长药隔重楼中甾体皂苷成分的分离与结构鉴定

目的 研究长药隔重楼Paris polyphylla Smith varh.pseudothibetica的化学成分.方法 采用硅胶柱层析、大孔吸附树脂、葡聚糖凝胶Sephadex LH-20、预装硅胶中压柱层析及半制备RP-HPLC等技术分离纯化单体化合物,根据理化性质及波谱数据鉴定其结构.结果 从长药隔重楼乙醇提取物中分离并鉴定了8个甾体皂苷类单体化合物,分别是偏诺皂苷元-3-O-β-D-葡萄吡喃糖苷(Ⅰ)、薯蓣皂苷元-3-O-а-L-阿拉伯呋喃糖基(1→4)-[а-L-鼠李吡喃糖基(1→2)]-B-D-葡萄吡喃糖苷(Ⅱ)、薯蓣皂苷元-3-O-а-D-葡萄吡喃糖基(1→)-[а-L-鼠李吡喃糖基(1→2)]-β-D-葡萄吡喃糖苷(Ⅲ)、偏诺皂苷元-3-а-L-鼠李吡喃糖基(1→2)-B-D-葡萄吡喃糖苷(Ⅳ)、偏诺皂苷元-3-O-а-L-阿拉伯呋喃糖基(1→4)-[а-L-鼠李吡喃糖基(1→2)]-β-D-葡萄吡喃糖苷(Ⅴ)、偏诺皂苷元-3-O-а-L-鼠李吡喃糖基(1→4)-a-L一鼠李吡喃糖基(1→4)-[а-L-鼠李吡喃糖基(1→2)]-β-D-葡萄吡喃糖苷(Ⅵ)、偏诺皂苷元-3-D-β-L-鼠李吡喃糖基(1→4)-[a-L-鼠李吡喃糖基(1→2)]-β-D-葡萄吡喃糖苷(Ⅶ)、偏诺皂苷元-3-O-β-D-木呋喃糖基(1→5)-а-L-阿拉伯呋喃糖基(1→4)-[а-L-鼠李吡喃糖基(1→2)]-β-D-葡萄吡喃糖苷(Ⅷ).结论 首次从长药隔重楼中分离并鉴定出化合物Ⅰ～Ⅷ.     

胡芦巴皂苷Ⅷ的结构鉴定

目的研究中国产胡芦巴Trigonella foenum-graecum L.种子的化学成分.方法采用硅胶色谱柱进行分离,通过物理、化学和光谱学方法鉴定化合物的结构.结果分离得到一甾体皂苷,命名为胡芦巴皂苷VIII,鉴定其结构为26-O-β-D-吡喃葡糖基-25(R)-5α-呋甾烷-20(22)-烯-2α,3β,26-三醇-3-O-β-D-吡喃木糖基(1→6)-β-D-吡喃葡糖苷.结论胡芦巴皂苷VIII为新化合物.     

蒺藜化学成分的研究

目的:研究蒺藜( Tribulusterrestris L.) 中生物活性物质。方法:用硅胶柱色谱、HPLC进行分离,根据光谱数据鉴定其结构。结果:分离纯化得到两种呋甾皂苷,确定其结构为26-O-β-D 吡喃葡糖基-(25 R,S)-5α- 呋甾-12-羰基-20(22)-烯基-3β,26-二醇-3-O-β-D-吡喃葡糖基(1 →4)-β-D-吡喃半乳糖苷(I) ;26 O-β-D-吡喃葡糖基-(25 R)-5α-呋甾-12-羰基 3β,22α,26 三醇-3-O-β-D-吡喃葡糖基(1→2)-β-D-吡喃半乳糖苷(II)。结论:I,II均为新化合物。     

