不同厂家香连丸中木香烃内酯和去氢木香内酯的含量测定

目的建立同时测定香连丸中木香烃内酯和去氢木香内酯含量的方法,分析不同厂家香连丸中两成分含量。方法采用高效液相色谱法,色谱条件:Chromsil C18色谱柱(4.6 mm×200 mm,5μm),以甲醇-水(65∶35)为流动相,流速1 m L·min-1,检测波长225 nm,柱温30℃。结果木香烃内酯、去氢木香内酯分别在0.009 4~0.023 6μg和0.021 8~0.108 8μg进样量范围内与峰面积呈良好的线性关系(r=0.999 6,0.999 2),木香烃内酯、去氢木香内酯的回收率均在95%~105%。不同厂家香连丸中木香烃内酯、去氢木香内酯的含量范围分别为0.16~0.83 mg·g-1和1.45~7.40 mg·g-1。结论该方法可准确测定香连丸中木香烃内酯、去氢木香内酯的含量,市售香连丸中两成分含量差别较大,需要加强其质量控制。     

RP-HPLC法同时测定保济丸中厚朴酚、和厚朴酚、木香烃内酯及去氢木香内酯的含量

目的:建立RP-HPLC法同时测定保济丸中厚朴酚、和厚朴酚、木香烃内酯及去氢木香内酯的含量。方法:采用AgilentExtent-C18(250 mm×4.6 mm,5μm)色谱柱,以乙腈-水(47∶53)为流动相,流速为1.0 mL.min-1,柱温为35℃,检测波长为225 nm。结果:厚朴酚、和厚朴酚、木香烃内酯及去氢木香内酯的浓度分别在2.744～137.2μg.mL-1(r=0.9999),2.836～141.8μg.mL-1(r=0.9999),3.164～158.2μg.mL-1(r=0.9998)及3.148～157.4μg.mL-1(r=0.9999)范围内与峰面积线性关系良好;方法回收率(n=3)为96.3%～102.7%,RSD为0.2%～1.7%。结论:本方法简便、准确,重复性好,可用于同时测定保济丸中厚朴酚、和厚朴酚、木香烃内酯及去氢木香内酯的含量。     

高效液相色谱法测定七味广枣丸中木香烃内酯和去氢木香内酯的含量

目的:建立高效液相色谱法测定七味广枣丸中木香烃内酯和去氢木香内酯含量。方法:采用Agilent ZORBAX EclipseSB-C18(4.6 mm×150 mm,5μm)色谱柱,流动相为5%乙腈-乙腈(58∶42),流速1 mL.min-1,检测波长为225 nm。结果:木香烃内酯和去氢木香内酯的保留时间分别约为21 min和24 min,与相邻峰的分离度大于1.5;线性范围分别为7.400~185.0μg.mL-1(r=0.9999)和5.950~148.8μg.mL-1(r=0.9998);平均回收率(n=6)分别为101.3%和97.0%,RSD均为1.6%。结论:该法操作简便,测定结果准确,重复性好,可用于七味广枣丸中木香烃内酯和去氢木香内酯的含量测定。     

HPLC法测定五味香连丸中木香烃内酯和去氢木香内酯的含量

目的建立五味香连丸中木香烃内酯和去氢木香内酯含量测定的方法。方法采用RP-HPLC法,Phenomenexluna C18(2)柱(5μm,250mm×4.60mm);流动相:甲醇-水(65:35);流速:1.0ml/min;检测波长225nm;柱温:室温。结果木香烃内酯平均回收率为101.8%,RSD=1.22%,去氢木香内酯平均回收率为99.16%,RSD=1.55%。结论本法准确可靠、灵敏度高、专属性强,可作为本制剂质量控制方法之一。     

HPLC法测定复方黄连素片中木香烃内酯和去氢木香内酯的含量

目的建立高效液相色谱法测定复方黄连素片中木香烃内酯和去氢木香内酯的含量方法。方法采用高效液相色谱法测定复方黄连素片中木香烃内酯和去氢木香内酯的含量。色谱柱为C18柱(250×4.6mm,5μm),流动相为乙腈-0.1%磷酸溶液(53∶47),检测波长为225nm。结果木香烃内酯在0.04～1.04μg范围内线性关系良好,r=0.9999,平均回收率99.60%,RSD(n=6)为1.58%;去氢木香内酯在0.04～1.02μg范围内线性关系良好,r=0.9999,平均回收率99.76%,RSD(n=6)为1.25%。结论方法简便、准确,重复性好,可作为复方黄连素片的定量控制方法。     

