感冒清热颗粒挥发油特征图谱及薄荷酮和胡薄荷酮的含量测定

目的:建立感冒清热颗粒中挥发油的特征图谱并测定其中薄荷酮和胡薄荷酮的含量。方法:Agilent HP-5毛细管柱(30 m×320 mm,0.25μm);进样口、检测器温度250℃;柱温:初始温度40℃,保持1 min,7℃.min-1升至100℃,保持12min,3℃.min-1升至150℃,保持8 min,10℃.min-1升至240℃,保持2 min;载气为氮气;流速:1 mL.min-1;不分流。结果:特征图谱中标定了6个共有峰。薄荷酮进样量在0.0211～0.422μg,胡薄荷酮进样量在0.0371～0.743μg内均呈良好的线性关系(r=0.9999);平均回收率分别为101.0%和97.5%,RSD均小于3%。结论:建立的气相色谱特征图谱及含量测定方法可从定性和定量两方面控制感冒清热颗粒中的挥发性成分,方法准确、可行,可作为感冒清热颗粒的质量控制方法。     

GC法同时测定明目上清片中4个成分的含量

目的:建立同时分析测定明目上清片中4个活性成分(柠檬烯、薄荷酮、薄荷脑和胡薄荷酮)的方法。方法:采用GC法,色谱柱为DB-1701毛细管色谱柱(30 m×0.3 mm,0.25μm),柱温采用程序升温(80℃保持1 min,5℃.min-1上升至120℃,保持1 min,再以50℃.min-1的速率升温至220℃,保持2 min);进样口温度:180℃;检测器:FID;检测器温度:250℃。结果:柠檬烯、薄荷酮、薄荷脑和胡薄荷酮线性范围分别为0.0103～0.507 mg·mL-1(r=0.9997)、0.0105～0.501 mg·mL-1(r=0.9999)、0.0082～0.412 mg·mL-1(r=0.9991)、0.0085～0.404 mg·mL-1(r=0.9998);平均加样回收率(n=6)分别为99.1%、97.6%、98.7%、98.3%,RSD分别为1.2%、1.8%、1.4%、1.5%。结论:该方法可用于明目上清片的质量检测。     

HPLC法测定藿香中胡薄荷酮的含量

目的：建立用高效液相色谱法测定藿香中胡薄荷酮含量的方法.方法：以甲醇-0.2％乙酸铵溶液（70：30）为流动相,Thermo BDS HYPERSIL C18（250 mm×4.6mm,5μm）为色谱柱,检测波长为252 nm,流速1.0ml·min-1.结果：胡薄荷酮进样量在0.211～2.111 μg的浓度范围内线性关系良好,r=0.999 9（n =5）,平均回收率为99.8％,RSD为1.2％.结论：该法结果准确、方法简便、分离度高,可用于藿香中胡薄荷酮的含量测定.     

GC法同时测定感冒退烧片中的薄荷酮和胡薄荷酮

目的 采用气相色谱内标法测定感冒退烧片中薄荷酮和胡薄荷酮的含量.方法 采用5％苯基-甲基聚硅氧烷(DB-5)毛细管柱,程序升温(初始温度120℃,以2℃·min-1升温至140 ℃,再以3℃·min-1升温至200℃,保持5 min),进样口温度240℃,检测器温度240℃.结果 2.3074 ～46.1475 ng薄...     

GC法测定感冒清热颗粒中胡薄荷酮的含量

目的:建立GC法测定感冒清热颗粒中胡薄荷酮的含量。方法:色谱柱为FFAP毛细管色谱柱(30 m×0.53 mm×1.0μm),柱温230℃,FID为检测器,选用乙酸乙酯作提取溶剂。结果:胡薄荷酮进样量在0.17～2.73μg范围内与峰面积线性关系良好(r=0.9999),平均加样回收率(n=6)为97.8%,RSD为1.0%。结论:该方法简便、可靠、准确,可用于该制剂的质量控制。     

