肝宁颗粒中大黄的质量控制

目的：建立肝宁颗粒中大黄的鉴别和含量测定方法。方法：采用薄层色谱法（TLC）鉴别大黄，采用高效液相色谱法（HPLC）测定大黄中的5种结合蒽醌。选用Nucleosil ODS柱，以甲醇-0．1％磷酸溶液（85：15）为流动相，检测波长430nm。结果：高效液相色谱法测定5种蒽醌的线性范围为芦荟大黄素0．0416～0．2912Mg，大黄酸0．0312～0．25984μg，大黄素0．04576～0．32032μg，大黄酚0．0496～0．3472μg，大黄素甲醚0．02064～0．14448μg；5种蒽醌的平均回收率均在96．6％～98．4%。结论：本方法简便，准确，灵敏度高，准确性强，重复性好，可用于肝宁颗粒的质量控制。     

栽培河套大黄根、茎、叶中游离葸醌类成分的含量分析

目的：利用HPLC法测定栽培河套大黄根、茎、叶中游离蒽醌的含量。方法：采用Agilent Zorbax SB-C18（4．6mm×250mm，5μm）色谱柱，以甲醇-0．1％磷酸（85：15）为流动相，流速：1．0mL·min^-1，检测波长为254nm，理论板数按大黄素峰计算不低于3000。结果：芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚5种成分的线性范围分别为0．046-0．232峭（r=0．9998）、0．069-0．343μg（r=0．9999）、0．063-0．314μg（r=0．9995）、0．060-0．298μg（r=0．9994）、0．032-0．161μg（r=0．9997）。河套大黄样品1（根）中上述5种成分的回收率（n=6）分别为97．31％（RSD为1．3％），96．73％（RSD为2．2％），98．85％（RSD为1．9％），98．96％（RSD为1．0％），98．11％（RSD为2．3％）。河套大黄根中上述5种成分的含量依次为0．42％-0．48％，0．06％-0．08％，0．40％-0．47％，1．90％-2．40％，0．44％-0．62％；茎中的含量依次为0，0，0．08％-0．1％，0．01％，0．03％-0．06％；叶中的含量依次为：0．01％，0，0．62％-0．90％，0．01％，0．05％-0．07％。结论：栽培河套大黄根、茎、叶中均含有游离蒽醌，其中根的含量最高，叶次之，茎最少；根中游离蒽醌最高为大黄酚，其次为大黄素甲醚，芦荟大黄素与大黄素的含量基本相同，大黄酸的含量最低。可针对河套大黄中含量较高的游离蒽醌进行开发。     

妇炎消胶囊质量标准的研究

目的：提高完善妇炎消胶囊的质量标准。方法：采用薄层色谱法鉴别败酱草;采用高效液相色谱法测定大黄中大黄素和大黄酚的含量;采用高效液相色谱法测定牡丹皮中芍药苷的含量。结果：大黄素在0.0080～0.2012μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为98.1％（RSD＝3.0％,n＝9）;大黄酚在0.0262～0.6550μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为102.4％（ RSD＝2.6％,n＝9）;芍药苷在0.0997～1.9937μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为103.3％（ RSD＝1.5％,n＝9）。结论：建立的方法准确可靠,适用于妇炎消胶囊的质量控制。     

新新扑滴鼻液的制备及质量控制

目的：制备新新扑滴鼻液，并建立质量控制方法。方法：采用可分光光度法测定新霉素的含量，用溴量法测定新福林的含量；用双波长分光光度法测扑尔敏的含量，结果：新霉素在16－40μg/ml范围内呈良好线性关系（r=0.9998)，平均回收率：101．2％，相对标准偏差（Relative standard deviation RSD)以下简称RSD，RSD＝3．99％，n=5,新福林平均回收率：100．2％，RSD＝0．41％，n=5，扑尔敏在12－28μg/ml范围内呈良好线性关系（r=0.9999)，平均回收率：99．93％，RSD＝0．70％，n=5)，结论：制定的质量控制方法能保证新新扑滴鼻液的质量。     