灯台七化学成分及抗癌活性研究

目的研究灯台七化学成分及抗癌活性。方法采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、半制备高效液相色谱等方法分离纯化,理化性质及现代波谱技术鉴定其结构。通过MTT法评价化合物4~8的抗癌活性。结果共分离鉴定了8个化合物,分别为β-蜕皮激素(1)、pinnatasterone(2)、豆甾醇(3)、豆甾醇-3-O-β-D-吡喃葡萄糖苷(4)、偏诺皂苷元3-O-α-L-鼠李吡喃糖(l→2)[α-L-阿拉伯呋喃糖(1→4)]-β-D-葡萄吡喃糖苷(5)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖(l→4)α-L-鼠李吡喃糖(1→4)-[α-L-鼠李吡喃糖(l→2)]-β-D葡萄吡喃糖苷(6)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖(l→4)-[α-L-鼠李吡喃糖基(1→2)]-β-D-葡萄糖苷(7)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖基(l→4)-[α-L-鼠李吡喃糖基(1→4)]-β-D-葡萄糖苷(8)。化合物5~8对结肠癌SW620和HT-29细胞有显著的抑制作用。结论化合物5~8均表现出很强的细胞毒活性。     

蒺藜果实中甾体皂苷类成分研究

目的研究蒺藜（Tribulus terrestrisL.）果实的皂苷类化合物。方法利用硅胶柱色谱、凝胶柱色谱、中低压色谱、高效液相色谱等手段进行分离,根据理化性质及波谱数据鉴定结构。结果从蒺藜果实中得到4个已知化合物,分别鉴定为（25R）-2α,3β-二醇-5α-螺甾烷-12-酮（门诺皂苷元）-3-O-{β-D-吡喃葡萄糖基-（1→2）-[β-D-吡喃木糖基-（1→3）]-β-D-吡喃葡萄糖基-（1→4）-β-D-吡喃半乳糖苷}（1）、26-O-β-D-吡喃葡萄糖基-（25R）-5α-呋甾-22-甲氧基-2α,3β,26-三醇-3-O-β-D-吡喃葡萄糖基-（1→2）-β-D-吡喃葡萄糖基-（1→4）-β-D-吡喃半乳糖苷（2）、海柯皂苷元-3-O-{β-D-吡喃葡萄糖基-（1→2）-[β-D-吡喃木糖基-（1→3）]-β-D-吡喃葡萄糖基-（1→4）-β-D-吡喃半乳糖苷}（3）、26-O-β-D-吡喃葡萄糖基-（25R）-5α-呋甾-12-羰基-20（22）-烯-3β,26-二醇-3-O-β-D-吡喃葡萄糖基-（1→4）-β-D-吡喃半乳糖苷（4）。结论化合物1和2为首次从该属植物中分离得到,化合物4为首次得到的25位R构型的甾体皂苷类单体化合物。     

维药斯亚旦化学成分研究

目的研究维药斯亚旦的化学成分。方法采用正相硅胶、ODS、Sephadex LH-20等柱色谱以及高效制备液相等手段进行分离纯化,并用化学方法和光谱方法鉴定了化合物的结构。结果从斯亚旦中分离鉴定了10个化合物,分别为:五加苷K(1)、常春藤皂苷元-3-O-α-L-鼠李糖基(1→2)-α-L-吡喃阿拉伯糖苷(2)、常春藤皂苷元-3-O-β-D-吡喃木糖基(1→3)-α-L-鼠李糖基(1→2)-α-L-吡喃阿拉伯糖苷(3)、quercetin-3-[6-ferulyl-β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl(1→2)-β-D-glucopyrano-side](4)、quercetin-3-sophorotriosides(5)、quercetin-3-glucosyl(1→2)-galactosyl(1→2)-glucoside(6)、quercetin-3-(6-feruloylglu-cosyl)(1→2)-galactosyl(1→2)-glucoside(7)、3-O-α-L-吡喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖常春藤皂苷元-28-O-α-L-吡喃鼠李糖基(1→4)-β-D-吡喃葡萄糖基(1→6)-β-D-吡喃葡萄糖(8)、3-O-β-D-吡喃葡萄糖基(1→6)-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖常春藤皂苷元-28-O-α-L-吡喃鼠李糖基(1→4)-β-D-吡喃葡萄糖基(1→6)-β-D-吡喃葡萄糖苷(9)和芦丁(10)。结论化合物1,4,5为首次从黑种草属中分离得到,化合物6为首次从该种中分离得到。     

