反相高效液相色谱法测定连翘不同药用部位有效成分的含量

目的比较青翘、老翘不同产地不同药用部位（果壳、种子、果柄）中连翘苷、连翘酯苷、槲皮素的含量。方法采用高效液相色谱法,Ameritech酷瑞C18（250mm×4．6mm,5μm）色谱柱,流动相为乙腈（A）-0．1％甲酸（B）（0～10min,18％～20％A;10～20min,20％～42％A;20～25min,42％A）,流速为1．0mL·min^-1,柱温30℃,检测波长连翘酯苷A、连翘苷为280nm,槲皮素为254nnl。结果青翘、老翘种子中均以连翘酯苷A为主,且其含量远高于连翘苷和槲皮素,果壳中以连翘酯苷A和连翘苷为主,而果柄中3种成分含量差异较小,此外,3种成分在青翘中的含量均高于老翘。结论本研究为连翘药材的质量评价和资源的合理利用提供了科学依据。     

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。     

加味银翘颗粒中多成分的同时鉴别和定量研究

目的；为制定简便、快捷的传统中药质量控制方法。方法；在同一块薄层板上同时鉴别了制剂中的栀子、连翘、牛蒡子，在另一块薄层板上同时鉴别了金银花和甘草。用高效液相法同时测定了该制剂中连翘苷和牛蒡子苷的含量。结果；通过方法学考察，连翘苷的进样量在18．96～379．2ng）（r=0．9999），牛蒡子苷的进样量在0．3228～6．456μg范围内，呈良好的线性关系（r=0．9996）。连翘苷的平均回收率为98．71％（n=9），RSD为2．22％，牛蒡子苷的平均回收率为100．00％（n=9），RSD为1．80％。结论：制剂中多成分的同时鉴别和定量测定简便、快捷、实用。     

HPLC法同时测定江西不同产地广东紫珠药材中连翘酯苷B和金石蚕苷的含量

目的：采用反相高效液相色谱法测定江西不同产地的广东紫珠药材中连翘酯苷B和金石蚕苷的含量。方法：使用Dia—monsil C18色谱柱（250mm×4．6mm，5μm），流动相为乙腈-0．5％磷酸（19：81），流速1．0mL·min^-1检测波长332nm。结果：连翘酯苷B、金石蚕苷进样量分别在0．2～2．0μg和0．28～2．8μg范围内，与峰面积呈良好线性关系；连翘酯苷B及金石蚕苷的平均回收率（n=6）分别为97．7％和101．8％，RSD分别为1．0％和1．7％。结论：本法简便、准确，重复性好，可作为广东紫珠药材的质量控制方法。     

风热感冒颗粒质量标准研究

目的建立风热感冒颗粒的质量控制方法。方法采用高效液相色谱法测定方中君药连翘中连翘苷的含量，同时对连翘、牛蒡子、菊花、板蓝根进行薄层色谱鉴别。结果连翘苷进样量在0．216～1．080μg范围内与峰面积线性关系良好（r=0．9995），平均加样回收率为98．47％，RSD为0．75％（n=6）；薄层色谱斑点清晰，阴性对照无干扰。结论所用方法准确，重现性好，可用于风热感冒颗粒的质量控制。     

抗炎口服液质量标准的研究

目的:建立抗炎口服液的质量标准。方法:采用TLC法对处方中的矮地茶、连翘进行鉴别;用固相萃取处理样品, RP-HPLC法测定连翘苷的含量。结果:在薄层色谱中能检出矮地茶、连翘;连翘苷在0．5～3．0μg线性关系良好,r=1．000 0, 平均回收率为98．2％,RSD为1．5％。结论:该方法准确可靠,能控制制剂的质量。     

HPLC法测定抗感Ⅰ号中连翘苷的含量

建立测定抗感Ⅰ号中连翘苷含量的HPLC法。采用Agilent Eclipse XDB-C18柱；流动相：乙腈-水（24：76）；流速：1.0mL·min；检测波长：277nm；柱温：30℃。连翘苷在0．10～0．50mg·mL^-1浓度范围内呈良好的线性关系（r=0．9999），方法回收率为98．79％，RSD为1．02％（n=9）。该方法简便、快速、准确，适用于抗感Ⅰ号中连翘苷的含量测定。     

高效液相色谱法同时测定注射用双黄连中绿原酸、连翘苷、黄芩苷的含量

目的：建立同时测定注射用双黄连中绿原酸、连翘苷及黄芩苷3组分含量的高效液相色谱方法。方法：采用Hypersil—C18（250mm×4．6mm，10μm），甲醇-乙腈-0．13％磷酸溶液为流动相梯度洗脱，流速为0．8ml·min^-1，检测波长为230nm。结果：绿原酸在0．10～2．03μg范围内线性关系良好（r=0．9997），连翘苷在0．10～1．94μg范围内线性关系良好（r=0．9999），黄芩苷在2．42～48．50μg范围线性关系良好（r=0．9991），平均回收率分别为99．6％（RSD 0．7％，n=9）、99．3％（RSD 1．3％，n=9），100．9％（RSD 1．9％，n=9）．结论：本法简单易行．可用于注射用双昔连的盾号控制．     

