珠子草总多酚含量研究

目的建立珠子草总多酚含量测定方法,并对珠子草中总多酚含量进行测定。方法采用普鲁士蓝法使酚类物质配位显色,紫外分光光度法测定。结果在0.5274～1.5821μg/ml范围内,没食子酸浓度与吸光度呈良好的线性关系。平均加样回收率99.26%,相对标准偏差(RSD)1.46%。结论分析方法操作简便,精密度及准确度高,重现性及稳定性好,可用于珠子草药材中多酚含量的测定。     

三蕊胶囊中维胺酯含量测定方法的改进

目的改进维胺酯的紫外分光光度检测方法,建立维胺酯的高效液相色谱含量测定方法.方法色谱柱为Hypersil C18,流动相为甲醇-水(90∶10),检测波长为370 nm.结果用紫外检测维胺酯含量在1.0～25.0 μg/ml范围内线性关系良好,平均加样回收率为107.2%(RSD为1.1%,n=9).而用高效液相检测维胺酯含量在1.6～32.0 μg/ml范围内线性关系良好,平均加样回收率为99.6%(RSD为2.0%,n=9).结论采用高效液相测定维胺酯含量方法专属,可排除有关物质和辅料的影响,比用紫外分光光度法测定更准确可靠.     

三蕊胶囊中维胺酯含量测定方法的改进

目的改进维胺酯的紫外分光光度检测方法,建立维胺酯的高效液相色谱含量测定方法。方法色谱柱为HypersilC18,流动相为甲醇-水(90∶10),检测波长为370 nm。结果用紫外检测维胺酯含量在1.0~25.0μg/m l范围内线性关系良好,平均加样回收率为107.2%(RSD为1.1%,n=9)。而用高效液相检测维胺酯含量在1.6~32.0μg/m l范围内线性关系良好,平均加样回收率为99.6%(RSD为2.0%,n=9)。结论采用高效液相测定维胺酯含量方法专属,可排除有关物质和辅料的影响,比用紫外分光光度法测定更准确可靠。     

枸杞多酚提取物中总多酚的测定

目的建立紫外分光光度法测定枸杞多酚提取物中的总多酚。方法采用紫外分光光度法测定枸杞多酚提取物中总多酚,用水稀释样品,加入显色剂Filin-Ciocalteu试剂,在760 nm处测定吸光度,用同样方法测定并绘制标准曲线。结果紫外分光光度法测定枸杞多酚提取物中总多酚的量分别为24.03%、26.38%、25.45%、28.27%、29.08%,线性范围1～8μg/mL,R2=0.999 5。平均回收率为103.5%,RSD<5%。结论该方法操作简单,准确可靠,适于枸杞多酚提取物中总多酚的测定。     

玳玳黄酮提取物的质量标准研究

目的：建立玳玳黄酮提取物的质量标准。方法：采用薄层色谱法鉴别玳玳黄酮提取物中的柚皮苷和新橙皮苷;采用紫外分光光度法测定玳玳黄酮提取物中总黄酮含量;采用高效液相色谱法同时检测玳玳黄酮提取物中柚皮苷和新橙皮苷的含量。结果：薄层色谱斑点清晰,易于识别,专属性强;紫外分光光度法新橙皮苷在4．44～26．64μg·mL-1范围内呈良好线性关系,平均加样回收率为99．92％（RSD=1．65％）;HPLC法柚皮苷在1.988—13．916μg·mL-1范围内呈良好线性关系,平均加样回收率为99．73％（RSD=1．56％）,新橙皮苷在1．992～13．944μg·mL-1范围内呈良好线性关系,平均加样回收率为99．58％（RsD=1．89％）。结论：所建方法操作简便,结果准确,可有效控制玳玳黄酮提取物的质量。     

高效液相色谱法与紫外光谱法测定索拉非尼原料药含量的比较

目的 分别采用高效液相色谱(HPLC)法与紫外分光光度(UV)法对相同批号的索拉非尼原料药进行含量测定并进行比较.方法 高效液相色谱法中,色谱柱为Inertsil ODS-3柱(250 mm×4.6 mm,5 μm),流动相为乙酸铵缓冲液(50 mmol/L)-乙腈(28:72),检测波长为265 nm,流速为1.0 mL/min,柱温为40℃,进样量为50μL.紫外分光光度法中,索拉非尼原料药样品溶液用甲醇配制,在265 mm波长处进行测定.结果 高效液相色谱法测得索拉非尼进样质量浓度在0.5～40 μg/mL(r=0.99999)范围内与峰面积线性关系良好,平均加样回收率为102.92%,RSD=1.30%(n=9).紫外分光光度法测得索拉非尼进样质量浓度线性范围是0.1～20 μg/mL(r=0.999 9).紫外分光光度法含量测定结果比高效液相色谱法平均高出1.067倍.结论 紫外分光光度法不适用于准确测定索拉非尼原料药的含量.高效液相色谱法的专属性好、稳定性、精密度以及加样回收率都较好,适用于索拉非尼原料药含量的准确测定.     