长药隔重楼的化学成分研究

目的 研究长药隔重楼的化学成分.方法 采用柱色谱方法单分离纯化单体化合物,通过波谱学方法鉴定其结构.结果 分离并鉴定了5个化合物,分别是△5,22-豆甾醇3-O-β-D-葡萄吡喃糖苷(I),20β-羟基蜕皮激素(Ⅱ),B-L-脱氧胸腺嘧啶苷(Ⅲ),偏诺皂苷元3-O-α-L-鼠李吡喃糖基-(1→2)-p-D-葡萄吡喃糖苷(Ⅳ)和偏诺皂苷元3-O-α-L-鼠李吡喃糖基-(1→4)-α-L-鼠李吡喃糖基-(1→4)-[α-L-鼠李吡喃糖基-(1→2)-]-β-D-葡萄吡喃糖苷(Ⅴ).结论 所有化合物均为首次从该植物中得到;其中化合物Ⅲ为首次从该属植物中分离得到.     

瘤果黑种草子的化学成分

目的研究中药瘤果黑种草子的化学成分。方法运用多种色谱方法分离化学成分;依据这些化学成分的理化性质和波谱(NMR、EI-MS)数据分析鉴定化合物的结构。结果从瘤果黑种草子中初步分离得到5个化合物,分别鉴定为胡萝卜苷(1)、常春藤皂苷元-3-O-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖苷(2)、常春藤皂苷元-3-O-β-D-吡喃木糖基-(1→3)-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖苷(3)、3-O-β-D-吡喃木糖基-(1→3)-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖常春藤皂苷元-28-O-β-D-吡喃葡萄糖酯苷(4)、山奈酚-3-O-β-D-吡喃葡萄糖基-(1→2)-β-D-吡喃半乳糖基-(1→2)-β-D-吡喃葡萄糖苷(5)。结论化合物4为首次从黑种草属植物中分离得到,化合物5为首次从该种植物中分离得到。     

南山藤的化学成分研究

从萝藦科南山藤属植物南山藤的干燥茎中分离鉴定了6个化合物:β-D-黄夹吡喃糖基-(1→4)-β-D-磁麻吡喃糖基-(1→4)-β-D-阿洛吡喃糖苷(1),β-D-黄夹吡喃糖基-(1→4)-β-D-磁麻吡喃糖苷(2),marsectohexol(3),drevogenin D 3-O-β-D-磁麻吡喃糖苷(4),dregeosides Da1(5),dregeosides A11(6)。其中,化合物1为新低聚糖,化合物4为首次从属内分得C21甾体苷。     

具有抗炎活性的双三糖链呋甾皂苷的合成

目的设计合成两个甲基原薯蓣皂苷的衍生物，分别为3，26-O-二{α-L-吡喃鼠李糖基-（1→2）-[α-L-吡喃鼠李糖基-（1→4）]-3，6-O-二特戊酰基-β-D-吡喃葡萄糖基}-22-甲氧基-25（R）-呋甾-5-烯-3β，26-二醇（1）和3，26-O-二{α—L-吡喃鼠李糖基-（1→2）-[a—L-吡喃鼠李糖基-（1→4）]-β-D-吡喃葡萄糖基}-22-甲氧基-25（R）-呋甾-5-烯-3β，26-二醇（2）。方法以薯蓣皂素为起始原料，采用逐步糖苷化策略，经10步反应制得目标化合物，总收率约为15％。结果与结论合成的两个双三糖链呋甾皂苷均为未见文献报道的新化合物．其结构经ESI-MS和^13C-NMR确证，初步生物活性筛选结果表明化合物1具有一定的抗炎活性。     

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.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

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.