感冒解毒灵颗粒的质量标准探讨

目的探讨感冒解毒灵颗粒的质量标准。方法采用薄层色谱法鉴别紫苏叶、川芎，HPLC法测定连翘苷含量。结果色谱条件：C18柱；乙腈-水（25：75）为流动相；流速为1．0ml／分，检测波长为277nm。连翘苷含量和峰面积Y=0．6096＋459．1246X，相关系数r=1．0000，表明连翘苷在0．1065—0．852μg之间呈良好的线性关系。加样平均回收率=99．65％；RSD=0．87％。结论HPLC法测定连翘苷含量简单，易操作，重复性好，可作为控制感冒解毒灵颗粒质量的一种方法。     

HPLC测定清热解毒口服液中4个成分的含量

目的 采用HPLC法测定清热解毒口服液中黄芩苷、绿原酸、连翘苷、连翘酯苷A的含量.方法 采用Zorbax EclipseXDB C18色谱柱(150 mm ×4.6 mm,5μm),柱温30℃,流动相为乙腈-0.3％磷酸溶液,梯度洗脱,流速1.0 mL· min-1,检测波长324 nm(绿原酸、连翘酯苷A)、276 nm(黄芩苷、连翘苷).结果 黄芩苷、绿原酸、连翘苷、连翘酯苷A的线性范围分别为0.182 ～0.912、0.061～0.304、0.037 ～0.183、0.013 ～0.065 μg,加样回收率分别为98.82％、96.94％、105.6％、95.74％(n=6).结论 所用方法操作简单,为全面控制清热解毒口服液的质量提供了一种可靠的检测方法.     

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.

     

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.     

2-(Acetoxyphenyl)-(Z)-styryl sulfides as cyclooxygenase inhibitors

2-(Acetoxyphenyl)-(Z)-styryl sulfides are described as selective cyclooxygenase-2 (COX-2) inhibitors, useful for treating inflammation and COX-2-mediated disorders including neoplasia. 2-(Acetoxyphenyl)-(Z)-styryl sulfide is claimed to be the most potent COX inhibitor in the series with a COX-2 selectivity ratio of 33. This compound is also claimed to be superior to celecoxib (Celebrex^®, Pfizer) in inhibiting cell growth of colorectal carcinoma cells. In this evaluation, the COX inhibitory activity of this compound is compared to that previously disclosed for diarylheterocycles and 2-(acetoxyphenyl)alkyl sulfides. The validity of the DLD-1 cell line in the growth inhibition studies is questioned based on recent literature reports indicating the lack of COX-2 expression in this cell line.     

Sleep-disordered breathing with chronic opioid use

Chronic opioid use for pain relief or as substitution therapy for illicit drug abuse is prevalent in our societies. In the US, retail distribution of methadone and oxycodone has increased by 824 and 660%, respectively, between 1997 and 2003. μ-Opioids depress respiration and deaths related to illicit and non illicit chronic opioid use are not uncommon. Since 2001 there has been an emerging literature that suggests that chronic opioid use is related to central sleep apnoea of both periodic and non-periodic breathing types, and occurs in ～ 30% of these subjects. The clinical significance of these sleep-related abnormalities are unknown. This review addresses the present knowledge of control of ventilation mechanisms during wakefulness and sleep, the effects of opioids on ventilatory control mechanisms, the sleep-disordered breathing found with chronic opioid use and a discussion regarding the future research directions in this area.     

Drug targets for cognitive enhancement in neuropsychiatric disorders

The investigation of novel drug targets for treating cognitive impairments associated with neurological and psychiatric disorders remains a primary focus of study in central nervous system (CNS) research. Many promising new therapies are progressing through preclinical and clinical development, and offer the potential of improved treatment options for neurodegenerative diseases such as Alzheimer's disease (AD) as well as other disorders that have not been particularly well treated to date like the cognitive impairments associated with schizophrenia (CIAS). Among targets under investigation, cholinergic receptors have received much attention with several nicotinic agonists (α7 and α4β2) actively in clinical trials for the treatment of AD, CIAS and attention deficit hyperactivity disorder (ADHD). Both glutamatergic and serotonergic (5-HT) agonists and antagonists have profound effects on neurotransmission and improve cognitive function in preclinical experiments with animals; some of these compounds are now in proof-of-concept studies in humans. Several histamine H3 receptor antagonists are in clinical development not only for cognitive enhancement, but also for the treatment of narcolepsy and cognitive deficits due to sleep deprivation because of their expression in brain sleep centers. Compounds that dampen inhibitory tone (e.g., GABA_A α5 inverse agonists) or elevate excitatory tone (e.g., glycine transporter inhibitors) offer novel approaches for treating diseases such as schizophrenia, AD and Down syndrome. In addition to cell surface receptors, intracellular drug targets such as the phosphodiesterases (PDEs) are known to impact signaling pathways that affect long-term memory formation and working memory. Overall, there is a genuine need to treat cognitive deficits associated with many neuropsychiatric conditions as well as an increasingly aging population.