GC法同时测定降香中4个成分的含量

目的:建立降香挥发油中反式-β-金合欢烯、β-没药烯、反式-橙花叔醇、金合欢醇的气相色谱含量测定方法。方法:色谱条件为HP-5 MS(30 m×0.25 mm,0.25μm)色谱柱,程序升温;进样口温度250℃,流速1.0 mL.min-1;分流比20∶1;FID检测器,温度250℃;载气:氮气。结果:反式-β-金合欢烯、β-没药烯、反式-橙花叔醇、金合欢醇的线性范围分别为0.011～0.212 mg.mL-1(r=0.9998),0.011～0.659 mg.mL-1(r=0.9999),0.051～10.200 mg.mL-1(r=0.9996),0.011～0.222 mg.mL-1(r=0.9998);加样回收率(n=9)分别为99.5%,98.4%,99.7%,96.6%。结论:该方法简便、准确,重复性好,为降香的质量控制提供了依据。     

二香合心软胶囊中橙花叔醇的含量测定

目的建立二香合心软胶囊中橙花叔醇的含量测定方法。方法反相高效液相色谱法,采用KromasilODS-1色谱柱(150mm×4.6mm,5μm),以甲醇-水(78∶22)为流动相,测定波长为213nm。结果橙花叔醇在50.4～504mg·L-1质量浓度范围内与峰面积之间线性关系良好,r=0.9994,回收率为100.2%,RSD为1.5%。结论方法简便、快速、准确,可作为控制二香合心软胶囊生产工艺和产品质量的方法。     

不同产地、不同采收期黄芪药材及饮片中毛蕊异黄酮葡萄糖苷及芒柄花素含量测定

目的:采用HPLC法测定不同产地、不同采收期黄芪药材及饮片中毛蕊异黄酮葡萄糖苷及芒柄花素含量。方法:采用Agilent ZORBAX Eclipse XDB-C18(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈-水,梯度洗脱,流速1 mL·min-1,柱温35℃,检测波长260 nm。结果:毛蕊异黄酮葡萄糖苷、芒柄花素线性范围分别为0.1272～12.72μg(r=0.9999)和0.003344～2.508μg(r=0.9999),平均回收率(n=6)分别为98.9%(RSD=1.7%)和99.0%(RSD=2.3%)。不同产地黄芪药材及饮片中毛蕊异黄酮葡萄糖苷和芒柄花素含量差异较大,生长年限6年的黄芪中毛蕊异黄酮葡萄糖苷和芒柄花素含量最高。结论:该方法简单快捷,适合于黄芪中黄酮类化合物的含量测定研究,为寻找更佳黄芪产地及黄芪采收期提供了依据。     

RP—HPLC法测定瓜蒌子中3，29-二苯甲酰基栝楼仁三醇含量

目的:建立 RP-HPLC 法测定瓜蒌子中3,29-二苯甲酰基栝楼仁三醇的含量。方法:采用 Polaris C_(18)色谱柱(250mm×4.6mm,5μm);以甲醇-水(93:7)为流动相,流速1.0 mL·min~(-1),紫外检测波长为230nm;柱温25℃;进样量5μL。结果:3,29-二苯甲酰基栝楼仁三醇线性范围为0.0484-2.4200μg(r=0.9999),3个浓度的回收率分别为96.19%,100.7%,100.6%(n=3);RSD 分别为3.3%,0.63%,1.2%。结论:本方法简单、重复性好、专属性强,可为评价不同产地的瓜蒌子药材质量提供科学依据。     

RP-HPLC法测定不同产地香青兰药材中迷迭香酸的含量

目的:建立香青兰药材中迷迭香酸含量测定方法,比较不同产地香青兰药材中迷迭香酸含量差异。方法:采用RP-HPLC法进行含量测定,色谱条件:Kromasil C_(18)色谱柱(250 mm×4.6 mm,5μm);流动相为甲醇-0.1%磷酸水溶液(40∶60);流速1.0 m L.min~(-1);柱温35℃;进样量20μL;检测波长330 nm。结果:迷迭香酸含量在0.0414~0.3726 mg.m L~(-1)浓度范围内与峰面积线性关系良好(r=0.9999),平均回收率为98.25%,RSD=0.53%(n=6);不同产地香青兰药材中迷迭香酸含量在0.425%~1.01%之间,差异较大。结论:本文建立了一种快速、准确、经济的测量香青兰药材中迷迭香酸含量的方法,为香青兰药材的质量控制奠定了基础。     

