添加前体物质对水培益母草中盐酸水苏碱含量的影响

目的探究盐酸水苏碱前体物质对益母草水培过程中产生盐酸水苏碱的影响。方法在益母草水培营养液中按不同浓度和时间分别添加盐酸水苏碱可能的前体物质L-脯氨酸和L-鸟氨酸,并采用HPLC-ELSD法测定各组盐酸水苏碱的含量。结果 L-脯氨酸添加的最佳浓度为0.5 mmol.L-1,最佳转化时间为96 h,盐酸水苏碱由对照的1.037%上升至1.585%;L-鸟氨酸添加的最佳浓度为1 mmol.L-1,转化时间为72 h时,盐酸水苏碱含量达到1.135%。结论添加前体物质L-脯氨酸和L-鸟氨酸,对益母草中盐酸水苏碱积累有效,且L-脯氨酸的效果优于L-鸟氨酸。     

产舒康颗粒中盐酸水苏碱的高效液相色谱法定量

目的建立产舒康颗粒中盐酸水苏碱的高效液相色谱法定量方法。方法通过强酸性阳离子交换树脂柱得到产舒康颗粒中盐酸水苏碱。高效液相色谱法测定条件:Spherisorb SCX柱150mm×4.6mm,5μm;流动相:甲醇-水(60:40)含0.05mol.L-1磷酸二氢钾;检测波长:215nm。结果盐酸水苏碱在1.0～5.0μg内线性关系良好,平均回收率96.21%,RSD=2.22%,三批颗粒中盐酸水苏碱含量分别为0.0304%,0.0276%,0.0191%。结论该方法简便、灵敏、准确,为控制产舒康颗粒的质量提供依据。     

薄层扫描法测定抗宫炎颗粒中盐酸水苏碱的含量

目的:采用薄层扫描法对抗宫炎颗粒中的盐酸水苏碱进行含量测定.方法:以正丁醇-盐酸-醋酸乙酯(12:4.5:1.5)为展开剂,2次展开.测定波长λS=515 nm,λR=650 nm.结果:本品加样回收率为98.9%,RSD为4.2%.3批样品中盐酸水苏碱含量分别为0.224,0.222,0.265 mg·g-1.结论:方法简便、可靠、实用,可用于该品种的质量控制.     

肾宁合剂中水苏碱的含量测定

目的:建立肾宁合剂中水苏碱的含量测定方法.方法:样品经强酸性阳离子交换树脂提纯,采用薄层扫描法测定.结果:盐酸水苏碱线性范围为4.32～12.96μg(r=0.997 8),平均回收率为97.15%,RSD为1.53%.结论:本试验建立的含量测定方法简便、准确,可用于控制制剂的质量.     

LC-MS/MS法测定益母颗粒中盐酸水苏碱的含量

目的建立益母颗粒中盐酸水苏碱含量的测定方法。方法采用LC-MS/MS法测定盐酸水苏碱的含量。使用Venusil HILIC色谱柱(100 mm×2.1 mm,3μm),以乙腈-水(70:30)为流动相,流速为0.3 mL·min-1。以电喷雾离子源(ESI)正离子模式将样品离子化,多反应监测(MRM)模式下对盐酸水苏碱(m/z144.06→57.96和m/z 144.06→84.01)进行测定。结果盐酸水苏碱浓度在4.68²34.0 ng·mL-1与峰面积线性关系良好(r=0.999 6),平均回收率为98.8%,RSD为1.5%(n=6)。结论该方法简便、可靠、准确,可作为益母颗粒中盐酸水苏碱的含量测定方法。     

HPLC-RID法测定益母草颗粒中盐酸水苏碱含量

目的建立益母草颗粒中盐酸水苏碱的含量测定方法。方法采用氨基柱,以乙腈-水(体积比80∶20)为流动相,流速是1mL.min-1,示差折光检测器,柱温40℃。结果盐酸水苏碱浓度在0.2mg.mL-1-1mg.mL-1范围内有良好的线性关系,r=0.9982,回收率为101.5%,RSD为2.5%(n=6)。结论本法专属性强,准确、简便,为益母草颗粒中盐酸水苏碱测定提供新的方法。     

花期对益母草药材中盐酸水苏碱和盐酸益母草碱含量的影响

摘 要: 目的 研究开花对益母草药材中盐酸水苏碱含量的影响。方法 在同一地区不同时期采收益母草药材样品;运用药典法水苏碱进行测定。 结果 开花过程中益母草药材中盐酸水苏碱的含量不断降低。 结论 开花对益母草药材中盐酸水苏碱含量影响较大。     

HPLC法测定肾八味胶囊中盐酸水苏碱含量

目的建立HPLC法测定肾八味胶囊中盐酸水苏碱的含量.方法色谱柱氨基柱(250 mm×4.6 mm,5 μm);柱温室温;流动相乙腈10 mmol·L-1KH2PO4水溶液(用磷酸调节pH 3.0)(2080);流速1 ml·min-1;检测波长203 nm.结果盐酸水苏碱的线性范围为0.05～2.50 mg·ml-1,r=0.999 7;平均回收率95.1%,RSD 1.8%(n=6).结论本方法简便,结果准确可靠,可用于控制肾八味胶囊中盐酸水苏碱的含量.     

HPLC法测定前列康胶囊的含量

目的建立前列康胶囊中水苏碱的含量测定方法.方法采用高效液相色谱法,spherisorb SCX柱,流动相:三乙胺比例为0.05%、磷酸二氢钾浓度为0.025 mol/L(以磷酸调pH为2.0)的水溶液.结果盐酸水苏碱在0.392～19.6μg范围内呈良好的线性关系.R=0.9999,回收率为96.9%.结论该法简便、灵敏、准确.     

HPLC法测定不同产地益母草中盐酸水苏碱的含量

目的:建立改性活性炭-中性氧化铝纯化方法,用HPLC法测定不同产地益母草中盐酸水苏碱的含量.方法:用三乙胺处理活性炭,制备载氮改性活性炭,益母草经乙醇提取后过改性活性炭-中性氧化铝柱,系统考察活性炭改性方式、用量、中性氧化铝用量、上样及洗脱流速、乙醇洗脱体积;采用-NH2柱在反相条件下测定不同产地益母草中盐酸水苏碱的含量.结果:在选定的色谱条件下盐酸水苏碱可以得到较好的分离,线性范围2.046～20.46μg,平均回收率为98.31％,RSD为1.434 1％(n=6).11个产地的益母草药材中盐酸水苏碱含量差异较大.结论:该方法测定准确、稳定、重复性好,可用于不同产地益母草药材及饮片的质量评价.     

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.     

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.