HPLC法考察人工栽培草珊瑚中异嗪皮啶,迷迭香酸和落新妇苷含量

目的考察不同栽培条件草珊瑚中异嗪皮啶,迷迭香酸和落新妇苷含量。方法样品来自不同栽培条件下的草珊瑚。采用HPLC测定异嗪皮啶、迷迭香酸和落新妇苷。色谱柱:ZORBAX SB-C18(250 mm×4.6 mm,5μm);流动相:A:乙腈-0.1%磷酸溶液(20:80),B:乙腈-0.1%磷酸溶液(90:10),由A到B梯度洗脱;流速:1 ml/min;检测波长:330、290nm。结果各组分含量与不同栽培条件有关。不同部位各组分含量差别显著。结论采用异嗪皮啶,迷迭香酸和落新妇苷进行多指标含量测定,能较全面反映草珊瑚品质;本实验区草珊瑚品质优良;地上部位有较高的药用价值。     

草珊瑚不同部位及不同采收期有效成分含量的考察

目的：探讨草珊瑚药材的采收及最佳采收期。方法高效液相色谱法测定异秦皮啶、迷迭香酸含量。结果异嗪皮啶在根中含量最高,其次是茎,叶中含量最低;迷迭香酸的含量则在叶中含量最高,根及茎中含量较低;不同的采收月份草珊瑚中有效成分的含量差异较大,异嗪皮啶的含量以3月、6月、7月3个月为最高;迷迭香酸的含量以2月、3月、11月、12月4个月的含量较高。结论草珊瑚药材的采收应以全草为宜,采收期为每年的2～7月较为适宜。     

中药草珊瑚中异嗪皮啶和总黄酮含量的分析研究

目的建立草珊瑚中主要有效成分异嗪皮啶和总黄酮的含量测定方法.方法异嗪皮啶的测定采用高效液相色谱法,μ-Bondapak C18柱,流动相为乙腈-0.1%磷酸(17∶83),检测波长为344 nm;总黄酮采用比色法测定.结果不同产地和采收季节草珊瑚药材中总黄酮和异嗪皮啶含量差异较大,总黄酮和异嗪皮啶含量在10～12月份期间较高.结论提供了对草珊瑚质量控制的方法,草珊瑚的采收季节应为每年10～12月.     

高效液相色谱波长切换法同时测定肿节风中多指标成分的含量

目的：建立肿节风药材中反丁烯二酸、异秦皮啶和落新妇苷的含量测定方法。方法：采用DiamonsilC18（200mm×4．6mm，5μm）柱，以乙腈为流动相A，以0．1％磷酸溶液为流动相B，梯度洗脱，检测波长分别切换为210，344nm，290nm。结果：反丁烯二酸在0．0710～1．4020μg范围内线性关系良好，平均回收率为103．0%，RSD为=1．1%；异嗪皮啶在0．071，6～0．716，0μg范围内线性关系良好，平均回收率为99．8％，RSD为1．9％。落新妇苷在0．0413～0．6195Mg范围内线性关系良好，平均回收率为99．5％，RSD为2．0％。结论：本方法简便、准确，重复性好，在同一色谱条件下可同时测定反丁烯二酸、异秦皮啶和落新妇苷的含量。     

HPLC法同时测定草珊瑚中富马酸、异嗪皮啶和迷迭香酸的含量

目的:建立HPLC法同时测定草珊瑚中富马酸、异嗪皮啶和迷迭香酸含量。方法:采用Ultimate XB C18(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈(A)-0.1%磷酸溶液(B),梯度洗脱(0～10 min,2%A→20%A;10～35 min,保持20%A),流速1.0 mL.min-1,检测波长为208 nm,柱温为30℃。结果:富马酸,异嗪皮啶和迷迭香酸的线性范围分别为0.0190～0.133(r=0.9999),0.0204～0.143(r=0.9999),0.0212～0.148μg(r=0.9999);平均回收率(n=6)分别为101.3%(RSD=1.4%),99.1%(RSD=1.1%),98.2%(RSD=1.9%)。结论:该方法简便、快速、准确,适用于草珊瑚中富马酸、异嗪皮啶和迷迭香酸的含量测定。     