HPLC法测定六经头痛片中的胡薄荷酮

目的建立测定六经头痛片中胡薄荷酮的高效液相色谱法。方法采用Agilent Zorbax SB C18色谱柱(250 mm×4.6mm,5μm);以乙腈–0.05%磷酸水溶液为流动相,进行梯度洗脱;检测波长256 nm;柱温30℃;体积流量1.0 mL/min;进样量10μL。结果胡薄荷酮在0.442 3~1 105.8 ng与峰面积线性良好(r=0.999 9),平均回收率为97.59%,RSD值为1.54%(n=6)。结论建立的方法专属性强、准确、快速,可有效地控制六经头痛片的质量。     

GC-MS测定莪术油聚氰基丙烯酸正丁酯毫微粒中4个成分的含量

目的:建立测定莪术油聚氰基丙烯酸正丁酯毫微粒(ZTO-PBCA-NP)中莪术油的主要成分β-榄香烯、莪术酮、莪术醇和莪术二酮含量的气相色谱-质谱方法。方法:采用HP-5MS毛细管色谱柱(30.0 m×250μm×0.25μm),进样温度250℃,不分流;程序升温:初始65℃恒温2 min,以5℃.min-1升至90℃恒温3 min,以20℃.min-1升至103℃恒温3 min,以8℃.min-1升至150℃恒温15 min,以20℃.min-1升至280℃。结果:β-榄香烯、莪术酮、莪术醇和莪术二酮进样浓度在4.00～40.00μg.mL-1范围内与峰面积呈良好线性关系(r=0.9979～0.9997);平均回收率(n=4)分别为98.3%(RSD=2.8%),99.4%(RSD=2.1%),95.5%(RSD=1.6%),101.2%(RSD=2.5%)。结论:该方法专属性强,准确度高,重复性好,可用于ZTO-PBCA-NP的质量控制。     

GC测定荆芥及荆芥油中的薄荷酮和胡薄荷酮

目的 测定荆芥及荆芥油中的薄荷酮和胡薄荷酮.方法 采用GC法.用PEG-20M石英毛细管柱(30 m×0.53 mm×1 μm),FID检测器,氮气为载气,柱温140%,气化室和检测器温度均为250°C,不分流进样.以萘为内标.结果 薄荷酮的线性范围为0.2～2.5 mg·ml-1(r=0.9999),胡薄荷酮的线性范围为0.2～2.5 mg·ml-1(r=0.9992);薄荷酮和胡薄荷酮的平均回收率(n=9)分别为99.0%、99.6%.结论 所建方法简便、准确,可同时测定荆芥以及荆芥油中的薄荷酮和胡薄荷酮.     

气相色谱法测定薄荷素油中薄荷脑、薄荷酮、薄荷脑乙酸酯、柠檬烯的含量

目的采用高效毛细管柱气相色谱法同时测定薄荷素油中主要成分薄荷脑、薄荷酮、薄荷脑乙酸酯、柠檬烯含量。方法色谱柱:HP-FFAP毛细管柱(25m×0.20mm×0.33μm),60℃～230℃程序升温,内标物环己酮。结果各组分线性关系良好,相关系数为1.0000。加样回收率:薄荷脑97.71%,薄荷酮102.18%,薄荷脑乙酸酯98.20%,柠檬烯97.30%。结论该方法简便、准确、可靠,可作为控制薄荷素油质量的方法。     

GC测定止咳丸中(-)薄荷酮和薄荷脑的含量

目的建立止咳丸中（-）薄荷酮、薄荷脑含量测定方法。方法色谱柱HP—FFAP毛细管柱（25m×0．2mm,0.3μm）;程序升温：初始温度90℃,保持2min,以6℃·min^-1的速率升至150℃,再以30℃·min^-1的速率升温至220℃,保持4min;载气为高纯氮,氢火焰离子化检测器（FID）,进样口温度：230℃;检测器温度：250℃;分流比为10：1,进样量1．0此。结果（-）薄荷酮在0．04486～0．8972mg·mL^-1（r=0．9997）内平均回收率为98．12％,RSD=0．86％;薄荷脑在0．06488～0．9732mg·mL^-1（r=0．9998）内平均回收率为100．91％,RSD=1．16％,均呈良好线性关系。结论本法快速、简便、准确、可靠,可用于控制止咳丸的质量。     

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.     

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.