色谱(PRE-HPLC)等手段进行分离纯化,根据理化性质和光谱数据对化合物进行了结构鉴定。结果从瓜蒌的正丁醇萃取部分分离得到10个化合物,分别鉴定为:甲基-β-D-吡喃果糖苷(methyl-β-D-frucopyranoside,1)、乙基-β-D-吡喃果糖苷(ethyl-β-D-frucopyranoside,2)、正丁基-β-D-吡喃果糖苷(n-butyl-β-D-fructopyranoside,3)、乙基-β-D-呋喃葡萄糖苷(ethyl-β-D-glu-cofuranoside4,)、正丁基-α-D-呋喃果糖苷(n-butyl-α-D-fructofuranoside5,)、正丁基-β-D-呋喃果糖苷(n-butyl-β-D-fructofuranoside,6)、bluemenol A(7)、cucumegastigmanesⅠ(8)、5-羟甲基糠醛(5-hydroxymethylfurfural9,)5、5,'-双氧甲基呋喃醛(5,5'-oxybis(methylene)difurfural1,0)。结论化合物1-8均为首次从该植物中分离得到。     

榆树根皮的化学成分（III）

目的研究榆树(Ulmus pumila L.)根皮中的化学成分。方法采用反复硅胶柱色谱法,凝胶柱色谱法,半制备HPLC等进行分离纯化;通过理化常数测定和光谱分析鉴定其化学结构。结果从榆树根皮正丁醇提取物中分离得到了6个化合物,即lyoniside(1)、(+)-lyoniresinol 3α-O-α-L-rh-amnopyranoside(2)、正丁基-O-β-D-吡喃果糖苷(n-butyl-O-β-D-fructopyranoside,3)、正丁基-O-α-D-呋喃果糖苷(n-butyl-O-α-D-fructofuranoside,4)、正丁基-O-β-D-呋喃果糖苷(n-butyl-O-β-D-fructo-furanoside,5)、胡萝卜苷(daucosterol,6)。结论化合物2-5为属内首次分离得到,化合物1为种内首次分离得到。     

黑果腺肋花楸幼苗的化学成分

目的对黑果腺肋花楸(Aronia melanocarpaElliot)幼苗乙醇提取物的化学成分进行研究。方法利用各种色谱技术进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果得到6个化合物,分别鉴定为:(-)表儿茶素(Ⅰ)、野樱苷(Ⅱ)、熊果苷(Ⅲ)、1,4二羟基2,6二甲氧基苯4OβD吡喃葡萄糖苷(Ⅳ)、正丁基αD呋喃果糖苷(Ⅴ)、正丁基βD呋喃果糖苷(Ⅵ)。结论化合物ⅡⅥ为首次从该属植物中分离得到。     

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.     

白蔹的化学成分研究

目的研究白蔹的化学成分。方法利用各种色谱法进行分离,根据理化性质和波谱分析鉴定化合物结构。结果从白蔹的氯仿和乙酸乙酯萃取部分又分离得到7个已知成分,分别鉴定为甲基-α-D-呋喃果糖苷(1)、甲基-β-D-吡喃果糖苷(2)、β-D-呋喃果糖甲苷(3)、β-D-呋喃果糖(4)、尿苷(5)、腺苷(6)、大黄素-8-O-β-D-吡喃葡萄糖苷(7)。结论化合物1、2、3、4、5、6为首次从该植物中分离得到。     

复方半边莲煎剂的化学成分研究

目的:研究复方半边莲煎剂的化学成分。方法:采用薄层色谱法、硅胶色谱法、凝胶柱色谱法对复方半边莲煎剂进行分离纯化,通过理化方法和波谱数据进行结构鉴定。结果:从复方半边莲煎剂中分离得到6个化合物,通过理化性质及波谱数据分析,分别鉴定为芹菜素-7-O-β-d-葡糖苷(1)、没食子酸(2)、木犀草素-7-O-β-d-葡糖苷(3)、橙皮苷(4)、正丁基-α-d-呋喃果糖苷(5)和正丁基-β-d-呋喃果糖苷(6)。结论:化合物1⁶均为首次从复方半边莲煎剂中分离得到。     

