978 resultados para Autriche, André (15..-16..) -- Portraits


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Background: Flying lemurs or Colugos (order Dermoptera) represent an ancient mammalian lineage that contains only two extant species. Although molecular evidence strongly supports that the orders Dermoptera, Scandentia, Lagomorpha, Rodentia and Primates form a superordinal clade called Supraprimates (or Euarchontoglires), the phylogenetic placement of Dermoptera within Supraprimates remains ambiguous. Results: To search for cytogenetic signatures that could help to clarify the evolutionary affinities within this superordinal group, we have established a genome-wide comparative map between human and the Malayan flying lemur (Galeopterus variegatus) by reciprocal chromosome painting using both human and G. variegatus chromosome-specific probes. The 22 human autosomal paints and the X chromosome paint defined 44 homologous segments in the G. variegatus genome. A putative inversion on GVA 11 was revealed by the hybridization patterns of human chromosome probes 16 and 19. Fifteen associations of human chromosome segments (HSA) were detected in the G. variegatus genome: HSA1/3, 1/10, 2/21, 3/ 21, 4/8, 4/18, 7/15, 7/16, 7/19, 10/16, 12/22 (twice), 14/15, 16/19 (twice). Reverse painting of G. variegatus chromosome-specific paints onto human chromosomes confirmed the above results, and defined the origin of the homologous human chromosomal segments in these associations. In total, G. variegatus paints revealed 49 homologous chromosomal segments in the HSA genome. Conclusion: Comparative analysis of our map with published maps from representative species of other placental orders, including Scandentia, Primates, Lagomorpha and Rodentia, suggests a signature rearrangement (HSA2q/21 association) that links Scandentia and Dermoptera to one sister clade. Our results thus provide new evidence for the hypothesis that Scandentia and Dermoptera have a closer phylogenetic relationship to each other than either of them has to Primates.

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于2010-11-23批量导入

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人工合成麝香作为一种新型污染物,其生态行为及生态效应已经越来越受到关注。城市土-水界面污染流是除农业面源污染以外第二大面源污染,其成分复杂,采用常规的理化监测方法很难对其生态安全性加以评价。本研究在水生生态毒理实验基础之上,利用城市标识污染物-重金属镉(Cd)、铅(Pb)、佳乐麝香(HHCB)和城市土壤模拟城市土-水界面污染流,并以斑马鱼、草鱼为对象,以超氧化物岐化酶(SOD),过氧化物酶(POD),过氧化氢酶(CAT),丙二醛(MDA),可溶性蛋白(SP)为生物标志物,对其急性和亚急性生态毒理过程进行模拟研究,并通过对联合毒性实验的开展,系统研究了Cd、Pb和HHCB的单一与联合毒性效应、机理和过程。主要结论如下: HHCB和Cd均为中等毒性污染物,Cd和HHCB对斑马鱼的96h-LC50值分别为30.33和4.45 mg/L;在HHCB和Cd的等毒性复合急性实验中,联合作用类型随暴露时间的延长从联合变为拮抗,HHCB是复合污染中的主要污染物。 对水体中总浓度0.95-15.16 mg/L 的Cd和0.14-2.22mg/L的HHCB7天急性毒性机理实验显示,暴露于单一Cd污染斑马鱼体内抗氧化酶活性升高,暴露4天后,其体内MDA含量升高;而在HHCB胁迫2-4天后抗氧化酶活性和MDA含量均降低;联合作用中Cd在暴露的前1-4天对抗氧化酶的变化起主要作用,而之后HHCB开始起主导作用;斑马鱼急性胁迫下,抗氧化系统的诱导是斑马鱼对Cd胁迫的最初反应之一,而对于受HHCB胁迫的斑马鱼,蛋白含量的降低相对于抗氧化系统来说是斑马鱼受到损害的更重要原因。 对水体中总浓度0.005-0.05mg/L的Cd、0.5-4mg/L的Pb和0.01-0.2mg/L的HHCB对草鱼不同器官的14天亚急性毒性机理研究显示:肝脏受污染物的毒性作用最为显著,体内生物标志物也最为敏感;在Cd和Pb胁迫下,肝脏和肾脏内抗氧化酶随浓度的升高被显著抑制,而HHCB对各器官SOD和CAT活性产生诱导作用; MDA在重金属胁迫下其含量变化均不明显,SP含量轻微降低,而在HHCB胁迫下却分别呈现显著的升高和降低的趋势,所以MDA和SP含量可以作为检测HHCB的生物标志物;复合作用下HHCB的加入能使草鱼各器官中抗氧化酶的活性有所升高, MDA含量显著大幅度升高,SP含量显著大幅度降低,HHCB和Cd表现出很强的协同作用,而且HHCB在复合污染中起主导作用。