高效液相色谱法测定盐酸氨基胍片中盐酸氨基膈的含量

目的：用高效液相色谱法(HPLC法)测定盐酸氨基胍片含量。方法：采用C18柱，以乙腈—0．025mol／LKH2PO4(含0．596三乙胺，pH＝3．5)(30：70)为流动相，检测波长为213nm。结果：盐酸免基瓜浓度在82～810μg/mL范围内与峰面积有良好的线性关系，r＝0．9998；平均回收率为100．0％，RSD＝0．96％，n＝9；日内差＝0．25％，日间差RSD＝0．11％。结论：HPLC法可以用于盐酸氨基胍片的含量测定。     

HPLC法测定胆康片中大黄素、大黄酚的含量

目的：建立测定胆康片中大黄素、大黄酚含量的HPLC方法。方法：色谱柱为Waters ODS C18（150mm×4．6mm，5μm），流动相为甲醇-0．1％磷酸溶液（85：15），流速为1．0ml·min^-1，检测波长为254nm。结果：大黄素的线性范围为0．03～0．21μg（r=0．9999）、大黄酚的线性范围为0．06～0．50μg（r=0．9998），大黄素平均回收率为97．9％、RSD为0．2％（n=6），大黄酚平均回收率为97．6％、RSD为0．4％（n=6）。结论：建立的方法简便、重复性好，可用于胆康片中大黄素、大黄酚的含量测定。     

紫外分光光度法测定戊二醛含量

目的：探讨用紫外分光光度法测定戊二醛溶液个戊二醛的含量。方法：在戊二醛特征吸收峰233nm波长处测定戊二醛含量。结果：戊二醛浓度在100～1200μg／mL范围内与吸收度线性关系良好，r＝0.9991(n＝5)，平均回收率99．44％，RSD＝1．98％。结论：紫外分光光度法简便、快速、准确，适用于戊二醛含量测定。     

UV测定大黄提取工艺产物总蒽醌含量

目的测定大黄溶剂萃取工艺提取物与SFE-CO2工艺提取物总蒽醌含量。方法先CHCl3超声振荡提取游离葸醌，再将残渣中结合蒽醌进行水解，CHCl3热回流提取；总蒽醌以0.5％Mg(Ac)2甲醇溶液显色，总葸醌含量在1．52-15.2μg/ml范围内，浓度与吸光度之间线性关系良好(γ=0．9997)；样品的平均回收率为98．85％，RSD为0．53％(n=6)。结果从总葸醌转移率来看，SFE-CO2工艺优于溶剂萃取工艺。     

测定大黄水提物中游离蒽醌类成分的含量

目的采用反相高效液相色谱法（RP—HPLC）同时测定大黄水提物中5种游离型蒽醌类衍生物的含量。方法色谱条件为固定相Inertsil ODS3 C18柱（250mm×4．6mm,5μm）;流动相为1％（体积分数）乙酸水溶液：甲醇=8：92,v／v;流速：1．0ml／min;柱温：30℃;检测波长：254nm。结果5种大黄游离型蒽醌类衍生物在该色谱条件下20min内分离良好,大黄酸、大黄素、芦荟大黄素、大黄酚、大黄素甲醚的线性范围分别是5～50、2～12、2～12、2～12、2～12mg／L,平均加样回收率（n=3）分别是大黄酸102．89％,相对标准偏差值（RSD）为2．97％、大黄素102．22％（RSD=4．60％）、芦荟大黄素101．87％（RSD=3．26％）、大黄酚103．90％（RSD=1．33％）以及大黄素甲醚103．67％（RSD=1．77％）。结论方法快速简便,结果准确,用来测定大黄水提物中5种游离型蒽醌类衍生物的含量结果令人满意,可作为大黄水提物的质量控制方法之一。     

DNA荧光法测定云硒冲剂中硒的含量

目的：建立云硒冲剂中硒的含量测定方法。方法：采用DAN荧光光度法进行硒含量测定，激发波长376nm，发射波长250nm。结果：采用本法测定云硒中硒的含量，回归主程为：Y＝3．84678X－1．98733（r＝0．99855）；平均回收率98．79％，CV＝2．32％（n＝5）；三批样品测定硒含量为9．50－10．66μg.ml^-1。结论：测定结果稳定，影响因素少，而且设备较其它硒含量测定方法简单常见，危险性又小，适于推广。     

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.