葛根正丁醇部位的化学成分研究

目的 研究葛根正丁醇萃取物的化学成分.方法 采用聚酰胺柱色谱、反相ODS柱色谱、凝胶柱色谱、制备液相色谱等方法进行分离纯化,根据化合物的理化性质及波谱数据鉴定其结构.结果 分离鉴定了12个化合物,分别为葛酚苷元A(1)、葛酚苷元B(2)、染料木素(3)、3′-甲氧基葛根素(4)、3′-羟基葛根素(5)、葛根素芹糖苷(6)、葛根素木糖苷(7)、大豆苷元(8)、大豆素7,4′-二葡萄糖苷(9)、大豆苷(10)、葛根素(11)、胡萝卜苷(12).结论 其中化合物1、2为首次从葛属植物中分离得到.     

葛根化学成分研究

摘要：目的:研究葛根化学成分。方法:通过大孔树脂、MCI柱以及制备型HPLC进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果:分离纯化得到23个化合物,分别为美佛辛-4’-O-葡萄糖苷(1)、3’-羟基葛根素芹菜糖苷(2)、大豆苷元-4’-葡萄糖苷(3)、葛根素芹菜糖苷(4)、大豆苷元-4’,7-二葡萄糖苷(5)、葛根素-6’’-O-木糖苷(6)、3’-羟基葛根素(7)、3’-甲氧基葛根素(8)、tuberosin(9)、毛蕊异黄酮苷(10)、葛根苷B(11)、葛根苷A(12)、3’-甲氧基大豆苷(13)、染料木素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷(14)、染料木苷(15)、刺芒柄花素(16)、formononetin-8-C-β-D-apiofuranosyl-(1→6)-O-β-Dglucopyranoside(17)、(+)-puerol B-2"-O-glucoside (18)、印度黄檀苷(19)、3’-甲氧基大豆苷元(20)、puerol B(21)、染料木素(22)、hydroxytuberosone(23)。结论:其中化合物10为首次从葛根中分离得到,研究结果丰富了葛根的化学成分。     

基于熵权逼近理想解排序法的西红花质量综合评价

目的 基于熵权逼近理想解排序(TOPSIS)法,综合评价不同产地西红花质量,为该药材的质量综合评价和优质产地筛选提供依据。方法 采用高效液相色谱(HPLC)波长切换法测定苦番红花素、西红花苷-Ⅰ、西红花苷-Ⅱ和西红花苷-Ⅲ含量,以4种成分总含量、干燥失重、总灰分、吸光度和浸出物作为评价指标,以熵权法计算各指标权重,结合TOPSIS法,对西红花质量进行综合评价。结果 熵权TOPSIS法分析结果显示,浙江、西藏、安徽、江苏、上海产西红花的相对贴近度(C_i)均值分别为0.654、0.396、0.426、0.326、0.341,浙江产西红花整体质量最佳。结论 建立的熵权TOPSIS法客观、全面、有效,可用于西红花质量综合评价。     

葛根异黄酮类成分的药理作用研究进展

葛根Pueraria lobata是药食同源中药,具有多种功效。现代药学研究表明异黄酮类是葛根的主要活性成分,已经分离到53个葛根异黄酮化合物,包括葛根素、大豆苷元、大豆苷、葛根素木糖苷、3''-羟基葛根素、染料木素、染料木苷、鹰嘴豆芽素A、芒柄花素、毛蕊异黄酮等,具有解酒护肝、降血糖、调血脂、缓解绝经性骨质疏松、抗肿瘤、心脏保护、抗炎、神经保护、抗氧化等药理作用。对葛根异黄酮类的药理作用进行综述,以期为该类成分的进一步研究和新药研发提供参考。     

脑得生片中10种成分的定量研究

目的建立HPLC法,对脑得生片中3′-羟基葛根素、葛根素、葛根素芹菜糖苷、3′-甲氧基葛根素、大豆苷、染料木苷、三七皂苷Rb_1、人参皂苷Rg_1、大豆苷元和人参皂苷Rb_1 10种有效成分进行定量分析。方法色谱条件:色谱柱为Kromasil C_(18)柱(250 mm×4.6 mm,5μm);流动相为乙腈-2.0 g·L~(-1)磷酸水溶液,梯度洗脱;流速为0.8 mL·min~(-1);检测波长为250和203 nm;柱温为35℃。结果 10个成分的峰具有良好的分离度;3′-羟基葛根素、葛根素、葛根素芹菜糖苷、3′-甲氧基葛根素、大豆苷、染料木苷、三七皂苷Rb_1、人参皂苷Rg_1、大豆苷元和人参皂苷Rb_1的线性范围分别为14.99～299.88,15.00～300.03,8.26～165.13,10.24～204.82,10.01～200.13,6.40～128.00,15.75～314.93,21.00～419.97,7.01～140.14和17.50～349.97μg·mL~(-1),相关系数分别为0.999 5,0.999 8,0.999 9,0.999 5,0.999 6,0.999 5,0.999 6,0.999 8,0.999 6和0.999 6;精密度、稳定性与重复性实验的RSD值均小于1.60%;10个对照品的加样回收率均在97.10%～98.48%之间,RSD值均在0.76%～1.56%之间;10批制剂中3′-羟基葛根素、葛根素、葛根素芹菜糖苷、3′-甲氧基葛根素、大豆苷、染料木苷、三七皂苷Rb_1、人参皂苷Rg_1、大豆苷元和人参皂苷Rb_1的平均含量分别为7.43,13.33,8.29,10.64,9.35,1.04,2.21,8.44,1.73和2.97 mg·g~(-1),RSD值分别为1.23%,0.82%,1.11%,1.24%,1.07%,1.58%,1.28%,0.86%,1.45%和1.28%。结论脑得生片中10种主要有效成分的含量检测方法操作简便、准确、可靠、稳定且重复性好,为该制剂的质量控制提供了有效的评价方法。     

