寒水石不同炮制方法对藏药洁白丸中没食子酸含量的影响

目的探讨寒水石不同炮制方法对藏药洁白丸中没食子酸含量的影响。方法采用热制、精制和猛制等方法对藏药洁白丸处方中的寒水石进行炮制,并采用HPLC法测定没食子酸的含量。色谱柱为WondaCract ODS-2C_(18)(250mm×4.6mm,5μm)柱;流速:1.0mL·min~(-1);柱温:40℃;检测波长:270nm;进样量:10μL;以流动相甲醇(A)~(-1)mL·L~(-1)磷酸溶液(B)(7∶93)洗脱15min。结果寒水石不同炮制方法中洁白丸的没食子酸含量为热制6.582mg·g~(-1),RSD值为1.53%;精制6.603mg·g~(-1),RSD值为0.12%;猛制未检出。结论不同炮制方法影响没食子酸含量,其中猛制的寒水石对没食子酸影响显著,不宜与诃子同方使用,为洁白丸合理配方提供理论依据。     

RP-HPLC法测定金果饮咽喉片中没食子酸的含量

目的建立金果饮咽喉片中没食子酸的含量测定方法。方法采用RP-HPLC测定,色谱柱为Sino Chrom ODS-APC18(250mm×4.6mm,5μm),流动相为甲醇-水-磷酸(6∶94∶0.2),流速1.0mL·min-1,检测波长266nm。结果没食子酸在6~36μg·mL-1浓度范围内呈良好的线性关系(r=0.9996),平均回收率为99.35%,RSD=0.85%。结论本方法准确、简便、重现性好,可作为金果饮咽喉片中没食子酸的含量测定方法。     

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.     

HPLC法同时测定宫炎平胶囊中没食子酸、槲皮素、山柰素的含量

目的:建立宫炎平胶囊中没食子酸、槲皮素和山奈素的含量测定方法。方法:应用高效液相色谱法测定,色谱柱为Agilent-SB C18(250 mm×4.6 mm,5μm),以甲醇和0.3%磷酸水溶液为流动相进行梯度洗脱,流速为1.0 ml·min-1,柱温30℃。结果:没食子酸、槲皮素和山奈素的线性范围分别为98.200~491.000μg·ml-1(r=0.999 9)、7.520~37.600μg·ml-1(r=0.999 9)、4.940~24.700μg·ml-1(r=0.999 9);平均加样回收率分别为96.74%(RSD=1.33%)、98.18%(RSD=1.70%)、97.04%(RSD=1.28%)结论:该方法简便易行、准确、重复性好。     

武当地区及其他产地茶叶中咖啡因和表没食子儿茶素没食子酸酯的含量测定

目的:采用HPLC法测定武当地区不同品种茶叶及其他地区茶叶的咖啡因和表没食子儿茶素没食子酸酯的含量。方法:以Luna-C18柱(250 mm×4.6 mm,5μm)为色谱柱,流动相为乙腈-0.2%磷酸水溶液,梯度洗脱,流速为0.75 ml·min^-1,检测波长为272 nm,柱温为25℃。结果:咖啡因和表没食子儿茶素没食子酸酯的线性范围分别为10.21~102.10μg·ml^-1(r=0.9994)、16.21~162.10μg·ml-1(r=0.9991),平均回收率分别为98.67%(RSD=1.86%,n=6),98.19%(RSD=2.28%,n=6)。结论:该方法用于武当地区及其他地区茶叶的咖啡因及表没食子儿茶素没食子酸酯含量的快速测定,具有简便、稳定性好、准确度高等特点,可以作为茶叶中咖啡因及表没食子儿茶素没食子酸酯含量的测定。     

HPLC法测定玛木然止泻胶囊中盐酸小檗碱与没食子酸的含量

目的采用高效液相色谱法测定玛木然止泻胶囊中盐酸小檗碱和没食子酸的含量。方法色谱柱为Ecosil C18色谱柱(250mm×4.6mm,5μm)。盐酸小檗碱流动相为乙腈-0.05mol·L~(-1)磷酸二氢钾溶液(30∶70),检测波长为345nm,流速为1.0mL·min~(-1);没食子酸流动相为甲醇-2mL·L~(-1)磷酸溶液梯度洗脱,检测波长为270nm,流速为1.0mL·min~(-1)。结果盐酸小檗碱和没食子酸分别在0.211~2.109(r=0.999 1)及0.207~2.071μg·mL~(-1)(r=0.999 6)范围内线性关系良好;平均加样回收率分别为98.20%(RSD=2.20%)和102.52%(RSD=1.28%)。结论该方法准确、简便、重复性好,可用于玛木然止泻胶囊的质量控制。     

HPLC测定覆盆子中没食子酸含量

目的 用高效液相色谱法测定覆盆子中没食子酸的含量.方法 采用Alltech C18柱(250 mm×4.6 mm,5μm),流动相为甲醇- 0.4%磷酸水溶液(10:90),流速1.0 mL·min-1,检测波长278 nm,柱温室温.结果 没食子酸在5.24～104.80 μg·mL-1浓度范围呈良好的线性关系,r=0.999 2,平均回收率为97.6%,RSD为1.9%.结论 本法稳定性、重现性好,可作为覆盆子药材质量控制的依据之一.     

UPLC法同时测定山茱萸生品与酒制品中5个组分的含量

目的:建立UPLC法同时测定山茱萸中没食子酸、5-羟甲基糠醛、莫诺苷、马钱苷和当药苷的含量。方法:ACQUITY UPLCTMHSS C18色谱柱(2.1 mm×100 mm,1.8μm);流动相:乙腈(A)-0.1%甲酸水(B);梯度洗脱(0～3 min,5%A;3～12min,5%A→20%A);流速:0.2 mL·min-1;检测波长:250 nm;柱温:30℃。结果:在上述条件下,没食子酸、5-羟甲基糠醛、莫诺苷、马钱苷和当药苷的质量浓度分别在10.50～525.2μg·mL-1(r=0.9993),10.85～542.5μg·mL-1(r=0.9994),13.50～652.4μg·mL-1(r=0.9999),11.85-592.6μg·mL-1(r=0.9992),5.06～252.8μg·mL-1(r=0.9991)范围内与色谱峰面积呈良好的线性关系;低、中、高浓度的平均加样回收率(n=3)均在97.5%～102.5%之间,RSD均小于2.9%。结论:该方法简便、快速、准确,重复性好,可用于山茱萸药材的质量控制。     

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。     

RP-HPLC法测定余甘子中诃黎勒酸、没食子酸、粘酸-2-O-没食子酸酯的含量

目的:建立RP-HPLC法同时测定余甘子(Phyllanthus emblica L.干燥成熟果实)中诃黎勒酸、没食子酸、粘酸-2-O-没食子酸酯含量。方法:采用Diamonsil C18柱(250 mm×4.6 mm,5μm),以甲醇-0.2%醋酸水溶液(19:81,v/v)为流动相;检测波长为275 nm;流速为1 mL.min-1;柱温为30℃。结果:诃黎勒酸、没食子酸、粘酸-2-O-没食子酸酯线性范围分别为0.235～1.176μg、0.185～0.924μg、0.418～2.09μg;平均回收率(n=6)分别为101.5%,99.20%,101.5%。结论:建立的方法简便,重现性好,可用于余甘子中诃黎勒酸、没食子酸、粘酸-2-O-没食子酸酯的含量测定。     

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.