中国沙棘果实的化学成分及其体外抗氧化活性研究

目的 研究中国沙棘果实的化学成分,并测定部分化学成分体外活性.方法 采用95%乙醇渗滤提得总浸膏,经溶剂萃取及柱层析分离,采用化学及光谱方法进行结构鉴定,并对小鼠视网膜色素上皮细胞(RPE)建立H2O2损伤模型,使用3种单体与细胞共孵育,进行MTT检测分析.结果 分得3个新化合物,分别鉴定为异鼠李素-3-O-β-D-(6-O-反式芥子酰基)槐二糖-7-O-α-L-鼠李糖苷(Ⅰ)、山柰素-3-O-β-D-(6-O-反式芥子酰基)槐二糖-7-O-α-L-鼠李糖苷(Ⅱ)和槲皮素-3-O-β-D-(6-O-反式芥子酰基)槐二糖-7-O-α-L-鼠李糖苷(Ⅲ).化合物Ⅲ对RPE有抗氧化活性,化合物Ⅰ则无,槲皮素活性最强.结论 研究结果可为中国沙棘的临床应用提供理论依据.     

多茎委陵菜中的黄酮苷类成分

目的研究多茎委陵莱（Potentilla multicaulis Bunge）中的化学成分。方法多茎委陵菜的70％乙醇提取物经大孔吸附树脂、硅胶柱层析、ODS柱层析及凝胶柱层析,采用化学及光谱学方法进行结构鉴定。结果分离纯化得到5个黄酮苷类化合物和1个挥发油。分别为翻白叶苷A（Ⅰ）、槲皮素-3-Oα-L-鼠李糖苷（Ⅱ）、槲皮素-β-O-β-D-葡萄糖苷（Ⅲ）、山柰酚-3-β-D-葡萄糖苷（Ⅳ）、异鼠李素-3-O-β--D-吡喃葡萄糖-7-O-α-L-吡喃鼠李糖苷（Ⅴ）、邻苯二甲酸二（2-乙基己基）酯（Ⅵ）。结论化合物Ⅰ-Ⅳ,Ⅵ均为首次在该植物中分离得到,化合物Ⅴ为首次从委陵菜属植物中分离得到。     

刺五加叶中黄酮类成分的分离与鉴定

目的分离、鉴定刺五加叶提取物中的化学成分。方法采用硅胶柱、ODS开放柱和制备液相等色谱方法分离,并通过NMR和MS等谱学技术确定结构。结果从提取物中分离得到9个黄酮类化合物,分别鉴定为异鼠李素-3-O-刺槐二糖苷(isorhamnetin-3-O-robinobioside,1)、山柰酚-3-O-刺槐二糖苷(kaempferol-3-O-robinobioside,2)、金丝桃苷(hyperin,3)、异鼠李素-3-O-β-D-半乳糖苷(isorhamnetin-3-O-β-D-galactopyranoside,4)、异鼠李素-3-O-β-D-鼠李糖基-(1→6)-[α-L-鼠李糖基-(1→2)]-β-D-半乳糖苷(isorhamnetin-3-O-α-L-rhamnopyranosyl-(1→6)-[α-L-rhamnopyranosyl-(1→2)]-β-D-galactopyr-anosid,5)、山柰酚-3-O-α-L-鼠李糖基-(1→2)-β-D-葡萄糖苷(kaempferol-3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside,6)、槲皮素-3-O-α-L-阿拉伯糖基-(1→2)-β-D-半乳糖苷(quercetin-3-O-α-L-arabinopyaranosyl-(1→2)-β-D-ga-lactopyranoside,7)、槲皮素(quercetin,8)山柰酚(kaempferol,9)。其中化合物1、2、4-7为首次从五加属植物中分离得到。结论     