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本项研究利用自行设计的国内首创的生物堆腐池对污染土壤中的石油降解条件进行研究,并优化其运行工艺参数。本研究采用三株真菌进行堆腐败石油污染土壤的实验。堆腐池为:长 * 宽 * 高 = 118.5 * 65.5 * 12.5 = 0.097M~3,通气、养分、水分等调控在好氧条件下进行。本实验设计了5个处理组,进行了室内小试实验和室外中试实验,探讨了污染土壤中石油的净化效果,为此技术推广应用奠定了基础。研究结果如下:1 室内模拟实验表明,P菌能有效地降解污染土壤的石油。在50天的时间,达到66.1%的降解率,比次位的土著F菌61.8%,高出近5个的百分点。说明,其可以高效降解污染土壤的石油,可以用于石油污染土壤的生物修复处理。2 通气的调控是本实验中微生物生长好坏的一个非常重要的指标。利用生物泥浆反应器进行室内堆腐实验的模拟。设计了6个处理的比较实验,反应容积为4710cm~3,在50天的实验过程中得出,通气为每立方米土,22.37m~3/min(通气10分),是最佳通气条件。3 在微生物降解污染土壤中,设计正交实验,确立了土壤生物修复的调控因子,表明,温度对实验过程的影响最大,养分次之,pH和温度作为调控因子,对实验过程的影响较小。最后确立条件:温度25 ℃,湿度20%(W/W),pH6-8,C:N:P为100:10:1。4 处理的污染土样组分,进行了GC/MS的谱图分析。表明,污染土壤中含有14,15,16,17,18烷,菲,萘等,还有烯烃和环烷烃,而且本底很高,说明本污染土壤是一个复杂的混合物。5 通过设计不同浓度,不同温度,进行了土壤中组分的挥发性实验。得出,在浓度一定时,温度高的挥发率大于温度低的;在温度一定时,低浓度挥发率高于高浓度的。而原始污染土壤中的挥发率则很低,可以忽略。6 通过室外堆腐实验中的呼吸强度,耗氧变化,油降解能力之间的实验观察,发现三者之间成正相关,调控前二者之间的变化,就可以促进油的降解,为该工艺的应用提供了技术参数。7 在二年度室外实验过程中,得出,白腐真菌P菌为一株良好的石油降解菌,在200天时间内,初始浓度为5.8%的石油污染土壤,石油降解率能达到79.1%,在其后,降解曲线上升平缓,其原因还需今后进一步研究。8 通过对温主观气体CH_4和N_2O二种温室气体的实验观测,研究了污染土壤在生物修复过程中的温室气体的排队放通量。结果表明,N_2O, CH_4通量较小,本实验堆腐过程中不是温室气体的一个源。

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A superhydrophobic surface has many advantages in micro/nanomechanical applications, such as low adhesion, low friction and high restitution coefficient, etc. In this paper, we introduce a novel and simple route to fabricate superhydrophobic surfaces using ZnO nanocrystals. First, tetrapod-like ZnO nanocrystals were prepared via a one-step, direct chemical vapor deposition (CVD) approach. The nanostructured ZnO material was characterized by scanning electron microscope (SEM) and X-ray diffraction (XRD) and the surface functionalized by aminopropyltriethoxysilane (APS) was found to be hydrophobic. Then the superhydrophobic surface was constructed by depositing uniformly ZnO hydrophobic nanoparticles (HNPs) on the Poly(dimethylsiloxane) (PDMS) film substrate. Water wettability study revealed a contact angle of 155.4 +/- 2 degrees for the superhydrophobic surface while about 110 degrees for pure smooth PDMS films. The hysteresis was quite low, only 3.1 +/- 0.3 degrees. Microscopic observations showed that the surface was covered by micro- and nano-scale ZnO particles. Compared to other approaches, this method is rather convenient and can be used to obtain a large area superhydrophobic surface. The high contact angle and low hysteresis could be attributed to the micro/nano structures of ZnO material; besides, the superhydrophobic property of the as-constructed ZnO-PDMS surface could be maintained for at least 6 months. (C) Koninklijke Brill NV, Leiden, 2010

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Structural relaxation by isothermal annealing below the glass transition temperature is conducted on a Zr64.13Cu15.75Ni10.12Al10 bulk metallic glass. The effect of structural relaxation on thermal and mechanical properties was investigated by differential scanning calorimetry and instrumented nanoindentation. The recovery of the enthalpy in the DSC curves indicates that thermally unstable defects were annihilated through structural relaxation. During nanoindentation, the structural relaxation did not have a significant influence on the serrated plastic flow behavior. However, Structural relaxation shows an obvious effect in increasing both the hardness and elastic modulus, which is attributed to the annihilation of thermally unstable defects that resulted from the relaxation.

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Thermal effects of the heat transfer at free surface (represented by Biot number) on the Rayleigh-Marangoni-Benard instability in a system of liquid-porous layers with top free surface are investigated numerically. The results indicate that this thermal effect can evidently lead to the mode transition of convection, which is overlooked in previous works. (C) 2010 Elsevier Ltd. All rights reserved.

