短刺海马的化学成分研究

目的:研究短刺海马的化学成分。方法:采用乙醇提取和硅胶柱色谱、Sephadex LH-20柱色谱等手段对样品进行分离纯化,再通过波谱分析并结合文献对照,鉴定化合物的结构。结果:从短刺海马乙醇提取物中分离得到9个化合物,经鉴定为胆甾醇(1)、胆甾-4-烯-3-酮(2)、3β,5α,9α-三羟基-(22E,24R)-麦角甾-7,22-二烯-6-酮(3)、24-甲基-5α-胆甾-7,22-二烯-3β,5,6β-三醇(4)、3β-羟基-7-甲氧基-胆甾-5-烯(5)、3β-羟基-胆甾-5-烯-7-酮(6)、肌酸酐(7)、鸟嘧啶(8)、腺嘌呤(9)。结论:9个化合物均为首次从短刺海马中分离得到。该结果可为短刺海马的合理利用和进一步产品开发奠定物质基础。     

扁小尖柳珊瑚Muricella sibogae化学成分研究

目的研究海洋动物扁小尖柳珊瑚Muricella sibogae的化学成分。方法采用硅胶柱色谱、Sephadex LH-20柱色谱、HPLC等手段对化合物进行分离纯化;利用理化性质和波谱分析方法,结合文献鉴定化合物的结构。结果从扁小尖柳珊瑚甲醇提取物中分离得到5个甾体化合物胆甾醇(1)、24-甲基-胆甾-5,22-二烯-3β-醇(2)、胆甾-5,22-二烯-3β-醇(3)、麦角甾-5,24(28)-二烯-3β-醇(4)、(Z)-豆甾-5,24(28)-二烯-3β-醇(5),2个二萜化合物13-去乙酰氧基calicophirin B(6)和Ophirin(7)。结论化合物1～7均为首次从该种柳珊瑚中分离得到。     

中国南海花刺柳珊瑚化学成分研究

目的研究花刺柳珊瑚Echinogorgia flora的化学成分。方法利用硅胶色谱、Sephadex LH-20、凝胶色谱、HPLC等手段对化学成分进行了分离纯化;通过理化性质,波谱分析结合参考文献,鉴定化合物的结构。结果从花刺柳珊瑚的甲醇氯仿混合溶剂提取物中,分离鉴定了15个单体化合物:(22E)-5α,8α-过氧化麦角甾-6,22-二烯-3β-醇(1),5α,8α-过氧化麦角甾-6-烯-3β-醇(2),(24E)-5α,8α-过氧化麦角甾-24-乙基-6,24-二烯-3β-醇(3),(22E)-5α,8α-过氧化麦角甾-24-乙基-6,22-二烯-3β-醇(4),(22E)-5α,8α-过氧化麦角甾-23-甲基-6,22-二烯-3β-醇(5),5α,8α-过氧化麦角甾-24-甲基-6,9(11),22-三烯-3β-醇(6),6-甲氧基-胆甾-7-烯-3β,5α-二醇(7),(22E)-24-乙基-胆甾-7,22-二烯-3β,5α,6β-三醇(8),24-亚甲基-胆甾-3β,5α,6β-三醇(9),(22E)-胆甾-7,22-二烯-3β,5α,6β-三醇(10),胆甾-5-烯-3β,7α-二醇(11),胆甾醇(12),24-亚甲基胆甾醇(13),丁烯酸内酯(14),N-2-(1,3-二羟基-4,8-十八二烯基-)-十六酰胺(15)。结论化合物(1-15)均为首次从该种柳珊瑚中得到。     

海洋真菌zp6次级代谢产物及其抗真菌活性研究

目的对海洋真菌zp6发酵液的乙酸乙酯萃取部分及其抑菌活性进行研究。方法采用硅胶柱色谱及高效液相色谱进行分离纯化,根据理化性质及各种光谱技术进行结构鉴定,采用滤纸片法对分离到的化合物进行抑菌活性研究。结果从该菌中分离纯化得到8个化合物:(22E)-3β,5α,9α-三羟基-麦角甾-7,22-二烯-6-酮(1)、5α,8α-环二氧-24-甲基麦角甾-6,22-二烯-3β-醇(2)、赤藓糖醇(3)、腺嘌呤核苷(4)、(24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇(5)、阿拉伯醇(6)、(7)、4-乙酰氧基苯甲酸(8)。结论化合物1和5具有抗真菌活性。     

中国南海聚裂丛柳珊瑚化学成分研究

目的研究聚裂丛柳珊瑚Rumphella aggregata的化学成分。方法利用硅胶色谱、Sephadex LH-20凝胶色谱、HPLC等手段对化学成分进行分离纯化;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。结果从聚裂丛柳珊瑚甲醇提取物中,共分离鉴定了15个单体化合物:胆甾醇(1)、(22E)-胆甾-5,22-二烯-3β-醇(2)、(22E)-麦角甾-5,22-二烯-3β-醇(3)、麦角甾-5,24(28)-二烯-3β-醇(4)、豆甾-5,24(28)-二烯-3β-醇(5)、柳珊瑚甾醇(6)、胆甾-7-烯-3β,5α,6β-三醇(7)、(22E)-胆甾-7,22-二烯-3β,5α,6β-三醇(8)、麦角甾-7-烯-3β,5α,6β-三醇(9)、(22E)-麦角甾-7,22-二烯-3β,5α,6β-三醇(10)、豆甾-7-烯-3β,5α,6β-三醇(11)、(22E)-豆甾-7,22-二烯-3β,5α,6β-三醇(12)、尿嘧啶(13)、咖啡因(14)、hydratoperidinin(15)。结论化合物1～15均为首次从该属柳珊瑚中分离得到,并首次对化合物hydratoperidinin(15)的1HNMR及13 CNMR信号进行了全归属。化合物12在10μg.mL-1浓度水平,对K562肿瘤细胞株的抑制率为39.17%。     

