正交试验法优选酒柴胡炮制工艺

目的：优选酒柴胡炮制工艺参数,为酒柴胡饮片的标准化、产业化生产提供参考。方法：采用正交试验法,以黄酒用量、酒炙温度、酒炙时间为炮制工艺的关键影响因素,以柴胡皂苷a和柴胡皂苷d总含量、醇溶性浸出物含量为考察指标,综合评分,优选炮制工艺。结果：最佳炮制工艺条件为柴胡与黄酒用量比为100∶10,酒炙温度135~145℃,酒炙时间5 min。酒柴胡呈微黄色,微有酒香味。结论：经验证,该炮制工艺稳定可行,为规范酒柴胡的饮片加工提供参考。     

正交法优选酒炙川芎的最佳炮制工艺

目的优选川芎的最佳炮制工艺。方法以川芎嗪的含量为评价指标,选择黄酒用量、闷润时间、炮制温度、炮制时间四个主要影响因素,用L9（34）正交设计表,采用方差分析法,对川芎进行酒炙工艺的优选。结果川芎的最佳炮制工艺,每50 g川芎饮片,加15 m l黄酒,闷润0.5 h,80℃烘制1h。结论本方法为规范酒炙川芎的炮制工艺,提高酒炙川芎的质量,提供了科学依据。     

Box-Behnken设计-效应面法优选酒黄连炮制工艺

目的 优选酒黄连的最佳炮制工艺。方法 以小檗碱等4种生物碱含量之和、醇浸膏得率、外观性状为评价指标,采用Box-Behnken设计-效应面法考察黄酒用量、闷润时间、炒制温度、炒制时间对其质量的影响,优选酒黄连的炮制工艺参数。结果 黄连最佳酒炙工艺为黄酒用量12 g（药材与黄酒用量比为1：12）,闷润时间75 min,炒制温度100 ℃,炒制时间为7 min。结论 优选的酒黄连炮制工艺合理可行,可制备出质量可控的酒黄连饮片。     

酒炙续断最佳炮制工艺的研究

目的：以续断皂苷Ⅵ为指标对续断的炮制工艺进行优选。方法：采用L9（3^4）正交试验进行筛选。结果：用10％的黄酒浸润，150℃的下锅温度，炒6min时为续断酒炙的最佳炮制工艺。结论：酒炙续断最佳炮制工艺是科学合理的，酒炙可使有效成分含量增加，其质量稳定可控。     

基于UPLC方法的酒当归微波炮制工艺研究

目的采用UPLC及化学计量学方法考察酒炙当归的最优微波炮制工艺,为从品质角度探讨当归酒炙工艺的规范化提供参考。方法选取黄酒量、闷润时间、微波功率、微波时间作为考察因素,采用正交实验法以阿魏酸、洋川芎内酯A、正丁基苯肽、藁本内酯、丁烯基苯肽为指标,筛选最优酒炙工艺,并对当归酒炙前后的成分含量进行主成分分析。结果酒炙当归最优工艺为每1g当归加黄酒0．5g,闷润时间5h、微波功率750W、微波时间3min。结论本研究首次采用UPLC及化学计量学方法对酒当归的微波炮制工艺进行研究。该炮制工艺加热温度可控,加热时间确定,加料量定量,指标性成分含量高,操作步骤少,耗时短,为当归酒炙工艺提供了一种新方法。     

星点设计-效应面法优化酒制巴戟天的炮制工艺

目的 以水晶兰苷为指标建立酒制巴戟天最佳炮制工艺。方法 采用星点设计-效应面法以辅料黄酒用量、润药时间为考察因素,水晶兰苷的含量变化为评价指标,优化酒蒸巴戟天的炮制工艺。结果 星点设计-效应面法优化酒制巴戟天的最佳炮制工艺为：辅料黄酒用量为10%（g/g）、浸润时间为1 h,蒸透,干燥。结论 以黄酒用量、浸润时间为考察因素,水晶兰苷为评价指标的响应面法能够用于优化酒蒸巴戟天的最佳炮制工艺。     

基于UPLC方法的酒当归微波炮制工艺研究

目的 采用UPLC及化学计量学方法考察酒炙当归的最优微波炮制工艺,为从品质角度探讨当归酒炙工艺的规范化提供参考。方法 选取黄酒量、闷润时间、微波功率、微波时间作为考察因素,采用正交实验法以阿魏酸、洋川芎内酯A、正丁基苯肽、藁本内酯、丁烯基苯肽为指标,筛选最优酒炙工艺,并对当归酒炙前后的成分含量进行主成分分析。结果 酒炙当归最优工艺为每1 g当归加黄酒0.5 g,闷润时间5 h、微波功率750 W、微波时间3 min。结论 本研究首次采用UPLC及化学计量学方法对酒当归的微波炮制工艺进行研究。该炮制工艺加热温度可控,加热时间确定,加料量定量,指标性成分含量高,操作步骤少,耗时短,为当归酒炙工艺提供了一种新方法。     

星点设计-效应面法优化虎杖姜炙炮制工艺

目的：采用星点设计-效应面法对姜炙虎杖的炮制工艺进行优化,为姜炙虎杖炮制规范提供科学依据。方法：以姜汁用量、炒制温度、炒制时间为自变量,以虎杖苷、白藜芦醇、大黄素的综合评分作为指标,采用Design Expert进行二次项回归拟合,优选最佳工艺并验证。结果：效应面优化后,姜炙虎杖的最佳炮制工艺为姜汁用量17%,炒制温度240℃,炒制时间11 min。结论：优化姜炙虎杖炮制工艺时采用星点设计-效应面法,得到的模型具有较高拟合度,预测性良好。     

酒制补骨脂炮制工艺优化

目的 优化补骨脂酒焙法炮制工艺,制定合理的炮制工艺参数.方法 以补骨脂素、异补骨脂素、补骨脂酚为测定指标,采用正交试验方法考察酒药比例、烘制时间和烘制温度对补骨脂炮制工艺的影响.结果 补骨脂酒焙法最佳炮制工艺是补骨脂药材100 g,加15％黄酒,烘制时间120 min,烘制温度140℃.结论 正交试验确定的最佳工艺合理...     

酒炙大黄工业化生产工艺实验研究

目的优选符合工业化生产的酒炙大黄饮片生产工艺。方法采用L9(34)正交设计考察炒制温度、炒制时间、投料量,以饮片外观性状、总蒽醌含量为指标,选择高效液相色谱法进行含量测定,进行机械化炮制与传统手工炮制比对研究,确定最佳工艺技术参数。结果最佳炮制工艺技术参数为,加入10%黄酒拌匀,焖透,置XCYD-750型自控温旋盖电热炒药机内,炒炙温度设定140℃,炒炙时间设定15 min。结论优选工艺稳定可行,适合工业化生产。     

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.

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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.