不同产地和生长年限川黄柏中小檗碱的含量测定

黄柏为著名的川产道地药材,始载于《神农本草经》,原名“蘖木”,列为上品,味苦,寒,无毒。黄柏的主要成分是生物碱,其中小檗碱具有抗菌、消炎等作用。《中国药典》2005年版第一部将川黄柏与关黄柏分别收载,黄柏即黄皮树(Phellodendron chinense Schneid．)的干燥树皮,习称“川黄柏”,具有清热燥湿、泻火除蒸、解毒疗疮等功能。为了提高黄柏的质量,保证临床用药的安全性、有效性、我们测定了四川三个产地与不同生长年限的黄柏中小檗碱的含量。     

TLC法和HPLC法分析关黄柏与川黄柏区别

目的:比较关黄柏和川黄柏的区别.方法:采用薄层色谱法定性鉴别盐酸小檗碱和盐酸巴马汀,高效液相色谱法对盐酸小檗碱进行定量分析.结果:关黄柏与盐酸巴马汀对照品有相应位置的斑点,而川黄柏则无.川黄柏中所含盐酸小檗碱高于关黄柏3~4倍.结论:关黄柏与川黄柏在有效成分及其含量上有显著区别.     

黄柏的化学成分和药理作用研究

黄柏为芸香科植物黄皮树（Phellodendron chinense Schneid．）或黄檗（Phellodendron amurense Rupr．）的干燥树皮。前者习称“川黄柏”,后者习称“关黄柏”。《中华人民共和国药典》1963—2000年版均作“黄柏”收载,规定来源于芸香科植物黄皮树（川黄柏,Phellodendron chinense Schneid．）和黄檗（关黄柏,Phellodendron amurense Rupr．）的干燥树皮。但《中华人民共和国药典（一部）》（2005版）将两者分开,以“川黄柏”、“关黄柏”单列。     

HPLC测定黄柏中的盐酸小檗碱、盐酸巴马汀和盐酸药根碱

目的测定黄柏中盐酸小檗碱、盐酸巴马汀和盐酸药根碱的含量,为完善质量评价提供依据。方法采用HPLC法。结果与结论四川9个产区黄柏的盐酸小檗碱含量平均为50.5840 mg.g-1,关黄柏为6.8583 mg.g-1;其中荥经产黄柏中盐酸小檗碱的含量最高,为86.5381 mg.g-1,说明荥经是黄柏的道地药材产区;9个产区黄柏的盐酸巴马汀含量很低,平均为0.1296mg.g-1,而关黄柏为3.1310 mg.g-1;黄柏盐酸药根碱平均含量是0.2956 mg.g-1,关黄柏中是0.2883 mg.g-1,二者较接近。     

粗皮对黄柏、关黄柏质量的影响

目的 分析黄柏、关黄柏粗皮及药材中盐酸小檗碱的分布情况.方法 采用HPLC法分别测定黄柏、关黄柏粗皮部分,去粗皮部分和原药材的盐酸小檗碱的含量,比较液相色谱图中色谱峰的差异.结果 盐酸小檗碱在粗皮中含量低,粗皮部位的色谱图与药材的色谱图不全相同.结论 粗皮成分应进一步分析,黄柏和关黄柏应严格按照药典的加工要求去除粗皮部位.     

黄柏药材的红外光谱鉴别

目的通过对黄柏药材的提取物(盐酸小檗碱)作红外光谱扫描,快速鉴别该药材的真伪。方法根据盐酸小檗碱在热水中溶解,在水或乙醇中微溶,在三氯甲烷中极微溶解,在乙醚中不溶解的特性,以及2010年版《中国药典(一部)》中黄柏项下的鉴别提取方法,以1%醋酸甲醇为溶剂对黄柏进行提取,用纯化水对黄柏提取物进行重结晶,用非极性大孔吸附树脂D101柱进行分离纯化,对洗脱液进行浓缩再结晶,对结晶干燥,并将其红外光谱与标准图谱进行比较。结果红外光谱鉴别结果表明,黄柏提取物(盐酸小檗碱)红外光谱与盐酸小檗碱标准图谱一致。结论红外光谱鉴别方法简便可靠、快速准确。     

川黄柏的化学成分及药理活性研究进展

川黄柏是芸香料黄槃属植物,别名黄皮树、灰皮树、川黄槃。2005年版《中国药典》将川黄柏干燥树皮纳入中药黄柏的基源植物。川黄柏归肾和膀胱经,性寒味苦,作用是解毒疗疮、清热燥湿及泻火除蒸,适用于带下阴痒、湿热泻痢、热淋涩痛和黄疸尿赤等疾病的治疗。     

黄柏与伪品黄柏的鉴别

黄柏为常用的中药,价格居高不下,我们在药品检查抽验中,常发现有伪造品,外观形状与真品颇为相似。中国药典1995年版一部规定,黄柏是芸香料植物黄皮树或黄檗的干燥树皮,前者习称“川黄柏”,后者习称“关黄柏”。现就黄柏与伪品黄柏     

HPLC法测定黄柏中小檗碱的含量

黄柏具清热燥湿,泻火除蒸,解毒疗疮的功效,收载于<中国药典>2000年版一部,无含量测定项目.黄柏含小檗碱,木兰花碱等多种生物碱[1].为控制黄柏的内在质量,本文建立HPLC法测定盐酸小檗碱含量的方法.本方法快速,方便,可靠.     

高效液相色谱法测定关黄柏与川黄柏的有效成分的含量分析

目的：采用高效液相色谱法：以十八烷基硅烷键合硅胶为填充剂;以乙腈一0．1％磷酸溶液（50：50）（每100ml加十二烷基磺酸钠0．1g）为流动相;流速1ml／min;检测波长265nm;理论板数按盐酸小檗碱峰计算不应低于4000。结果：川黄柏中所含有抗病原微生物作用的活性成分盐酸小檗碱高于关黄柏中所含盐酸小檗碱,平均约3—4倍。川黄柏中不合盐酸巴马丁,关黄柏中盐酸巴马丁含量比较高。     

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.