清热解毒口服液主要活性成分的定量分析

目的:建立清热解毒口服液中黄芩苷、栀子苷、连翘苷、绿原酸的定量测定方法.方法:色谱柱Shim-Pack VP-ODS C18色谱柱(250 mm×4.6 mm,5 μm);流动相甲醇-0.1%磷酸梯度洗脱;检测波长为227 nm.结果:黄芩苷、栀子苷、连翘苷、绿原酸分别在0.200 2~2.002 mg·ml-1(r=0.999 8)、0.144 6~1.446 mg·ml-1(r=0.999 9)、0.102 8~1.028 mg·ml-1(r=0.999 9)、0.129 8~1.298 mg·ml-1(r=0.999 5)范围内线性关系良好;其各自平均回收率分别为96.49%、96.09%、95.64%和97.82%.结论:该方法准确、简便、快速,可以用于定量测定清热解毒口服液中黄芩苷、栀子苷、连翘苷、绿原酸的含量.     

不同采收时期及干燥方法对栀子中栀子苷含量的影响

目的:评价不同采收期以及不同干燥方法对栀子苷的影响.方法:应用高效液相色谱法测定,色谱柱为Agilent Zorbax XDB-C18色谱柱(150 mm×4.6 mm,5 μm);流动相为乙腈-水(15:85),流速1.0 ml·min-1;柱温:30℃;检测波长238 nm.结果:栀子苷的线性范围为0.31～155.76 μg·ml-1(r=0.999 9),加样回收率为100.9%(RSD=1.2%);定量分析了6个采收时间、12种干燥方法的栀子中栀子苷含量.结论:不同采收时期、不同干燥方法对栀子中栀子苷的含量有一定的影响.     

HPLC法测定栀子柏皮软胶囊中栀子苷和小檗碱的含量

目的:建立栀子柏皮软胶囊中指标性成分栀子苷和小檗碱的含量测定方法。方法:采用 Diamonsil ODS-C_(18)柱(5μm,4.6 mm×150 mm);栀子苷的测定以乙腈-水(15:85)为流动相,流速:1.0 mL·min~(-1),检测波长为238 nm;小檗碱的测定以乙腈-0.05%磷酸水溶液-十二烷基硫酸钠(55:45:0.1)为流动相,流速:1.0 mL·min~(-1),检测波长为265 nm。结果:栀子苷的线性范围为10.2～50.3 mg·mL~(-1),平均回收率为96.8%(n=9),RSD 为1.5%;小檗碱在9.5～66.4μg·mL~(-1)浓度范围内线性关系良好,平均回收率为97.4%(n=9),RSD 为1.3%。结论:本方法简便、灵敏,重现性好,适用于栀子柏皮软胶囊的质量控制。     

UPLC法快速测定栀子复方制剂中栀子苷和西红花苷-1含量

目的建立快速测定栀子复方制剂复方牛黄消炎胶囊、清胃黄连丸和龙泽熊胆胶囊中栀子苷和西红花苷-1的方法。方法采用UPLC法。色谱柱为BEH C18柱(50mm×2.1mm,1.7μm);流动相:甲醇-水以不同梯度洗脱;流速:0.3mL·min~(-1);检测波长:0~7min为238nm,7~20min为440nm;柱温:30℃;进样量为2μL。结果 3种复方制剂中栀子苷在0.010~1.000mg·mL~(-1)范围内呈良好的线性关系(r=0.999 9),平均回收率分别为98.2%,99.9%和100.3%,RSD分别为1.3%,1.4%和1.0%;西红花苷-1在0.1~10.0μg·mL~(-1)范围内呈良好的线性关系(r=0.999 9)。平均回收率分别为99.6%,97.4%和98.3%,RSD分别为1.3%,1.4%和1.5%。结论栀子苷和西红花苷-1在20min内获得良好分离,该方法简便、准确、快速,可用于栀子复方制剂中栀子苷和西红花苷-1的测定。     

HPLC法测定肝宁丸中栀子苷的含量

目的:应用高效液相色谱法对肝宁丸中栀子苷进行含量测定.方法:选用依利特Hypersil C18分析柱(150 mm×4.6 mm,5μm),乙腈-水(11:89)为流动相,检测波长为238 nm,流速1.0 ml · min-1.结果:栀子苷在0.016 7～0.333 2 mg·ml-1具有良好的线性关系,r=1.000 0,平均回收率为96.10%,RSD为0.96%.结论:本试验所确定的质量分析方法稳定可靠,可作为肝宁丸中栀子苷的含量测定方法.     

