太行山区不同产地连翘中连翘苷、连翘酯苷A的含量测定

目的：采用HPLC法测定太行山区不同产地、不同采集时间连翘中连翘苷及连翘酯苷A的含量。方法：采用Agilent ZORBAX Eclipse XDB-C18（250mm×4.6mm,5μm）色谱柱,测定连翘苷以乙腈-水（25∶75）为流动相,等度洗脱;流速为1.0ml·min-1;检测波长为277nm。测定连翘酯苷A以乙腈-0.4％冰醋酸溶液（15∶85）为流动相,等度洗脱,流速为1.0ml·min-1;检测波长为330nm。结果：连翘苷和连翘酯苷A线性范围分别为0.206～2.060μg和0.120～1.200μg,平均回收率分别为99.52%（RSD=1.74%）和99.63%（RSD=1.21%）。结论：太行山区不同产地连翘中连翘苷和连翘酯苷A含量差异较大,7月份采集连翘中连翘苷、连翘酯苷A含量最高。含量测定方法准确、快速,适用于连翘的质量控制。     

连翘中连翘苷含量测定方法的试验研究

目的改进高效液相色谱法测定连翘中连翘苷的含量测定方法。方法采用甲醇索氏提取,中性氧化铝柱层析分离纯化、高效液相色谱法测定连翘中连翘苷含量。结果改进了高效液相色谱法测定连翘中连翘苷的含量测定方法。结论该连翘苷含量测定方法准确、重现性好、回收率为97.09%、含量限度制定合理、可行,可较好地控制连翘质量。     

高效液相色谱法测定蒙药连翘四味汤散中多指标成分的含量

目的：建立同时测定蒙药连翘四味汤散（连翘、拳参、麦冬、木通）中活性成分连翘苷、连翘酯苷A、没食子酸和木通苯乙醇苷B的含量测定方法。方法：采用RP-HPLC法,色谱柱为Promosil C₁₈柱（4.6mm×250mm,5μm）,以乙腈-1.0%磷酸水为流动相梯度洗脱,流速为1mL·min^-1,柱温40℃,检测波长为277nm（连翘苷）、330nm（连翘酯苷A和木通苯乙醇苷B）和272nm（没食子酸）,进样量为10μL。结果：连翘四味汤散中连翘苷的含量在0.038~0.051mg·g^-1之间、连翘酯苷A的含量在0.127~0.135mg·g^-1之间、没食子酸的含量在0.079~0.085mg·g^-1之间、木通苯乙醇苷B的含量在0.0096~0.0103mg·g^-1之间。结论：该方法快速简便、稳定可靠,适用于连翘四味汤散的质量控制。     

连翘中芦丁和连翘酯苷A的含量测定方法分析

目的：对连翘中芦丁和连翘酯苷A的含量测定方法进行分析探讨,为今后的研究工作提供可靠的参考依据。方法采取反相高效液相色谱法,选用ThermoODS C18色谱柱,流动相为甲醇-浓度为2 g/L冰醋酸（20：80）,波长为329 nm。结果芦丁与连翘酯苷A的进样量在0.0210~0.4219μg和0.0152~0.3058μg之间存在良好的线性关系,芦丁与连翘酯苷A的平均回收率为102.6%和103.4%。结论采取反相高效液相色谱法对连翘中芦丁与连翘酯苷A的含量进行测定时具有操作简单,结果准确可靠,稳定性与精密度良好等优势,值得关注并推广。     

高效液相色谱法同时测定连翘叶中连翘酯苷A和连翘苷含量

目的建立同时测定连翘叶中连翘酯苷A和连翘苷含量的高效液相色谱法。方法采用AgilentZorbaxSB—C18柱（150mm×4．6mm,5μm）,以甲醇-0．1％磷酸溶液（32：68）为流动相,检测波长为227nm,流速为1．0mL／min,进样量为10txL,柱温为30℃。结果连翘酯苷A、连翘苷进样量分别在293．170～3664．624ng（r=0．999980）和333．760—4172．000ng（r=0．999991）范围内与相应峰面积皇良好线性关系,平均回收率分别为97．00％（RSD：1．88％）和99．97％（RSD=2．11％）。结论该法操作简便、结果准确、专属性强,可用于同时测定连翘叶中连翘酯苷A和连翘苷的含量。     

HPLC 法测定清热胶囊中连翘苷的含量

目的：建立 HPLC 法测定清热胶囊中连翘苷含量。方法：取清热胶囊样品经中性氧化铝柱预处理,再以 Dia-monsil C18（250 mm ×4.6 mm,5μm）为色谱柱,乙腈-水（25∶75）为流动相,检测波长为277 nm,流速为1.0 ml／ min。结果：连翘苷含量与峰面积在0.2160~2.16μg 范围内具有良好的线性关系（r =0.9997）;平均回收率为99.7%,RSD 为1.18%（n =9）。结论：该方法简便、准确、重复性好,可用于清热胶囊中连翘苷的含量测定。     

高效液相法测定清热解毒注射液中连翘苷的含量

目的采用高效液相色谱法（HPLC）测定清热解毒注射液中连翘苷的含量。方法高效液相外标法,以C18化学键和硅胶为固定相,以乙腈-水（25：75）为流动相,检测波长为278nm。结果连翘苷的平均回收率为99.1%,RSD为1.52%（n=6）。连翘苷在1.625～9.75μg范围内进样量与峰面积值呈良好线性关系。结论此方法简便、准确,可用于含量的测定。     

HPLC法测定芩连片中连翘苷的含量

目的：采用高效液相色谱法测定芩连片中连翘苷的含量。方法：色谱柱为Hypersil C18（150mm×4．6mm,5μm）,以乙腈-水（25：75）为流动相,流速1．0ml·min^-1,检测波长277nm。结果：连翘苷进样量在0．20～1．61μg范围内与峰面积具有良好的线性关系,r为0．9999,回收率98．0％（RSD=0．98％,n=6）。结论：方法操作简便,精密度好,结果准确可靠,适用于芩连片中连翘苷含量的测定。     

HPLC法同时测定连翘中芦丁和连翘酯苷的含量

目的：建立测定连翘中芦丁和连翘酯苷含量的方法.方法：采用HPLC法.色谱柱为Thermo ODS C18（250 mm×4.6 mm,5 μm）,流动相：甲醇-0.2%冰醋酸溶液（20：80）,流速1 ml·min-1,检测波长：329 nm,柱温30℃.结果：芦丁、连翘酯苷的进样量分别在0.023 2-0.464 μg（r=0.999 9）和0.050 6~1.012 μg（r=0.999 9）范围内呈良好线性关系;平均回收率分别为101.6%（RSD＝1.38%,n＝6）和100.8%（RSD＝1.26%,n＝6）.结论：本方法简便、准确,适用于连翘的分析测定和质量控制.     

HPLC测定小儿双清颗粒中连翘苷的含量

目的建立小儿双清颗粒中连翘苷的含量测定方法。方法采用HPLC法,以依利特Hypersil ODS2（5μm,4.6mm×200mm）为色谱柱,以乙腈-水（23∶77）为流动相,检测波长为278nm,流速为1.0mL.min-1。结果连翘苷的线性范围为0.1108～0.5540μg（r=0.999 4）,平均回收率（n=5）为99.1%,RSD为0.78%。结论此方法简便准确,重复性好,可用于该制剂的质量控制。     

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.

---

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.     

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.