反相高效液相色谱法同时测定败酱草中槲皮素、山奈酚的含量

目的建立反相高效液相色谱法同时测定败酱草中槲皮素、山奈酚的含量。方法采用Odyssil C18(250mm×4.6 mm,5μm)色谱柱,流动相为甲醇-0.1%磷酸(55:45),流速为1.0 m L·min-1,检测波长为360 nm,柱温为25℃,进样量为10μL。结果槲皮素进样量在0.024~0.706μg内与峰面积呈良好的线性关系(r=0.999 9),平均加样回收率为100.0%,RSD为3.1%;山奈酚进样量在0.020~0.609μg内与峰面积呈良好的线性关系(r=0.999 8),平均加样回收率为99.9%,RSD为1.5%。结论该方法简便、快速、具有良好的重现性,可用于败酱草中槲皮素和山奈酚的含量测定。     

反相高效液相色谱-二极管阵列检测法测定驱白马日白热斯丸中槲皮素和山奈酚的含量

目的建立反相高效液相色谱-二极管阵列检测(RP-HPLC-PAD)法测定维吾尔成药驱白马日白热斯丸中槲皮素和山奈酚含量。方法色谱柱:安捷伦HC-C18柱(250 mm×4.6 mm,5μm);流动相:甲醇-0.4%磷酸溶液(47∶53);检测波长:365 nm;柱温:30℃;流速:1.0 m L·min-1。结果槲皮素和山奈酚分别在0.5~30.0μg·m L-1(r=0.999 9)和0.5~20.0μg·m L-1(r=0.999 8)浓度范围内呈良好的线性关系,平均回收率分别为102.2%(RSD=1.18%,n=5)和96.9%(RSD=1.22%,n=5)。结论该方法简便、快速、准确,具有良好的重复性和回收率,可作为该药物的定量分析方法 ,为进一步开发利用维药资源提供了参考依据。     

HPLC同时测定余甘子叶中槲皮素和山奈酚的含量

目的建立HPLC同时测定余甘子叶中槲皮素和山奈酚含量的方法。方法色谱柱：Thermo Hypersil BDS C18（4.6 mm×250 mm,5μm）,梯度洗脱流动相：乙腈-0.1%磷酸溶液,流速：1.0 ml/min,检测波长：370 nm,柱温：30℃,进样体积：20μl。结果槲皮素和山奈酚分别在0.003~0.06μg/μl（r=0.9995）、0.001015~0.0203μg/μl（r=0.9993）范围内呈良好的线性关系,平均回收率（n=6）分别为98.83%（RSD=2.73%）、101.58%（RSD=2.21%）。结论建立了同时测定槲皮素和山奈酚含量的方法,可进一步完善余甘子叶的质量控制体系。     

HPLC法同时测定蚕豆花中槲皮素和山奈酚的含量

目的建立HPLC法测定蚕豆花中的槲皮素和山奈酚含量的方法。方法测定槲皮素和山奈酚的色谱条件为色谱柱Inert Sustain C18（250mm×4.6mm,5μm）;以乙腈（A）∶0.4%磷酸水溶液（B）为流动相进行梯度洗脱,流速为0.8m L·min^-1;检测波长为365nm;柱温为30℃。结果槲皮素进样量在0.034~0.272μg范围内（r=0.9999）,山奈酚进样量在0.040~0.317μg范围内（r=0.9998）线性关系良好,平均回收率槲皮素为99.20%（RSD%=0.81,n=6）,山奈酚为98.39%（RSD%=1.49,n=6）。结论本法操作简便快捷、稳定性高、重现性好,为蚕豆花药材的质量评价提供依据。     

高效液相色谱法同时测定银黄胶囊中绿原酸和黄芩苷的含量

目的:建立同时测定银黄胶囊中绿原酸和黄芩苷的含量高效液相色谱法(HPLC)。方法:色谱柱为SymmetryR-C18(250 mm×4.6 mm,5μm);流动相为甲醇-0.1%磷酸溶液梯度洗脱,流速为1.0 m L/min,检测波长为318nm,柱温为30℃。结果:绿原酸在进样量0.217 4~2.174 0μg范围内与峰面积线性关系良好(r=0.999 8)(n=5),平均回收率为99.26%(n=6),RSD为0.56%;黄芩苷在进样量0.807 6~8.076 0μg范围内与峰面积线性关系良好(r=0.999 9)(n=5),平均回收率为98.43%(n=6),RSD为1.07%。结论:该含量测定方法简单可行,重复性好,为有效控制银黄胶囊的质量提供依据。     