HPLC测定鼻窦炎颗粒中的栀子苷

目的:采用HPLC法测定鼻窦炎颗粒中的栀子苷.方法:色谱柱为Agilent ZORBAX SB-C18(250 mm×4.6 mm,5μm),流动相为水.乙腈.磷酸(86:14:0.01),检测波长238 am,流速1.0 ml·min-1,柱温30℃.结果:栀子苷浓度3.36～126μg·ml-1,与峰面积的线性关系良好(r=0.999 9),平均加样回收率98.09%,RSD=1.69%.结论:所建方法准确、重复性好,可用于测定鼻窦炎颗粒中的栀子苷.     

高效液相色谱法测定五味沙棘散中栀子苷的含量

目的:建立高效液相色谱法测定五味沙棘散中栀子苷的含量.方法:色谱柱为Waters Xttera C18(4.6 mm×250mm,5μm),流动相为乙腈一水(13:87),流速为1.0 mL·min-1,柱温为25℃,检测波长为238 nm.结果:在10.24～102.4 mg·L-1范围内,栀子苷的进样浓度与吸收峰积分值呈良好的线性关系,r=0.9995,平均回收率为100.77%,RSD为1.73%.结论:该方法简便,准确,可用于五味沙棘散中栀子苷的含量测定.     

多波长高效液相色谱法测定四季三黄胶囊中4种主药成分含量

目的 :同时测定四季三黄胶囊中大黄酸、黄芩苷、盐酸小檗碱和栀子苷的含量。方法 :紫外 -可见四波长同时检测的高效液相色谱法。色谱柱为 Diamonsil C1 8柱 (2 5 0 mm× 4 .6 mm ,5μm) ;流动相为甲醇 (A)水 (B) (含 0 .0 33mol/ L磷酸二氢钾 ,0 .3%磷酸 ) ;流速为 1ml/ min;柱温为 32 o C;检测波长为 2 2 8nm(大黄酸 ) ,2 78nm(黄芩苷 ) ,35 0 nm(盐酸小檗碱 ) ,2 36 nm(栀子苷 ) ;线形梯度洗脱。结果 :平均回收率分别为大黄酸 97.9%、黄芩苷 98.4 %、盐酸小檗碱 10 2 .2 %、栀子苷 99.3%。结论 :为四季三黄胶囊提供了更全面、有效的质控方法。     

龙胆泻肝胶囊中龙胆苦苷与栀子苷的含量测定

目的建立同时测定龙胆泻肝胶囊中龙胆苦苷和栀子苷含量的高效液相分析法。方法采用WatersSunfire C18色谱柱(4.6 mm×250 mm,5μm);乙腈和0.1%磷酸溶液为流动相,梯度洗脱;流速:1.0 mL.min-1;柱温:25℃;检测波长:237和270 nm。结果龙胆苦苷在0.285 8～1.429 0μg(r=0.999 9)、栀子苷在0.402 0～2.010 0μg(r=0.999 8)范围内呈良好的线性关系;龙胆苦苷回收率98.99%(RSD=1.20%),栀子苷回收率99.08%(RSD=0.94%)。结论该方法简便、准确,重复性好,可用于同时测定龙胆泻肝胶囊中栀子苷和龙胆苦苷含量。     

高效液相色谱法测定连朴饮不同煎液中栀子苷的含量

目的:考察用合煎液(传统汤剂)、分煎液(配方颗粒汤剂)方法制备的连朴饮汤剂中栀子苷含量的变化。方法:建立高效液相色谱(HPLC)法,采用Diamonisl C18柱(200 mm×4.6 mm,5μm);流动相为乙睛∶水(20∶80);流速为1 mL·min-1;检测波长为238 nm。结果:连朴饮分煎液中栀子苷平均含量比合煎液中栀子苷平均含量高。结论:与传统汤剂比较,连朴饮配方颗粒汤剂中栀子苷的含量高。     

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.     

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.     

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.