延年乐口服液中淫羊藿苷的鉴别和含量测定

目的:建立延年乐口服液中淫羊藿的鉴别和含量测定的标准,以增加对制剂主药的质量控制.方法:以淫羊藿苷作对照品,采用薄层色谱法做鉴别;高效液相色谱法做含量测定.结果:检出供试品淫羊藿苷清晰的斑点;含量测定淫羊藿苷浓度18.968～113.808μg/ml范围内线性关系良好(r=1.000),平均回收率为97.45%,RSD为1.70%.结论:本法测定淫羊藿苷简便、专属性强、准确、重现性好,可用于延年乐口服液淫羊藿苷鉴别和含量测定.     

HPLC法测定鹿仙口服液中淫羊藿苷的含量

建立鹿仙口服液中淫羊藿苷的含量测定方法。采用高效液相色谱法测定鹿仙口服液中淫羊藿苷的含量 ,使用 C18柱 ,乙腈 -水 (2 5∶ 75 )为流动相 ,检测波长为 2 70 nm。结果淫羊藿苷浓度在 9～ 4 7μg/ ml范围内线性关系良好 ,本法重现性好 ,精密度高 ,平均回收率为 99.4 % ,RSD =2 .1% ,可用于鹿仙口服液质量控制     

紫外分光光度法和高效液相色谱法测定淫羊藿总黄酮含量的比较研究

目的:比较紫外分光光度法和高效液相色谱法测定淫羊藿总黄酮含量的差异,探讨淫羊藿总黄酮含量测定方法的可靠性。方法:紫外分光光度法以淫羊藿苷为指标性成分,在270 nm 波长处进行测定。高效液相色谱法以 ZORBAX SB-C_(18)柱(250mm×4.6 mm,5μm)为分析柱,乙腈-水梯度洗脱,流速1.0 mL·min~(-1),检测波长为270 nm。经紫外光谱识别的黄酮类成分(部分经 ESI-MS 确认),除朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ和宝藿苷Ⅰ以自身对照外,其他黄酮类成分均以淫羊藿苷为参比进行定量,淫羊藿总黄酮含量等于朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ、宝藿苷Ⅰ和其他黄酮成分含量之和。结果:紫外分光光度法,淫羊藿苷在2.45～24.50μg·mL~(-1)范围内线性关系良好(r=0.9996),测得淫羊藿总黄酮含量以淫羊藿苷计为56.6%。高效液相色谱法中,与淫羊藿苷紫外光谱相似的33个色谱峰,MS 归属了其中10个主要成分均为黄酮类成分。朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ和宝藿苷Ⅰ分别在0.093～1.852μg(r=0.9998)、0.107～2.136μg(r=0.9997)、0.094～1.876μg(r=0.9998)、0.098～1.956μg(r=0.9998)线性关系良好,淫羊藿总黄酮含量为35.6%。结论:紫外分光光度法和高效液相色谱法测定的淫羊藿总黄酮含量差异显著,紫外分光光度法的准确性有待进一步考证。     

RP-HPLC测定淫羊藿不同品种和部位中柔藿苷和淫羊藿苷

目的:为了对中药淫羊藿中柔藿苷和淫羊藿苷含量进行系统研究,测定了淫羊藿不同品种和药用部位的柔藿苷和淫羊藿苷含量。方法:采用RP-HPLC法对3个品种多个样品进行测定,以BECKMAN COULTER_(TM)-C_(18)柱(带预柱)为色谱柱,流动相为乙腈-水(25∶75),流速1.0mL·min~(-1),检测波长为270nm。结果:柔藿苷在0.19642-1.9642μg范围内呈良好的线性关系,淫羊藿苷在0.19335-1.9335μg范围内呈良好的线性关系。巫山淫羊藿同一植株体的不同部位中柔藿苷和淫羊藿苷的分布均为叶>根>茎。巫山淫羊藿同一植株的任何部位都是柔藿苷含量高于淫羊藿苷,而淫羊藿和箭叶淫羊藿叶中都是淫羊藿苷含量高于柔藿苷。结论:巫山淫羊藿中以柔藿苷为主要成分,淫羊藿和箭叶淫羊藿中以淫羊藿苷为主要成分。     

不同产地和品种淫羊藿中淫羊藿苷的HPLC分析

目的:对中药淫羊藿中淫羊藿苷的含量分析进行方法学研究,并测定淫羊藿的不同产地、不同品种、不同药用部位的淫羊藿苷的含量。方法:采用RP-HPLC技术对7个品种2 3个样品进行测定。以PERKIN EIMER SH/5C₁₈柱为分析柱,流动相为乙腈水 36%乙酸( 2 5∶73.5∶1 .5)流速1 .0ml/min。UV检测波长270nm。结果:本方法测定淫羊藿苷含量在0.0212～0.127μg ,0.53～1.696μg范围内呈良好的线性关系。不同产地、不同品种、不同药用部位的淫羊藿其淫羊藿苷的含量为0.00307%～1.55%。同一植株不同部位中淫羊藿苷的含量分布叶>叶茎>茎>根。结论:淫羊藿由于产地不同、品种不同其淫羊藿苷的含量相差悬殊。本测定方法为筛选优良品种和扩大药源提供了简便易行的方法     

