瑞香狼毒化学成分的研究

从瑞香狼毒 (StellerachamaejasmeL .)中分离得到 3个化合物 ,根据理化数据和NMR数据分别鉴定为S (+) 3 羟基 1,5 二苯基 1 戊酮 (1) ,西瑞香素 (2 )和 (- ) 7 甲氧基狼毒素 (3) .其中化合物 1为新化合物 ,化合物 3为首次分得的旋光纯的 7 甲氧基狼毒素     

瑞香狼毒化学成分研究(Ⅴ)挥发油化学成分研究

目的 通过对瑞香狼毒的化学组成进行分离,分别鉴定其化学成分.方法 所选取的方法为超声提取,乙醇提取,以及硅胶柱层析进行分析,通过IDNMR,2DNMR及MS方法来确定瑞香狼毒的组成结构.结果 分别得到5种化合物,通过对其光谱数据进行分析,确定这5种化合物分别为新瑞香素(I),-谷甾醇(II),伞形花内酯(III)、东莨菪素(IV)和胡萝卜苷(V).结论 其中为新天然产物的是化合物I,首次分离得到的为化合物3,即旋光纯的7-甲氧基狼毒素.     

抗肿瘤剂 LV:Genkwadaphnin 和 Yuanhuacine对P-388淋巴性白血病细胞核酸合成的影响

作者从芫花(Daphne genkwa)花的甲醇提取物分离得两个瑞香烷二萜酯的活性成份,分别为12-苯甲酰氧瑞香毒素(Genkwadaphnin,Ⅰ)和芫花酯甲(Yuanhuacine,Ⅱ)。根据Ⅱ的IR、~1H-NMR和~(13)C-NMR谱,作者认为,Ⅱ与后来报道的odoracin和gnidilatidin为同一化合物。     

狼毒的有效成分及其药理活性研究进展

狼毒是毒属植物瑞香科瑞香狼毒 (Stellera chamaejasmeL.)或大戟科狼毒大戟 (Euphorbia fischeriana Stued.)、月腺大戟 (Euphorbia ebracteolata Hayata.)的根 ,有逐水祛痰、散结杀虫之功效 ,为常用中药。近年的研究发现 ,狼毒提取物对肿瘤细胞有较强的抑制活性 ,此外还有抗菌和抗病毒作用 ,是一个理想的天然药物开发品种。1 　 化学成分研究1 .1　瑞香狼毒　六十年代初 ,我国的研究者从瑞香狼毒的根中分离出一种酸性物质 ,定为狼毒素 (chamaejamine) ,后来确定了其双氢双黄酮的结构。目前瑞香狼毒中已知的成分主要有倍半萜内酯、二萜生…     

瑞香狼毒中化学成分的结构鉴定

从瑞香狼毒的根茎中分离得到4个化合物,通过1H-NMR,13C-NMR及EI-MS,ESI-MS的数据分析,分别鉴定为1,5-二苯基-1-戊酮(I),1,5-二苯基-2-烯-1-戊酮(II),对羟基桂皮酸正二十二酯(III),咖酸正二十酯(IV),其中化合物I和II为新天然产物,化合物III和IV为首镒从该科植物中得到的桂皮酸衍生物与高级脂肪醇形成的酯.     

芫花花蕾中甾醇类化合物的分离与鉴定

目的对瑞香科瑞香属植物芫花(Daphne genkwa Sieb.et Zucc.)花蕾中的甾醇类化学成分进行分离与结构鉴定。方法运用硅胶﹑Sephadex LH-20柱色谱﹑重结晶等分离手段进行甾醇类化合物的分离纯化,根据理化性质及波谱数据鉴定其化学结构。结果从芫花花蕾的体积分数95%乙醇提取物中分离得到6个化合物,分别鉴定为:豆甾-5-烯-3β,7α-二醇(stigmasta-5-ene-3β,7α-diol,1)、豆甾-5-烯-3β,7β-二醇(stigmasta-5-ene-3β,7β-diol,2)、豆甾-4-烯-3β,6β-二醇(stigmasta-4-ene-3β,6β-diol,3)、7-ketositosterol(3β-hydroxysitost-5-ene-7-one,4)、过氧化麦角固醇(ergosterol peroxide,5)和β谷甾醇-3β-吡喃葡萄糖苷-6'-O-棕榈酸酯(β-sitosteryl-3β-glucopyranoside-6'-O-palmitate,6)。结论化合物2⁶为首次从瑞香属植物中分离得到,化合物1为首次从芫花植物中分离得到。     

瑞香毒素类化合物的化学及其生理作用

近几年来,陆续报道了一新类型的二萜类化合物——瑞香毒素(Daphnetoxin)类化合物,它们的含量很低,但具有很强的生理活性,引起了人们的注意。这些化合物都是从瑞香科或大戟科植物中分离出来。由于许多     

了哥王化学成分的分离与鉴定

目的对了哥王(Wikstroemia indical)根茎的化学成分进行研究。方法采用反复硅胶柱色谱、Sephadex LH-20凝胶柱色谱、制备薄层色谱等方法进行分离纯化,根据理化性质及波谱数据确定化合物的结构。结果从了哥王体积分数75%乙醇提取物的氯仿和乙酸乙酯萃取部分得到12个化合物,分别为胡萝卜苷(daucosterol,1)、16-妊娠双烯醇酮(16-dehydropregnenolone,2)、大黄素甲醚(physcion,3)、大黄酚(chrysophanol,4)、山柰酚(kaempferol,5)、芹菜素(apigenin,6)、槲皮素(quercetin,7)、西瑞香素(daphnoretin,8)、β-谷甾醇(β-sitosterol,9)、西瑞香素-7-O-β-D-葡萄糖苷(daphnoretin-7-O-β-D-glucoside,10)、triumbelletin(11)、伞形花内酯(umbelliferone,12)。结论化合物2是从瑞香科(Thymelaeaceae)植物中首次分离得到;化合物11是从荛花属(Wikstroemia)植物中首次分离得到。     

瑞香狼毒抗肿瘤作用实验研究进展

中药瑞香狼毒(stellerachamaejasmeL.,SC)为瑞香科植物瑞香狼毒的根[1],是药用狼毒的正品 ,因其主要分布在我国西北地区 ,故又被称为西北狼毒。狼毒用于治疗肿瘤在我国已有悠久的历史 ,本文拟就SC的抗肿瘤作用实验研究进展作一综述。1瑞香狼毒的水提物和醇提物的抗肿瘤研究1.1瑞香狼毒体外抗肿瘤作用以小鼠P388为靶细胞 ,研究瑞香狼毒和狼毒素的体外抗肿瘤作用 [2]。结果 ,瑞香狼毒水提物 (SCLA)显著抑制P388细胞生长 ,抑制率与药物浓度及处理时间呈正相关 ,即0.25～16g/L(相当生药 )SCLA处理24h ,细胞生长抑制率为2.8 %～88.4 % ;2g…     

芫花根醇提物中三个新的双黄酮类化合物

目的研究芫花根次生代谢产物的化学组成。方法芫花根以95％乙醇于60-70 ℃提取7 d。提取物以硅胶、Sephadex LH-20及HPLC等方法加以分离。分离产物以1D和2D NMR,MS,UV,IR及CD鉴定其结构。结果 从芫花根醇提物中分离出3个双黄酮,其结构被鉴定为毛瑞香素H-3-甲醚（1）、毛瑞香素H-3″-甲醚（2）和毛瑞香素G-3″-甲醚（3）。结论化合物1,2和3为新的双黄酮类化合物。     

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.