杏仁提取条件的探讨

目的：研究苦杏仁中有效成分苦杏仁苷的最佳提取条件。方法：采用2次重复的正交实验法，以加水倍量，提取时间，提取次数3个因素，每个因素选取3个水平进行实验。结果：因素A（加水倍量）有显著影响，因素B（提取时间）和因素C（提取次数）对苦杏仁苷的含量有极显著影响。结论：最佳提取工艺A2B2C2，即用10倍量提取2次，每次1h。     

正交试验优选新疆苦巴旦杏仁中苦杏仁苷提取工艺

目的:优选新疆苦巴旦杏仁中苦杏仁苷的提取工艺。方法:以苦杏仁苷含量为定量指标,通过单因素试验优选出的微波灭酶时间、苦巴旦杏仁细粉与石油醚比例、脱脂粕与95%乙醇的比例为考察因素,用正交试验优选最佳提取工艺。结果:最佳提取工艺为微波灭酶3.5min,苦巴旦杏仁细粉与石油醚比例为1∶6进行脱脂,脱脂粕与95%乙醇为1∶30进行纯化,在此条件下苦杏仁苷的含量为3.21%。结论:该提取工艺合理、简单、可行,可为大生产提供理论依据。     

新疆桃仁中苦杏仁苷含量测定新方法研究

目的：建立桃仁中苦杏仁苷灵敏度高、适用性强的高效液相色谱测定新方法,并对收集于新疆地区的41批代表性药材进行含量测定。方法：样品采用索氏提取器脱脂、加入70％甲醇回流的方法灭酶和提取,色谱柱为SymmetryC18（4．6mm×150mm,5μm）,以水-乙腈为流动相梯度洗脱,流量1mL·min^-1,柱温35℃,检测波长210nm。结果：方法学验证各项指标均符合要求,41批新疆桃仁中苦杏仁苷含量在2．05％-3．62％范围内,平均含量为3．04％±0．29％。结论：所建立测定方法简便、稳定、易行,可用于新疆桃仁中苦杏仁苷含量测定和质量控制。     

不同产地苦杏仁中苦杏仁苷含量比较研究

目的测定3种不同产地苦杏仁中苦杏仁苷含量,为苦杏仁的质量研究提供参考依据。同时,通过对不同来源苦杏仁中苦杏仁苷含量的测定,为比较它们的含量和寻找苦杏仁的优良产地,在实际应用中选择高产、优质的苦杏仁提供科学依据。方法取山西、内蒙古、甘肃3个产地的苦杏仁粉末,甲醇超声提取苦杏仁苷,在检测波长207nm下用高效液相色谱法测定各自含量,采用AgilentHC—C18色谱柱（250×4．6mm,5μm）,流动相：乙腈－0．1％磷酸溶液f8：92）,柱温：30℃,流速：1ml／min。结果不同产地的苦杏仁苷含量存在差异,它们的苦杏仁苷含量的大小如下：内蒙古〉甘肃〉山西。苦杏仁苷在0．008～0．080mg／ml范围内线性关系良好,回归方程：Y=14．28833X—1．67706,r=0．9999,加样回收率为99．34％,RSD=0．69％。结论内蒙古、山西、甘肃三个产地的苦杏仁苷含量均符合药典要求,但三者之间含量存在差异,因此在实际用药中应注意产地对苦杏仁临床药效的影响。     

两种灭酶方法对苦杏仁及苦巴旦杏仁中苦杏仁苷含量的影响简

目的 比较两种灭酶方法对苦杏仁和苦巴旦杏仁中苦杏仁苷含量的影响.方法 分别用沸水煮5 min或10 min、蒸30 min对苦杏仁和苦巴旦杏仁进行灭酶处理,用紫外分光光度法测含量,分析灭酶方法对苦杏仁苷含量的影响.结果 苦杏仁中沸水煮10 min或5 min所得苦杏仁苷含量分别为2.8％和2.1％,蒸30 min所得苦杏仁苷含量为2.5％,苦巴旦杏仁沸水煮10 min所得苦杏仁苷含量为1.0％.结论 苦杏仁用两种灭酶方法处理后,沸水煮10 min所得苦杏仁苷含量最高.用沸水煮法对苦杏仁和苦巴旦杏仁进行灭酶处理,苦杏仁中苦杏仁苷的含量高于苦巴旦杏仁的含量.     