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42CrMo合金钢C含量高、合金元素含量多、淬硬倾向大,焊接性能差。激光焊接具有功率密度高、焊接变形小等优点,适合焊接传统工艺难焊的同种或异种金属。通过额定功率为3kW的Nd∶YAG固体激光器焊接42CrMo,采用光学显微镜(OM)、扫描电镜(SEM)、X衍射、硬度仪分析了焊缝区域组织、成分和硬度变化。研究结果表明:焊缝区域组织为马氏体,热影响完全淬火区的组织为马氏体+贝氏体组织,热影响不完全淬火区的组织为贝氏体。从焊缝正面到焊缝背面的硬度分布表明:由于焊缝正面有保护气体的作用提高了焊缝正面熔池的冷却速度,使焊缝背面的硬度低于焊缝正面的硬度。

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本论文对滇金足草(Goldfussia yunnanensis)、凋缨菊(Camchaya loloana)和长喙吴萸(Evodia vestia)的化学成分进行了研究,通过色谱分离得到40个化合物。主要基于波谱数据鉴定了它们的结构,其中10个为新化合物。 1.从滇金足草地上枝叶的95%乙醇提取物中共分离鉴定了16个化合物:泽漆内酯A(1)、18-羟基泽漆内酯A(2)、18-氧代泽漆内酯A(3)、18-羟基-3-O-β-D-吡喃葡萄糖-泽漆内酯A(4)、3-O-β-D-吡喃葡萄糖-泽漆内酯A(5)、3-O-β-D-吡喃半乳糖-泽漆内酯A(6)、6-E-肉桂酰哈巴俄苷(7)、E-哈巴俄苷(8)、5,6-异亚丙二氧基哈巴俄苷(9)、β-谷甾醇(10)、β-胡萝卜苷(11)、齐墩果酸(12)、肉桂酸(13)、麦角固醇(14)、硬脂酸(15)和丁二酸(16)。其中2-7为新化合物。5,6-异亚丙二氧基哈巴俄苷(9)以人工产物形式得到。 2.从凋缨菊地上枝叶的95%乙醇提取物中分离并鉴定了13个化合物:凋缨菊内酯A~C (17-19)、1β-乙酰基凋缨菊内酯C(20)、b-谷甾醇(10)、β-胡萝卜苷(11)、羽扇豆醇(21)、桦木醇(22)、桦木酸(23)、芥子醇(24)、紫丁香苷(25)、咖啡酸(26)和熊果酸(27)。其中化合物17-20为桉叶烷内酯类新化合物。化合物17、18、20对细胞株HepG2的GI50依次为7.80、7.08、4.99 µg/mL。 3.从长喙吴萸(E. vestia)地上枝叶的95%乙醇提取物中分离并鉴定了13个化合物:佛手内酯(28)、花椒毒素(29)、异茴芹内酯(30)、七叶内酯(31)、东莨宕素(32)、瑞香素(33)、异紫花前胡内酯(34)、茵芋碱(35)、山刈碱(36)、白鲜碱(37)、黄柏酮(38)、柠檬苦素(39)和对羟基苯甲醛(40)。 4.综述了1990—2007年期间从菊科植物中发现的桉叶烷-12,6内酯的化学结构、生物活性、生物转化及化学合成方面的研究进展。 Phytochemical investigation on Goldfussia yunnanensis, Camchaya loloana, and Evodia vestia, led to the isolation of 40 compounds, 10 of which were new ones. 1. Six new compounds were isolation from 95% ethanolic extract of the aerial parts of G. yunnanensis, and identified as 18-hydroxyhelioscopinolide A (2), 18-oxohelioscopinolide A (3), 18-hydroxy-3-O-β-D-glucopyranosylhelioscopinolide A (4), 3-O-β-D-glucopyranosylhelioscopinolide A (5),3-O-β-D-Galactopyranosyl helioscopinolide A (6), 6-O-trans-cinnamoyl E-harpagoside (7). The known compounds isolated were helioscopinolide A (1), E-harpagoside A (8), 5,6-isopropylidene E-harpagoside A (9), β-sitosterol (10), β-daucosterol (11), oleanolic acid (12), cinnamic acid (13), ergosterol (14), stearic acid (15) and succinic acid (16). Compound 9 was an artifact. 2. Four new compounds, loloanolides A – C (17 - 19) and 1β-acetoxy-loloanolide C (20), were isolation from 95% ethanolic extract of the aerial parts of C. loloana. The known ones were β-sitosterol (10), β-daucosterol (11), lupeol (21), betulin (22), betulinic acid (23), sinapyl (24), syringin (25), caffeic acid (26) and ursolic acid (27). The GI50 values of compounds 17, 18 and 20 to HepG2 cell line were 7.80, 7.08 and 4.99 µg/mL, respectively. 3. Thirteen were isolated from 95% ethanolic extract of the aerial parts of E. vestia for the first time. They were determined to be bergapten (28), xanthotoxin (29), isopimpinellin (30), esculetin (31), scopoletin (32), daphnetin (33), marmesin (34), skimmianine (35), confusameline (36), dictamine (37), obacunone (38), limonin (39) and p-hydroxy phenyl aldehyde (40). 4. The structures, biological activities, biotransformation and chemical syntheses of eudesmane-12, 6-olides from the Asteraceae during 1990-2007 were reviewed.

