通关藤浸膏中绿原酸的稳定性考察

目的:考察通关藤浸膏中绿原酸稳定性的影响因素。方法:采用高效液相色谱(HPLC)法测定通关藤浸膏在不同溶剂、不同光线以及不同受热时间下绿原酸的含量变化。结果:通关藤浸膏中的绿原酸在有机溶剂中更稳定;光照和受热温度是影响绿原酸稳定性的重要因素。结论:通关藤浸膏中的绿原酸在不同条件下稳定性不同,该结果可为通关藤浸膏的制备、贮存、分析及其相关制剂的生产提供参考。     

不同产地通关藤饮片中绿原酸及总酚酸的含量比较

目的测定并比较不同产地通关藤饮片的绿原酸及总酚酸含量。方法用高效液相色谱（HPLC）法测定绿原酸的含量，用紫外可见分光光度（UV）法测定总酚酸的含量。结果云南产通关藤饮片的绿原酸、总酚酸含量最高，贵州次之，其他产地饮片的绿原酸含量也均超过了0．5mg／g，总酚酸含量也均超过了17mg／g。结论云南产通关藤饮片是最理想的提取绿原酸及总酚酸的原料，其他各产地的通关藤饮片也可用于生产。     

不同产地通关藤药材中总皂苷与通关藤苷B的含量比较

［摘要］目的考察不同产地通关藤药材中总皂苷及通关藤苷B的含量。 方法以通关藤苷B为对照品,分别采用紫外分光光度法和高效液相色谱法测定总皂苷和通关藤苷B的含量,并对测定方法进行了系统的方法学考察。结果广西、四川、湖北等地通关藤药材中总皂苷平均含量分别为5.7%,5.3%,4.8%;通关藤苷B平均含量分别为0.22%,0.27%,0.20%。结论广西产通关藤药材中总皂苷含量较高,四川产通关藤药材中通关藤苷B的含量较高。     

HPLC-ELSD法检测消癌平丸中通关藤苷H的含量及稳定性考察

目的:测定消癌平丸中通关藤苷H的含量,并考察其稳定性。方法:采用高效液相色谱-蒸发光散射检测器(HPLC-ELSD)法测定消癌平丸中通关藤苷H的含量;分别于下列条件测定消癌平丸中通关藤苷H的含量:(1)温度(25±2)℃、相对湿度(60±10)%,将3批消癌平丸放置0、3、6、9、12个月;(2)温度(30±2)℃、相对湿度(65±5)%,将3批消癌平丸放置0、1、2、3、6个月;(3)温度(40±2)℃、相对湿度(75±5)%,将3批消癌平丸放置0、1、2、3、6个月。结果:通关藤苷H的进样量在0.390 2³.902 0μg范围内与峰面积积分值呈良好线性关系(r=0.998 0);平均加样回收率为99.03%,RSD=1.75%。通关藤苷H在条件(1)下基本稳定,在条件(2)和(3)下不稳定,其RSD>3%。结论:采用HPLC-ELSD法测定消癌平丸中通关藤苷H的含量,样品中通关藤苷H与其他色谱峰完全分离,且峰形良好,可作为消癌平丸中通关藤苷H的含量测定方法。稳定性试验结果显示,通关藤苷H在消癌平丸中不稳定,不宜作为消癌平丸的质量控制指标。     

比色法测定不同产地通关藤药材中C_(21)甾体总苷含量

目的:建立通关藤中C21甾体总苷含量测定方法,比较28个产地通关藤中C21甾体总苷含量。方法:以Tenacigenoside A为标准品,香草醛-高氯酸显色,在469nm波长处测定C21甾体总苷含量。结果:通关藤中C21甾体总苷含量在34.091～121.049mg·g-1之间,平均为66.591mg·g-1。不同产地通关藤药材中C21甾体总苷含量差异较大,其中以云南金平产通关藤药材中总苷含量最高,广西、贵州和安徽产的药材中总苷含量相对较低。同一产地不同批次的药材,总苷含量也有较大的差异。结论:本方法简便、快速、准确,可用于不同产地通关藤中C21甾体总苷的含量测定。     