苦杏仁酶法转化桃叶珊瑚苷为桃叶珊瑚苷苷元的分析

目的：对桃叶珊瑚苷的苦杏仁酶法转化和桃叶珊瑚苷苷元的LC—MS色谱分析进行研究。方法：从苦杏仁中提取苦杏仁酶，用3，5-二硝基水杨酸（DNS）法测定苦杏仁酶的活力；将苦杏仁酶与桃叶珊瑚苷在37℃温孵60min后，低温乙酸乙酯萃取获得苷元，并对苷和苷元分别在流动相为甲醇-水（10：90）条件下的LC—MS色谱行为进行分析。结果：苦杏仁酶的酶活力为174U·mg-1，桃叶珊瑚苷苷元的转化得率为31．41％，得到的苷元纯度在93．23％以上。结论：本方法简单经济，获得的苷元纯度高，低温密封能保持苷元稳定。     

不同煎煮时间对苦杏仁苷含量的影响

目的确立“火单”法炮制苦杏仁的最佳煎煮时间。方法采用HPLC法在215nm波长下，测定煎煮不同时间的苦杏仁药材中苦杏仁苷的含量，所得结果进行比较。结果煎煮5分钟与煎煮10分钟的苦杏仁药材中苦杏仁苷含量较高，而煎煮15分钟的苦杏仁药材中苦杏仁苷的含量有所下降，以后随着煎煮时间的增加，苦杏仁苷的含量也逐渐下降，煎煮30分钟的苦杏仁药材含量已明显降低。     

苦杏仁3种提取工艺中苦杏仁苷提取率的比较

目的比较3种杏仁提取工艺中苦杏仁苷提取率.方法以硝酸银滴定法测量3种苦杏仁提取工艺中苦杏仁苷的含量并计算提取率.结果 3种提取方法提取率,分别为95.77%、64.88%、55.61%,其中蒸馏苦杏仁水法最高,醇提苦杏仁苷法次之.结论三种提取方法均可得到较高的提取率.     

苦杏仁中苦杏仁酶的闪式提取工艺研究

目的 建立苦杏仁中苦杏仁酶的闪式提取工艺,并对其工艺条件进行优化.方法 以苦杏仁酶总活力为指标,考察了氨水浓度、提取液用量、提取时间、中和终点pH值和沉淀时乙醇体积分数对闪式提取工艺的影响:采用二硝基水杨酸(DNS)法测定苦杏仁酶的比活力,并计算其总活力.结果 苦杏仁酶的最佳提取工艺条件为:取50.0 g脱脂苦杏仁粉,...     

清金消咳胶囊的工艺改进及质量标准

清金消咳丸胶囊为我院自制制剂，是根据中医理论以及长期的临床经验而形成的经验制剂，疗效确切，主要由苦杏仁、前胡、金银花、鱼腥草等１２味中药组成，具有清肺润燥、止咳化痰的作用，用于治疗感冒咳嗽、急慢性支气管炎等。因原制备方法中水煎煮２次，１h／次，从而导致有效成分苦杏仁苷大部分被水解。本方法中苦杏仁苷改用醇提，制粒后再与药材水提物相混合，较好地解决了苦杏仁苷被水解的问题。１仪器与试剂苦杏仁、前胡、鱼腥草、金银花购于广东省饮片厂；苦杏仁苷标准品（定量用）、氯原酸购于中国药品生物制品鉴定所；清金消咳胶囊…     

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.     

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.