板栗种仁的化学成分(Ⅳ)

目的分离并鉴定板栗种仁的化学成分。方法采用硅胶柱色谱、凝胶柱色谱和重结晶等多种分离方法对板栗种仁的体积分数为95%的乙醇溶液回流提取物进行分离,并通过NMR、ESI-MS等多种谱学方法对分离得到的化合物进行结构鉴定。结果分离得到5个化合物,分别鉴定为(6S,9S)6-羟基-3-酮-α-紫罗兰醇-9-O-β-D-葡糖苷[(6S,9S)6-hydroxyl-3-oxo-α-ionol-9-O-β-D-glu-copyranoside,1]、(6S,9R)6-羟基-3-酮-α-紫罗兰醇-9-O-β-D-葡糖苷[(6S,9R)6-hy-droxyl-3-oxo-α-ionol-9-O-β-D-glucopyranoside,2]、5-羟基-2-羟甲基吡啶(5-hydroxyl-2-hydroxylm-ethylpyridine,3)、α-D-呋喃果糖甲苷(methyl-O-α-D-fructofuranoside,4)、正丁基-O-β-D-呋喃果糖苷(n-butyl-O-β-D-fructofuranoside,5)。结论这5个化合物均为首次从栗属植物中分离得到。     

合掌消的化学成分

目的研究萝科鹅绒藤属植物合掌消(Cynanchum amplexicaule Sieb.et Zucc.)的化学成分。方法利用各种色谱技术进行分离,根据光谱数据鉴定结构。结果从合掌消中分离得到5个已知成分,分别鉴定为descurainin(1)、saropeptate(2)、丁香脂素(3)、(-)-lyoniresinol 3α-O-β-D-glucopy-ranoside(4)和正丁基-β-D-吡喃果糖苷(5)。结论化合物1-5均为首次从该植物中分离得到。     

茶叶正丁醇萃取物化学成分的分离与鉴定

目的对茶叶正丁醇萃取物的化学成分进行研究,以进一步明确茶叶的化学成分。方法采用反复硅胶柱色谱、羟丙基葡聚糖凝胶柱色谱和重结晶等多种分离方法对茶叶体积分数70%乙醇回流提取物的正丁醇萃取物进行分离纯化,并根据理化性质和NMR谱数据对分离得到的化合物进行结构鉴定。结果分离得到10个化合物,分别鉴定为山柰酚(kaempferol,1)、槲皮素(quercetin,2)、山柰酚-3-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside,3)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,4)、山柰酚-3-O-芸香糖苷(kaempferol-3-O-rutinoside,5)、芦丁(rutin,6)、槲皮素-3-O-α-L-呋喃阿拉伯糖苷(quercetin-3-O-α-L-arabinofuranoside,7)、正丁基-β-D-吡喃果糖苷(n-butyl-β-D-fructopyranoside,8)、绿原酸甲酯(methyl chlorogenate,9)、尿嘧啶(u-racil,10)。结论化合物8~10为首次从山茶属植物中分离得到;化合物7为首次从植物茶中分离得到。     

狭叶荨麻地上部分化学成分的研究

目的研究狭叶荨麻地上部分的化学成分.方法利用多种色谱法进行分离纯化,通过理化性质和波谱数据分析进行结构鉴定.结果从狭叶荨麻地上部分分离并鉴定了7个化合物,分别为东莨菪素(I)、反式-4-羟基桂皮酸(Ⅱ)、5-羟甲基糠醛(Ⅲ)、正丁基-β-D-吡喃果糖苷(Ⅳ)、赤藓醇(V)、β-谷甾醇(Ⅵ)、胡萝卜苷(Ⅶ).结论7个化合物均首次从狭叶荨麻地上部分分离得到.     

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.