RP-HPLC法测定胃痛七味散中木香烃内酯和去氢木香内酯的含量

目的:建立以反相高效液相色谱法测定胃痛七味散中木香烃内酯和去氢木香内酯含量的方法。方法:色谱柱为Zorbax SB-C18(150mm×4.6mm,5μm),流动相为甲醇-水(62.5∶37.5),检测波长为225nm。结果:木香烃内酯的进样量在16.8～252μg范围内与峰面积积分值呈良好的线性关系(r=0.9993),平均回收率为97.70%(RSD=1.24%,n=6);去氢木香内酯的进样量在27.2～408μg范围内与峰面积积分值呈良好的线性关系(r=0.9998),平均回收率为97.98%(RSD=1.30%,n=6)。结论:本法简便、灵敏、快速,可用于胃痛七味散的质量控制。     

HPLC法测定肠康片中木香烃内酯和去氢木香内酯的含量

目的建立肠康片中木香烃内酯和去氢木香内酯的HPLC含量测定方法。方法色谱柱为安捷伦Eclipse-XDB-C18柱（250mm×4.6mm,5μm）,甲醇-水（65：35）为流动相,流速：1.0mL.min-1,检测波长为225nm,柱温：35℃。结果木香烃内酯在0.045～0.89μg范围内线性关系良好（r=0.99996）,平均回收率为98.5%,RSD=0.2%（n=6）;去氢木香内酯在0.058～1.17μg范围内线性关系良好（r=1.0000）,平均回收率为100.8%,RSD=0.2%（n=6）。结论方法准确可靠,可作为肠康片的质量控制方法。     

HPLC法测定归脾丸中木香烃内酯和去氢木香内酯的含量

目的 建立HPLC法测定归脾丸中木香烃内酯和去氢木香内酯的含量的方法.方法 采用HPLC法,色谱柱为Agilent Eclipse SB-C18柱（150mm×4.6mm,5μm）,流动相为乙腈：0.1%磷酸溶液（45：55）,流速为1.0mL·min-1,检测波长为225nm.结果 木香烃内酯在0.1018～1.018μg间线性良好,r=0.9999,平均回收率为99.37%,RSD（n=9）为1.2%;去氢木香内酯在0.1034～1.034μg间线性良好,r=0.9999,平均回收率为98.60%,RSD（n=9）为0.9%.结论 该方法灵敏、准确、简便、重复性好,可作为归脾丸的定量控制方法.     

HPLC法测定五味麝香丸中木香烃内酯和去氢木香内酯的含量

目的:建立了HPLC法同时测定五味麝香丸中木香烃内酯和去氢木香内酯含量的方法。方法:色谱柱:WelchromMaterials柱C₁₈（250mm×4.6mm,5μm）,流动相:甲醇-水（65:35）;检测波长:225nm;流速:1.0ml·min^-1。结果:木香烃内酯在0.0115～0.1150mg·ml^-1的浓度范围内呈良好的线性关系（r=0.9999）,平均回收率为99.00%（RSD=0.90%）;去氢木香内酯在0.0119～0.1190mg·ml^-1的浓度范围内呈良好的线性关系（r=0.9998）,平均回收率为99.23%（RSD=1.02%）。结论:本方法快速、灵敏、准确,适用于五味麝香丸中木香的含量测定。     

RP-HPLC法同时测定雪胆胃肠丸中木香烃内酯和去氢木香内酯的含量

目的:建立以反相高效液相色谱法同时测定雪胆胃肠丸中木香烃内酯和去氢木香内酯含量的方法。方法:色谱柱为Shim-pack VP-ODS(150mm×4.6mm,5μm),流动相为甲醇-水(60∶40),检测波长为225nm。结果:木香烃内酯、去氢木香内酯的检测浓度分别在13.6～272.0、11.25～225.0μg·mL-1范围内与各自峰面积积分值呈良好的线性关系(r均为0.9998);二者平均回收率分别为99.47%和99.62%,RSD分别为1.75%和1.14%(n均为6)。结论:本方法简便易行、准确可靠,可用于雪胆胃肠丸的质量控制。     

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.     

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.