荜澄茄超临界二氧化碳提取工艺及其镇痛活性评价

目的以超临界二氧化碳（SC-CO2）技术优化荜澄茄挥发性有效成分的提取工艺,并评价其镇痛活性。方法采用正交试验考察萃取压力、萃取温度、CO2流量、时间等对于SC-CO2提取工艺的影响,观察荜澄茄SC-CO2提取物对于化学及物理刺激所致疼痛的抑制作用。结果优选SC-CO2提取工艺为：压力20mPa、温度40℃、CO2流量6kg.h^-1、时间2h,萃取率可达30.7%。提取物可显著抑制醋酸及高热所致疼痛反应,镇痛率可达30%以上。结论荜澄茄SC-CO2工艺在提取效率方面具有显著优势,所得萃取物具有良好的镇痛活性。     

紫草中有效成分提取方法的研究

目的优选紫草中有效成分的提取方法。方法.用乙醇60℃以下提取和CO2超临界萃取,用高效液相色谱法,以左旋紫草素含量为考察指标,进行不同提取方法的比较研究。结果:CO2超临界萃取法左旋紫草素含量是乙醇提取法的3倍。结论紫草有效成分的提取以CO2超临界萃取法为优。萃取的条件是:萃取罐的温度为35℃,萃取压力为25Mpa,CO2流量为40L/h,萃取时间为3h。     

超临界CO_2萃取药桑黄酮的工艺研究

目的优选出药桑黄酮的超临界CO2较佳萃取工艺。方法以黄酮提取率为指标,依次用单因素试验和正交设计法考察了压力、温度、CO2流量以及夹带剂用量对超临界萃取的综合影响,并与超声波提取法进行了比较。结果影响超临界萃取的主要因素依次是压力、夹带剂用量、CO2流量和萃取温度,较优的萃取条件（以300g样品计）为压力35MPa、夹带剂用量200mL、CO2流量10kg.h-1及温度45℃;超临界萃取物黄酮含量为超声波提取物的67倍。结论超临界流体萃取的效率远优于传统提取方法,适于药桑黄酮的大规模提取。     

超临界萃取海马骨粉脂肪工艺及其脂肪酸组成分析

目的研究海马骨粉脂肪萃取工艺及其脂肪酸组成分析。方法利用CO2超临界流体萃取(SFE-CO2)技术,在单因子试验的基础上,采用正交实验设计方法对三斑海马骨粉动态萃取条件进行工艺优化。采用优化的萃取方法,对成年的三斑海马的脂肪进行萃取,并利用GC-MS技术对其脂肪酸的组成进行了分析。结果与结论实验显示:萃取压强对海马骨粉油脂萃取率的影响最大,其次是萃取时间、萃取温度和CO2流量; 经正交实验得到萃取海马骨粉油脂最佳工艺条件为:萃取压强为35 MPa,萃取温度为58℃,萃取时间135min,CO2流量为15L/h,在此优化条件下海马骨粉脂质萃取率为1.81%。经GC-MS分析,所得萃取物中主要含15种脂肪酸,其中不饱和脂肪酸占总脂肪酸的39.10%,EPA和DHA分别占不饱和脂肪酸的5.55%和11.00%。     

紫苏、辛夷混合挥发油提取与包合工艺研究

目的：优选辛夷、紫苏挥发油提取和包合的最佳工艺。方法：利用正交实验设计超临界流体萃取辛夷、紫苏挥发油,选择萃取的温度、压力、时间和二氧化碳（CO2）流量为考察因素,以挥发油提取率为考察指标,优选最佳提取工艺;应用响应面法优选挥发油包合工艺,以挥发油与β-环糊精（β-CD）的比例、包合温度和包合时间为考察因素,以包合物得率和挥发油包合率为指标优选挥发油包合工艺。结果：超临界CO2萃取辛夷、紫苏挥发油的最佳工艺：萃取的温度为40℃,压力为30 MPa,时间为1.5 h,CO2流量为60 kg·h-1;挥发油包合的最佳工艺：挥发油与β-CD之比为1∶8,包合温度为60℃,包合时间4 h。结论：本研究确定了辛夷、紫苏挥发油超临界CO2萃取的最佳工艺及包合工艺,优化了工艺参数,经验证表明本工艺稳定、可行。     

