天女木兰叶中甾类化合物的分离与鉴定

目的对天女木兰叶的化学成分进行分离和结构鉴定。方法采用硅胶、凝胶柱色谱和重结晶等分离方法对天女木兰叶的体积分数为90%的乙醇溶液提取物进行成分分离;通过谱学分析方法结合化合物理化性质对分离得到的化合物进行结构鉴定。结果分离得到8个化合物,分别鉴定为豆甾-4-烯-3,6-二酮(stigmast-4-en-3,6-dione,1),豆甾-4-烯-3β,6β-二醇(stigmast-4-en-3β,6β-diol,2),5α,8α-过氧-(22E,24R)-麦角甾-6,22-二烯-3β-醇[5α,8α-epidioxy-(22E,24R)-ergosta-6,22-dien-3β-ol,3],豆甾-4-烯-6β-羟基-3-酮(stigmast-4-en-6β-ol-3-one,4),β-谷甾醇(β-sitosterol,5),(22E,24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇[(22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol,6],豆甾-5-烯-3β,7α-二醇(stigmast-5-en-3β,7α-diol,7),胡萝卜苷(daucosterol,8)。结论化合物2-4、6、7为首次从木兰属植物中分离得到,化合物1为首次从该植物中分离得到。     

卵叶海桑化学成分的分离与鉴定

目的研究中国南海红树植物卵叶海桑的化学成分。方法用硅胶、Sephadex LH-20等柱色谱方法进行分离纯化,通过理化性质和核磁共振氢谱、碳谱数据确定化合物的结构。结果分离得到7个化合物,分别鉴定为:20S,24R-环氧达玛烷-3β,25-二醇(ocotillol,1)、熊果酸(2)、白桦脂醇(3)、羽扇豆醇(4)、1β-羟基羽扇豆醇(5)、β-谷甾醇(6)、谷甾-4-烯-3-酮(7)。结论以上化合物均为首次从该植物中分离得到,其中化合物1、5、7为首次从该属植物中分离得到。     

山楂叶的化学成分

目的对蔷薇科山楂属植物山楂(Crataegus pinnatifidaBge.)的叶子部分的化学成分进行研究。方法运用硅胶、Sephadex LH-20柱色谱?ODS柱色谱、制备HPLC等分离手段进行化学成分的分离纯化,根据理化性质及波谱数据鉴定其结构。结果从山楂叶体积分数为80%乙醇的提取物中分离得到7个化合物。分别鉴定为18,19-seco,2α,3β,-dihydroxy-19-oxo-urs-11,13(18)-dien-28-oic acid(1)、3,9-dihydroxy-megastigma-5-ene(2)、(3S,5R,6R,7E)-megatsigmane-7-ene-3-hydrox-y-5,6-epoxy-9-O-β-D-glucopyranoside(3)、(Z)-3-hexenyl-6-O-β-D-xylopyranosyl-(1″-6′)-β-D-gluco-pyranoside(β-primeveroside)(4)、苯甲酸(5)、对羟基苯丙酸(6)、反式对羟基桂皮酸(7)。结论化合物1-4为首次从该属植物中分离得到,5-7为首次从该种植物中分离得到。     

滇产两面针化学成分的分离与鉴定

目的对滇产两面针(Zanthoxylum nitidum(Roxb.)DC.)中的化学成分进行研究。方法运用硅胶柱色谱、Rp~(-1)8柱色谱和Sephadex LH-20柱色谱等分离手段对滇产两面针的体积分数为95%的乙醇提取物中的化学成分进行分离纯化,根据理化性质及波谱数据分析对化合物进行结构鉴定。结果从滇产两面针体积分数为95%的乙醇提取物中分离得到10个化合物,分别被鉴定为γ-崖椒碱(γ-fagarine,1)、茵芋碱(skimmianie,2)、白鲜碱(dictamnine,3)、左旋丁香树脂酚[(-)-syringaresinol,4]、博落回醇碱(bocconoline,5)、花椒木精(zanthoxyline,6)、4-甲氧基~(-1)-甲基-2-喹诺酮(4-methoxy~(-1)-methyl-2-quinolone,7)、大叶桉亭(robustine,8)、rhoifoline B(9)、6β-hydroxymethyldihydronitidine(10);运用二维核磁共振技术HM QC和HM BC将化合物10的核磁共振氢谱(1H-NM R)和核磁共振碳谱(13C-NM R)进行了一一归属。结论化合物6-9为首次从该种植物中分离得到,化合物10为首次从花椒属植物中分离得到的新结构化合物。     

洋紫荆中化学成分的分离与鉴定

目的研究洋紫荆中的化学成分.方法采用硅胶、聚酰胺、Sephedex LH-20柱色谱分离纯化,理化常数和谱学方法鉴定结构.结果 分离得到7个化合物和1个混合物,鉴定为friedelin(1)、24(R)-9,19-cyclolanost-3-one-24,25-diol(2)和24(S)-9,19-cyclolanost-3-one-24,25-diol(3)的混合物、豆甾烷-3-酮(4)、豆甾烷-4-烯-3-酮(5)、豆甾烷-3β-醇-6-酮(6)、豆甾烷-5-烯-3β-醇-7-酮(7)、β-谷甾醇(8)、大黄素甲醚(9).结论 化合物2和3的混合物、5、7、9为首次从该属植物中分离得到.     