HPLC法同时测定牛黄宁宫片中6种成分的含量

目的:建立同时测定牛黄宁宫片中6种成分含量的方法。方法:采用高效液相色谱法。色谱柱为TC-C_(18),流动相为甲醇-0.05%磷酸(梯度洗脱),流速为1.0 m L/min,检测波长为280 nm,柱温为25℃,进样量为10μL。结果:甘草苷、盐酸小檗碱、连翘苷、黄芩苷、大黄素和大黄酚检测质量浓度线性范围分别为3.2~320μg/m L(r=0.999 9)、8.8~880μg/m L(r=0.999 8)、5.6~560μg/m L(r=0.999 5)、2.0~200μg/m L(r=0.999 9)、4.4~440μg/m L(r=0.999 9)、2.0~200μg/m L(r=0.999 7);精密度、稳定性、重复性试验的RSD<6.0%;加样回收率分别为96.34%~97.25%(RSD=0.33%,n=6)、96.12%~98.06%(RSD=0.82%,n=6)、96.36%~99.09%(RSD=1.02%,n=6)、95.84%~97.32%(RSD=0.65%,n=6)、95.83%~97.92%(RSD=0.88%,n=6)、98.60%~99.65%(RSD=0.42%,n=6)。结论:该方法操作简便,精密度、稳定性、重复性好,可用于牛黄宁宫片中6种成分含量的测定。     

白花蛇舌草中黄酮类抗肿瘤活性成分的HPLC分析

目的:建立一种同时测定白花蛇舌草中黄酮类抗肿瘤活性成分槲皮素和山柰酚含量的方法。方法:采用高效液相色谱(HPLC)法,色谱柱为AlltimaC1(8250mm×4.6mm,5μm),流动相为甲醇(A)-0.5%冰醋酸(梯度洗脱),检测波长为350nm。结果:槲皮素、山柰酚的进样量分别在0.0062～0.2440μg(r=0.9998)、0.0078～0.3106μg(r=0.9999)范围内与各自峰面积积分值呈良好线性关系;平均回收率分别为101.84%(RSD=1.79%,n=6)和99.04%(RSD=2.90%,n=6)。结论:本方法简便、准确、重复性好,可用于白花蛇舌草药材的质量控制。     

HPLC法同时测定金钱草中槲皮素、槲皮素-3-甲醚及山奈酚的含量

目的：建立金钱草药材中槲皮素、槲皮素-3-甲醚及山奈酚三个活性成分的HPLC含量测定方法。方法：采用Eclipse XDB-C18色谱柱（150 mm×4.6 mm,5μm）,流动相为甲醇-水,等度洗脱（036 min,46%甲醇-1‰磷酸水）,流速为0.8 ml·min-1,检测波长为370 nm,柱温为30℃。结果：槲皮素、槲皮素-3-甲醚及山奈酚的线性范围分别为0.0220.357μg（r=0.999 9）、0.0190.312μg（r=0.999 9）及0.0120.200μg（r=0.999 9）;平均回收率分别为100.1%（RSD=1.79%）、97.4%（RSD=1.98%）和102.8%（RSD=1.90%）。结论：本方法稳定,重复性好,操作简单,可用于金钱草药材的质量控制。     

HPLC-DAD法同时测定中药金钱草中6种活性成分的含量

摘 要 目的：建立HPLC DAD法同时测定中药金钱草中绿原酸、槲皮素、山奈酚、山奈酚-3-O-β-D-葡萄糖苷、芦丁、蒙花苷6种活性成分的含量。方法: Diamonsil C₁₈(200 mm×4.6 mm,5 μm)色谱柱,流动相为甲醇(A)0.3%-磷酸水溶液(B),梯度洗脱,流速：1.0 ml·min^-1,检测波长：360 nm,柱温：30℃。结果: 绿原酸、槲皮素、山奈酚、山奈酚-3-O-β-D-葡萄糖苷、芦丁、蒙花苷的质量分别在0.031~0.624 μg(r=0.999 6) 、0.019~0.386 μg( r=0.999 6)、0.027~0.534 μg (r=0.999 7) 、0.032~0.644 μg(r=0.999 8)、0.019~0.376 μg (r=0.999 8) 、0.017~0.340 μg(r=0.999 7) 内与峰面积呈良好的线性关系。绿原酸、槲皮素、山奈酚、山奈酚-3-O-β-D-葡萄糖苷、芦丁、蒙花苷的平均加样回收率分别为97.35%、97.98%、98.43%、99.57%、98.02%和97.92%,RSD分别为0.87%、1.53%、1.46%、1.24%、1.10%和1.41%(n=6)。结论:该方法简便、准确、重复性好,可用于金钱草药材多成分的质量控制研究。     

油菜花粉中槲皮素和山柰素总含量的HPLC法测定

目的:建立油菜花粉中槲皮素与山柰素总含量的HPLC法的测定方法.方法:以HPLC法定量分析山柰素、槲皮素总含量.色谱条件:色谱柱:Eclipse XDB-C8(150mm×4.6mm,5μm),流动相:甲醇-0.4%磷酸溶液(50:50),检测波长:360nm,流速:1.0mL·min-1,进样量:10μL,以峰面积外标法定量.结果:山柰素与槲皮素的峰与其他色谱峰分离良好,槲皮素在进样量(0.029～0.73μg)、山柰素在进样量(0.053～1.315μg)的范围内,线性关系良好,回归方程分别为:槲皮素线性方程y=3 727.7X-6.0,相关系数r=0.999 9;山柰素线性方程Y=3 932.6X 3.5,相关系数r=0.999 9.槲皮素平均回收率为99.6%,RSD=1.6%,山柰素平均回收率为99.6%,RSD=2.0%.结论:本方法结果准确,重现性好,可以作为油菜花粉中槲皮素和山柰素总含量的定量分析方法.     

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.     

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.