牛蒡子脱脂工艺的研究

目的研究超临界CO2萃取牛蒡子最佳脱脂工艺及其油脂的化学成分。方法采用均匀设计法以萃取压力、萃取温度、萃取时间为因素,考察超临界CO2萃取牛蒡子的最佳脱脂工艺条件,并对该工艺条件进行了中试验证;对牛蒡子超,临界萃取油进行GC—MS分析。结果最佳脱脂工艺为萃取压力32MPa、萃取温度48℃、萃取时间40min,且中试验证的萃取物平均萃取率为6．44％,牛蒡子苷元平均萃取率为0．21％;萃取油共分离出32个化学成分,主要成分为亚油酸。结论采用均匀设计法可以快速、准确地确定超临界CO2萃取技术对牛蒡子进行脱脂的最佳工艺。     

葡萄籽中原花青素的超临界CO2萃取工艺优选

目的：探讨超临界CO2流体萃取葡萄籽中原花青素的方法，选出最佳的提取工艺参数。方法：以原花青素含量为指标，考察了萃取温度、压力、CO2流量、萃取时间4个因素对葡萄籽中原花青素的超临界CO2流体萃取的影响。结果：以甲醇做夹带剂，药材质量30g，萃取压力32MPa，萃取温度40℃，CO2流量为10L·h^-1的条件下萃取60min为最佳工艺。结论：超临界CO2萃取法提取葡萄籽中原花青素耗时少、准确、效率高。     

超临界CO2萃取薏苡仁油工艺条件优化

目的应用超临界CO2萃取技术提取薏苡仁中的薏苡仁油，优化工艺条件。方法利用1L与600L的超临界萃取装置，考察原料水份、压力、时间与温度等参数对薏苡仁油提取得率的影响。结果优化得到用超临界CO2萃取技术从薏苡仁中提取薏苡仁油的工艺参数。结论超临界CO2萃取技术可用于薏苡仁油的提取，适用于工业化生产。     

超临界二氧化碳萃取咳喘穴位贴片药材的工艺研究

目的:探讨超临界二氧化碳(CO2)萃取咳喘穴位贴片药材的最优工艺。方法:采用单因素实验设计,以超临界萃取物总重量、萃取物中丁香酚得率、药渣盐酸麻黄碱的残留率为评价指标,优选最佳工艺条件。结果:初步实验得出优化工艺条件为:萃取压力为24MPa,萃取温度为45℃,解析压力Ⅰ为6Mpa,解析温度Ⅰ为55℃,夹带剂为75%乙醇,用量为25%,药粉粒度为40目,萃取时间为2h,流量20~25L.h-1。结论:采用超临界CO2萃取技术提取咳喘穴位贴片药材,时间短,有效成分收率高,工艺合理可行,符合经皮给药系统的设计要求。     

超临界CO2提取香附、当归挥发油的工艺研究

目的确定舒经克痛软胶囊中挥发油成分的提取路线并优化工艺参数。方法采用超临界CO2萃取法，使用正交试验设计方案，以提取率为指标，对萃取温度、萃取压力、分离压力和分离温度等影响因素进行考察。结果萃取压力、分离压力、分离温度对提取率的影响具有显著性意义，萃取温度无显著性意义。采用超临界CO2萃取法萃取舒经克痛软胶囊中挥发油成分的最佳工艺条件为：香附：萃取压力15mPa、萃取温度45℃、分离压力10mPa、分离温度30℃；当归：萃取压力25mPa、萃取温度50℃、分离压力8mPa、分离温度40℃。结论该方法简便，可靠，选择性高，适工业化生产。     

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.

---

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.