城南细辛化学成分研究(Ⅰ)

目的研究城南细辛的活性化学成分.方法利用柱层析方法分离化合物,理化性质以及光谱方法(UV、IR、NMR、MS)鉴定化合物.结果从城南细辛中离分得3个化合物,鉴定为1-细辛脂素(Ⅰ),1-芝麻脂素(Ⅱ)和β-谷甾醇(Ⅲ).结论化合物Ⅰ、Ⅱ、Ⅲ均为首次从该植物中分离得到.     

假地枫皮中黄酮类化合物研究

目的对假地枫皮进行化学成分研究。方法采用色谱和光谱法分离鉴定假地枫皮的化学成分。结果分离得到三个化合物,分别鉴定为槲皮苷(querc itrin,Ⅰ)、槲皮素(quercetin,Ⅱ)、未知化合物(Ⅲ)。结论Ⅰ、Ⅱ均为首次从该植物中分离得到。     

南葶苈子的化学成分

目的对十字花科植物播娘蒿(Descurainiasophia(L )WebbexPrantl)的种子南葶苈子提取物的化学成分进行分离鉴定。方法南葶苈子的乙醇提取物经D10 1大孔树脂用水及不同体积分数的乙醇洗脱,硅胶柱色谱分离,通过波谱( 1H NMR ,13 C NMR)分析和化学方法鉴定其结构。结果所得到的2个化合物分别被鉴定为4 戊烯酰胺( 4 pentenamide ,Ⅰ)、5 羟甲基糠醛( 5 hydrox ymethylfurfural,Ⅱ)。结论化合物Ⅰ为一个新天然产物;化合物Ⅱ为首次从播娘蒿属植物中分离得到。     

楤木化学成分的研究

目的 研究楤木的化学成分.方法 采用硅胶柱层析、Sephadex LH-20、ODS柱层析、半制备型高效液相色谱等分离方法进行分离纯化,经理化性质和波谱数据分析鉴定化合物结构.结果 分离鉴定了4个三萜皂苷类化合物,分别鉴定为elatoside K methyl ester(Ⅰ)、araloside Amethyl ester(Ⅱ)、pseudoginsenoside RTl butyl ester (Ⅲ)和太白楤木皂苷Ⅰ(Ⅳ).结论 化合物Ⅰ为新化合物,化合物Ⅱ～Ⅳ均为首次从该植物中分离得到.     

桑椹的化学成分

目的对桑科植物桑 (MorusalbaL .)的果实桑椹醇提取物中的化学成分进行提取分离和结构鉴定。方法色谱技术进行分离 ,MS、NMR和IR光谱解析及与对照品比较鉴定化合物。结果共分离得到 7个化合物 ,根据理化性质和谱学分析鉴定了其中的 5个化合物 ,分别为 3 ,4 丙叉基苯甲酸 (2 ,2 dimethyl 1 ,3 dioxa benzo[d]pentane 6 carboxylicacid,Ⅰ )、水杨酸 (salicylicacid ,Ⅱ )、琥珀酸 (succinicacid ,Ⅲ )、胡萝卜苷 (daucosterol,Ⅳ )和己六醇 (1 ,2 ,3 ,4,5 ,6 hexanehexanol,Ⅴ )。结论化合物Ⅰ、Ⅱ、Ⅴ为首次从本属中分离得到的化合物     

黄心卫矛的化学成分研究

目的 研究黄心卫矛Euonymus macropterus Rupr.的化学成分.方法 采用色谱技术分离纯化,并通过波谱技术及理化性质鉴定化合物结构.结果 从黄心卫矛根部的乙醇提取物中分离得到6个化合物,分别鉴定为2-hydroxy hexacosanoicacid,ethyl ester(Ⅰ)、9,12-eicosadienoic acid(9Z,12Z)-,2-hydroxy-3-[[(9Z)-1-oxo-9-oetadecen-1-y1]oxy]pro-pyl ester(Ⅱ)、表木栓醇(Ⅲ)、羽扇豆醇(Ⅳ)、二十烷醇(Ⅴ)、硬脂酸(Ⅵ).结论 以上化合物均首次从黄心卫矛中分离得到,其中,化合物Ⅰ、Ⅱ、Ⅴ、Ⅵ为首次从卫矛属植物中分离得到,化合物Ⅰ首次作为天然产物分离得到.     

刺五加种子的化学成分

目的分离鉴定五加科五加属植物刺五加(Acanthopanaxsenticosus(Rupr .etMaxim .)Har rms)种子的75 % ( φ)乙醇提取物中的化学成分。方法用硅胶柱色谱进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果得到4个化合物,分别鉴定为:3 Оrhamnopyranosyl ( 1 2 ) ara binopyranosyloleanolicacid(化合物Ⅰ)、hederagenin 3 O βglucuronopyranoside(化合物Ⅱ)、oleanolicacid 3 O βglucuronopyranoside(化合物Ⅲ)和齐墩果酸(化合物Ⅳ)。结论化合物Ⅱ、Ⅲ为首次从该属植物中分得     

板蓝根化学成分研究

目的从板蓝根中分离化学成分。方法板蓝根95%乙醇提取物经硅胶吸附,不同溶剂洗脱部分经硅胶柱层析反复分离纯化,测定所得化合物的理化常数和波谱数据,鉴定其化学结构。结果从氯仿及正丁醇部位分离得5个化合物,分别鉴定为4—(1,2,3—三羟基丙基)—2,6—二甲氧基苯—1—O—β—D—葡萄糖苷(Ⅰ)、香草醛(Ⅱ)、甘露醇(Ⅲ)、琥珀酸(Ⅳ)、苯甲酸(Ⅴ)。结论化合物Ⅰ、Ⅱ、Ⅲ为首次从板蓝根药材中分离,具有一定的参考价值。     

南海海绵Hyrtios erectus的肿瘤细胞毒活性成分研究

目的对中国南海海绵Hyrtios erectus的细胞毒活性化学成分进行研究。方法采用多种色谱技术对化合物进行分离纯化,应用光谱技术和理化性质,结合文献对照,鉴定化合物的结构。并用MTT法测定化合物的细胞毒活性。结果从海绵Hyrtios erectus的脂溶性部分共分离得到5个化合物,其结构鉴定为:Hyr-tiosal(Ⅰ),12-βHydroxy-16-scalaren-24,25-olide(Ⅱ),5-Hydroxy-1H-indole-3-ethanol(Ⅲ),胆甾醇(Ⅳ),邻苯二甲酸二丁酯(V)。结论化合物为首次从海绵Hyrtios erectus中分离得到,化合物Ⅰ和Ⅱ显示了较强的细胞毒活性。     

苦味西葫芦果实的三萜类化学成分

目的对苦味西葫芦(Cucurbita pepocv.Dayangua)果实的抗炎活性部位的化学成分进行分离、鉴定。方法采用各种色谱技术进行分离,应用1H NMR1、3C NMR谱学技术确定化合物的结构。结果从抗炎活性部位分离得到4个化合物,分别鉴定为:乙酸蛇麻脂醇酯(lupeol acetate,Ⅰ)、β乙酸香树脂醇酯(βamyrin acetate,Ⅱ)i、somultiflorenol(Ⅲ)i、somultiflorenone(Ⅳ)。结论其中化合物Ⅰ、Ⅱ、Ⅲ为首次从南瓜属植物中分离得到,Ⅳ为首次从本植物中分离得到。     

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.