响应曲面法优化延胡索中延胡索乙素的提取工艺

目的以延胡索乙素为指标成分对中药延胡索的提取工艺进行优化,以利于工业化生产。方法采用响应曲面法对提取工艺进行优化,通过考察乙醇体积分数、提取时间、溶媒用量及其交互作用对中药延胡索中延胡索乙素提取率的影响。模拟得出了延胡索乙素的提取回归方程,确定了延胡索乙素的最佳提取条件。结果优化得到的最佳工艺参数:乙醇体积分数为87.16%,提取时间为105.13 min,液料比为1∶7.13。在该工艺条件下,提取物中延胡索乙素的含量质量分数为0.183%。结论该提取工艺对延胡索提取物中的延胡索乙素提取优化效果显著,方法稳定、可行。     

正交试验优选双水相分配与超声提取集成法提取分离连钱草总黄酮的工艺

目的:优选双水相分配与超声提取集成法提取分离连钱草总黄酮的最佳工艺。方法:以超声提取时间、丙醇体积分数、料液比、(NH4)2SO4浓度为考察因素,连钱草总黄酮提取率为考察指标,通过正交试验优选其最佳提取工艺条件。结果:本法最佳提取工艺条件为超声提取时间30min,丙醇体积分数为50%,料液比1:30,(NH4)2SO4用量为30%。结论:本法操作简便、条件温和、效率高,具有较大优势。     

超声提取延胡索总生物碱的研究

目的考察超声对延胡索的干燥粉末中总生物碱提取的影响,探讨、改进延胡索总碱的提取工艺。方法以活性成分延胡索乙素、原阿片碱二者的含量为指标,采用单因素轮换试验法,考察超声时间、温度、功率以及提取溶媒的酸度、用量、体积分数等因素对提取的影响。结果实验确定延胡索总生物碱提取条件为超声时间60min,提取温度40℃,超声功率350W,提取溶媒用量30倍,乙醇体积分数70%,醋酸调pH3.5。结论此提取方法的提取率高,温度低,时间短,提取工艺简便,在工业化生产中可以降低能耗,提高经济效益。     

正交试验优选十一方药酒的超声提取工艺

目的:优选十一方药酒的超声提取工艺。方法:以大黄酚含量、人参皂苷Rg1含量与总固体量为考察指标,通过单因素试验优选浸泡时间、药材粉碎度、白酒体积分数、料液比、超声提取时间、提取次数;以白酒体积分数、料液比、提取时间、提取次数为因素,通过正交试验优选十一方药酒的超声提取工艺。结果:优选的超声提取工艺为料液比(1∶5,g/ml),50%白酒超声提取1次,时间为75 min。结论:该优选工艺合理可行,可为十一方药酒的制备工艺选择提供参考。     

正交试验法优选延胡索中延胡索乙素提取工艺

摘 要 目的：优选延胡索中延胡索乙素的最佳提取工艺。方法: 选用L9（34）正交试验设计,以提取物中延胡索乙素的含量为指标,考察乙醇浓度、乙醇用量、提取温度和提取时间对提取效果的影响。结果: 最佳提取工艺为按料液比1∶10（g·ml^-1）加入浓度为60%的乙醇溶液,以80 °C为提取温度,加热回流提取3 次,每次1 h。结论: 优选得到提取工艺稳定、合理、可行、操作简单,能耗低,较大限度地提高了延胡索的综合利用率。     

超声提取大叶茜草素的工艺研究

目的研究超声提取茜草中大叶茜草素的工艺。方法进行单因素超声提取实验,考察超声功率、占空比、提取时间、乙醇体积分数、料液比等因素对大叶茜草素提取率的影响。结果实验范围内,最适宜的工艺提取条件为:提取时间30min,超声功率600～800W,料液比(g·mL-1)1∶5,乙醇体积分数70%,占空比(s/s)5∶1,在此条件下大叶茜草素的平均提取率为1.07%。结论采用超声提取工艺,提取时间短,方法简单可行,有较高的工业应用价值。     

响应曲面法优化超声提取芒果叶中芒果苷的工艺研究

目的优选芒果叶中的芒果苷的超声提取工艺。方法选择液料比、超声功率、提取温度和提取时间为自变量,以芒果苷的提取率为响应值,利用响应曲面法分析优选最佳提取工艺。结果最佳工艺条件为:液料比50mL·g-1,超声功率438 W,提取温度46℃,提取时间30min。在此条件下,芒果苷提取率为4.04%。结论优选的工艺稳定、可行。     

超声-微波辅助提取无花果果实总黄酮工艺的优化

目的 验证在超声-微波法下,无花果果实黄酮的最佳提取条件。方法 采用超声-微波提取法从不同种类的无花果中提取黄酮类化合物。结果 通过单因素试验,考察液料比、乙醇体积分数、微波时间、微波功率、超声时间、超声功率对黄酮类化合物提取率的影响。在单因素的基础上,采用六因素三水平正交试验确定为：青皮的最佳提取条件为液料比70∶1、乙醇体积分数55%、微波功率340 W、微波时间60 s、超声功率350 W、超声时间35 min;波姬红的最佳提取条件为液料比45∶1、乙醇体积分数90%、微波功率420 W、微波时间45 s、超声功率350 W、超声时间40 min。布兰瑞克的最佳提取条件为液料比45∶1、乙醇体积分数60%、微波功率320 W、微波时间135 s、超声功率350 W、超声时间40 min。在此条件下,无花果果实（青皮、波姬红、布兰瑞克）总黄酮的平均提取率,分别为0.42%,0.51%,0.37%。结论 采用单因素试验和正交试验的方法研究了超声波辅助提取无花果中总黄酮的工艺条件,确定了最佳提取条件。     

延胡索中延胡索乙素双相动态提取方法研究

目的探讨延胡索有效成分的最佳双相动态提取工艺。方法以延胡索乙素含量为指标,采用L9(34)正交试验设计对提取工艺进行优化,考察酸浓度、溶剂倍数、提取时间、提取温度对延胡索乙素含量的影响。结果延胡索乙素的最佳提取工艺为加酸浓度2.0%的硫酸,10倍量溶剂,100℃提取1次,提取时间3 h。结论优选得到的工艺确实可行,便于生产质量控制。     

Box-Behnken设计-响应面法优选雪松松针中蛇床子素的提取工艺

目的:优选雪松松针中蛇床子素的提取工艺。方法:采用高效液相色谱法测定蛇床子素含量。在单因素考察的基础上,以乙醇体积分数、提取时间、料液比为考察因素,以蛇床子素含量为响应值,采用Box-Behnken设计-响应面法优选雪松松针中蛇床子素的提取工艺,并进行验证试验。结果:确定的最佳提取工艺为乙醇体积分数88%,料液比1∶20(g/mL),提取2次、每次57min。在此工艺条件下,提取得到蛇床子素的平均含量为0.675 7 mg/g(RSD=1.78%,n=3),与预测值0.680 9 mg/g的相对误差为0.59%。结论:优选的最佳提取工艺方法简便、可行,可用于雪松松针中蛇床子素的提取。     

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.