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毛壳霉属(Chaetomium)和曲霉属(Aspergillus)真菌产生多种具有生物活性的化合物。为系统阐明两属微生物的次生代谢物,对三种毛壳霉、两种曲霉真菌分别进行固态发酵,以色谱和波谱技术研究发酵物中的成分,分离鉴定了51个化合物,其中23个为新化合物,测试了部分化合物对肿瘤细胞的活性。 1、从螺卷毛壳霉(C. cochloides)固态发酵物中分离鉴定了11个化合物,3个新化合物为螺卷毛壳霉素A~C(1~3)。化合物1、3及dethio-tetra (methylthio) chetomin(4)对Bre-04、Lu-04和N-04细胞株生长抑制的GI50值为0.05~7.0 μg/mL。 2、从印度毛壳霉(C. indicum)固态发酵物中鉴定的三个异喹啉生物碱印度毛壳霉素A~C(12~14)代表两类骨架新颖的异喹啉生物碱。 3、从巴西毛壳霉(C. brasiliense)固态发酵物中鉴定了11个化合物,其中Mollicellins I~J(15~16)、2-Hydroxymethyl-6-methylmethyleugenin(19)为新化合物。化合物16和Mollicellin H(18)对Bre-04、Lu-04、N-04细胞株生长抑制的GI50值在2.5~8.6 μg/mL。 4、从土曲霉(A. terreus)固态发酵物中鉴定了18个化合物。5个为新化合物为Terretonin A~D(24~27)和Asterrelenin(28),24~27为二倍半萜化合物,28为吲哚生物碱。 5、从杂色曲霉(A. versicolor)固态发酵物中鉴定了16个化合物。9个新的化合物Brevianamides K~N (40~43)、Averins A~C (44~46)和Glyanphenines A~B (47~48)代表三种类型的生物碱。 6、综述了1997-2007年间新的二倍半萜的研究进展。 The fungi of the genera Chaetomium and Aspergillus produce various secondary metabolites with biological activities. In order to systematically study the secondary metabolites, the solid-state fermented rice culture of three species of Chaetomium and two of Aspergillus were chemically studied. By the means of chromatograhy and spectroscopy, 55 compounds were isolated and identified, among of them 23 were new ones. The biological activities of some compounds were investigated. 1. From the fungus C. cochliodes, three new epipolythiodioxopiperazines, chaetocochins A-C (1-3) were isolated, together with 8 known ones (4-11). Compounds 1, 3 and 4 showed growth inhibitory effects against cancer cell lines Bre-04, Lu-04 and N-04 with GI50 values from 0.05 to 7.0 μg/mL. 2. Three novel isoquinolines Chaetoindicins A-C (12-14) were isolated and identified from the fungus C. indicum. Chaetoindicin A, Chaetoindicins B-C represented two classes of novel carbon skeletons. 3. Three new compounds, Mollicellins I-J (15-16), and 2-hydroxymethyl-6-methylmethyleugenin (19), were isolated from C. brasiliense. Compound 16 and Mollicellin H (18) showed growth inhibitory effects against cancer cell lines Bre-04, Lu-04 and N-04 with GI50 values from 2.5 to 8.6 μg/mL. 4. Eighteen compounds were isolated from the fungus A. terreus. Terretonin A-D(24 - 27)and Asterrelenin(28) are new compounds belonging to sesterterpoids and indole-ralated alkaloid, respectively. 5. From the fungus A. versicolor, sixteen secondary metabolites, including nine new ones, Brevianamides K-N (40-43), Averins A-C (44-46), and Glyanphenines A-B (47-48), were isolated and identified. Brevianamides K-N (40-43), Averins A-C (44-46), and Glyanphenines A-B (47-48) represented three classes of alkaloids. 6. New sesterterpenes and their bioactivities reported from 1997 to 2007 were summarized.

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本论文由四部分组成,前三部分为实验论文,第四部分为文献综述。第一、二部分分别报道了中药西藏胡黄连和鸡矢藤的化学成分研究结果。从两种药用植物中共分离和鉴定了32个化学成分,其中3个为新化合物。第三部分为黄芪多糖的提取工艺研究。第四部分概述了近年来植物多糖的研究进展。 第一章为西藏胡黄连化学成分研究。通过正、反相硅胶柱层析等分离方法从药用植物西藏胡黄连(Picrorhiza scrophulariiflora Pennell)的根茎中共分离纯化出7个化合物。运用MS、1H-NMR、13C-NMR、DEPT、HSQC和HMBC等现代谱学方法,结合理化分析对这些化合物的结构进行了分析鉴定。7个化合物中有两个是酚性的葡萄糖苷类成分:西藏胡黄连酚苷D (1)、4-O-β-D-(6-O-vanilloyl glucopyranosyl) vanillic acid (6);四个苯乙基苷类化合物:plantamajoside (2)、plantainoside D (3)、西藏胡黄连苷A (4) 和西藏胡黄连苷F (5);一个苯基小分子化合物:香豆酸甲酯 (7)。其中化合物1和5未见文献报道,确定为新化合物;化合物3为首次从该种植物中分到。 第二章为鸡矢藤化学成分研究。从鸡矢藤(Paederia scandense (Lour) Merrill)全草中分离出25个化合物,通过理化常数和波谱数据鉴定了它们的结构。