金莲花多苷片中四种黄酮类化合物的含量测定

目的测定金莲花多苷片中四种黄酮类成分的含量。方法采用高效液相色谱法,以乙腈-0.2%磷酸溶液为流动相,流速为1.0 mL/min,柱温为室温,在360nm波长处,同时测定金莲花中四种黄酮类成分的含量。结果荭草素-2"-O-β-L-半乳糖苷、荭草苷、牡荆苷及槲皮素进样量分别在0.1976~1.9760μg、0.1010~1.0100μg、0.0604~0.6040μg、0.0608~0.6080μg范围内线性关系良好,平均回收率分别为99.17%、98.09%、99.15%、98.54%,RSD分别为1.05%、0.90%、0.54%。0.73%。结论本方法简单准确,重复性良好,适用于金莲花多苷片的含量测定。     

高效液相色谱法测定金莲花胶囊中3种黄酮苷含量

目的 建立金莲花胶囊中荭草苷、牡荆苷和槲皮素的含量测定方法.方法 采用高效液相色谱法,色谱柱为Alltima HP C18柱(250mm×4.6 mm,5μm),流动相为乙腈-1%冰醋酸溶液(15:85),流速为1.0 mL/min,检测波长为360 nm.结果 在上述色谱条件下,槲皮素、荭草苷、牡荆苷分别在2~16,8~64,5~40 μg/mL范围内与峰面积积分值线性关系良好,平均回收率分别为97.66%(RSD=2.06%),99.86%(RSD=1.89%),98.87%(RSD=2.64%).结论 该方法简便、准确、快速,可用于金莲花胶囊的质量控制.     

HPLC法测定导赤冲剂中异牡荆苷和异荭草苷的含量

目的 建立导赤冲剂中异牡荆苷和异荭草苷的含量测定方法.方法 采用高效液相色谱法,色谱柱为迪马C18柱,流动相为四氢呋喃-乙腈-0.2％磷酸水溶液(66∶ 22∶ 12),流速为1.0 mL?nin-1,柱温为35℃,检测波长为330 nm.结果 异荭草苷在0.82～4.08 μg范国内与峰面积积分值呈良好的线性关系(r=0.9990),平均加样回收率为96.4％,RSD为2.7％;异牡荆苷在0.79～3.96 μg范围内与峰面积积分值呈良好的线性关系(r=0.9999),平均加样回收率为98.8％,RSD为2.6％.结论 建立的含量测定方法简便、准确、灵敏,可用于导赤冲剂中异牡荆苷和异荭草苷的含量测定.     

三叶青片剂的质量标准研究

目的研究三叶青片剂的质量标准,为其质量控制奠定基础。方法采用薄层色谱(TLC)法鉴别三叶青片剂中荭草苷、异荭草苷、牡荆素、牡荆素鼠李糖苷及异牡荆素;采用三乙胺显色紫外-可见分光光度(UV-Vis)法,测定三叶青片剂中总黄酮的含量;建立高效液相色谱(HPLC)法测定三叶青片剂中8个主要成分(荭草苷、异荭草苷、牡荆素、牡荆素鼠李糖苷、异牡荆素、绿原酸、新绿原酸及隐绿原酸)的含量,Welch Ultimate XB-C 18色谱柱(4.6 mm×150 mm,2.7μm),梯度洗脱,检测波长:330 nm,流速:0.4 mL·min-1。结果薄层色谱法鉴别三叶青片剂中荭草苷、异荭草苷、牡荆素、牡荆素鼠李糖苷、异牡荆素的展开剂为乙酸乙酯∶甲酸∶甲苯∶水=8∶1∶1∶1,AlCl 3显色后紫外光365 nm下检视;紫外-可见分光光度法测定总黄酮含量,以牡荆素计,在1.85~11.1μg·mL-1范围内与吸光度值呈良好的线性关系,平均加样回收率为98.43%,RSD为2.46%。建立的高效液相色谱法,在考察的浓度范围内,8个成分的浓度与峰面积呈良好的线性关系(r>0.9990),平均回收率为96.88%~99.25%,RSD为1.94%~2.47%。结论本试验建立薄层色谱法鉴别三叶青片剂中荭草苷、异荭草苷、牡荆素、牡荆素鼠李糖苷及异牡荆素,用紫外-可见分光光度法测定三叶青片剂中总黄酮含量,用高效液相色谱法测定8个主要成分含量,为三叶青片剂的质量控制提供参考。     

