工业大麻研究.Ⅰ.甲醇提取物的石油醚萃取和正丁醇萃取部分的化学成分

从工业大麻甲醇提取物的石油醚萃取部分分离鉴定了14个化合物,分别为B-谷甾醇(1)、豆甾醇(2)、二十二烷酸甲酯(3)、△5,22-豆甾醇乙酸酯(4)、α-菠菜甾醇(5)、表无羁萜醇(6)、无羁萜酮(7)、四氢大麻酚(8)、大麻二酚(9)、大麻二酚酸(10)、cannabielsoic acid A(11)、大麻酚(12)、催叶萝芙叶醇(13)和去氢催叶萝芙叶醇(14).从正丁醇萃取部分分离鉴定了15个化合物,分别为芦丁(15)、槲皮素-3-O-α-L-鼠李糖苷(16)、山奈酚-3-O-α-L-鼠李糖苷(17)、芹菜素-7-O-α-L-鼠李糖苷(18)、芹菜素-7-O-β-D-吡喃葡萄糖苷(19)、木犀草素-7-O-β-D-吡喃葡萄糖苷(20)、1,3,6,7-四羟基-2-C-β-D-吡喃葡萄糖口山酮(21)、牡荆素(22)、荭草素(23)、芹菜素-6,8-二-C-β-D-吡喃葡萄糖苷(24)、牡荆素-2"-O-α-L-鼠李糖苷(25)、荭草素-2"-O-β-D-吡喃葡萄糖苷(26)、肌醇甲醚(27)、肌醇(28)、尿嘧啶(29).其中化合物3、4、5、21、24、27、29为首次报道从该属植物中得到.     

密蒙花中黄酮类成分的分离与鉴定

目的对密蒙花(Buddleja officinalis Maxim.)中的黄酮类成分进行研究,为其资源开发与利用提供依据。方法综合应用大孔吸附树脂、正相硅胶、反相ODS和Sephadex LH-20等柱色谱以及高效液相色谱法对密蒙花中黄酮类成分进行分离纯化,并结合单体成分的理化性质与核磁共振波谱数据鉴定其结构。结果与结论从密蒙花体积分数70%乙醇溶液的提取物中分离鉴定了11个黄酮类化合物,分别为木樨草素(1)、木樨草素-7-O-葡萄糖苷(2)、木樨草素-7-O-芸香糖苷(3)、芹菜素-7-O-β-D-葡萄糖苷(4)、芹菜素-7-O-β-D-芸香糖苷(5)、蒙花苷(6)、芹菜素-7-O-β-D-葡萄糖醛酸苷(7)、芹菜素-4'-O-β-D-葡萄糖醛酸苷(8)、芹菜素-7-(2'-α-L-鼠李糖基)芸香糖苷(9)、密蒙花新苷(10)、山柰酚-3-O-芸香糖苷(11),其中,化合物7~9、11均为首次从醉鱼草属植物中分离得到。     

丫蕊花的化学成分

从百合科丫蕊花属植物丫蕊花(Ypsilandra thibetica Franch)全草中分离鉴定了8个化合物,分别为:偏诺皂苷元(1),偏诺皂苷元-3-O-α-L-呋喃阿拉伯糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(2),偏诺皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(3),偏诺皂苷元-3-O-α-L-吡喃葡萄糖(1→4)-α-L-吡喃鼠李糖(1→4)-[α-L-吡喃鼠李糖(1→2)]-β-D-吡喃葡萄糖苷(4),薯蓣皂苷元(5),薯蓣皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(6),木犀草素(7),木犀草苷(8)。其中化合物1,2,5,7,8均首次在丫蕊花植物中分到。     