HPLC法测定云南不同产地白花丹的不同部位中白花丹醌的含量

目的:建立白花丹药材中白花丹醌的反相高效液相色谱测定方法,以分别考察云南不同产地白花丹药材的不同部位中白花丹醌的含量。方法:色谱柱为 Kromasil C_(18)柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(70:30),流速为1.0mL·min~(-1),检测波长为254 nm,柱温为25℃。结果:白花丹醌在25.3～253μg·mL~(-1)范围内,具有良好的线性关系,r=0.9998;平均回收率为99.0%,RSD=1.4%(n=6)。不同产地白花丹药材地上部分的白花丹醌含量分别为0.046%(嘎洒),0.079%(勐养),0.134%(嘎东),0.032%(曼东),0.047%(曼阁),0.057%(曼老);根部的白花丹醌含量分别为0.842%(嘎洒),1.04%(勐养),1.44%(嘎东),0.763%(曼东),0.639%(曼阁),1.97%(曼老)。结论:本法简便、准确,灵敏度高,重复性好,可用于控制白花丹药材质量。     

不同产地牛至药材中原儿茶酸的含量分析

目的建立牛至中原儿茶酸的含量测定方法,并测定不同产地牛至药材中原儿茶酸的含量.方法采用高效液相色谱法,Attima C18柱(4.6 mm×250 mm,5 μn),流动相为甲醇-0.15%醋酸水溶液(991),流速1.0 mL·min-1,检测波长260mm.结果线性回归方程为Y=-28.83 3 267X,r=0.999 9,线性范围为0.096 6～0.483 2μg,平均回收率为99.96%.10个不同产地牛至药材,原儿茶酸含量存在一定差异.结论本方法简便、稳定、可靠,可用于牛至中原儿荼酸的含量测定.不同产地牛至药材中原儿茶酸的含量存在一定差异,以贵州、安徽产牛至药材中原儿荼酸的含量较高.     

HPLC-ELSD内标法测定知母药材中菝葜皂苷元含量

目的:建立 HPLC—ELSD 内标法,测定知母药材中菝葜皂苷元含量。方法:采用胆同醇为内标,Kromasil C_(18)柱(250mm×4.6mm,5μm),以甲醇为流动相,流速1 mL·min~(-1)。柱温为30℃。蒸发光散射检测器漂移管温度为50℃,蒸发温度为70℃,以氮气为雾化气,压力为1.03×10~5Pa。结果:菝葜皂苷元进样浓度存0.02～0.50 mg·mL~(-1)内,进样量的常用对数与对照品峰和内标峰面积比值的常用对数成良好线性关系(r=0.9995);平均回收率(n=5)为96.3%,RSD 为2.1%。结论:建立的内标方法准确、快速,是控制知母药材质量较理想的方法。对我国北方主要知母产地药材中菝葜皂苷元含量测定和比较表明不同产地野生知母质量差异较大。     

HPLC法测定枇杷叶中一种橙花叔醇苷的含量

目的:建立HPLC法测定枇杷叶中倍半萜苷—橙花叔醇苷的含量。方法:采用HPLC法测定,色谱柱为Waters Symmetry C18(250 mm×4.6 mm,5μm);流动相为乙腈-水(29∶71);体积流量1.0 ml/min;柱温30℃;检测波长210nm。结果:倍半萜苷在0.009 629~2.006μg/ml(r=0.999 6)范围内与峰面积呈良好的线性关系,平均回收率为96.23%。结论:该方法操作简单,结果准确,专属性好,可用于枇杷叶的质量控制。     

HPLC法测定不同来源甘草中甘草酸的含量

目的:建立以高效液相色谱法测定甘草中有效成分甘草酸含量的方法,并测定不同产地和基原甘草药材中甘草酸的含量。方法:色谱柱为Hypersil-C18(250mm×4.6mm,5μm),流动相为甲醇-0.2mo·lL-1醋酸铵溶液-冰醋酸-三乙胺(64:36:1.5:0.02),流速为1.0mL·min-1,检测波长为252nm,柱温为30℃。结果:甘草酸检测浓度在0.0416～0.2080mg·mL-1范围内与峰面积积分值呈良好线性关系(r=0.9999);平均回收率为101.3%,RSD=1.22%(n=9)。结论:不同来源甘草药材中甘草酸的含量差异较大,野生甘草中甘草酸的含量高于家种。     

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.