RP-HPLC法测定四逆散滴丸中芍药苷的含量

目的建立测定四逆散滴丸中芍药苷含量的方法。方法采用高效液相色谱法,用Dia-monsilTM-0DS柱,以乙腈-0.5%醋酸（32∶68）为流动相,检测波长230nm,流速1ml/min测定自制四逆散滴丸中芍药苷的含量。结果芍药苷在15～75μg/ml浓度范围内有良好的线性关系（r=0.9998）,回收率为99.7%,RSD为0.94%。结论本法测定四逆散滴丸中白芍苷的含量,结果准确,可行。     

高效液相色谱法测定白芍药材中芍药苷和芍药内酯苷的含量

目的:建立高效液相色谱法测定白芍药材中芍药苷和芍药内酯苷含量的方法.方法:采用高效液相色谱法,色谱柱:Kromasil ODS2 (4.6 mm×250 mm,5 μm),流动相:甲醇-0.1％磷酸溶液(用1％氢氧化钠溶液调节pH值至4.2)(34:66);流速:1.0 mL·min-1,检测波长:230 nm.结果:芍药内酯苷在0.018～0.576 μg范围内呈线性关系(r=0.9999),芍药苷在0.028～0.896μg范围内呈线性关系(r=0.9999);芍药内酯苷加样回收率为98.18％(n=6),RSD值小于2％,芍药苷加样回收率为98.26％(n=6),RSD值小于2％.结论:本研究所建方法灵敏、简便,能同时准确测定白芍药材中芍药苷和芍药内酯苷的含量.     

高效液相色谱法同时测定五加中剌五加苷B、苷E的含量

目的测定甘肃产五加中剌五加苷B、苷E的含量。方法高效液相色谱法,ODSKromasal柱。水乙晴(955)为流动相,检测波长222nm,柱温度25℃。结果本文可同时测定剌五加苷B、苷E的含量。剌五加苷B、苷E分别在0.064～0.320μg/ml;0.074～0.370μg/ml范围内峰面积与浓度呈线性关系,平均回收率分别为102.5%,RSD=4.2%,95.5%,RSD=4.6%。结论剌五加苷B、苷E在红毛五加中含量最高;茎皮中含量最高;剌五加苷E的含量高于苷B。     

高效液相色谱法同时测定五加中刺五加苷B、苷E的含量

目的：测定甘肃产五加中刺五加苷B、苷E的含量。方法：高效液相色谱法,ODSKromasal柱。水：乙晴（95：5）为流动相,检测波长222nm,柱温度25℃。结果：本文可同时测定枣五加苷B、苷E的含量。刺五加苷B、苷E分别在0．064－0．320μg/ml;0.074-0.370μg/ml范围内峰面积与浓度呈线性关系,平均回收率分别为102．5％,RDS=4.2%,95.5%,RSD=4.6%。结论：剂五加苷Ｂ、苷Ｅ在红毛五加中含量最高,茎皮中含量最高,刺五加苷Ｅ的含量高于苷Ｂ。     

高效液相色谱法同时测定骨筋丸胶囊中龙胆苦苷和芍药苷的含量

建立高效液相色谱法测定骨筋丸胶囊中龙胆苦苷和芍药苷的含量方法。色谱柱:十八烷基键合硅胶柱;流动相:甲醇-水梯度洗脱;流速:1.0 mL.min-1;检测波长:230 nm;柱温:30℃。龙胆苦苷在0.1659μg～1.244μg、芍药苷在0.02978μg～0.2234μg范围内呈良好的线性关系;龙胆苦苷的平均回收率为98.4%,RSD=1.64%,芍药苷的平均回收率为96.8%,RSD=2.43%。本方法简便快捷,准确可靠,确保了骨筋丸胶囊的质量。     

妇炎消胶囊质量标准的研究

目的：提高完善妇炎消胶囊的质量标准。方法：采用薄层色谱法鉴别败酱草;采用高效液相色谱法测定大黄中大黄素和大黄酚的含量;采用高效液相色谱法测定牡丹皮中芍药苷的含量。结果：大黄素在0.0080～0.2012μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为98.1％（RSD＝3.0％,n＝9）;大黄酚在0.0262～0.6550μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为102.4％（ RSD＝2.6％,n＝9）;芍药苷在0.0997～1.9937μg范围内呈良好的线性关系（r＝1.0000）,平均回收率为103.3％（ RSD＝1.5％,n＝9）。结论：建立的方法准确可靠,适用于妇炎消胶囊的质量控制。     

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.

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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.