多腺悬钩子黄酮类化学成分研究

目的研究藏药多腺悬钩子的黄酮类成分。方法采用各种柱色谱技术对其成分进行分离纯化,根据理化性质和波谱分析鉴定化合物的结构。结果从中分离得到8个黄酮类化合物,经鉴定分别为:槲皮素(1),5,7,4′-三羟基双氢黄酮(2),木犀草素(3),木犀草素-7-O-β-D-葡萄糖苷(4),5,7,3′-三羟基-8,4′,5′-三甲氧基黄酮(5),香叶木素-7-O-β-D-葡萄糖苷(6),槲皮素-3-O-β-D-葡萄糖基-7-O-α-L-鼠李糖苷(7)和槲皮素3-O-β-D-葡萄糖苷(8)。结论所有化合物均为首次从该植物中分离得到。     

扬子毛茛中的化学成分研究

目的研究扬子毛茛的化学成分.方法应用多种色谱方法和色谱材料进行提取、分离和纯化,用各种现代光谱方法并结合文献对分得的化合物进行结构解析.结果从扬子毛茛的95%乙醇提取物中分到十三个化合物,其中五个为黄酮苷类化合物,分别命名为芹菜素-4'-O-α-L-鼠李糖苷(1),芹菜素-7-O-β-D-葡萄糖苷-4'-O-α-L-鼠李糖苷(2),芹菜素-8-C-α-L-阿拉伯糖苷(3),芹菜素-8-C-β-D-半乳糖苷(4),小麦黄素-7-O-β-D-葡萄糖苷(5);其余八个分别为小麦黄素(6),木犀草素(7),东莨菪内酯(8),秦皮乙素(9),滨蒿内酯(10),阿魏酸(11),原儿茶酸(12)和小毛茛内酯(13).此外还对这些化合物的体外抗癌活性进行了初步的测试.结论化合物1-12为首次从该属植物中分到,化合物13为首次从该种植物中分到,其中化合物1为新的天然产物,化合物2和3首次报道了其碳谱数据.生物活性测试结果表明化合物1对BEL-7407及A549细胞的IC50值分别为43及77μg·mL-1,化合物8和10对KB细胞的IC50分别为78和44μg·mL-1,对HL-60细胞的IC50均为85μg·mL-1.化合物7对所测试的四种肿瘤细胞株均显示一定的细胞毒活性,其对KB,BEL-7407,A549及HL-60细胞的IC50分别为51,55,44和10μg·mL-1.     

黄花蒿水提物黄酮苷类成分研究

采用HP-20大孔吸附树脂、MCI柱色谱、硅胶柱色谱、中压液相色谱、葡聚糖凝胶Sephadex LH-20柱色谱及制备液相色谱等多种色谱技术,从黄花蒿水提物的正丁醇部位分离得到21个黄酮苷类化合物。根据化合物的理化性质和波谱数据确定了它们的结构,分别为甲氧基万寿菊素-7-O-β-D-吡喃木糖-(1→6)-β-D-吡喃葡萄糖苷(1)、荭草苷(2)、芹菜素-6-C-β-D-吡喃葡萄糖-8-C-β-L-吡喃阿拉伯糖苷(3)、芹菜素-6-C-β-D-吡喃半乳糖-8-C-β-L-吡喃阿拉伯糖苷(4)、芹菜素-6-C-β-L-吡喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(5)、芹菜素-6-C-α-L-呋喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(6)、槲皮素-3-O-β-D-吡喃葡萄糖苷-(1→2)-β-D-吡喃葡萄糖苷(7)、芹菜素-6-C-α-L-吡喃阿拉伯糖-8-C-β-D-吡喃葡萄糖苷(8)、芹菜素-6,8-二-C-吡喃葡萄糖苷(9)、万寿菊素-7-O-β-D-吡喃葡萄糖苷(10)、木犀草素-6-C-吡喃葡萄糖苷(11)、牡荆素(12)、山柰酚-3-O-β-吡喃半乳糖-(1→2)-β-吡喃葡萄...     

