不同种獐牙菜中獐牙菜苦苷含量比较

目的比较不同品种獐牙菜植物中獐牙菜苦苷含量,为合理选择利用资源提供依据。方法甲醇超声提取獐牙菜植物中的活性成分,通过HPLC测定其中的獐牙菜苦苷含量。色谱条件：ZORBAX SB-C18（4.6mm×150mm,5μm）色谱柱,流动相为水-乙腈（92∶8）,流速1mL·min^-1,柱温25℃,检测波长为238nm。结果獐牙菜苦苷在检测范围内线性良好（r=0.9994）,加样回收试验的平均回收率为99.2%,重复性试验RSD为1.73%（n≥5）。几种獐牙菜中獐牙菜苦苷含量在0.58%～12.86%。结论獐牙菜苦苷含量在獐牙菜属植物中种间差别比较大。     

11种獐牙菜及近缘植物中有效成分的高效液相色谱测定

建立了獐牙菜中3种苦味甙,即獐牙菜苦甙(swertiamarin)、獐牙菜甙(sweroside)、龙胆苦甙(gentiopicroside)及一种　酮甙──獐牙菜　酮甙(swertianolin)的高效液相色谱定量分析方法(μ-BondpakC₁₈柱,水—甲醇—异丙醇—四氢呋喃=65:30:5:1作流动相);对11种獐牙菜及近缘植物椭圆叶花锚、坚龙胆进行了含量测定,并对他们之间的异同进行了比较。     

不同种獐牙菜中獐牙菜苦苷含量比较

目的 比较不同品种獐牙菜植物中獐牙菜苦苷含量,为合理选择利用资源提供依据。方法 甲醇超声提取獐牙菜植物中的活性成分,通过HPLC测定其中的獐牙菜苦苷含量。色谱条件： ZORBAX SB-C₁₈(4.6 mm×150 mm,5 μm)色谱柱,流动相为水-乙腈(92∶8),流速1 mL·min^-1,柱温25 ℃,检测波长为238 nm。结果 獐牙菜苦苷在检测范围内线性良好(r=0.999 4),加样回收试验的平均回收率为99.2%,重复性试验RSD为1.73%(n≥5)。几种獐牙菜中獐牙菜苦苷含量在0.58%~12.86%。结论 獐牙菜苦苷含量在獐牙菜属植物中种间差别比较大。     

HPLC法测定八味獐牙菜丸中獐牙菜苦苷的含量

目的：建立八味獐牙菜丸中獐牙菜苦苷的含量测定方法。方法：色谱柱为岛津VP-ODSC18（250mm×4.6mm,5μm）,流动相为甲醇-水（20∶80）,检测波长为237nm。结果：獐牙菜苦苷进样量在0.12～0.60mg·ml-1范围内峰面积与浓度呈良好的线性关系,相关系数为0.9999,平均回收率为97.70%,RSD值为1.85%（n=9）。结论：方法快速,准确,重复性好,可作为八味獐牙菜丸的质量指标。     

高效液相色谱法测定显脉獐牙菜中獐牙菜苦苷的含量

目的建立测定显脉獐牙菜中獐牙菜苦苷含量的高效液相色谱方法。方法C18（4.6 mm×200 mm,5μm）色谱柱,流动相为甲醇-水（25∶75）,流速为1.0 mL·min^-1,检测波长为239 nm,柱温为25℃。结果獐牙菜苦苷在1.52-15.22μg线性良好,相关系数r为0.999 95,平均回收率为97.8%,RSD小于3%（n=6）。结论本方法操作简便,分离效果好,灵敏度高,重现性好,可为显脉獐牙菜质量控制提供参考。     

狭叶獐牙菜的两个新环烯醚单萜甙

本文报道狭叶獐牙菜(Swertia angustifolia)中两个新的环烯醚单萜甙的结构。分别命名为狭叶獐牙菜苦甙(angustiamarin,Ⅰ)和狭叶獐牙菜甙(angustioside,Ⅱ),此外还鉴定了獐牙菜甙(sweroside,Ⅲ),獐牙菜苦甙(swertiamarin,Ⅳ)和表优士特莫甙(epi-eustomoside,Ⅴ)。     

HPLC法测定印度獐牙菜中5种有效成分含量

目的建立HPLC法测定印度獐牙菜中獐芽菜苦苷、龙胆苦苷、獐牙菜苷、芒果苷和齐墩果酸的含量。方法采用AgilentTC-C18柱,流动相：甲醇-0.02%磷酸水溶液,梯度洗脱,流速：1.0mL.min-1,检测波长：254nm、210nm,柱温：25℃。结果 5种成分均达到基线分离,线性良好。结论本法快速、准确可用于印度獐牙菜的含量测定。     

高效液相色谱法测定2种獐牙菜中龙胆苦苷的含量

目的建立测定川东獐牙菜、显脉獐牙菜中龙胆苦苷含量的高效液相色谱方法。方法HYPERSILBDSC18（4.6mm×200mm,5μm）色谱柱,流动相为甲醇-水梯度洗脱（MeOH%：0min,15%;40min,45%）,流速为1.0mL·min^-1,检测波长为276nm,柱温为25℃。结果龙胆苦苷在0.22～6.50μg线性良好,r=0.99996,平均回收率为96.30%,RSD〈3%（n=6）。结论本方法操作简便,分离效果好,灵敏度高,重现性好,为控制川东獐牙菜和显脉獐牙菜质量提供参考。     

不同采收期龙胆中龙胆苦苷、獐牙菜苦苷和獐牙菜苷的变化研究

目的研究不同采收期龙胆中龙胆苦苷、獐牙菜苦苷、獐牙菜苷的变化规律。方法采用Welchrom C_(18)色谱柱(250mm×4.6 mm,5μm);流动相:甲醇–水(25∶75);检测波长:270(龙胆苦苷)、240 nm(獐芽菜苦苷和獐牙菜苷);体积流量:1.0 m L/min;柱温:25℃;进样量为10μL。分别采收9、10月上、中、下旬的龙胆,考察其中龙胆苦苷、獐牙菜苦苷、獐牙菜苷的变化。结果在9—10月,龙胆中龙胆苦苷、獐牙菜苦苷和獐牙菜苷的量基本呈现同步上升、同步下降趋势。在9月中旬最高,9月下旬最低。与9月下旬比较,10月上旬的量有所回升,而10月下旬的量再次呈下降趋势。结论龙胆药材最佳采收季节为9月中旬,此时龙胆苦苷、獐芽菜苦苷和獐牙菜苷的量最高。     

龙胆科生药中2种苦甙的含量测定

报道龙胆科植物５属３２种５９个产地的生药，加甲醇超声后，直接用ＨＰＬＣ法测定了獐牙菜苦甙（ｓｗｅｒｔｉａｍａｒｉｎ）和龙胆苦甙（ｇｅｎｔｉｏｐｉｃｒｏｓｉｄｅ）的含量，流动相：１０％甲醇→５０％甲醇梯度洗脱，柱温：５０℃，内标，３－（邻－甲氧基－苯氧基）１，２－丙二醇（ｇｕａｉｆｅｎｅｓｉｎ）检测波长２５４ｎｍ，流速：１ｍＬ／ｍｉｎ，进样５μＬ，获得满意结果。     

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.     

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.