25个化合物中包括一个蒽醌类成分:茜根定-1-甲醚 (1);两个香豆素:异东莨菪香豆素 (2)和5-羟基-8-甲氧基吡喃香豆素 (3);两个香豆素-木脂素化合物:臭矢菜素 B (4)和臭矢菜素 D (5);一个木脂素:异落叶松树脂醇 (6);两个黄酮:diadzein (7)和蒙花苷 (8);三个三萜类化合物:齐墩果酸 (9)、乌苏酸 (10)和 3-O-β-D-吡喃葡萄糖基乌苏烷 (11);三个甾体及其糖苷:b-谷甾醇 (12)、胡萝卜苷 (13)和(24R)-豆甾-4-烯-3-酮 (14);六个小分子化合物:对羟基苯甲酸 (15),咖啡酸 (16),香豆酸 (17),丁烯二酸 (18),3,5-二甲氧基-4-羟基苯甲酸(19),咖啡酸-4-O-β-D-吡喃葡萄糖苷(20);五个环烯醚萜类化合物:鸡矢藤苷 (21),鸡矢藤酸 (22),鸡矢藤酸甲酯 (23),saprosmoside E (24)和paederoside B (25)。其中化合物25未见文献报道,为新化合物。化合物1~8、11、14、15~20为首次从该化合物中分离得到。同时对鸡矢藤中环烯醚萜类化合物做了高效液相-串联质谱(HPLC-MSn)分析,探讨了这类化合物的质谱裂解规律。 第三章为黄芪多糖的提取工艺研究。首先确定了黄芪多糖含量的测定方法,并进行了方法学验证;其次探讨了黄芪中黄芪多糖的提取工艺,确定以酶法-Sevag法联用来去除黄芪多糖中的蛋白质,可使其提取物中黄芪多糖总含量达到70%以上。 第四章为近年来植物多糖的研究进展。主要包括植物多糖的提取纯化、多糖的定性定量检测方法、多糖的结构分析和多糖的药理活性。 This dissertation consists of four parts. The first and second parts reports the studies on the chemical constituents of medicinal plants of Picrorhiza Scrophulariiflora and Paederia scandens. The third part is about the extract technique of Astragalan Polysaccharide (APS). The last part reviews the progress of the studies on plant polysaccharides.   The first chapter is about the chemical constituents of P. Scrophulariiflora which is widely used as an important medicine to treat various immune-related diseases. A new phenyl glycoside, scrophenoside D (1) and a new phenylethyl glycoside, scroside F (5), together with five known compounds, plantamajoside (2), plantainoside D (3), scroside A (4), 4-O-β-D-(6-O-vanilloylglucopyranosyl) vanillic acid (6); and methyl-p-coumarate (7) were isolated from the stems of P. scrophulariiflora. Their structures were elucidated by spectroscopic and chemical methods. The second chapter is about the chemical constituents of medicinal herb of P. scandens. Twenty-five compounds were isolated and purified by normal and reversed phase silica gel column chromatography. By physicochemical properties and spectral analysis, their structures were identified as rubiadin-1-methylether (1), isoscopoletin (2), 5-hydroxyl-8-methoxyl-coumarin (3), cleomiscosin B (4), cleomiscosin D (5), isolariciresinol (6), diadzein (7), linarin (8), oleanolic acid (9), ursolic acid (10), 3-O-β-D-glucopyranosyloxyl-ursane (11), b-sitosterol (12), b-daucosterol (13), (24R)-stigmast-4-ene-3-one (14), p-hydroxyl-benzoic acid (15), caffic acid (16), coumaric acid (17), trans-butenedioic acid (18), 3,5-dimethoxyl-4-hydroxylbenzoic acid (19), caffeic acid 4-O-β-D-glucopyranoside (20), paederoside (21), paederosidic acid (22), paederosidic acid methyl ester (23), saprosmoside E (24), paederoside B (25). Among them, compound 25 is a new compound. Compounds 1~8、11、14、15~20 were isolated from this plant for the first time. Futhermore, we studied the HPLC-MSn analysis and investigation of fragmentation behavior of the sulfur-containing iridoid glucosides. The third chapter is about the extracting process of Astragalan Polysaccharide (APS). The method of the content determination is built. The optimum condition of extraction of polysaccharides from Radix Astragali is defined and the more effective way to remove protein is combined enzyme method with Sevag method, by which the content of polysaccharides extract can be up to 70%. The last part is a review of the research progress of the plant polysaccharides, which includes its extraction, isolation, purification, determination, structure analysis, and pharmacology.

