西沙海绵Agelas aff .nemoechinata化学成分研究△

目的 研究西沙海绵Agelas aff .nemoechinata的化学成分。方法 利用Sephadex LH-20凝胶色谱、硅胶色谱、ODS色谱、HPLC等手段对化学成分进行了分离纯化;通过理化性质,波谱分析方法结合文献对照,鉴定化合物的结构。结果 从南海海绵甲醇溶剂提取物中,分离鉴定了8个单体化合物：尿嘧啶(1)、胸腺嘧啶(2)、1-H-吡啶酮(3)、胸腺嘧啶-2’-脱氧核苷(4)、2-甲酰胺吡咯(5)、3-醛基吲哚(6)、6-羟基-4,4,7a-三甲基-5,6,7,7a-四氢苯并呋喃-2(2H)酮(7)、5-氨基戊酸(8)。结论 化合物1~8均为首次从该种海绵中分离得到。化合物7 在50 μg/mL_-1浓度水平,对K562白血病细胞株、P388白血病细胞株和HeLa肿瘤细胞株的抑制率分别是38.29%、23.23%和95.57%。     

一种西沙掘海绵Dysidea sp.的化学成分研究

目的 对西沙掘海绵Dysidea sp.进行化学成分研究;方法 运用正相硅胶柱色谱、反相ODS柱色谱、凝胶Sephadex LH-20柱色谱以及高效液相色谱(HPLC)等多种分离手段对西沙掘海绵Dysidea sp.化学成分进行分离纯化;并通过理化性质、波谱学数据等结构信息鉴定其化合物的结构。结果发现：从西沙掘海绵Dysidea sp.中分离鉴定了8个化合物,分别为dictyoceratin C（1）、dactyloquinone B（2）、aminoquinone（3）、dictyoceratin A（4）、dactyloquinone D（5）、dactyloquinone E（6）、(1R*,2E,4R*,7E,10S*,11S*,12R*)-10,18-diacetoxydolabella-2,7-dien-6-one（7）和?,?-unsaturated ester（8）,结论 化合物1?6和8均为首次从该属海绵中分离得到。     

西沙海绵Dysidea granulosa 化学成分研究

目的 研究中国西沙群岛海绵Dysidea granulosa的化学成分。 方法 利用薄层色谱、硅胶色谱、Sephadex LH-20色谱、MPLC、半制备HPLC等方法对化学成分进行分离纯化;通过NMR、MS等方法,并结合文献,鉴定化合物的结构。结果 从西沙海绵Dysidea granulosa的甲醇粗提取物中,分离得到6个化合物： Honulactone A (1), Honulactone B(2), Honulactone E (3), Honulactone F (4), 2-(2’,4’-Dibromophenoxy)-4,6-dibromophenol (5), 3,5-Dibromo-6-chloro-2-(2,4- dibromophenoxy)phenol (6)。结论 化合物1、2、3、4均为首次从该种海绵中分离得到。     

山莓化学成分研究

目的对山莓的化学成分进行研究。方法采用硅胶柱色谱、Sephadex-20柱色谱、重结晶,并经高效液相色谱等技术提取分离山莓的化学成分,用UV、IR、EI-MS、ES-MS及NMR等光谱方法鉴定化合物结构。结果从山莓乙醇提取物的石油醚部位分离得到化合物1～6,分别鉴定为豆甾醇(1)、β-谷甾醇(2)、胡萝卜苷(3)、Homofukinolide(4)、Bakkenolide-B(5)、Bakkenolide-D(6);从二氯甲烷部位分离得到化合物7～10,分别鉴定为4-羟基-3-甲氧基苯甲酸(7)、芹菜素(8)、木樨草素(9)、山莓素(10)。结论化合物4、5、6、7、8、9首次从山莓子中分离得到,化合物10是新化合物。     

鸡冠花子的化学成分研究

目的:分离鉴定鸡冠花子的化学成分。方法:采用硅胶柱色谱、Sephadex-20柱色谱、重结晶及制备高效液相色谱等技术提取分离鸡冠花子的化学成分,用UV、IR、EI-MS、ES-MS、1H-NMR、13 C-NMR、HMQC及HMBC等光谱方法鉴定化合物结构。结果:从鸡冠花子乙醇提取物的石油醚部位分离得到3个化合物,分别鉴定为棕榈酸(1)、对羟基苯甲醛(2)、齐墩果酸(3);从二氯甲烷部位分离得到6个化合物,分别鉴定为stigmast-5-en-3-ol,oleate(4)、4-羟基-3-甲氧基苯甲酸(5)、胡萝卜苷(6)、芹菜素(7)、木樨草素(8)、鸡冠花苷(9)。结论:化合物4～6首次从鸡冠花子中分离得到,化合物9是新化合物。     

