HPLC法测定红花跌打胶囊中羟基红花黄色素A的含量

目的 建立高效液相色谱法测定红花跌打胶囊中羟基红花黄色素A的含测方法.方法 采用高效液相色谱法,紫外检测器C18柱(4.6 mm×250 mm,5 μm),以甲醇-乙腈-0.7%磷酸溶液(26:2:72)为流动相,检测波长为403 nm,对样品中的羟基红花黄色素A进行测定.结果 通过方法学的系统考察和3批样品的含量测定,建立了制剂中羟基红花黄色素A的高效液相色谱的含量测定方法:线性范围为0.001 2~0.121 7 mg·mL-1,平均回收率99.5%.回归方程Y=584.79X-0.160 4,r=1.结论 本方法简便,快速,准确,灵敏度高,重复性好,可用于红花跌打胶囊中羟基红花黄色素A含量的测定.     

红花鼻炎丸中羟基红花黄色素A的含量测定方法考察

目的:建立红花鼻炎丸中羟基红花黄色素A的含量测定方法.方法:采用反相高效液相色谱法,色谱主为C18柱,以甲醇-乙腈-0.7％磷酸(19∶2∶79)为流动相,流速:1.0mL/min,检测波长为403nm.结果:羟基红花黄色素A在0.01657～0.6628μg范围内呈良好的线性关系,r=-1.000,平均回收99.9％,RSD为0.1％(n=9).结论:实验所用方法专属性强、重现性好、精密度高,能准确地对羟基红花黄色素A进行含量测定.     

HPLC法测定乐脉颗粒中羟基红花黄色素A的含量

目的建立测定乐脉颗粒中羟基红花黄色素A含量的高效液相色谱法。方法采用迪马Diamonsil C18色谱柱,甲醇-0.1%磷酸（30∶70）为流动相,流速1.0mL·min^-1,检测波长403nm,柱温：35℃。结果羟基红花黄色素A在0.0053～0.106mg·mL^-1范围内线性关系良好（r=0.9998）。乐脉颗粒的平均加样回收率为99.5%,RSD=1.8%（n=9）。结论该方法简便快速,适用于乐脉颗粒中羟基红花黄色素A的含量测定。     

HPLC法测定正天丸和正天胶囊中羟基红花黄色素A的含量

目的:建立HPLC法测定正天丸和正天胶囊中羟基红花黄色素A的含量。方法:以十八烷基硅烷键合硅胶为填充剂,以甲醇-乙腈-0.7%磷酸溶液(26∶2∶72)为流动相,检测波长为403 nm。结果:羟基红花黄色素A在6.038 4～150.96μg·mL-1范围内呈良好的线性关系;平均回收率为100.0%,RSD=0.8%(n=6)。结论:本方法准确、快速、重现性好,可用于测定正天丸、正天胶囊中羟基红花黄色素A的含量。     

不同干燥方法对红花中有效成分的影响

目的比较不同干燥方法对红花提取物中有效成分羟基红花黄色素A的影响。方法采用高效液相色谱法测定红花各干燥产物中羟基红花黄色素A的含量,以其为指标,对不同干燥方法进行考察。结果采用真空干燥,喷雾干燥,冷冻干燥所得的产物中羟基红花黄色素A的含量分别为3.21%,8.55%,8.20%。结论相比真空干燥,喷雾干燥和冷冻干燥更适于红花提取物的干燥。     

HPLC法测定苏木-7汤中羟基红花黄色素A的含量

目的：建立蒙成药苏木-7汤中羟基红花黄色素A的含量测定方法测定苏木-7汤中羟基红花黄色素A的含量。方法采用高效液相色谱法。结果羟基红花黄色素A线性范围为0.1304～1.304μg（0.9997）,平均加样回收率101.07%,RSD为1.7%（n=5）。结论该方法灵敏、准确、重复性好、专属性强,适合苏木-7汤的质量控制。     

LC-MS/MS法测定藏药十三味红花丸中羟基红花黄色素A的含量

目的:建立测定藏药十三味红花丸中羟基红花黄色素A含量的方法。方法:样品经甲醇-水(80∶20,V/V)提取,0.22μm微孔滤膜滤过后采用液相色谱-串联质谱(LC-MS/MS)法测定其中羟基红花黄色素A的含量。色谱柱为AgilentZorbaxSB-C18(50mm×2.1mmI.D.,3.5μm),流动相为水(含0.1%甲酸)-乙腈(含0.1%甲酸),梯度洗脱;离子源为电喷雾离子化源(ESI源),离子源温度为500℃,以多反应监测(MRM)方式分别监测离子对m/z611.2→491.2(羟基红花黄色素A)和m/z268.9→159.0(内标染料木素)。结果:羟基红花黄色素A的检测浓度在10～1000ng·mL-1范围内同其与内标的峰面积比值呈良好线性关系(r=0.9989);平均加样回收率在93.8%～106.2%范围内,RSD均<4.90%(n=9)。结论:该方法快速、灵敏,结果准确,适用于藏药十三味红花丸的质量控制。     

七味红花殊胜丸质量标准研究

目的：建立七味红花殊胜丸质量标准。方法：采用薄层色谱法（TLC）对处方中红花进行定性鉴别;用高效液相色谱法（HPLC）测定羟基红花黄色素A含量。结果：TLC定性鉴别分离效果好,斑点显色清晰。羟基红花黄色素A的进样浓度在13.18~79.10μg·ml-1范围内与峰面积积分值呈良好线性关系（r=0.9998）;平均回收率为98.2%,RSD=1.27%（n=6）;每丸含红花以羟基红花黄色素A计应不少于1.0mg。结论：标准可用于该制剂的质量控制。     

反相高效液相色谱法测定红花清肝十三味丸中羟基红花黄色素A的含量

目的:建立红花清肝十三味丸中羟基红花黄色素A的含量测定方法.方法:采用反相高效液相色谱法,色谱柱为Agilent Eclipse XDB-C18柱(250 mm×4.6 mm,5 μm),流动相为甲醇-0.18%乙酸溶液(20:80),检测波长为403 nm,流速为1.0 mL·min-1.结果:羟基红花黄色素A在0.168～16.8 μg范围内具有良好的线性关系,r=0.999 9,平均加样回收率为99.76%,RSD为0.6%.结论:本方法快速、准确,重复性好,可用于红花清肝十三味丸中羟基红花黄色素A的含量测定.     

HPLC法测定新红花-8味丸中羟基红花黄色素A的含量

目的：建立新红花-8味丸的含量测定方法。方法：样品用25%甲醇溶液稀释,在C18柱上以甲醇-乙腈-0.7%磷酸（26∶2∶72）为流动相,在波长403nm处检测羟基红花黄色素A。结果：羟基红花黄色素A在0.126~1.686μg范围内呈良好的线性关系,r=0.9999,平均回收率为100.30%,RSD为0.91%。结论：本法灵敏、准确、简易易行、重现性好。     

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.