HPLC同时测定芍苓消银片中芍药苷、落新妇苷、绿原酸、迷迭香酸和甘草酸的含量

目的 建立同时测定芍苓消银片中芍药苷、落新妇苷、绿原酸、迷迭香酸和甘草酸含量的HPLC。 方法 采用Diamonsil C₁₈(250 mm×4.6 mm,5 μm)色谱柱,流动相为乙腈(A)-0.1%甲酸(B)系统,梯度洗脱;多种波长下同时检测。结果 芍药苷、落新妇苷、绿原酸、迷迭香酸和甘草酸的保留时间依次为44.2,57.5,28.6,72.3,90.6 min,回归方程依次为：y=33 605 228x-124 483,r=0.999 9,线性范围为3.25~60.5 μg·mL^-1;y=101 354 460x-100 4,r=0.999 9,线性范围为6.5~130 μg·mL^-1;y=119 599 014x+22 521,r=1.000 0,线性范围为0.98~19.6 μg·mL^-1;y=104 333 261x-365 9,r=0.999 9,线性范围为0.75~15 μg·mL^-1;y=24 700 178x+7 185,r=0.999 9,线性范围为8~160 μg·mL^-1。平均加样回收率依次为98.7%,100.4%,99.6%,102.1%,102.3%,RSD依次为为2.17%,0.74%,2.64%,1.39%,1.93%。结论 本方法操作较为简便,测定结果准确可靠,重复性好,能排除其他成分的干扰,可用于该制剂的质量控制。     

产地及生长年限对土茯苓中落新妇苷含量的影响

目的 考察产地和生长年限对土茯苓中落新妇苷含量的影响,了解近年来土茯苓商品的来源和各地产土茯苓落新妇苷含量的分布情况。方法 实地调查、采集并采用HPLC测定落新妇苷的含量。结果 目前市场上土茯苓商品主要来自国内南方各省,此外还有部分来自越南。国产土茯苓有约70%的样品落新妇苷含量不符合中国药典2015版规定,而越南产土茯苓含量全部符合规定,且远高于限度要求。结论 不同产地土茯苓落新妇苷含量差别较大,生长年限对土茯苓中落新妇苷含量影响较小,越南产土茯苓能否供药用尚需做进一步研究。     

肿节风药材的HPLC指纹图谱研究及其异嗪皮啶与迷迭香酸的含量测定

目的：研究肿节风药材的高效液相色谱（HPLc）指纹图谱,并测定药材中异嗪皮啶与迷迭香酸的含量,以建立药材有效的质量评价方法。方法：色谱柱为Inertsil ODS-4（250mm×4．6mm,5μm）,流动相为0．1％磷酸溶液．乙腈（梯度洗脱）,流速为1．0ml／min,检测波长为342nm。结果：所得肿节风药材的HPLC指纹图谱分离度、精密度、重复性和稳定性均良好;10批肿节风药材指纹图谱的平均相似度为0．853,不同产地样品的指纹图谱差异不大,但4个代表性色谱峰的峰面积有所区别。异嗪皮啶与迷迭香酸的质量浓度均在5-500mg／ml范围内与各自峰面积积分值呈良好的线性关系（r分别为0．9995、0．9989）;平均加样回收率分别为105．20％、99．52％,RSD分别为1．39％、1．56％（n均为6）;10批肿节风药材中异嗪皮啶与迷迭香酸的含量存在明显差异,尤以迷迭香酸含量差异较大。结论：该方法简便、准确、重复性好,可以作为肿节风药材的质量控制方法。     

红旱莲不同部位金丝桃苷含量测定

目的 比较了红旱莲药材不同部位（茎、叶、花、果）中金丝桃苷的含量差异。方法 采用高效液相色谱法进行测定,采用C₁₈（4.6 mm×250 mm,5 μm）色谱柱,乙腈-0.1%磷酸为流动相,360 nm为检测波长,流速为1.0 mL·min^-1,柱温30 ℃。结果 金丝桃苷的线性范围为2.904～58.08 μg·mL^-1,相关系数r=0.999 8,平均回收率为 95.1%,RSD为1.3%;红旱莲药材不同部位（茎、叶、花、果）中金丝桃苷的含量分别为0.405、3.221、2.260、0.371 mg·g^-1。结论 红旱莲中不同部位中金丝桃苷含量具有显著差异,叶中含量最高。     

HPLC法测定土茯苓中落新妇苷及黄杞苷

目的:建立HPLC法测定土茯芩中落新妇苷及黄杞苷的含量.方法:采用Phenomenex-C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-水-磷酸(22:78:0.1)为流动相;流速0.1 mL·min-1,检测波长290 nm,柱温40℃.结果:落新妇苷及黄杞苷的线性范围分别为0.082～8.2μg,0.022～2.2μg(r=0.999 9);平均回收率分别为102.3%(RSD=1.37%),97.82%(RSD=0.79%).结论:所建立HPLC法可同时测定土茯芩落新妇苷及黄杞苷的含量.     

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.     

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.