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钮子瓜(Zehneria maysorensis Arn.)是一种常用的中草药,其性味苦、凉,主要功效为清热利湿、散风止痛,主治膀胱炎、头痛。体外活性筛选实验表明,袋花忍冬(Lonicera saccata Rehd.)95%乙醇提取物的乙酸乙酯部分对血管紧张素转化酶显示较强的抑制活性。为明确钮子瓜的药用物质基础和袋花忍冬中具有ACE抑制活性的成分,首次对两个植物的成分进行了研究。 1. 从钮子瓜95%乙醇提取物中主要通过色谱方法首次分离了14个化合物,通过波谱方法鉴定为(2S,3S,4R,10E)-2-[(2R)-2-羟基二十四烷酰基氨基]-10-十八烷-1,3,4-三醇(1)、(2S,3S,4R)-2-二十四烷酰基氨基-十八烷-1,3,4-三醇 (2)、胡萝卜苷(3)、swertish (4)、苯甲酸(5)、水杨酸(6)、loliolide (7)、胸腺嘧啶(8)、尿嘧啶(9)、(23Z)-9,19-环阿尔廷-23-烯-3β,25-二醇(10)、(20S,22E,24R)-5α,8α-表二氧-麦角甾-6,22-二烯-3β-醇(11)、十六烷酸 1-甘油酯(12)、大豆脑苷Ⅰ(13)和(22E,24S)-24-甲基-5α-胆甾-7,22-二烯-3β,5α,6β-三醇(14)。其中化合物4为一黄酮碳苷,具有旋转异构现象,有止痛作用;化合物6具有抗炎、镇痛、减热的活性,它们可能是钮子瓜药用物质基础的一部分。 2. 从袋花忍冬95%乙醇提取物中首次分离并鉴定了16个已知化合物:胡萝卜苷(3)、(20S,22E,24R)-5α,8α-表二氧-麦角甾-6,22-二烯-3β-醇(11)、十六烷酸 1-甘油酯(12)、E-p-coumaryl behenate (15)、谷甾醇(16)、2,6-dihydroxyhumula-3(12), 7(13),9(E)-triene (17)、环阿尔廷-25-烯-3β,24ξ-二醇 (18)、二十四烷酸 (19)、2,4-二羟基-3,6-二甲基苯甲酸甲酯 (20)、乌苏酸 (21)、柚皮素 (22)、木犀草素 (23)、柏双黄酮(24)咖啡酸 (25)、洋芹素(26)和木犀草素-7-O-β-D-葡萄糖苷 (27)。其中木犀草素(23)和咖啡酸(25)含量较高,它们为抑制ACE活性的成分。 3.综述了黄酮碳苷的旋转异构现象。 Zehneria maysorensis is a folk medicine for the treatment of cystitis and headache. The ethyl acetate soluble fraction of the 95% ethanol extract of Lonicera saccata showed obvious ACE inhibitory activity in vitro. To reveal their active constitutents, they were subjected to chemically study. From the 95% ethanol extract of the whole plants of Zehneria maysroensis fourteen compounds were isolated for the first time. On the basis of spectral data and/or by comparison with authentic samples, they were characterized to be (2S,3S,4R,10E)-2-[(2R)-2-hydroxytetracosanoylamino]-10-octadecene-1,3,4-triol (1), (2S,3S,4R)-2-tetracosanoylamino-1,3,4-octadecanetriol (2), daucosterol (3), swertish (4), benzoic acid (5), salicylic acid (6), loliolide (7), thymine (8), uracil (9), (23Z)-9,19-cycloart-23-ene-3β,25-diol (10), (20S,22E,24R)-5α,8α-epidioxy-ergosta- 6,22-diene-3β-ol (11), 2,3-dihydroxypropyl hexadecoate (12), soya-cerebroside (13) and (22E,24S)-24-methyl-5α-cholesta-7,22-diene-3β,5α,6β-triol (14). Compound 4, a C-glycosylflavone, showed a very interesting rotational isomerism. Compounds 4 and 6 may be the active constituents of Zehneria maysorensis considering their sedative and anti-inflammation activity, respectively. From the whole plants of Lonicera saccata, sixteen compounds were isolated for the first time. On the basis of spectral data and/or by comparison with authentic samples, they were identified to be daucosterol (3), (20S,22E,24R)-5α,8α-epidioxy- ergosta-6,22-diene-3β-ol (11), 2,3-dihydroxypropyl hexadecoate (12), E-p-coumaryl behenate (15), β-sitosterol (16), 2,6-dihydroxyhumula-3(12),7(13),9(E)-triene (17), cycloart-25-ene-3β,24ξ-diol (18), tetracosanoic acid (19), methyl 2,4-dihydroxy- 3,6-dimethylbenzoate (20), ursolic acid (21), naringenin (22), luteolin (23), cupressuflavone (24), caffeic acid (25), apigenin (26) and luteolin-7-O-β-D- glucopyranoside (27). Luteolin (23) and caffeic acid (25) were the ACE inhibitory active constituents. Rotational isomerism for C-glycosylflavonoid was reviewed.

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八月瓜属植物五枫藤(Holboellia latifolia Wall.)和驳骨草属植物小驳骨(Gendarussa vulgaris Nees)均为药用植物, 前者化学成分研究不深入, 后者的化学成分未见报道。川西茶藨(Ribes takare D. Don)为茶藨子属植物, 没有化学成分的报道。本论文对三个植物的化学成分和活性成分进行了研究, 主要通过色谱方法分离得到了48 个化合物, 采用波谱分析或与已知标准品对照等手段鉴定了它们的结构, 其中有1 个新的原小檗碱类化合物和3 个新的联苯类化合物,发现了具有细胞毒活性和α-葡萄糖苷酶抑制活性的化合物。1、从五枫藤地上部分的95%乙醇提取物中分离得到了12 个化合物: 五加苷K (1)、hederagenin 3-O- α-L-rhamnopyranosyl-(1→2)- α-L-arabinopyranoside (2)、β-萘乙酸(3) 、3-O-α-L-rhamnopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-α-L-arabinopyranosyl oleanolic acid 28-O-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl ester (4) 、3-O- α-L-rhamnopyranosyl-(1→2)-O- β- D-glucopyranosyl-(1→2)- α-L-arabinopyranosyl oleanolic acid (5) 、3-O-( β-D-glucopyranosiduronic acid)-oleanolic acid 28-O- β-D-glucopyranoside (6)、lup-20(29)-en-3-one (7)、lupeol (8)、β-谷甾醇(9)、齐墩果酸(10)、乌苏酸(11)、β-胡萝卜苷(12)。化合物1 对Lu-06、N-04 和Bre-04 癌细胞株的GI50 分别是0.77µg/mL、1.26 µg/mL 和1.55 µg/mL, 化合物2 对N-04 癌细胞株的GI50 为2.44 µg/mL。