野葛化学成分研究

目的研究野葛(Pueraria lobata)根的化学成分。方法利用溶剂提取,硅胶柱色谱和凝胶色谱等手段进行分离、纯化,根据理化性质和波谱数据进行结构鉴定。结果分离鉴定了14个化合物,分别为大豆苷元(1),芒柄花苷(2),大豆苷(3), 3′-甲氧基葛根素(4),葛根素(5),葛苷B(6),大豆苷元-8-C-芹菜糖基-(1-6)-葡萄糖苷(7), 3′-羟基葛根素(8),葛根素木糖苷(9),大豆苷元-7,4′-O-二葡萄糖苷(10),葛根素-4′-O-葡萄糖苷(11),美佛辛-4′-O-葡萄糖苷(12), sissotorin(13),葛苷C(14)。结论化合物11和13为首次从野葛的根中分离得到。     

粉葛资源产业化过程废弃物中的黄酮类化学成分分析

目的:研究粉葛采收及加工过程废弃物中黄酮类化学成分的组成和含量,为该品种资源的综合开发与合理利用提供依据。方法:以江西产粉葛品种"赣葛2号"为对象,采用超高效液相色谱-四极杆-飞行时间质谱和高效液相色谱技术分别检测葛根(带皮或去皮)、葛根皮、葛花、葛须根、葛茎、葛根头、葛根渣(带皮或去皮)以及沉淀葛粉后的工业废水(带皮或去皮)干物质中的黄酮类化学成分组成和含量。结果:所建立的7种黄酮类成分(葛根素、大豆苷、鸢尾黄素-7-O-木糖葡萄糖苷、染料木苷、鸢尾苷、大豆苷元、葛花苷)的含量测定方法的线性、精密度、重复性、稳定性、加样回收率均符合要求。共鉴定出12个黄酮类化学成分,其中葛根、葛根皮、葛茎、葛须根、葛根头、葛根渣和工业废水干物质中的黄酮类成分种类基本一致,主要为葛根素、大豆苷、染料木苷、大豆苷元、丙二酰基黄豆苷元;葛花中主要含有鸢尾黄素-7-O-木糖葡萄糖苷、染料木苷、鸢尾苷、葛花苷、6″-O-木糖基黄豆黄苷,但未检出葛根素、大豆苷及苷元等成分。葛根素含量以葛根头中最高,达5.765%;葛根、葛根渣及废水干物质各带皮样品中葛根素含量均较相应的去皮样品更高。结论:粉葛资源产业化过程的废弃物含有种类丰富、含量较高的黄酮类化合物,可作为获取葛根素等黄酮类化学成分的重要原料资源加以开发利用。     

正交试验-多元回归法优化葛根的乙醇提取工艺

目的 优化葛根药材中葛根素的提取工艺.方法 采用乙醇为溶媒提取葛根药材,以葛根素转移率和出膏率为指标,运用正交试验及多元回归分析多指标综合优化葛根药材的提取条件.结果 葛根提取的最佳条件为:90％乙醇提取两次,每次6倍量乙醇,提取时间为2h.葛根素的转移率为89.85％,浸膏得率为14.92％.结论 该数据处理方法优化葛根提取工艺结果准确、高效,具有一定的推广价值.     

维药小檗根传统切制工艺与产地趁鲜切制工艺的比较研究

目的: 探讨建立维药小檗根饮片的产地趁鲜切制工艺.方法: 采用HPLC法测定两种不同工艺切制小檗根饮片的小檗碱含量,测定不同工艺切制小檗根饮片的浸出物、炮制时间.结果:小檗根趁鲜切制饮片的小檗碱含量、浸出物的含量明显高于传统切制工艺切制饮片(36.9%、22.4%), 工艺周期由9 d缩短为3 d,小檗碱损失最大的工序是润药.结论:建议小檗根在产地加工时趁鲜洗净、切薄片、干燥.不仅解决了小檗根药材不易干燥,饮片加工炮制时软化时间长、有效成分容易流失的问题,而且降低了生产成本,保证了饮片质量的稳定.     

宁夏黄芩不同干燥方法与药材质量的相关性研究

目的研究宁夏栽培黄芩采用不同干燥方法进行产地加工时药材中4种化合物成分的变化规律,确定最佳产地加工干燥方法。方法采用HPLC法评价不同干燥方法的黄芩药材中4种化合物的含量。结果 80℃为最佳干燥温度。结论黄芩产地鲜切为最佳加工方法,即将黄芩鲜药材蒸30min后切片,置于烘箱中80℃烘干。其结果可为规范黄芩产地加工提供依据。     

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.     

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.