吉祥草甾体类化学成分研究

目的研究吉祥草甾体类化学成分。方法采用硅胶、Sephadex LH-20等色谱技术进行分离纯化,通过理化方法和波谱数据进行分析和结构鉴定。结果从吉祥草中分离鉴定了9个甾体类化合物,分别为薯蓣皂苷元(1)、奇梯皂苷元(2)、潘托落皂苷元(3)、β-豆甾醇(4)、β-豆甾醇-3-O-β-D-吡喃葡萄糖苷(5)、kitigenin 5-O-β-D-glucopyrannoside(6)、pentologenin 5-O-β-D-glucopyrannoside(7)、薯蓣皂苷元-3-O-β-D-吡喃葡萄糖苷(8)、25(S)-5β-1β-3β-diol(9)。结论化合物8和9为首次从该属植物中分离得到。     

绵萆薢中甾体成分的分离与结构鉴定Ⅰ

目的对绵萆薢中甾体类成分进行研究,为其在中医药及临床方面的研究提供依据。方法采用大孔吸附树脂、正相硅胶、反相ODS、Sephadex LH-20等柱色谱及制备型高效液相色谱等方法对其所含甾体类成分进行分离、纯化,并结合化合物的理化性质与波谱学数据鉴定结构。结果与结论从绵萆薢中分离鉴定了10个甾体,分别为薯蓣皂苷元(1,diosgenin)、薯蓣皂苷次级皂苷A(2,prosapogenin A of dioscin)、diosgenin 3-O-β-D-glucopyranosyl(1→3)-β-D-glucopyranoside(3)、薯蓣皂苷次级皂苷B(4,prosapogenin B of dioscin)、薯蓣皂苷(5,dioscin)、纤细皂苷(6,gracillin)、7-oxodioscin(7)、(3β,7β,25R)-spirost-5-ene-3,7-diol-3-O-β-D-glucopyranosyl-(1→3)-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside(8)、orbiculatoside B(9)、borassoside B(10)。化合物8和10为从薯蓣属植物中首次分离得到,化合物3、4、7为从该种植物中首次分离得到。     

丫蕊花的化学成分

从百合科丫蕊花属植物丫蕊花(Ypsilandra thibetica Franch)全草中分离鉴定了8个化合物,分别为:偏诺皂苷元(1),偏诺皂苷元-3-O-α-L-呋喃阿拉伯糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(2),偏诺皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(3),偏诺皂苷元-3-O-α-L-吡喃葡萄糖(1→4)-α-L-吡喃鼠李糖(1→4)-[α-L-吡喃鼠李糖(1→2)]-β-D-吡喃葡萄糖苷(4),薯蓣皂苷元(5),薯蓣皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(6),木犀草素(7),木犀草苷(8)。其中化合物1,2,5,7,8均首次在丫蕊花植物中分到。     

忍冬叶中黄酮类成分的分离与鉴定

目的为忍冬(Lonicera japonicaThunb.)叶中黄酮类化学成分药效学物质基础提供依据。方法采用反复硅胶柱色谱法、Sephadex LH-20柱色谱法等对忍冬叶进行分离纯化,并通过理化常数测定和波谱分析对分离得到的化合物进行结构鉴定。结果从忍冬叶75%乙醇提取物中分离得到7个黄酮类化合物,并鉴定其结构分别为5,7,4′-三羟基-8-甲氧基黄酮(5,7,4′-trihydroxy-8-me-thoxyflavone,1)、木犀草素(luteolin,2)、苜蓿素(tricin,3)、山萘酚-7-O-β-D-吡喃葡萄糖苷(kaempferol-7-O-β-D-glucopyranoside,4)、木犀草素-7-O-β-D-吡喃葡萄糖苷(luteolin-7-O-β-D-glu-copyranoside,5)、洋芹素-7-O-β-D-吡喃葡萄糖苷(apigenin-7-O-β-D-glucopyranoside,6)、香叶木素-7-O-β-D-吡喃葡萄糖苷(diosmetin-7-O-β-D-glucopyranoside,7)。结论化合物1、4为首次从忍冬属植物中分离得到,化合物3、6、7为首次从植物忍冬中分离得到。     