海洋真菌Rhizopus sp.菌丝体中化学成分的研究

目的对海洋真菌Rhizopus sp.菌丝体的丙酮和甲醇萃取部分进行化学成分的研究.方法采用硅胶柱色谱、凝胶柱色谱、高效液相色谱等手段,利用理化和波谱分析方法,对海洋真菌Rhizopus sp.菌丝体中的化合物进行分离鉴定.结果与结论从该真菌菌丝体中分离得到6个化合物.经光谱数据分析,鉴定其结构为5α,8α-过氧麦角甾-6,22-二烯-3β-醇(1)、1-O-9(Z)-十八碳烯酰甘油酯(2)、麦角甾-7,22-二烯-3β,5α,6β-三醇(3)、麦角甾-8(9),22-二烯-3β,5α,6β,7α-四醇(4)、戊五醇(5)、尿素(6).这些化合物均为首次从该真菌菌丝体中分离得到.     

短指软珊瑚中的生态活性物质

目的研究南海短指软珊瑚（Sinulariasp．）的生态活性物质。方法利用硅胶柱色谱、SephadexLH-20及HPLC等层析手段,对短指软珊瑚粗提物进行分离纯化,应用现代波谱技术（NMR、MS等）鉴定化合物结构。结果从该珊瑚中分离鉴定了7个甾醇类化合物,分别是：麦角甾-7,24（28）·二烯-3β,5β,6β-三醇（1）,（24R）麦角甾7,22二烯-3β,5β,6α-三醇（2）,麦角甾-24（28）-烯-3B,5α,6β-三醇（3）,（24S）-24-甲基-麦角甾-7-烯-3β,5α,6β三醇（4）,23-去甲基柳珊瑚甾-7-烯。3β,5α,6β-三醇（5）,过氧化麦角甾醇（6）,胆甾醇（7）。结论除海洋无脊椎动物中常见的胆甾醇和过氧化麦角缁醇外,这些化合物均为具有3β,5α,6β-三羟基结构片段的麦角甾醇类似物。初步的体外活性测试实验表明这些化合物对细菌、真菌和藻类有不同程度的抑制作用。     

沐浴角骨海绵的化学成分研究（Ⅰ）

首次报道运用波谱及GC-MS等方法从沐浴角骨海绵(Spongia of ficinalis L)中分离鉴定出8个单羟基甾醇化合物。1 22,23-甲撑基胆甾-5,7-二烯-3β-醇,2胆甾-5,7-二烯-3β-醇,3胆甾-5,7,25-三烯-3β-醇,4豆甾-5-烯-3β-醇,5豆甾-7,16,25-三烯-3β-醇,6豆甾-5,7,22-三烯-3β-醇,7麦角甾-5,7-二烯-3β-醇,8(22-E)麦角甾-7,22-二烯-3β-醇。     

海绵共附生真菌Purpureocillium lilacinum的化学成分及T细胞调节活性研究

目的 对海绵Hymeniacidon sp.共附生真菌Purpureocillium lilacinum的化学成分及T细胞调节活性进行研究。方法 运用硅胶柱色谱、凝胶柱色谱及高压液相色谱等色谱技术对真菌乙酸乙酯粗提物进行分离纯化得到单体化合物,通过现代波谱（核磁共振,质谱）及光谱（旋光）的综合运用并结合文献对照对化合物结构进行鉴定,运用流式实验对化合物T细胞调节活性进行测试。结果 共分离获得5个甾体化合物,鉴定为(24R)-豆甾-4-烯-6β-醇-3-酮（1）、(22E,24R)-麦角甾-7,22-二烯-3β,5α,9α-三醇-6-酮（2）、(22E,24R)-麦角甾-7,22-二烯-3β,5α-二醇-6-酮（3）、麦角甾-5,24-二烯-3β-醇-7,23-二酮（4）及(22E,24R)-麦角甾-5,8,22-三烯-3β-醇-7-酮（5）。体外活性筛选实验中,化合物2~5在2.5 μmol/L时对刀豆蛋白A（ConA）诱导的T细胞增殖显示抑制活性,化合物5在10 μmol/L时对CD3+T细胞的增殖显示显著抑制活性,所有受试化合物对CD4+/CD8+ T细胞分化活性均无影响。结论 化合物1~4为首次从P. lilacinum中分离获得。本文是对化合物1~5 T细胞调节活性的首次报道。     

中国南海短指软珊瑚化学成分研究

目的研究短指软珊瑚Sinulariasp.的化学成分。方法利用硅胶色谱、Sephadex LH-20凝胶色谱、HPLC等手段对化学成分进行分离纯化;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。结果从短指软珊瑚甲醇提取物中,共分离鉴定了11个单体化合物:胆甾醇(1)、(22E)-麦角甾-5,22-二烯-3β-醇(2)、胆甾-5,20-二烯-3β-醇(3)、麦角甾-5,24(28)-二烯-3β-醇(4)、柳珊瑚甾醇(5)、3β-羟基胆甾-5-烯-7-酮(6)、3β-羟基麦角甾-5,24(28)-二烯-7-酮(7)、(22E)-3β-羟基麦角甾-5,22-二烯-7-酮(8)、3β-羟基麦角甾-5-烯-7-酮(9)、(22E)-3β-羟基胆甾-5,22-二烯-7-酮(10)、鲨肝醇(11)。结论化合物6～10为首次从该属软珊瑚中分离得到。化合物7在10μg.mL-1浓度水平,对K562肿瘤细胞株的抑制率为22.74%,对HeLa肿瘤细胞株的抑制率为9.98%。     

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.