2、从小驳骨地上部分的95%乙醇提取物中分离得到了1 个原小檗碱类新化合物13-hydroxyl gusanlung A (25), β-谷甾醇(9)、齐敦果酸(10)、β-胡萝卜苷(12)、棕榈酸(1-)甘油酯(13)、棕榈酸(14)、阿苯哒唑(15)、阿苯哒唑砜(16)、阿苯哒唑亚砜(17)、aurantiamide acetate (18)、华良姜素(19)、芫花素(20)、(-)-丁香树酯醇(21)、gusanlung B (22) 、eupteleasaponinsⅤ acetate (23)、gusanlungA (24)、刺五加苷E (26)、岩白菜素(27)、咖啡酸(28)。化合物25 对肝癌细胞株(HepG2) 的GI50 为2.08 µg/mL。3、从川西茶藨地上部分的95%乙醇提取物中分离鉴定了22 个化合物: β-谷甾醇(9) 、β- 胡萝卜苷(12) 、O-acetyloleanolic aldehyde (29),4,7,8-trimethoxy-2,3-methylenedioxydibenzofuran (30) 、3', 5-dimethoxy-3, 4-methylenedioxybiphenyl (31) 、桦木醇(32) 、6,7-dimethoxy-1-methyl-3,4-dihydroquinolin-2-one (33)、3'-hydroxy-5-methoxy-3,4-methylenedioxybiphenyl (34) 、7-hydroxy-4,8-dimethoxy-2,3-methylenedioxydibenzofuran (35)、桦木醛(36)、没食子酸(37) 、6β- 羟基-4- 烯-3- 酮- 豆甾醇(38) 、5α, 8α-epidioxy-(22E,24R)-ergosta-6, 22-dien-3β-ol (39)、verrucofortine (40)、6-methoxycalpogoniumisoflavone A (41)、2-羟基二苯甲酮(42)、桦木酸(43), 3, 5-二甲氧基苯甲酸-4-O-β-D-吡喃葡萄糖苷(44)、洋芹素(45)、刺槐素(46)、水杨酸(47)、洋芹素-5-O- β-D-葡萄糖苷(48), 化合物30、31 和35 为新的联苯化合物。化合物30的α-葡萄糖苷酶抑制率为10.2% (1.00 mg/mL); 化合物35 的抑制率为17.2% (1.00mg/mL)。4、综述了1960 年以来原小檗碱类化合物药理活性研究进展。 Plants Holboellia latifolia Wall and Gendarussa vulgaris Nees, are used as folkmedicine. Ribes takare D. Don belongs to the genus Ribes. The three plants have notbeen chemically studied in detail. Chemical and bioactive study of three plants led tothe isolation of 48 compounds by chromatography. Their structures were elucidatedon the basis of spectroscopic evidence or comparison with authentic samples. Amongthe 48 componds isolated one protoberberine alkaloid and three biphenyls are newones. Cytotoxic and α-glucosidase inhibitory compounds had been found.1. Twelve compounds were isolated from the 95% ethanol extract of the aerial partof H. latifolia Wall. They were characterized as fellow: eleutheroside K (1),hederagenin-3-O- α-L-rhamnopyranosyl-(1→2)- α-L-arabinopyranoside (2),2-naphthyl acetic acid (3),3-O-α-L-rhamnopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-α-L-arabinopyranosyl oleanolic acid 28-O-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl ester (4), 3-O- α-L-rhamnopyranosyl-(1→2)-O- β- D-glucopyranosyl-(1→2)- α-L-arabinopyranosyl oleanolic acid (5),3-O-( β-D-glucopyranosiduronic acid)-oleanolic acid-28-O- β-D-glucopyranoside (6),lup-20(29)-en-3-one (7), lupeol (8), β-sitosterol (9), oleanolic acid (10), ursolicacid (11), and β-daucosterol (12). Compound 1 showed moderate cytotoxicity againstLu-06 (GI50, 0.77 µg/mL), N-04 (GI50, 1.26 µg/mL) and Bre0-4 (GI50=1.55 µg/mL)and compound 2 showed moderate cytotoxicity against N-04 (GI50=2.44 µg/mL).2. A new protoberberine alkaloid, 13-hydroxyl gusanlung A (25), was isolated fromthe aerial part of Gendarussa vulgaris Nees, together with β-sitosterol (9), oleanolicacid (10), β-daucosterol (12), glycerol monopalmitate (13), palmific acid (14),albendazole (15), albendazole sulphone (16), albendazole sufloxide (17), aurantiamideacetate (18), kumatakenin (19), genkwanin (20), (-)-syringaresinol (21), gusanlung B(22), eupteleasaponinsⅤ acetate (23), gusanlung A (24), eleutheroside E (26),bergenin (27) and caffeic acid (28). Compound 25 showed cytotoxicity against HepG2 cells (GI50, 2.08 µg/mL).3. Phytochemical study of the Ribes takare D. Don led to the isolation of three newbiphenyls, 4,7,8-trimethoxy-2,3-methylenedioxydibenzofuran (30), 3', 5-dimethoxy-3,4-methylenedioxybiphenyl (31) and 7-hydroxy-4,8-dimethoxy-2,3-methylenedioxydibenzofuran (35), along with nineteenknown compounds, β-sitosterol (9), β-daucosterol (12), O-acetyloleanolic aldehyde(29), betulin (32), 6,7-dimethoxy-1-methyl-3,4-dihydroquinolin-2-one (33),3'-hydroxy-5-methoxy-3, 4-methylenedioxybiphenyl (34), betulinic aldehyde (36),gallic acid (37), stigmast-4-en-6β-ol-3-one (38), 5α, 8α-epidioxy-(22E, 24R)-ergosta-6,22-dien-3β-ol (39), verrucofortine (40), 6-methoxycalpogonium isoflavone A (41),2-hydroxybenzophenone (42), betulinic acid (43), 3,5-dimethoxygallic acid-4-O- β-D-glucopryranoside (44), apigenin (45), acacetin (46), salicylic acid (47) andapigenin-5-O- β-D-glucopryranoside (48). α-Glucosidase inhibitory rates ofcompound 30 and 35 were respectively 10.2% and 17.2% at a concentration of 1.00 mg/mL).4. Pharmacological activities of protoberberines were summarized.