续断壮骨胶囊中总皂苷和川续断皂苷VI含量测定

目的：建立续断壮骨胶囊中总皂苷和川续断皂苷遇的含量测定方法。方法：采用高氯酸显色,紫外-可见分光光度法测定总皂苷含量。采用高效液相色谱法测定川续断皂苷遇含量,Agilent C18柱（250 mm 215;4.6 mm,5μm）,乙腈-0.15%三氟乙酸水溶液（29∶71）为流动相,检测波长215 nm ,流量1.0 mL/min。结果：总皂苷平均含量为86.3%,平均加样回收率为99.88%, RSD =1.52%;川续断皂苷遇在64～320μg/mL 范围内呈良好线性关系（r =0.9995）,平均加样回收率为100.4%, RSD =0.77%。结论：所建方法准确,能快速测定续断壮骨胶囊总皂苷和川续断皂苷遇的含量,可用于该制剂的质量控制。     

泽泻提取物三萜类成分含量测定研究

目的:建立紫外-可见分光光度法和高效液相色谱法测定泽泻提取物中三萜类成分含量。方法:采用紫外-可见分光光度法,以5%香草醛(用冰醋酸配制)-高氯酸显色,在555 nm波长处测定吸光度,计算泽泻提取物总三萜含量;应用高效液相色谱法同时测定泽泻提取物中12个三萜类成分,采用Ultimate XB-C18色谱柱(4.6 mm×150 mm,5μm),以乙腈-5%甲醇水为流动相梯度洗脱,流速1.0 m L·min-1,检测波长208 nm。结果:紫外-可见分光光度法测定总三萜含量,以23-乙酰泽泻醇B计,质量浓度在5.9~15.6μg·m L-1范围内与吸光度值呈良好线性关系(r=0.999 1),平均加样回收率99.05%,RSD为2.3%;高效液相色谱法测定12个泽泻三萜类成分含量,在考察的浓度范围内,线性关系良好(r>0.999 0),回收率均在95.89%~99.33%范围内,RSD为2.0%~3.4%。泽泻提取物中12个三萜类成分的含量:泽泻醇A 5.71%~5.95%、泽泻醇B 3.47%~3.99%、泽泻醇C 2.53%~2.97%、泽泻醇G 3.07%~3.93%、泽泻醇L 3.65%~3.99%、23-乙酰泽泻醇A 2.39%~3.02%、23-乙酰泽泻醇B 10.56%~11.32%、23-乙酰泽泻醇C 9.44%~9.86%、16-羰基-23-乙酰泽泻醇A 0.63%~3.14%、16-羰基-24-乙酰泽泻醇A 1.08%~1.21%、11-去氧泽泻醇B 2.29%~2.85%、24-乙酰泽泻醇A 4.04%~5.02%。结论:经方法学验证,本文建立的紫外-可见分光光度法可以用于检测泽泻提取物中总三萜含量,高效液相色谱法可用于检测泽泻提取物中12个泽泻三萜类成分含量。     

蒙药山沉香醋酸乙酯提取物中开环异落叶松树脂酚和总木脂素含量测定

目的：分别建立高效液相色谱法和紫外-可见分光光度法测定蒙药山沉香（Syringa pinnatifolia.）醋酸乙酯提取物中开环异落叶松树脂酚[（-）-secoisolariciresinol,SECO]含量和总木脂素含量。方法：采用95%乙醇对山沉香加热回流提取,采用醋酸乙酯萃取。利用高效液相色谱法,测定山沉香醋酸乙酯提取物中SECO含量。色谱柱：Agilent C₁₈色谱柱,流动相：甲醇-0.1%甲酸溶液,流速：0.5 mL·min^-1,柱温：30℃,检测波长：280 nm。利用紫外-可见分光光度法,以SECO为标准品,于280 nm波长处测定山沉香醋酸乙酯提取物中总木脂素含量。结果：高效液相色谱法中,SECO质量浓度在0.028~0.280 mg·mL^-1范围内与峰面积线性关系良好,线性方程为：Y=2 838.6X+59.354（r²=0.999 7）;平均加样回收率（n=9）为99.27%,RSD为1.55%（n=9）。紫外-可见分光光度法中,SECO质量浓度在0.002 6~0.084 0 mg·mL^-1范围内与吸光度线性关系良好,线性方程为：Y=21.393X+0.03（r²=0.999 4）;平均加样回收率为100.06%,RSD为1.12%（n=9）。结论：该方法操作简便可靠,适用于山沉香醋酸乙酯提取物中总木脂素及有效成分的含量测定及质量控制。     

新麻滴鼻液中盐酸麻黄碱与硫酸新霉素的含量测定

目的:建立新麻滴鼻液中盐酸麻黄碱和硫酸新霉素的含量测定方法.方法:用高效液相色谱法测定样品中盐酸麻黄碱的含量;用分光光度法测定样品中硫酸新霉素的含量.结果:盐酸麻黄碱在0.05～1.50 g·L-1范围内线性关系良好,r=0.999 8,平均回收率为101.28%(RSD≤1.16%);硫酸新霉素在60～420 IU·mL-1范围内线性关系较好,r=0.999 0,平均回收率为102.19%(RSD≤2.74%).结论:所建立的测定方法准确、重复性好、实用.     

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.     

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.     

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.