反相高效液相色谱法测定金银花及抗感颗粒中绿原酸的含量

目的建立反相高效液相色谱法测定抗感颗粒中绿原酸的含量。方法采用Hypersil C18(250mm×4.6mm,5μm)色谱柱;以乙腈-0.4%磷酸溶液(13∶87)为流动相,流速为1.0mL.m in-1,柱温为室温,检测波长为327nm,以外标法测定了金银花药材及抗感颗粒中绿原酸的含量。结果绿原酸在2.24~26.88μg.mL-1内呈线性关系。绿原酸在制剂中的平均回收率(n=5)为99.3%(RSD=0.99%)。结论该方法准确、简便、重现性好,可用于抗感颗粒的质量控制。     

RP-HPLC法测定抗感颗粒中芍药苷和绿原酸的含量

目的:建立同时测定抗感颗粒中芍药苷和绿原酸含量的方法。方法:采用反相高效液相色谱法。色谱柱为HypersilODS柱,流动相为甲醇-水-冰醋酸(28:72:0.5),流速为1.0mL·min-1,检测波长分别为235nm和327nm,进样量为10μL,柱温为25℃。结果:芍药苷进样量在1.628～4.884μg范围内与峰面积积分值线性关系良好(r=0.9996,n=5),平均加样回收率为99.97%,RSD=1.32%;绿原酸进样量在0.584～1.752μg范围内与峰面积积分值线性关系良好(r=0.9997,n=5),平均加样回收率为100.19%,RSD=1.37%。结论:该方法简便易行,结果准确稳定,可用于抗感颗粒的质量控制。     

高效液相色谱程序可变波长法测定银黄颗粒中绿原酸和黄芩苷的含量

目的:测定银黄颗粒中绿原酸、黄芩苷的含量。方法:利用二极管阵列检测器的程序可变波长功能,在绿原酸、黄芩苷的最大吸收波长(λmax)同时测定银黄颗粒中绿原酸、黄芩苷含量。HiQsilC18色谱柱;柱温为30℃;流动相为甲醇(A)-0.2%磷酸(B);流速为1mL.min-1;梯度洗脱,0～5min,40%A;5～15min,40%A线性增加至80%A;15min后,80%A;检测波长程序设置为0～5min,327nm(绿原酸);5～15min,280nm(黄芩苷)。结果:绿原酸进样量在0.072～0.72μg范围内线性关系良好(r=0.9999),黄芩苷进样量在0.91～9.1μg范围内线性关系良好(r=0.9999),绿原酸、黄芩苷平均加样回收率为98.0%,97.6%,RSD分别为1.43%,1.87%。结论:该方法简便、准确,具有较好的重复性,可作为银黄颗粒制剂的质量控制方法。     

高效液相色谱法测定清肝颗粒中绿原酸的含量

目的 　建立 HPL C法测定清肝颗粒中绿原酸含量的方法。方法 　采用 Nova-pak C1 8色谱柱 ,流动相 :甲醇 -冰醋酸 -三乙胺 (14∶ 86∶ 1∶ 0 .3 ) ,流速 :1ml· min- 1 ,检测波长 :3 2 7nm,室温下对清肝颗粒中的绿原酸进行含量测定。结果　绿原酸在 0 .2 5 6～ 0 .5 12μg范围内 ,线性关系良好 (r=0 .99981) ;平均加样回收率为 99.5 3 % ,RSD为 1.5 2 % (n=6)。结论 　本方法准确 ,简便 ,灵敏度高 ,结论可靠 ,可作为清肝颗粒的质量控制标准。     

高效液相色谱法测定小儿清热宁颗粒中绿原酸和黄芩苷的含量

目的:建立以高效液相色谱法测定小儿清热宁颗粒中绿原酸和黄芩苷含量的方法。方法:色谱柱为SymmetryShieldRPC18,流动相绿原酸、黄芩苷分别为乙腈-0·4%磷酸溶液(13∶87)、甲醇-水-冰醋酸(50∶50∶1),检测波长分别为327、274nm,流速为1·0ml/min,进样量为20μl,柱温为25℃。结果:绿原酸、黄芩苷进样量分别在0·1040μg~1·040μg(r=0·9998)、0·6240μg~6·240μg(r=0·9997)范围内与峰面积积分值呈良好的线性关系,平均回收率分别为96·4%(RSD=1·4%)、98·0%(RSD=1·1%)。结论:本方法简便、准确,重现性、专属性好,可用于小儿清热宁颗粒的质量控制。     

