HPLC测定益肾丸中淫羊藿苷的含量

目的：研究益肾丸中淫羊藿苷的含量。方法：采用高效液相色谱法对益肾丸中有效成份淫羊藿苷的含量进行测定。结果：淫羊藿苷的含量在0．15-0．7μg范围内呈良好的线形关系（r=0．9999），RSD（％）为1．49（n=6）。结论：本法灵敏、准确、重现性好，可作为测定益肾丸中淫羊藿苷的含量测定方法。     

高效液相色谱法测定固肾丸中淫羊藿苷的含量

目的：研究固肾丸（主要成分为淫羊藿、熟地、当归等）的质量控制标准。方法：采用高效液相色谱法测定主药淫羊藿苷含量，色谱柱为KromasilC18柱（250mm×4．6mm，5μm）；以纯化水冰醋酸乙腈（69：1：30）为流动相；检测波长为270nm流速：1．0mL·min^-1。结果：淫羊藿苷在0．5-10Mg范围内具有良好线性关系（r=0．9999），平均回收率为99．6％，RSD为1．6％。结论：该法灵敏、简便，重现性好，可作为该制剂的质量控制标准。     

反相高效液相色谱法测定淫羊藿中淫羊藿苷的含量

目的建立用于测定淫羊藿中淫羊藿苷含量的反相高效液相色谱法。方法采用ZORBAX Ecilpse XDB-C18（150mm×4．6mm,5μ）色谱柱;以水-乙腈（74：26,V/V）为流动相;检测波长270nm;流速1．0mL·min^-1,柱温25℃。结果淫羊藿昔质量浓度在5～50mg·L^-1内与其峰面积之间线性关系良好（r=0．9999）,平均加样回收率为100．32％,RSD为0．44％。结论本方法操作简便、快速,结果准确,可用于淫羊藿中淫羊藿苷的含量测定。     

HPLC测定巴仙苁蓉强肾胶囊中淫羊藿苷含量

目的：建立HPLC测定巴仙苁蓉强肾胶囊中淫羊藿苷含量。方法：采用AgilentTC—C18反相色谱柱（250mm×4．6mm,5μm）,以乙腈-水（28：72）为流动相;流速为1．0ml·min^-1;检测波长270nm;柱温：30℃。结果：淫羊藿苷在0．101～1．825μg范围内线性关系良好（r=0．9999,n=6）,平均加样回收率为99．2％,RSD为1．5％（n=6）。结论：本方法操作简便,结果准确、可靠,可用于巴仙苁蓉强肾胶囊中淫羊藿苷的含量测定。     

高效液相色谱法测定穿龙骨刺片中淫羊藿苷的含量

目的：建立高效液相色谱法测定穿龙骨刺片中淫羊藿苷的含量。方法：Agilent C18色谱柱（250mm×4．6mm，5μm），0．075mol·L^-1磷酸溶液（用三乙胺调pH=4．5）-乙腈（75：25）为流动相，流速0．8ml·min^-1检测波长270nm。结果：淫羊藿苷在进样量0．02～0．16μg范围内，与峰面积呈良好的线性关系（r=0．9999），平均回收率为99．2％（RSD=1．0％，n=9）。结论：方法准确可靠、重复性好，简便快速，可用于该制剂的质量控制。     

高效液相色谱法测定安神补脑片中淫羊藿苷含量简

目的建立测定安神补脑片中淫羊藿苷含量的高效液相色谱法。方法采用KromasilC18柱（250mm×4．6mm,5μm）,流动相为乙腈-水（35：65）,流速为0．7mL／min,检测波长为270nm,柱温为30℃。结果淫羊藿苷质量浓度在5．03～50．3μg／mL范围内与峰面积呈良好线性关系（r=0．9998）,平均回收率为98．97％,RSD=1．44％（n=6）。结论该方法灵敏、简便、准确,重现性好,线性关系良好,可作为测定安神补脑片中淫羊藿苷含量的方法。     

高效液相色谱法测定老年咳喘片中淫羊藿苷含量

目的建立测定老年咳喘片中淫羊藿苷含量的高效液相色谱（HPLC）法。方法色谱柱为HC—C18柱（250mm×4．6mm,5μm）,流动相为乙腈-水（25：75）,检测波长为270nm。结果淫羊藿苷进样量的线性范围是0．0144～0．8640μg,方法的平均回收率为98．69％,RSD=0．67％（n=6）,5批样品中淫羊藿苷含量在0．435～0．462mg／g之间。结论HPLC法快速、准确,可用于该制剂中淫羊藿苷的含量测定。     

反相高效液相色谱法测定强筋健骨颗粒中淫羊藿苷的含量

目的建立复方制剂强筋健骨颗粒中的有效成分淫羊藿苷的含量测定方法。方法采用高效液相色谱法,色谱条件：色谱柱Kromasil Cus（4．6mm×250mm,5μml以乙腈-水（25：75）为流动相;检测波长：270nm;流速：1．Oml／min;柱温：25℃。结果本法可用来测定强筋健骨颗粒中淫羊藿苷的含量。淫羊藿苷在0．01949—0．3898μg范围内成良好线性关系,y=0．9998,平均回收率为99．90％,RSD为1．11％。结论本测定方法简便可行、重复性好,可用于本制剂中有效成分淫羊藿苷的含量测定。     

HPLC法测定房陵黄酒保健药酒中淫羊藿苷的含量

目的：建立房陵黄酒保健药酒中主要成分淫羊藿含量测定的方法。方法：采用高效液相色谱法对房陵黄酒保健药酒中的主药淫羊藿测定淫羊藿苷含量,采用Diamonsil^TM（钻石）C18（250mm×4．6mm,5μm）,水-乙（70：30）为流动相,检测波长270nm,柱温30℃,流速1．0ml·min^-1。结果：淫羊藿苷在0．194～1．940μg范围内呈良好的线性关系,r=0．9999;平均回收率为98．22％（RSD=1．93％,n=6）。结论：所建立的方法快速准确、重复性好、简便易行,可作为房陵黄酒保健药酒的质量控制方法。     

反相高效液相色谱法测定益肾壮骨颗粒中淫羊藿苷含量

目的建立益肾壮骨颗粒中淫羊藿苷的含量测定方法。方法采用反相高效液相色谱（RP—HPLC）法,色谱柱为Kromasil C18柱（200mm×4．6mm,5μm）,流动相为乙腈-水（25：75）,检测波长为270nm。结果淫羊藿苷进样量在0．248～1．240μg范围内与峰面积线性关系良好（r=0．9999）．平均回收率为98．82％,RSD=0．44％（n=6）。结论所用方法简便、准确、重现性好,可用于益肾壮骨颗粒的质量控制。     

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.

---

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.