高效液相色谱法测定健汝美口服液中淫羊藿苷含量

目的测定健汝美口服液中淫羊藿苷的含量。方法采用高效液相色谱法(HPLC法),色谱柱为C18柱(200mm×4.6mm,5μm),以乙腈-水(30∶70)为流动相,检测波长为270nm。结果淫羊藿苷进样量线性范围是0.26～2.60μg,平均加样回收率为99.28%,RSD为0.82%。结论HPLC法快速、准确,可用于健汝美口服液的质量控制。     

HPLC测定康脑舒口服液中淫羊藿苷的含量

目的　建立康脑舒口服液中淫羊藿苷的含量测定方法。方法　采用高效液相色谱法 ,UbondapskC18色谱柱 ,流动相为乙腈 -水 (7∶3) ,紫外检测波长 2 70nm。结果　淫羊藿苷在 0 3～ 1 0mg·ml-1范围内线性关系良好(r=0 9999) ,平均回收率为 95 85 % ,RSD =2 3% (n =4 )。结论　该法操作简便、快速 ,可用于口服液中淫羊藿苷的含量测定     

RP—HPLC法测定巫山淫羊藿中4种成分的含量

目的:用 HPLC 梯度洗脱法测定巫山淫羊藿中4种主要成分的含量,考察了淫羊藿属苷 A、双藿苷 A、朝藿定 C 和淫羊藿苷在巫山淫羊藿不同部位中的分布。方法:采用 RP-HPLC 法测定,以 BECKMAN COULTER_(TM)-C_(18)(10μm,4.6 mm×250mm)为色谱柱,流动相为乙腈-水,梯度洗脱(0 min,乙腈-水比例为20:80;5 min,比例为30:70;10 min,比例为50:50),流速为1 mL·min~(-1),检测波长270 nm。结果:淫羊藿属苷 A 在0.188μg～1.880μg,淫羊藿苷在0.214μg～2.140μg,双藿苷 A在0.240μg～2.400μg,朝藿定 C 在0.282μg～2.820μg范围内呈良好线性关系;重复性实验的 RSD 分别为1.2%,1.3%,1.2%,1.2%。巫山淫芋藿不同部位双藿苷 A 和朝藿定 C 的含量较大,同一植株的不同部位中朝藿定 C 的分布为根>叶>茎。双藿苷 A 的分布为根>茎>叶,淫羊藿属苷 A 和淫羊藿苷含量较少。结论:巫山淫羊藿根中的化学成分以朝藿定 C 为最高,双藿苷 A 为次,而巫山淫羊藿叶中也以朝藿定 C 含量为最高。     

HPLC同时测定21种淫羊藿中朝藿定C和淫羊藿苷的含量

目的:建立同时测定淫羊藿药材中朝藿定C和淫羊藿苷含量的高效液相色谱方法。方法:采用Elite SinoChrom ODS-AP(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈(A)-水(B),梯度洗脱(0~8 min,27%A;8~30 min,27%A→29%A),流速1 mL.min-1,检测波长270 nm。结果:朝藿定C进样量在0.130~3.89μg,淫羊藿苷在0.0294~1.47μg范围内呈良好线性关系(r=0.9999);朝藿定C和淫羊藿苷平均回收率(n=9)分别为103.9%,100.0%;淫羊藿药材中朝藿定C和淫羊藿苷的含量分别为0.02%~7.80%,0.01%~1.74%。结论:该方法简便、快速、准确,重复性好,可作为淫羊藿药材中朝霍定C和淫羊藿苷的含量测定方法。     

不同产地和品种淫羊藿中淫羊藿苷的HPLC分析

目的 :对中药淫羊藿中淫羊藿苷的含量分析进行方法学研究 ,并测定淫羊藿的不同产地、不同品种、不同药用部位的淫羊藿苷的含量。方法 :采用RP HPLC技术对 7个品种 2 3个样品进行测定。以PERKIN EIMER SH/5C18柱为分析柱 ,流动相为乙腈 水 36%乙酸 ( 2 5∶73.5∶1 .5)流速 1 .0ml/min。UV检测波长 2 70nm。结果 :本方法测定淫羊藿苷含量在 0 .0 2 1 2～ 0 .1 2 7μg ,0 .53～ 1 .696μg范围内呈良好的线性关系。不同产地、不同品种、不同药用部位的淫羊藿其淫羊藿苷的含量为 0 .0 0 30 7%～ 1 .55%。同一植株不同部位中淫羊藿苷的含量分布叶 >叶茎 >茎 >根。结论 :淫羊藿由于产地不同、品种不同其淫羊藿苷的含量相差悬殊。本测定方法为筛选优良品种和扩大药源提供了简便易行的方法     

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.     

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.     

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.