RP-HPLC法测定抗感胶囊中绿原酸的含量

目的RP-HPLC法测定抗感胶囊中绿原酸的含量。方法采用十八烷基硅烷键合硅胶柱;流动相:甲醇-0.4%磷酸(20∶80),检测波长为327 nm;流速为1.0 m l.m in-1。结果抗感胶囊中绿原酸的回归曲线A=3×106C?7180,r=0.9998,线性范围为0.08112~0.97344 mg.L-1,平均回收率为99.8%,RSD=1.2%(n=5)。结论该方法简便,结果准确。     

高效液相色谱法测定银翘解毒颗粒中绿原酸含量

目的建立测定银翘解毒颗粒绿原酸含量的高效液相色谱法。方法色谱柱为Kromasil KR100-5C柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.4%磷酸溶液(11∶89),柱温25℃,检测波长327 nm。结果绿原酸的检测进样量在0.064 5～0.516 0μg范围内与峰面积呈良好的线性关系(r=1.000 0),平均加样回收率为100.87%,RSD=1.98%(n=7)。结论所用方法简单、快捷准确,可作为银翘解毒颗粒的质量控制方法。     

高效液相色谱法测定抗感颗粒中绿原酸的含量

目的 采用高效液相色谱法测定抗感颗粒中绿原酸的含量. 方法以十八烷基硅烷键合硅胶为填充剂,色谱柱为VP ODS C₁₈柱(4.6 mm × 250 mm,5 μm),乙腈-0.4%磷酸溶液(16:84)为流动相,流速1.0 mL•min^-1,检测波长327 nm. 结果 绿原酸进样量在0.12～0.96 μg范围内与峰面积具有良好的线性关系,r＝0.999 8,平均回收率99.65%,RSD=1.36%(n＝6). 结论 该方法操作简便,精密度好,结果 准确可靠,适用于抗感颗粒中绿原酸含量的测定.     

HPLC多波长法测定刺五加颗粒中5个化合物的含量

目的:建立HPLC多波长法测定刺五加颗粒中5个化合物(原儿茶酸、刺五加苷B、绿原酸、刺五加苷E和异嗪皮啶)的含量。方法:采用Agilent Zorbax SB-C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈(A)-0.5%醋酸溶液(B)为流动相,梯度洗脱(0～10 min,10%A;10～20 min,10%A→13.5%A;20～70 min,13.5%A→15.5%A),流速0.6 mL.min-1,检测波长为270 nm(0～51 min,测定原儿茶酸、刺五加苷B、绿原酸和刺五加苷E)、345 nm(51～70 min,测定异嗪皮啶),柱温24℃。结果:原儿茶酸、刺五加苷B、绿原酸、刺五加苷E和异嗪皮啶浓度分别在0.935～187μg.mL-1(r=1.0000)、1.52～303μg.mL-1(r=1.0000)、2.74～547μg.mL-1(r=1.0000)、3.62～723μg.mL-1(r=1.0000)、0.510～102μg.mL-1(r=1.0000)范围内呈良好线性关系;高、中、低浓度的平均回收率(n=3)分别为97.8%～102.6%、98.0%～103.5%、96.8%～104.8%,RSD分别为0.8%～4.0%、1.3%～4.0%、0.9%～4.0%。结论:该方法可用于刺五加颗粒的质量控制。     

HPLC法测定感咳清颗粒中绿原酸的含量

目的:建立感咳清颗粒中绿原酸的含量测定方法.方法:采用RP-HPLC法,Kromasil C18色谱柱(150 mm×4.6 mm,5μm),用乙腈-0.4%磷酸(10∶90)为流动相,流速为1.0 mL·min-1,检测波长为327 nm.结果:在选定的实验条件下,绿原酸在0.15～0.75μg的范围内呈良好的线性关系,r=0.999 6,平均回收率98.77%,RSD为1.30%(n=6).结论:该方法操作简便,结果准确,可作为该制剂中绿原酸的含量测定方法.     

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.