甘草叶中酚酸和黄酮甙类成分的分离鉴定

自甘草(Glycyrrhiza uralensis Fiseh)的干燥叶中分离到7个甙类成分,经化学方法和光谱分析确定结构为原儿茶酸-1-O-β-D-呋喃木糖酯甙(1-O-protocatechuyl-β-D-xylopyranose,Ⅰ)、洋芹素-6,8-C-二葡萄糖甙(vicenin-2,Ⅱ)、异鼠李素-3-O-芸香糖甙(narcissin,Ⅲ)、山柰酚-3-O-芸香糖甙(nicotiflorin,Ⅳ)、山柰酚-3-O-β-D-葡萄糖甙(astragalin,Ⅴ)、槲皮素-3-O-芸香糖甙(rutin,Ⅵ)和槲皮素-3-O-β-D-葡萄糖甙(isoquercitrin,Ⅶ)。其中,Ⅰ是新化合物,命名为乌拉尔新甙(uralenneoside);Ⅲ在本属植物中为首次报道;Ⅲ～Ⅶ在乌拉尔甘草中首次分得。Ⅱ～Ⅶ都是已知活性成分。     

沙棘黄酮的化学成分及药理作用研究进展

目的:综述沙棘黄酮的化学成分及其药理作用,为其进一步研究和开发提供参考。方法:以"沙棘""沙棘黄酮""沙棘总黄酮""Hippophae rhamnoides L.""Sea buckthorn flavonoids""Total flavonoids of Hippophae rhamnoides L."等为关键词,组合查询2008年1月-2018年9月在中国知网、万方数据、维普网、中国生物医学文献服务系统(SinoMed)和PubMed等数据库中的相关文献,对沙棘黄酮的化学成分及药理作用进行归纳与总结。结果与结论:共检索到相关文献158篇,其中有效文献46篇。沙棘中的黄酮类化学成分含量较高,广泛存在于沙棘的果实、籽和沙棘叶中,主要有异鼠李素、槲皮素、山柰酚、杨梅素、芦丁、儿茶素等黄酮苷元及其苷类(如异鼠李素-3-O-β-D-葡萄糖苷、槲皮素-3-O-β-D-葡萄糖苷、山柰酚-3-O-芸香糖-7-O-鼠李糖苷等)。沙棘黄酮的药理作用包括抗血栓形成、降血脂、抗动脉粥样硬化、降血压、降血糖、增强免疫功能、抗肿瘤、抗菌、抗辐射等。但沙棘黄酮发挥的药理作用是基于单体化学成分还是多种化学成分联合作用目前并不明确,建议今后沙棘黄酮的研究工作可结合疾病发生的特点,多层次、多方位、多靶点深入探讨其作用机制和功效,以便更加有效地利用沙棘黄酮的活性成分。     

沙葱化学成分的分离与结构鉴定Ⅰ

目的对产自内蒙古阿拉善盟的百合科葱属植物沙葱的化学成分进行研究,为其在食品营养和药理活性方面的研究提供依据。方法采用大孔吸附树脂、Sephadex LH-20等柱色谱及制备型高效液相色谱法等手段对其化学成分进行分离、纯化,并结合化合物的理化性质与波谱学数据鉴定结构。结果从沙葱中分离鉴定了7个单体成分,分别为山柰酚-3-O-β-D-吡喃葡萄糖苷(1)、山柰酚-3-O-β-D-芸香糖苷(2)、山柰酚-3-O-β-D-吡喃葡萄糖基(1→4)-β-D-吡喃葡萄糖苷(3)、山柰酚-3-芸香糖苷-4'-吡喃葡萄糖苷(4)、山柰酚-3-O-芸香糖苷-7-O-葡萄糖醛酸苷(5)、山柰酚-3-O-β-D-吡喃葡萄糖基(1→4)[α-L-吡喃鼠李糖基(1→6)]-β-D-葡萄糖苷(6)、山柰酚-3-O-龙胆二糖苷-4'-O-β-D-吡喃葡萄糖苷(7)。结论化合物4、6、7为从葱属植物中首次分离得到,化合物1、2、3和5为首次从该植物中分离得到。     