齿叶白鹃梅叶中黄酮类成分的分离与结构鉴定

目的研究齿叶白鹃梅叶的化学成分。方法采用硅胶柱色谱、重结晶和Sephadex LH-20凝胶柱色谱的方法进行化学成分的分离和纯化,根据化合物的理化性质和波谱数据鉴定其结构。结果分离得到6个黄酮类化合物,经鉴定为芹菜素(apigenin1,),木犀草素(luteolin,2),槲皮素(querce-tin,3),槲皮素-3-O-β-D-葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,4),芹菜素-7-O-β-D-葡萄糖苷(apigenin-7-O-β-D-glucopyranoside,5),芹菜素-7-O-β-D-新橙皮糖苷(apigenin-7-O-β-D-neosphero-side,6)。结论化合物1-6均首次从此植物中分离得到。     

马尾松松针的黄酮类化学成分的分离鉴定

目的：研究松科植物马尾松松针亲水性部分的化学成分。方法：利用Sephadex-LH 20、ODS和硅胶等柱色谱技术进行分离纯化，根据化合物的理化性质和光谱数据进行结构鉴定。结果：从马尾松松针的醋酸乙酯和正丁醇萃取部分分离得7个黄酮类化合物，其化学结构分别确定为3＇，5-二羟基-4＇-甲氧基二氢黄酮-7-O-α-L-鼠李糖基（1→6）-β-D-葡萄糖苷（1），3＇，5-二羟基-4＇-甲氧基二氢黄酮-7-O-β-D-葡萄糖（1→2）-α-鼠李糖苷（2），4＇，5-二羟基二氢黄酮-7-O-α-L-鼠李糖基（1→2）-β-D-葡萄糖苷（3），木犀草素（4），木犀草素-7-O-吡喃葡萄糖苷（5），槲皮素（6）和双氢槲皮素（7）。结论：化合物1～5为首次从本植物中分离得到。     

中药北刘寄奴中黄酮类成分的分离与鉴定

目的研究中药北刘寄奴(Siphonostegia chinensis Benth.)的化学成分。方法采用正相硅胶、反相ODS、Sephadex LH-20等柱色谱及高效液相色谱等手段进行分离纯化,并通过理化性质与光谱分析方法鉴定了化合物的结构。结果从北刘寄奴体积分数为95%的乙醇提取物中分离鉴定了8个黄酮类单体成分,分别为芹菜素(apigenin,1)、芹菜苷(apigentrin,2)、木犀草素(luteolin,3)、木犀草素-7-O-β-D-葡萄糖苷(luteolin-7-O-β-D-glucopyranoside,4)、槲皮素-3-O-β-D-葡萄糖苷(quer-cetin-3-O-β-D-glucopyranoside,5)、槲皮素-3-O-α-L-鼠李糖苷(quercetin-3-O-α-L-rhamnopyranoside,6)、isoscutellarein 8-glucuronide(7)、大豆素(daidzein,8)。结论其中化合物4～8为首次从阴行草属中分离得到。     

火绒草中的黄酮苷类成分

目的研究火绒草[Leontopodium leontopodioides(Wild.)Beauv.]中黄酮苷类化学成分。方法采用反复硅胶柱色谱法、Sephadex LH-20柱色谱法、ODS柱色谱法和反复重结晶等方法进行分离纯化,并通过理化常数测定和波谱分析鉴定了其化学结构。结果从体积分数为60%的火绒草乙醇溶液提取物中分离得到5个化合物,并鉴定其结构为:芹菜素-7-O-β-D-吡喃葡萄糖苷(apigenin-7-O-β-D-glu-copyranoside1)、木犀草素-4′-O-β-D-吡喃葡萄糖苷(luteolin-4′-O-β-D-glucopyranoside2)、6-羟基-木犀草素-7-O-β-D-吡喃葡萄糖苷(6-hydroxyluteolin-7-O-β-D-glucopyranoside3)、6-羟基-芹菜素-7-O-β-D-吡喃葡萄糖苷(6-hydroxyapigenin-7-O-β-D-glucopyranoside4)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside5)。结论化合物4,5为首次从火绒草属植物中分离得到,化合物2,3为首次从本植物火绒草中分离得到。     

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.

     

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.     

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.     

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.