野菊花的化学成分

目的:研究菊科菊属植物野菊花(Chrysanthemum indicum L.)的化学成分.方法:采用硅胶柱层析、凝胶柱层析、重结晶等方法进行化学成分的分离与纯化,并运用核磁共振、质谱等波谱技术鉴定化合物的结构.结果:分离并鉴定了13个化合物:其中黄酮类9个,分别为金合欢素(acacetin,1)、木犀草素(luteolin,2)、芹菜素(apigenin,3)、异泽兰黄素(eupatilin,4)、麦黄酮(tricin,5)、5,7,3',4'-Tetrahydroxy-6,5'-dime-thoxyflavone(6)、芹菜素-7-O-β-D-葡萄糖苷(apigenin-7-O-β-D-glucopyranoside,7)、木犀草素-7-O-β-D-葡萄糖苷(luteolin-7-O-β-D-glucopyranoside,8)、蒙花苷(linarin,9);倍半萜类成分3个:cumambrin-A(10)、野菊花内酯(yejuhualactone,11)、7-(2-hydroxy-2-propyl)-10-methyl-4-methyleneperhydro-naphthalene-3,5,6-triol(12);甾体类成分1个:β-胡萝卜苷(β-daucosterol,13).结论:化合物4～7为该植物中首次分得,其中化合物5,6为该属植物中首次分得.     

绵萆薢中甾体类成分的分离与鉴定Ⅱ

目的对绵萆薢的化学成分进行研究。方法将大孔吸附树脂、硅胶、Sephadex LH-20、正相硅胶、ODS等柱色谱与制备型高效液相色谱法相结合进行化合物的分离制备,并通过理化性质与核磁共振波谱数据鉴定化合物的结构。结果从绵萆薢中分离鉴定了12个单体成分,分别鉴定为原薯蓣皂苷(protodioscin,1)、甲基原薯蓣皂苷(methyl protodioscin,2)、原纤细皂苷(protogracillin,3)、甲基原纤细皂苷(methyl protogracillin,4)、伪原薯蓣皂苷(pseudoprotodioscin,5)、伪原纤细皂苷(pseudoprotogracillin,6)、26-O-β-D-glucopyranosyl-3β,23,26-triol-25(R)-furosta-5,20(22)-dien-3-O-α-L-rhamnopyranosyl(1→4)-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside(7)、豆甾醇(stigmasterol,8)、β-谷甾醇(β-sitosterol,9)dioscoreavilloside A(10)、绵萆薢苷B(spongioside B,11)及粉背薯蓣G(hypoglaucin G,12)。结论在对绵萆薢的化学成分进行研究的过程中,分离鉴定了12个甾体类化合物。其中化合物5~8和10为首次从该种植物中分离得到,并首次对化合物7的核磁数据进行了报道。     

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.     

吉祥草中的一个新甾体皂苷(英文)

对吉祥草地上部分的化学成分进行研究。采用多种色谱手段进行分离纯化,得到单体化合物,通过理化性质及1D,2DNMR方法确定了化合物的结构。分离得到一个新的孕甾烷型甾体皂苷,命名为1α,3β-dihydroxy-5β-pregn-16-ene-20-one-1-O-αL-arabinosy1-(1→2)-α-L-rhamnoside。另鉴定了6个已知化合物,分别为β-香树脂醇(2),豆甾醇(3),α-菠甾醇-3-O-葡萄糖苷(4),柚皮素(5),β-谷甾醇(6),胡萝卜苷(7),其中化合物2,4,5为首次在该植物中分离得到。     

宽叶重楼化学成分研究

目的对重楼属植物宽叶重楼根茎的化学成分进行研究,为扩大重楼属植物的药用资源提供科学依据。方法采用硅胶柱层析,Sephadex LH-20及RP-C18等分离技术进行纯化单体化合物,根据理化性质及波谱数据鉴定其结构。结果从宽叶重楼根茎乙醇提取物的正丁醇部分中分离得到了7个化合物,分别为β-谷甾醇(1)、胡萝卜苷(2)、2-苯乙基-β-D-葡萄糖苷(3)、没食子酸(4)、芦丁(5)、偏诺皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-葡萄糖苷(6)、重楼皂苷Ⅶ(7)。结论 7个化合物均为首次从该种植物中分离得到,其中化合物3、4为首次从该属植物中分离得到。     

红背叶中酚酸类成分研究

为了研究红背叶的化学成分,采用硅胶、ODS、MCI以及Sephadex LH-20等柱色谱方法从红背叶根95%乙醇提取物中分离得到8个酚酸类成分,根据化合物的波谱数据分别鉴定为没食子酸-7-O-β-(6’-O-香草酰基)-葡萄糖苷(1)、没食子酸(2)、没食子酸乙酯(3)、丁香酸(4)、丁香酸葡萄糖苷(5)、3,5-二甲氧基-4-羟基苯甲酸-7-O-β-D-葡萄糖苷(6)、3,4-二甲氧基苯酚-1-O-α-L-鼠李糖-(1→6)-β-D-葡萄糖苷(7)和3,4,5-三甲氧基苯酚-1-O-β-D-(6’-O-没食子酰基)-葡萄糖苷(8)。其中化合物1为新化合物,化合物4～8为首次从山麻杆属植物中分离得到,其余化合物为首次从该植物中分离得到。     

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.