中国南海群海绵Agelas mauritiana的化学成分研究

目的 对采自南中国海海域的群海绵(Agelas mauritiana)的化学成分进行研究。方法采用硅胶色谱柱、Sephadex LH-20凝胶色谱柱、高效液相色谱等色谱方法,对Agelas mauritiana正丁醇萃取物进行分离纯化;应用现代波谱技术对化合物进行化学结构鉴定;用MTT法对化合物进行体外人肺癌细胞株A549细胞生长抑制活性测试。结果 共分离得到8个化合物,分别鉴定为:agelasine A(1)、agelasine B(2)、epi-agelasine C(3)、(-)agelasine D(4)、agelasine E(5)、agelasine F(6)、(-)ageloxime D(7)、aurantiamide acetate(8)。体外活性筛选中,这些化合物对A549显示出不同程度的生长抑制活性,化合物1~3的活性与阳性对照阿霉素相近。结论 化合物1、2、4、5、6、8为首次从该种海绵中分离得到。首次选用A549对化合物1~7的活性进行评价,化合物2、3的显著生长抑制活性为进一步深入研究提供了依据。     

长柱金丝桃的化学成分研究

目的研究长柱金丝桃的化学成分。方法利用硅胶柱色谱、高效液相色谱等技术对长柱金丝桃甲醇提取物进行分离纯化,通过波谱数据分析鉴定其化学结构,利用噻唑蓝(MTT)法测试化合物抗肿瘤活性。结果从长柱金丝桃中共分离出10个化合物,均无抗肿瘤活性,分别鉴定为:isodauc-6-ene-10β,14-diol(1)、10-oxoisodauc-3-en-15-al(2)、10β-hydroxyisodauc-6-en-14-al(3)、artabotrol(4)、saniculamoid B(5)、1β-6α-dihydroxy-4(15)endesmene(6)、5-epi-eudesm-4(15)-eno-1β,6β-diol(7)、15-hydroxu-T-muurolol(8)、oplopanone(9)、larixol(10)。结论化合物1~10均为首次从该属植物中分离得到。     

北五味子藤茎化学成分的分离与鉴定

目的分离并鉴定北五味子藤茎的化学成分。方法采用硅胶柱色谱、凝胶柱色谱、氧化铝柱色谱和重结晶等多种分离方法,对北五味子藤茎体积分数为95%乙醇的冷浸提取物进行分离,并通过NMR等多种方法对分离得到的化合物进行结构鉴定。结果分离得到8个化合物,分别鉴定为(-)schisandrin B(1)、五味子醇B((+)-schizandrol B,2)、五味子素C((-)-schisandrinc,3)、五味子甲素((+)-deoxyschizandrin,4)、(+)-gomisin M1(5)、(-)-dihydroguaiaretic acid(6)、(-)-aus-trobailiguan6(7)、尿嘧啶(uracil,8)。结论化合物5~8为首次从北五味子藤茎中分离得到。     

中华隐孔菌子实体化学成分及细胞毒活性研究

目的 分离鉴定中华隐孔菌(Cryptoporus sinensis Sheng H. Wu &; M. Zang)子实体的化学成分。方法 采用硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱、HPLC 等分离方法,对中华隐孔菌子实体甲醇提取物的二氯甲烷萃取部分进行分离,根据理化性质和波谱数据鉴定化合物结构。采用MTT法对化合物进行细胞毒活性测定。结果 分离鉴定了4个已知的隐孔菌酸化合物,分别是隐孔菌酸B(1)、隐孔菌酸B甲酯(2)、隐孔菌酸G(3)、1,1″-二羧基隐孔菌酸D(4)。抗肿瘤活性筛选表明,化合物1~4具有弱的细胞毒活性,对肿瘤细胞PC-3、PANC-1、A549和MCF-7的半数抑制浓度大于100 µmol•L^-1。结论 化合物1~4 均是首次从该种真菌中分离得到。 关键词：中图分类号：     

中国南海海绵Haliclona baeri的化学成分研究

目的 对采自中国南海海域海绵Haliclona baeri 95 %乙醇提取物的乙酸乙酯部位的化学成分进行研究。方法 运用薄层色谱、正相Silica gel柱色谱、SephadexLH-20柱色谱以及HPLC等色谱分离手段;通过NMR、MS等波谱学方法,并结合文献报道,鉴定化合物的结构。结果 从海绵H. baeri中分离并鉴定了5个吲哚生物碱,分别为：(1H-indol-3-yl) oxoacetamide (1)、1H-indole-3-acetamide (2)、1H-indole-3-ethylethanoate (3)、1H-indole-3-carboxylic acid ethyl ester (4)和1H-indole-3-carboxylic acid (5)。结论 化合物1-4为首次从该属海绵中分离得到。对化合物1进行生物活性测试,该化合物没有表现出明显的细胞毒、抗核因子κB、抗菌、抗病毒和抗污损活性。     

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.     

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.     

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.