利用响应面分析法优化金银花中的绿原酸的超声提取工艺

目的 优化金银花中绿原酸的超声提取工艺。方法 以绿原酸得率为指标,采用响应面分析法,考察料液比、提取时间、乙醇浓度等不同因素对提取条件的影响,优选最佳提取工艺。结果 超声提取法的最佳提取条件为：料液比为1∶14,乙醇浓度为58%,提取时间为27 min,绿原酸得率为1.39%。结论 该优化工艺简便稳定、重复性好,可用于金银花绿原酸的提取。     

利用响应面分析法优化金银花中的绿原酸的超声提取工艺

目的优化金银花中绿原酸的超声提取工艺。方法以绿原酸得率为指标,采用响应面分析法,考察料液比、提取时间、乙醇浓度等不同因素对提取条件的影响,优选最佳提取工艺。结果超声提取法的最佳提取条件为：料液比为1∶14,乙醇浓度为58%,提取时间为27 min,绿原酸得率为1.39%。结论该优化工艺简便稳定、重复性好,可用于金银花绿原酸的提取。     

桔梗中总黄酮的提取工艺优化

目的优选从桔梗根、茎、叶中提取总黄酮的最佳工艺,并在最佳提取条件下测定桔梗根、茎、叶中总黄酮的含量。方法以总黄酮含量为指标,采用正交实验,考察了乙醇体积分数、超声时间和超声次数对总黄酮得率的影响。结果提取总黄酮的最佳工艺为A3B3C3,即乙醇体积分数70%,超声时间50min,超声次数3次。在最佳实验条件下,分别测得桔梗根、茎及叶中总黄酮的含量分别为0.027%,0.039%和0.26%。结论该工艺简单可行,是提取桔梗中总黄酮的有效途径。     

正交实验法优选药用红树植物老鼠簕总黄酮提取工艺

目的以老鼠簕为对象,优选出两种黄酮提取工艺中的最佳提取条件。方法利用L_9(3~4)正交设计法优选药用红树植物老鼠簕总黄酮提取工艺,以老鼠簕总黄酮含量为指标,分别对索氏提取中的乙醇浓度、提取温度、提取时间和超声提取法中提取时间、乙醇浓度、液料比等因素进行考查,优选老鼠簕总黄酮的最佳提取条件。结果索氏提取法中,提取温度对总黄酮提取率影响最大,最佳提取条件为60%乙醇提取液,在85℃下提取2.5h。超声提取法中,乙醇浓度对提取率的影响最大,提取最佳条件为50%乙醇提取液,液料比为40:1,浸提50min,提取2次。结论超声提取方法优于索氏提取法,总黄酮提取量可达3.82%。     

超声提取麦冬总黄酮的工艺研究

目的 优化超声技术提取麦冬总黄酮的工艺条件.方法 采用L9(34)正交试验法,考察乙醇浓度、乙醇用量、提取时间、提取次数对超声提取的影响,以总黄酮含量为考核指标,确定最佳提取条件.结果 最佳提取工艺为加12倍生药量的60%乙醇,超声提取3 次,每次45min.结论 此方法 是一种简单、快捷、高效、可行的提取.     

药用菊花总黄酮提取方法的比较

目的 优化药用菊花总黄酮提取工艺.方法 通过对冷浸法、索提法、回流法、超声法等几种提取方法的研究和比较,采用正交试验设计优选药用菊花总黄酮的最佳提取工艺.结果 不同处理方法所得结果不同,李氏提取法(甲醇)所得浸膏重量及其得率均最高;超声法(70%乙醇)所得总黄酮含量及得率最高.结论 超声法为药用菊花总黄酮的最佳提取方法,其最佳提取条件是溶剂为70%乙醇,料液比为1:30,超声温度为60℃,超声时间为30min.     

泽漆中总黄酮超声提取工艺优化研究

目的研究泽漆总黄酮超声提取法的最佳提取工艺,在此基础上采用分光光度法测定不同部位总黄酮的含量。方法正交设计试验寻找超声提取法提取泽漆总黄酮的最佳工艺条件,以芦丁为考察指标,通过分光光度法对泽漆不同部位总黄酮含量进行精密测定。结果乙醇浓度50%,物料比1∶25,超声提取时间20 min,超声提取温度60℃为最佳提取工艺。泽漆叶中总黄酮含量最高,根次之,茎最低。结论优选的泽漆总黄酮提取工艺方法,简便易行,快速灵敏,实验结果准确可靠。     

正交试验法优化忍冬叶中总黄酮的提取工艺

目的：确定提取忍冬叶总黄酮的最佳工艺备件。方法：采用正交试验法，分别考察乙醇冷浸、回流和超声提取对提取率的影响，并与乙醇索氏提取以及水提取最佳工艺比较。用分光光度法测定总黄酮含量。结果：在不同的乙醇提取工艺中，总黄酮含量高低顺序为回流法≈索氏提取法＞超声法≈冷浸法。在不同的水提取工艺中，总黄酮含量高低顺序为回流法＞超声法≈碱水冷浸法＞冷浸法。结论：提取忍冬叶总黄酮的最佳备件为：12倍量60％乙醇，水浴回流提取2次，每次1．5h。     

复方槐花颗粒中槐花和侧柏叶总黄酮提取工艺的优化

目的 优选复方槐花颗粒中槐花和侧柏叶总黄酮最佳提取工艺。方法 采用超声浸提法对复方槐花颗粒中槐花和侧柏叶总黄酮进行提取,以乙醇体积分数、超声功率、超声时间和料液比为考察因素,通过单因素试验和正交优选,确定较优提取工艺,并与常规的热回流提取法进行比较研究。结果 超声浸提法最佳提取工艺条件为：用60%乙醇,在料液比1:10和超声功率40kHz条件下超声波辅助连续提取2次,每次15min,槐花和侧柏叶总黄酮提取率可达93.31%。结论 该工艺研究为复方槐花颗粒中槐花和侧柏叶总黄酮共提提供一种新方法和思路,具有耗时短、能耗低、溶剂用量少和提取效率高等优势。     

超声法与连续回流法提取黄芪总黄酮的工艺对比研究

目的:对比研究超声法和连续回流法提取黄芪总黄酮的工艺。方法:以乙醇浓度、提取时间、固液比、提取温度为考察因素,黄芪总黄酮提取率为考察指标,采用正交试验优选最佳提取工艺条件。结果:要获得相同的提取率,超声法效率更高,其最佳提取工艺为乙醇浓度75%,超声提取时间20min,固液比1∶10,超声提取温度25℃,提取率为0.325%。结论:与连续回流法比较,采用超声法提取黄芪总黄酮具有快速、节省溶剂、提取的有效成分含量高等优点。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.