华东覆盆子根中没食子酸的提取工艺优选及含量测定

目的:优选华东覆盆子根中没食子酸的提取工艺,并建立其含量测定方法。方法:采用高效液相色谱法测定华东覆盆子根中没食子酸的的含量。通过正交设计试验考察料液比、提取时间和盐酸浓度对没食子酸得率的影响。结果:没食子酸在4.082~40.815μg·ml-1(r=0.999 9)范围内呈良好的线性关系;平均加样回收率为101.28%,RSD=1.08%(n=6)。最佳提取工艺为料液比1∶15,加热回流2.5 h,盐酸浓度4.2%。结论:优选出的提取工艺简单可行,建立的含量测定方法稳定可靠,可用于提取和测定华东覆盆子根中的没食子酸。     

HPLC测定三味蔷薇胶囊中的没食子酸

目的 采用HPLC测定三味蔷薇胶囊中的没食子酸.方法 采用Zorbax Eclipse XDB-C18柱(150 mm×3.9 mm,5 μm),流动相为乙腈-0.2%磷酸溶液(2:98),柱温35℃,流速0.8 mL·min.1,检测波长270 nm.结果 没食子酸3.306-66.12 μg·mL-1与峰面积的线性关系良好(r=0.9996),平均回收率为98.38%(RSD-1.41%,n=9),精密度和重复性的RSD分别为1.15%、1.83%.结论 所建方法简便、快速、灵敏、准确.     

RP-HPLC法测定六味地黄丸中没食子酸的含量

目的:建立 RP-HPLC 法测定六味地黄丸中没食子酸含量的方法。方法:色谱柱:日本岛津 GL Sciences Inc.C_(18)(250mm×4.6mm,5μm),流动相:甲醇-0.1%醋酸水溶液(30∶70),流速:1mL·min~(-1),检测波长为273nm。结果:没食子酸在4-40μg·mL~(-1)范围内,峰面积积分值与浓度呈良好的线性关系(r=0.9995);平均回收率为99.5%,RSD 为2.1%。结论:该法准确、快速、灵敏,重复性好。     

高效液相色谱法测定石榴皮中没食子酸的含量

目的:建立石榴皮提取物中没食子酸含量的高效液相色谱测定法.方法:色谱条件Zobax SB-C18柱(250 mm×4.6 mm,5μm),柱温40℃,用甲醇,石油醚,乙醇,磷酸二氢钾,磷酸梯度洗脱,检测波长为280 nm.结果:没食子酸在0.062 1～0.4140μg范围内呈良好的线性关系,r=0.999 9.平均加样回收率为100.14%,RSD为1.99%.3批样品中石榴皮的含量为9.28～9.52 mg·g-1.结论:本方法精密可靠,可作为石榴皮药材质量控制的方法.     

RP-HPLC测定鬼针草属药材中的没食子酸

目的 比较不同种属和不同药用部位鬼针草中没食子酸的含量.方法 采用RP-HPLC法,用Kromasil C18柱(250mm×4.6 mm,5 μm),柱温为25℃,流动相为甲醇-0.1%磷酸水溶液(8:92),检测波长为274 nm,流速为1 ml·min-1.结果 没食子酸进样量0.03～0.30 μg与峰面积具有良好的线性关系,回归方程为:Y=8.108×104X-3.160×104(r=0.9999,n=6),平均回收率为101.2%.三叶鬼针草根、茎、叶和狼把草、白花鬼针草、婆婆针、三叶鬼针草中没食子酸的含鼍分别为6.16%、6.95%、9.26%、6.99%、8.5%、9.78%、10.3%.结论 所用方法简便、准确、重复性好,可作为控制鬼针草属药材质量的方法;从没食子酸含量的角度考虑,以三叶鬼针草的叶入药最好.     

HPLC测定不同产地的头花蓼中没食子酸的含量

目的 测定不同产地头花蓼中没食子酸的含量.方法 采用依利特Hypersil C18色谱柱(150 mm×4.6 mm,5μm),以乙腈-0.4%磷酸(5:95)为流动相,流速0.8 ml·min-1,检测波长272 nm.结果 没食子酸的线性范围为0.0816～0.4896μg(r=0.9996),平均回收率为97.7%,RSD=0.6%.结论 所建方法准确、简便,可评价不同产地头花蓼质量.     

高效液相色谱法测定复方虫草胶囊中没食子酸的含量

目的:建立测定复方虫草胶囊中没食子酸含量的方法。方法:采用反相高效液相色谱法。色谱柱为ODS C18柱(250 mm×4.6 mm,5μm),甲醇-0.1%磷酸水溶液为流动相,流速为1.0 ml·min-1,检测波长为270 nm,柱温:室温。结果:没食子酸在4.16～24.96μg浓度范围内与峰面积呈线性关系,平均回收率为101.75%,RSD为0.53%(n=5)。结论:方法简便,结果准确,可用于复方虫草胶囊的质量控制。     

高效液相色谱法检测减肥通便茶类保健品中没食子酸的含量

目的建立HPLC法检测减肥通便类保健食品中没食子酸的含量。方法采用Agilent SB-C18柱(4.6mm×250 mm,5μm);柱温为30℃;流动相为甲醇-0.1%磷酸(5∶95);流速为1.0 mL·min-1;检测波长为273 nm;以外标法计算含量。结果没食子酸浓度在2.589¹03.6μg·mL-1内呈良好线性关系,Y=35.03X-1.308,r=1.000,平均回收率为100.5%,RSD为1.9%。结论本方法可用于测定减肥通便类保健食品中没食子酸的含量,灵敏度高、操作简便、准确可靠。     

RP-HPLC测定不同产地和药用部位景天三七中的没食子酸

目的 采用RP-HPLC法测定景天三七不同产地和药用部位中没食子酸的含量.方法 采用Kromasil C18色谱柱(250mm×4.6 mm,5μm),流动相为甲醇-5%醋酸溶液(5;95),流速1 ml·min-1,柱温30℃,检测波长274 nm.结果 没食子酸0.2026～1.2056μg与峰面积的线性关系良好;同归方程为;Y=3.627 × 106X+7.089×105(r=0.9998,n=6);平均回收率为99.5%,RSD=0.73%(n=9).结论 所建方法 简便、准确、重复性好,可用于控制民族药景天三七药材的质量.     

HPLC法测定维药刺山柑种子中没食子酸和芦丁的含量

目的建立刺山柑种子中没食子酸和芦丁的含量测定方法。方法采用Phnomenex色谱柱(250mm×4.6mm,5μm),以乙腈-2mL·L-1磷酸溶液为流动相,流速为1.0mL·min-1,检测波长为254nm,梯度洗脱。结果没食子酸在1.4¹4.0μg、芦丁在1.414.0μg、芦丁在1.4²8.0μg范围内呈良好的线性关系,没食子酸平均回收率为99.9%,RSD为2.0%;芦丁平均回收率为100.6%,RSD为1.3%。结论 HPLC法测定没食子酸和芦丁的含量,方法简便可行,重复性和分离效果好,可为刺山柑的进一步开发利用及质量控制提供依据。     

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.