天师栗种子中黄酮类成分的分离与结构鉴定

目的 对天师栗(Aesculus wilsonii Rehd.)干燥成熟种子中的黄酮类成分进行分离纯化,以期丰富其物质基础。方法 联合应用多种色谱学及波谱学技术对天师栗干燥成熟种子中的黄酮类化合物进行分离纯化和结构鉴定。结果 从体积分数70%乙醇提取物中分离得到了12个黄酮类化合物,分别为山柰酚-3-O-[β-D-木糖基-(1→2)]-β-D-葡萄糖苷(1)、山柰酚-3-O-[2-O-β-D-木糖基-6-O-α-L-鼠李糖基]-β-D-葡萄糖苷(2)、槲皮素3-O-α-L-鼠李糖苷(3)、槲皮素-3-O-木糖基(1→2)葡萄糖苷(4)、芦丁(5)、槲皮素-3-O-β-(2^G-O-β-木糖基-6^G-O-α-鼠李糖基)葡萄糖苷(6)、槲皮素-3-O-β-木糖基-(1→2)-β-葡萄糖基-3′-O-β-葡萄糖苷(7)、quercetin-3′-O-β-D-glucopyranosyl-3-O-rutinoside(8)、aescuflavoside(9)、槲皮素-3′-甲氧基-3-O-β-D-芸香糖苷(10)、(–)-表儿茶素-5-O-β-D-...     

郁金香黄酮葡糖醛酸苷对微血管的保护作用[英]／Budzianowski J…／／Phytother Res．-1999，13（2）．-166～168

郁金香是一种著名的观赏植物。研究发现它含有具较高药理活性的黄酮类化合物。曾对郁金香变种Tulipa gesneriana L.ver.paradae(TGP)花被的极性部位进行分离鉴定,得到了槲皮素和山柰酚的3-O-β-芸香糖苷-7-O-β-葡糖醛酸苷、槲皮素和山柰酚的3-O-β-龙胆二糖苷-7-O-β-葡糖醛酸苷以及槲皮素和山奈酚的3-O-β-葡糖苷-7-O-β-葡糖醛酸苷。     

岗松枝叶正丁醇萃取部位的化学成分

从岗松（Baeckea frutescens L.）枝叶正丁醇萃取部位分离鉴定了12个化合物，分别为：槲皮素（1），杨梅素（2），槲皮素3-O-α-L-吡喃鼠李糖苷（3），杨梅素3-O-α-L-吡喃鼠李糖苷（4），槲皮素3-O-α-L-呋喃阿拉伯糖苷（5），槲皮素3-O-β-D-吡喃木糖苷（6），槲皮素3-O-α-L-吡喃阿拉伯糖（7），槲皮素4′-O-β-D-吡喃葡萄糖苷（8），山柰酚 3-O-α-L-呋喃阿拉伯糖苷（9），山柰酚3-O-α-L-吡喃鼠李糖苷（10），myricetin 3-O-（2′′-O-galloyl）-α-L-rhamnopyranoside（11），myricetin 3-O-（3′′-O-galloyl）-α-L-rhamnopyranoside（12）。其中化合物5~12为首次从该植物枝叶中分离得到。     

白叶蒿的化学成分研究

目的:研究白叶蒿的化学成分。方法:对白叶蒿全草的70%乙醇提取物及其极性部位进行系统化学成分分离,采用硅胶、ODS RP-18、Sephadex LH-20等柱色谱方法进行分离,并根据化合物的理化性质和波谱数据鉴定其结构。结果:从乙酸乙酯和正丁醇部位分离得到11个化合物,分别鉴定为羽扇豆醇(1)、芹菜素(2)、木犀草素(3)、异鼠李素(4)、十七烷酸单甘油酯(5)、东莨菪内酯(6)、伞形花内酯(7)、山柰酚-3-O-鼠李糖苷(8)、山柰酚-3-O-葡糖苷(9)、山柰酚-3-7-二鼠李糖苷(10)、甘露醇(11)。结论:化合物1¹1均为首次从白叶蒿中分得。该试验结果可为白叶蒿活性成分的进一步开发及临床应用奠定基础。     

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.     

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.     

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.     

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.