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本论文由三章组成。第一章介绍了中药蜘蛛香的化学成分的研究成果,第二章为羧甲基魔芋葡苷聚糖-壳聚糖为细胞膜的天冬酰胺酶人工细胞的研究,第三章综述了人工细胞在生物医学领域的应用。 第一章报道了中药蜘蛛香(Valeriana wallichii)根部乙醇提取物的化学成分,采用正、反相硅胶层析等分离方法和MS、NMR等多种波谱手段,从中共分离鉴定出17个化合物,分别为缬草素(valtrate,1),valechlorine(2),homobadrinal(3),baldrinal(4),乙酰缬草素(acevaltrate 5),valeriotetrate C(6),valeriotetrate B(7),对羟基苯乙酮(4'-hydroxy-acetophenone 8),7-hydroxy valtrate(9),8-methylvalepotriate(10),1,5-dihydroxy-3,8-epoxyvalechlorine A(11),二氢缬草素(didrovaltrate 12),胡萝卜苷(13),橙皮苷 (hesperidin 14),prinsepiol-4-O-β-D-glucopyranoside(15),longiflorone(16),乙基糖苷(17)。其中化合物6、7、10、和11为新化合物,化合物9、15、16为首次从该植物中得到。新化合物11为含有氯原子的刚性骨架环烯醚萜,并且确定了其绝对构型。 第二章报道了以羧甲基魔芋葡苷聚糖(CKGM)和壳聚糖(CS)为膜的固定化L-天冬酰胺酶人工细胞研究成果。利用羧甲基魔芋葡苷聚糖和壳聚糖两种生物相容性很好的天然多糖之间的静电吸引力,在非常温和的条件下制备成具有半透过性膜的人工细胞,将治疗儿童急性成淋巴细胞性白血病(ALL)的药物L-天冬酰胺酶包裹在内。通过考察温度和pH对人工细胞的影响,结果表明以CKGM- CS为膜的L-天冬酰胺酶人工细胞对温度和pH的稳定性和耐受性均高于自由酶,说明CKGM-CS对酶具有保护作用,而且小分子底物和产物可以自由进出膜内外,而包裹在膜内的生物大分子则不能泄露出来。 第三章综述了微囊化人工细胞的研究进展。 This dissertation consists of three parts. In the first part, the chemical constituents from the root of Valeriana wallichii were reported. In the second part, preparation and characteristics of L-Asparaginase Artificial cell were reported. The third part is a review on progress of microcapsule artificial cell. The first chapter is about the isolation and identification of the chemical constituents from the root of V. wallichii. Seventeen compounds were isolated from the ethanol extract of roots of V. wallichii through repeated column chromatography on normal and reversed phase silica gel. By the spectroscopic and chemical evidence, their structures were elucidated as valtrate (1), valechlorine (2), homobadrinal (3), baldrinal (4), acevaltrate (5), valeriotetrate C (6), valeriotetrate B (7), 4'-hydroxy-acetophenone (8), 7-hydroxy valtrate (9), 8-methylvalepotriate (10), 1,5-dihydroxy-3,8-epoxyvalechlorine A (11), didrovaltrate (12), daucosterol (13), hesperidin (14), prinsepiol-4-O-β-D-glucopyranoside (15), longiflorone (16), and ethyl glucoside (17). Among them, 6, 7, 10, and 11 are new compounds. 15, 16 and 9 were isolated from this plant for the first time. The absolute configuration of compound 11, an unusual iridoid bearing a C-10 chlor-group and an oxo-bridge connecting C-3 and C-8 resulting in a rigid skeleton, was confirmed. The second chapter is about the semi-permeable microcapsule of carboxymethyl konjac glucomannan-chitosan for L-asparaginase immobilization. Carboxymethyl konjac glucomannan-chitosan (CKGM-CS) microcapsules, which have good biocompatibility, prepared under very mild conditions via polyelectrostatic complexation, were used for immobilize L-asparaginase-a kind of drug for acute lymphoblastic leukemia (ALL). The activity and stability under different temperature and pH of the enzyme loaded-microcapsules were studied. The results indicated the immobilized enzyme has better stability and activity contrasting to the native enzyme. The study illustrates that the L-asparaginase could be protected in CKGM-CS microcapsules, the substrate and product could pass through the system freely.