蜂胶挥发油中高良姜素与白杨素的含量测定

目的:建立蜂胶挥发油中高良姜素与白杨素的含量测定方法。方法:采用高效液相色谱法,选用色谱柱为Agilent ZORBAX Extend(150mm×4.6mm,5μm)C18柱;流动相为甲醇-0.15%磷酸溶液(60∶40),流速为1.0mL/min,检测波长为268nm。结果:高良姜素进样量的质量浓度在0.01031～0.16500μg/mL范围内,线性关系良好(r=0.9996),平均回收率为98.79%,RSD=2.78%;白杨素在0.00938～0.15000μg/mL范围内,线性关系良好(r=0.9998);平均回收率为98.73%,RSD=2.89%。结论:该法简便、快速、准确,重现性好,适用于蜂胶挥发油的质量控制。     

HPLC法测定蜂珍膏中白杨素的含量

目的:建立以高效液相色谱法测定蜂珍膏中白杨素含量的方法.方法:色谱柱:Zorbox SB-C18柱(150 mm×4.6 mm, 5μm);流动相:甲醇-0.1%甲酸;梯度洗脱:0→35 min,甲醇-0.1%甲酸比例由50:50→75:25(v/v);流速:1.0 ml·min-1;检测波长:267 nm;柱温:25℃;进样量:10.0μl.结果:白杨素在0.61～4.3 μg·ml-1 (r=0.9996)范围内与峰面积积分值呈良好的线性关系;平均加样回收率为99.3%,RSD=1.4%(n=6).结论:本方法可靠、灵敏、准确、易行,可用于蜂珍膏的质量控制.     

加杨树叶中3种黄酮类成分的含量测定

目的 建立同时测定加杨树叶中的槲皮素、高良姜素、白杨素含量的分析方法。方法 采用高效液相色谱法,色谱柱Agilent TC C18柱（4.6 mm×250 mm,5μm）,流动相：甲醇-0.1%甲酸,梯度洗脱：0∽5 min,甲醇25%→55%,5∽25 min,甲醇55%→65%,25∽35 min,甲醇65%→75%;流速：1.0 mL.min 1;检测波长：264 nm;柱温：30℃。结果 加杨树叶中槲皮素、高良姜素、白杨素分离效果良好,线性范围分别为3.7∽120,2.5∽80和3.125∽100μg.mL 1;平均加样回收率分别为99.0%,100.1%,101.4%。结论 该方法准确可靠、结果稳定、重复性好,可为评价加杨树叶的质量提供依据。     

HPLC法测定北刘寄奴中木犀草素和芹菜素的含量

目的:建立同时测定北刘寄奴中木犀草素和芹菜素含量的HPLC方法。方法:采用Inertsil ODS-3(4.6 mm×150 mm,5μm)色谱柱,以乙腈-0.5%磷酸(28∶72)为流动相,流速1.0 mL.min-1,检测波长340 nm,柱温35℃。结果:木犀草素和芹菜素进样量分别在0.2168～1.951μg和0.0684～0.615μg范围内与峰面积呈良好的线性关系(r=0.9999);木犀草素和芹菜素平均加样回收率(n=5)分别为99.7%和99.1%,RSD分别为0.99%和1.5%。结论:该方法简便、准确、可靠,可用于中药北刘寄奴中木犀草素和芹菜素含量的测定。     

HPLC法同时测定芩连片中黄芩苷﹑黄芩素和汉黄芩素的含量

目的建立同时测定芩连片中黄芩苷、黄芩素和汉黄芩素含量的HPLC方法。方法采用Dia-monsil C18柱(200 mm×4.6 mm,5μm)分离,以甲醇-体积分数为0.4%的磷酸溶液为流动相梯度洗脱,流速为1.0 mL.min-1,检测波长为277 nm,柱温为35℃。结果黄芩苷、黄芩素及汉黄芩素的线性范围分别为36.8～368.0 mg.L-1(r=0.999 7)、1.75～17.5 mg.L-1(r=0.999 8)、1.50～15.0mg.L-1(r=0.999 9),黄芩苷、黄芩素、汉黄芩素的平均回收率分别为97.3%(RSD=1.8%)、101.1%(RSD=1.8%)、99.0%(RSD=2.0%)。结论 HPLC法可用于芩连片的质量控制。     