红药中一个新的β-萘甲酸双糖苷类化合物(英文)

为了研究红药(Chirita longgangensis var.hongyao)茎的化学成分,运用多种色谱方法进行分离纯化,从其甲醇提取物中分离得到3个化合物,并根据理化性质和波谱数据鉴定其结构分别为1,4-dihydroxy-2-naphthalenecarboxylic acid methyl ester-4-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside(1),isotaxiresinol 4-O-methyl ether(2)和(R)-7-hydroxy-α-dunnione(3)。其中,化合物1为新的β-萘甲酸双糖苷化合物,化合物2为首次从该属植物中分离得到,且首次提供了化合物2的核磁波谱数据,化合物3为首次从该植物中分离得到。     

温郁金挥发油的化学成分

目的对温郁金(Curcuma wenyujin)挥发油的化学成分进行研究。方法采用硅胶柱色谱、正反相MPLC及HPLC等进行分离纯化,通过波谱分析鉴定其结构。结果从温郁金挥发油中分离得到10个化合物,鉴定为莪术醇(1)、莪术二酮(2)、(4S,5S)-germacrone-4,5-epoxide(3)、germa-crone-1,10-epoxide(4)、新莪术二酮(5)、(5R,6R,7αR)-5-isopropenyl-3,6-dimethyl-6-vinyl-5,6,7α-tetrahydro-4H-enzofuran-2-one(6)、hydroxyisogermafurenolide(7)、(5R,6R,7aS)-5-isopropenyl-3,6-dimethyl-6-vinyl-5,6,7,7-αtetrahydro-4-Hbenzo-furan-2-one(8)、脱-氢1,8-桉叶素(9)、p-menth-2-ene-1,8-diol(10)。并通过核磁共振手段对其碳氢信号进行了全归属。结论化合物6、7为新的天然产物;化合物4、8、10为首次从该属植物中分离得到;化合物4、6、7、8、10为首次从该种植物中分离得到。     

肥牛木枝条化学成分的分离与鉴定

目的对肥牛木[Cephalomappa sinensis(Chun et How)Kosterm.]的化学成分进行研究。方法用多种色谱技术对化合物进行分离纯化,并根据化合物的理化性质及波谱数据鉴定化合物的结构。结果从肥牛木的枝条乙醇提取物中分离得到6个化合物,分别鉴定为羽扇豆醇(1)、乙酰油桐酸(2)、没食子酸(3)、(3S,5R,6S,7E,9R)-3,6-dihydroxy-5,6-dihydro--βionol(4)、(3,β4,α5α,6αH,7E,9S)-3,4-dihydroxy-5,6-dihydro-β-ionol(5)、东莨菪素(6)。结论化合物1、4和5均为首次从该植物中分离得到。     

猴耳环化学成分的分离与鉴定及抗氧化活性测定

目的研究猴耳环(Pithecellobium clypearia Benth.)的化学成分,并采用DPPH和ABTS法考察分离得到的化合物的体外抗氧化活性。方法采用Sephadex LH-20柱色谱、ODS柱色谱、硅胶柱色谱﹑制备HPLC等分离手段对猴耳环枝叶的化学成分进行分离,通过理化性质及波谱数据进行化合物结构鉴定,采用DPPH和ABTS自由基清除法对分离得到的化合物进行体外抗氧化活性评价。结果从猴耳环的枝叶中分离得到7个单体化合物,分别鉴定为:(+)-lyoniresinol(1)、protocatechuic acid methy ester(2)、(2R,3R)-7,8,3',4'-tetrahydroxydihydroflavonol(3)、(2R,3S)-5,7,3'-tri-Omethyl-(-)-epicatechin(4)、木犀草素(luteolin,5)、槲皮素(quercetin,6)和没食子酸(gallic acid,7)。结论化合物1~4为首次从猴耳环植物中分离得到。化合物1~7均具有一定的抗氧化活性。     

脚骨脆的化学成分研究

目的研究脚骨脆小枝和叶的化学成分。方法采用乙醇提取,提取物经萃取后以硅胶、凝胶和MCI等柱色谱法及高效液相色谱法进行分离纯化,采用波谱法进行结构鉴定。结果从该植物共分离得到8个化合物,其结构鉴定为:(6R,7E,9R)-9-hydroxymegastigm-4,7-dien-3-one,(6S,7E)-6-hydroxy-4,7-megastig-madiene-3,9-dione,(3S,5R,6S,7E)-5,6-epoxy-3-hydroxymegastigm-7-en-9-one,(6E,9S)-9-hydroxymegastigm-4,6-dien-3-one,caseamembrin A,casearlucin B,β-谷甾醇和胡萝卜苷。结论前6种化合物为首次从该植物中分离得到。     

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.