UPLC-MS/MS法同时测定通关藤药材中3种皂苷的含量

目的:建立同时测定通关藤药材中通关藤苷A、H、I含量的方法。方法:采用超高效液相色谱-串联质谱法,色谱柱为Phenomenex Kinetex XB-C18,流动相为0.1%甲酸溶液-乙腈(梯度洗脱),流速为0.2 m L/min,柱温为40℃,进样量为5μL,离子源为电喷雾离子源,多反应离子监测模式,正离子扫描,离子源喷射电压为5 500 V,雾化气压力为60 psi,加热气压力为60 psi,帘气压力为20 psi,去溶剂温度为600℃。结果:通关藤苷A、H、I检测质量浓度线性范围分别为0.1~10 ng/m L(r=0.999 7)、0.025~10 ng/m L(r=0.999 5)、0.025~10 ng/m L(r=0.998 9);定量限分别为0.1、0.025、0.025 ng/m L,检测险分别为0.05、0.012 5、0.012 5ng/m L;精密度、稳定性、重复性试验的RSD均小于4.0%;加样回收率分别为97.67%~99.00%(RSD=0.47%,n=6)、95.00%~101.67%(RSD=2.59%,n=6)、96.67%~103.33%(RSD=2.83%,n=6)。结论:该方法操作简便,精密度、稳定性、重复性好,可用于通关藤药材中通关藤苷A、H、I含量的同时测定。     

通关藤药材藤茎皮部和木部中总皂苷及苷B的含量测定

目的 测定通关藤药材藤茎皮部和藤茎木部中总皂苷及苷B的含量。方法以通关藤苷B为对照品,以香草醛一冰醋酸．高氯酸显色,采用比色法在467nm处测定通关藤药材藤茎皮部和藤茎木部中总皂苷的含量,用高效液相色谱法测定通关藤药材苷B的含量,并对测定方法进行了系统的方法学考察。结果对结果数据T检验表明通关藤药材藤茎皮部和藤茎木部中总皂苷及苷B的含量并无显著差异。结论本试验方法简便、准确、重现性好,为合理选择通关藤药材药用部位提供参考。     

多指标成分结合多元统计分析法综合评价黔产黑骨藤质量

目的 建立多指标成分结合多元统计分析的综合质量评价方法，综合评价黑骨藤药材的质量。方法 以贵州不同产地的11批黑骨藤药材为样品，采用高效液相色谱法测定其中新绿原酸、隐绿原酸、绿原酸、原花青素A2、异绿原酸A、异绿原酸C的含量，并采用聚类热图分析、灰色关联度分析（GRA）和熵权逼近理想解排序（TOPSIS）法综合评价其质量。结果 含量测定的方法学考察结果均符合相关规定，各待测成分在各自进样量范围内线性关系和准确度均良好。11批样品中绿原酸、隐绿原酸、新绿原酸、原花青素A2、异绿原酸A、异绿原酸C的含量分别为3.650～7.302、0.888～2.575、1.371～2.386、0.947～1.469、0.084～0.169、0.725～1.067 mg/g；各成分含量差异显著，其中以绿原酸含量最高，异绿原酸A最低。综合聚类热图、GRA和TOPSIS分析结果显示，样品S5和S10的综合质量相对较好。结论 所建立的含量测定方法准确、稳定、简便，结合多元统计分析方法，可用于黑骨藤药材的质量评价。在11批不同产地样品中，以贵州省安顺市西秀区旧州镇和蔡官镇所产样品的质量相对较好。     

HPLC法测定不同产地返魂草中绿原酸的含量

目的建立同时测定不同产地返魂草中绿原酸含量的方法。方法采用HPLC法。色谱柱为Diamonsil ODS C18柱(4.6 mm×250 mm,5μm),流动相为乙晴-体积分数为0.4%的磷酸水溶液,检测波长为326 nm;流速为1 mL.min-1。结果绿原酸质量在62~301 ng内与峰面积呈良好的线性关系,平均回收率为99.2%,RSD为0.91%(n=9);5个产地返魂草中绿原酸含量分别为0.95、0.720、.55、0.64、0.44 mg.g-1。结论HPLC法可用于返魂草中绿原酸的含量测定;5个产地的返魂草中绿原酸含量有明显差异,吉林通化返魂草中绿原酸含量最高。     

RP-HPLC法测定四藤片中绿原酸的含量

建立HPLC法测定四藤片中绿原酸的含量。采用Diamonsil C18柱;以甲醇-1.2%冰醋酸（v/v）（15∶85）为流动相;检测波长为327nm。绿原酸进样量在0.02-1.0μg范围内线性关系良好,r=0.99999,加样回收率为104.40%,RSD%为0.49%。所建立的方法简便易行、准确、重现性好,可用于四藤片的质量控制。     

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.