HPLC法测定紫果西番莲叶中白杨素的含量

目的:建立测定紫果西番莲叶中白杨素含量的方法。方法:样品经硅胶柱色谱分离纯化后进行高效液相色谱分析。色谱柱为HypersilODSC18(250mm×4.6mm,5μm),流动相为乙腈-0.1磷酸(18:82),流速为1.0mL.min-1,检测波长为220nm,进样量为10μL。结果:白杨素进样浓度在0.012～0.120mg.mL-1范围内与峰面积积分值呈良好线性关系(r=0.9980);平均加样回收率为99.41%,RSD=1.6%(n=6)。结论:该方法准确、可靠、重复性好,可用于西番莲属植物中白杨素含量的测定。     

HPLC法测定冠心通胶囊中丹参素的含量

建立冠心通胶囊中丹参素的HPLC测定方法。色谱柱为Hypersil C18,流动相为甲醇-水-冰醋酸(8∶91∶1),流速:1.0mL·min-1,柱温:30℃,检测波长:281nm,丹参素在0.052~0.520μg范围内呈良好的线性关系(r=0.9998),平均回收率为100.8%,RSD=1.4%(n=5)。方法准确可靠,操作简便,稳定性好。     

HPLC法同时测定阿娜尔妇洁液中蛇床子素和欧前胡素的含量

目的建立HPLC法同时测定阿娜尔妇洁液中蛇床子素和欧前胡素含量的方法。方法色谱柱为C18(250mm×4.6mm,5μm),柱温25℃;流动相为甲醇-水(65∶35),流速1.0mL·min-1;检测波长310nm。结果蛇床子素和欧前胡素分别在0.051~0.816μg(r=0.9996)和0.026~0.416μg(r=0.9998)范围内线性关系良好,平均回收率分别为98.4%和98.7%,RSD分别为1.2%(n=6)和2.1%(n=6)。结论方法简便,结果准确,重现性好,可用于阿娜尔妇洁液中蛇床子素和欧前胡素的含量测定。     

反相高效液相色谱法测定黄芩素长循环脂质体中黄芩素含量

目的建立RP-HPLC法测定黄芩素长循环脂质体中黄芩素的含量。方法色谱柱:Anglent HC-18(4.6 mm×250 mm,5μm);流动相:水-乙腈-甲醇(50∶30∶20);柱温:30℃;流速:1 mL/min;检测波长:280 nm。结果辅料及溶剂对黄芩素测定无干扰,黄芩素在0.1~1μg猤范围内线性关系良好(r=0.999 5),黄芩素平均加样回收率为98.46%(RSD=0.89%)。结论本法便捷、准确、重复性好,可用于黄芩素长循环脂质体含量的测定。     

RP-HPLC法测定气血双生合剂中淫羊藿苷、蛇床子素、五味子甲素与五味子乙素的含量

目的:建立高效液相色谱法测定气血双生合剂中淫羊藿苷、蛇床子素、五味子甲素、五味子乙素含量的方法.方法:Ultimate XB-C18柱(4.6mm×150 mm,5μm);流速:1.0mL·min-1;柱温:30℃;流动相:乙腈-水梯度洗脱;并切换检测波长;进样量:5μL.结果:淫羊藿苷在浓度为5.015～80.24μg·mL-1时线性关系良好,r=0.9999,平均回收率为100.2%,RSD为1.3%(n=6);蛇床子素在浓度为2.750～44.00μg·mL-1时线性关系良好,r=0.9997,平均回收率为100.40%,RSD为1.7%(n=6);五味子甲素在浓度为5.320～85.12μg·mL-1时线性关系良好,r=0.9997,平均回收率为101.2%,RSD为1.2%(n=6);五味子乙素在浓度为2.810～44.96μg·mL-1时线性关系良好,r=0.9996,平均回收率为101.9%,RSD为1.6%(n=6).结论:该方法简单、准确,能同时测定几种有效成分的含量,可作为气血双生合剂的质量控制.     

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.