马尾松松针抗血小板聚集活性的成分考察

目的：研究马尾松松针体外抗血小板活性的成分。方法：利用活性跟踪分离方法和大孔吸附树脂（diaion HP-20）、葡聚糖凝胶（toyopearl HW-40）、反相硅胶（0DS）及硅胶柱色谱进行分离纯化，根据化合物的理化性质和光谱数据鉴定结构。结果：从马尾松松针60％乙醇提取物的醋酸乙酯萃取部位分离得到3个具有体外抗血小板聚集活性的化合物，分别鉴定为：木犀草素-7-O-吡喃葡萄糖苷（Ⅰ）、阿魏酸（Ⅱ）和槲皮素（Ⅲ）。结论：松针提取物的体外抗血小板聚集活性的物质基础是黄酮等多酚类化合物，而非之前所预期的大量存在于该植物中的木脂素类和原花青素类化合物。     

松针叶绿素-胡萝卜素软膏的体外抗甲型流感病毒作用研究

目的 观察松针叶绿素-胡萝卜素软膏的体外抗甲型流感病毒作用.方法 接种甲型流感病毒于狗肾传代细胞(MDCK),评价松针叶绿素-胡萝卜素软膏的细胞毒性及体外抗病毒作用.结果 松针叶绿素-胡萝卜素软膏对MDCK细胞的半数中毒浓度(TC50)为56 μg· mL-1,治疗和预防给药方式均有抗甲型流感病毒作用,半数抑制浓度(IC50)分别为30、29μg·mL-1,治疗指数(TI)均为1.9.结论 松针叶绿素-胡萝卜素软膏具有明显的抗流感病毒作用,且在安全浓度范围内呈现一定的量效关系,浓度越高抗病毒作用增强.     

松针提取物毒性研究

松针属于松科植物尾松的针状叶。松针主要含挥发油、黄酮类、树脂,并含有丰富营养成分,具有良好的保健和药用价值。我们对松针提取物的急性毒性和遗传毒性进行了初步研究,结果作如下简要报导。 小鼠急性毒性试验,经口LD_(50)大于10/kg,属于实际无毒类物质。     

松属植物化学成分研究进展

松属植物品种较多,化学成分复杂。该文综述了近年国内外对松属植物松塔、松树皮、松针中化学成分的研究,以期为松属植物的进一步开发利用提供参考。     

治疗睡眠障碍、焦虑新药——脑宁糠浆

“脑宁糖浆”是以松针为主要成分的新制剂。松针别名松毛,系松科松属植物马尾松pinus ma-ssoniana lambert的新鲜松针叶.松针主含有松香酸、挥发油α蒎、β蒎、莜、黄酮、檞皮素、山李酚、树酯烃、乙酸龙脑脂(bornylacetate)、维生素A、维生素C、胡萝卜素及维生素B_1、维生素B_2、维生素E和K等.松针苦温、无毒主治风湿、疮痈肿毒、生发、安五脏、守中、延年.多种资料记载松针有治疗失眠、神经衰弱、养心安神、养肝明目以及补血活血的作用。以松针为主要原料制成的脑宁糖浆毒性低,对中枢神经系统有镇静作用为一种有效的安眠镇静药。     

红松松针化学成分的分离与鉴定

目的研究红松松针的化学成分,为松属植物的化学分类学研究提供依据。方法采用反复硅胶、聚酰胺、ODS、Sephadex LH-20柱色谱等方法进行分离纯化,根据理化性质和1H-NMR、13C-NMR等技术对分离得到的化合物进行结构鉴定。结果从红松松针中分离得到10个化合物,分别鉴定为epirhododendrin(1)、(+)-rhododendrol(2)、覆盆子酮(frambinone,3)、massonianoside E(4)、松脂醇(pinoresinol,5)、罗汉松脂醇(matairesinol,6)、bornylp-coumarate(7)、salicifoliol(8)、β-谷甾醇(β-sitosterol,9)、胡萝卜苷(daucosterol,10)。结论化合物1和8为首次从松属植物中分离得到,2~7为首次从红松松针中分离得到。     

松针临床应用及药理研究概况

松针(Pine needles)为松科松属植物的针状叶。别名:猪鬃松毛、松毛、山松须。其植物来源主要有西伯利亚红松(Pinus sibirica(coud)Mayr),黑松(Pinus thunbergii Parl),油松(Pinus tabrleaformis Carr),红松(Pinus koraiensis sieb et Zucc),华山松(Pinus armandii Franch),云南松(Pinus yun naenis Franch),马尾松(Pinus massoniana Lamb)等。松香、松实、松针历代均入药用。松针,其味苦、性温,归心、脾     

马尾松不同部位莽草酸含量分析

目的:测定马尾松不同部位的莽草酸含量,为其合理开发利用提供参考.方法:采用反向离子对高效液相色谱法测定马尾松不同部位的莽草酸含量.结果:马尾松嫩松针的含量最高,其次为马尾松的较老松针、老松针和枝,老皮含量最低.结论:马尾松的嫩松针、较老松针具有较高开发价值.     

雪松松针的化学成分及药理作用研究概述

松针(Pine needle)系松科(Pinaceae)松属(Pinus)植物的叶,别名猪鬃松叶、松毛,始载于《名医别录》列为上品,历代本草中均有记载,明代李时珍《本草纲目》云:"松针,气味苦、温、无毒,久服令人不老,轻身益气,主风湿疮,生毛发,安五脏,守中,不饥延年"。雪松是松科Pianaceae雪松属CedrusTrew植物的统称,该属共有4种,大西洋雪松(C.atlantica)、短叶雪松(C.brevifolia)、喜马拉雅雪松(C.deodara)和黎巴嫩雪松(C.libani),均为高大乔木,原产于地中海、喜     

松针叶绿素-胡萝卜素膏对HP定植的胃溃疡大鼠的作用

目的研究松针叶绿素-胡萝卜素膏对HP定植的乙醇烧灼型胃溃疡大鼠的作用。方法采用幽门螺杆菌多次重复感染乙醇烧灼型胃溃疡大鼠,造成HP感染相关的胃溃疡模型,然后再给药。取血清和胃组织等样本,检测不同处理组溃疡指数及血清和胃组织中的超氧化物歧化酶(SOD)、丙二醛(MDA)、前列腺素E2(PGE2)以及胃泌素(GAS)等指标的含量,观察松针叶绿素-胡萝卜素膏的抗胃溃疡作用。结果松针叶绿素-胡萝卜素膏能有效抑制此种胃溃疡模型,可能机制是增强SOD、PGE2的活性,同时抑制MDA、GAS的活性。结论松针叶绿素-胡萝卜素膏对HP定植的乙醇烧灼型胃溃疡具有治疗作用。     

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.     

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.