908 resultados para 14 alpha-dihydroxy-13(15)-ene-16(12 alpha)-abietanolide


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Thesis (doctoral)--Ruprecht-Karls-Universitat zu Heidelberg.

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El principal objetivo de este trabajo ha sido la elaboraci?n de un programa integral de entrenamiento en la preparaci?n de los futbolistas; dependiendo en una buena medida del sistema de preparaci?n a largo plazo, en este caso para este estudio nos centramos en la Etapa de Especializaci?n Deportiva. Analizando la literatura sobre el tema y los diferentes estudios se establecieron unos criterios de selecci?n de informaci?n concerniente a las tendencias de preparaci?n moderna; todo esto orientado a la poblaci?n, sus particularidades y caracter?sticas individuales. Se dise?? y se aplic? un programa de entrenamiento en j?venes futbolistas en la etapa de especializaci?n deportiva, queriendo evaluar las principales caracter?sticas de juego en el futbol a trav?s de los fundamentos t?cnicos b?sicos. Los resultados de la aplicaci?n del programa en su gran mayor?a fueron significativos, con relaci?n a la evaluaci?n inicial. Unas variables presentaron unas ganancias desde el punto de vista condicional y otras desde el punto de vista futbol?stico.

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This report documents the expansion of 4K and expenditure of funds in Fiscal Years 2014-15 and 2015-16; provides 2015-16 projections for the number of at-risk four-year-olds in each school district and the number of at-risk four-year-olds served in a publicly funded program using available information; details the results of the CIRCLE assessment, which was administered to children in publicly-funded four-year-old (4K) and five-year-old (5K) kindergarten during the 2014-15 school year; describes the four language and literacy assessments that measure 4K and 5K students’ abilities during the 2015-16 school year; and discusses how 4K quality can be defined and the important role of teacher-child instructional interactions in assessing quality of publicly-funded 4K.

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Synthesis of 5, 5-dimethyl- 7-methoxy-4 -oxatricyclo[4,3,1,0(3,7)]- decan-2-one 3a, a novel heterocyclic ring system present in morellin 1, and its 3-substituted derivatives 3b-e, is described from the Diels-Alder adducts 7, available from 1-methoxycyclohexa-1,4-dienes 4. Two routes, which involved the halocyclisation and the oxidative addition, were investigated for the conversion of the adducts 7 into 3. While the halocyclisation method resulted in mixtures, excellent yields of the target molecule were obtained by the second method. Solvolysis of the bromoether 9 resulted in a mixture of rearranged products 10, 13, 15 and 16.

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El estudio se realizó en la granja ovina de los hermanos Campos Borras localizada en el municipio de Monegrillo, comarcas de Monegros, provincia de Zaragoza, Comunidad Autónoma de Aragón, localizada en las coordenadas geográficas 41° 38´ 15” latitud norte y 0° 25´ 03” de longitud Este, con el objetivo de evaluar el efecto de la edad al primer parto sobre la productividad de ovino de carne (Rasa Aragonesa) en una explotación de zona semiárida en Zaragoza, España, Se utilizó una base de dato de registros desde 1994 hasta el 2010, la cual fue depurada antes de su análisis en una hoja de cálculo de Excel® de la suite de Microsoft Office. Todos los análisis estadísticos se analizaron mediante el paquete estadístico SAS®, versión 9.1.3. Los registros se agruparon de acuerdo a la edad al primer parto: Grupo 1: 11 a 14 meses, Grupo 2: 15 a 16 meses, Grupo 3: 19 a 22 meses y Grupo 4: 23 hasta 53 meses. Las diferencias entre grupos se analizaron mediante ANOVA y test de Duncan Se evaluó la fertilidad de dos maneras: 4 años desde su fecha de nacimiento y 4 años desde su primer parto. En ambas evaluaciones se midieron las mismas variables (número de partos, intervalo entre parto y prolificidad). Encontrando que la edad al primer parto no influyó sobre la fertilidad de las ovejas evaluadas desde su nacimiento hasta los 4 años, aunque se observaron diferencias significativas (P<0.01) entre todos los grupos cuando se evaluó. Debido a que se encontró un mayor número de partos en las ovejas que tienen una edad menor al primer parto y cuando la fertilidad se evaluó desde su primer parto se encontró que no existía ninguna diferencia significativa entre grupos, siendo la media general 5.4 partos, lo que quiere decir que la edad al primer parto no repercute en su fertilidad en sus próximos 4 años. Palabras Claves: Rasa Aragonesa, Edad al primer parto, Productividad.

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Title Varies: 1913/14, Anniversary Bulletin; 1914/15-1915/16, Five (-Six) Years' and Progress; 1925, Anniversary Report

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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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海洋是一个巨大的天然产物宝库,约占地球表面积70%的海洋蕴藏着80%的生物资源。由于海洋生态环境的特殊性,导致海洋生物能够产生大量结构独特多变和活性特殊多样的代谢产物。我国海域辽阔,海洋资源丰富,为寻找结构新颖、生理活性独特的先导化合物,加强对海洋资源的开发利用,本论文对中国沿海的三种海洋红藻和两株放线菌次生代谢产物以及生物活性进行研究,为新药研究与开发提供模式结构和药物前体。 对红藻似瘤凹顶藻Laurencia similis乙酸乙酯萃取物进行分离纯化,从中得到单体化合物35个,通过波谱学方法(IR、MS、NMR等)鉴定了他们的结构。分别为:2, 2, 5, 5, 6, 6-sixibromo-3, 3-bi-1H-indole (1),3,5-dibromo- 1-methyl-indole (2),3',5',6,6'-tetrabromo-2,4-dimmethyldiphenyl ether (3),1,2,5- tribromo-3-bromoamino-7-bromomethylnaphthalene (4),2,5,8-tribromo-3-bromo- amino-7-bromomethylnaphthalene (5),2,5,6-tribromo-3-bromoamino-7-bromo- methylnaphthalene (6), 2,5,6,5',6'-pentabromo-3,4,3',4'-tetramethoxybenzophenone (7), (4E)-1-bromo-5-[(1'S*,3'R*)-3'-bromo-2',2'-dimethyl-6'-methylenecyclohexyl] -3-methylpent-4-ene-2,3-diol (8),4-hydroxy-Palisadin C (9),Isopalisol (10),Luzonensol (11),Palisadin B (12),Aplysistatin (13),Palisadin A (14),5-Acetoxypalisadin B (15),Aristolan-1(10)- en-9-ol (16),Aristol-8-en-1-one (17),Aristolan-9-en-1-one (18),Aristolan-1(10)-en- 9-one (19),Aristofone (20),Aristolan-1(10)-8-diene (21),Aristolan-1,9-diene (22),10-Hydroxyaristolan-9-one (23),7,11,15-trimethyl-3-methylene-hexadecan-1,2-diol (24),3β-Hydroxyergosta- 5,24(28)-dien-7-one (25),Isofucosterol (26),β-sitosterol (27),豆甾-4-烯-3α,6β-二醇 (28),Cholesta-5-en-3β-ol (29),Stigmasterol (30),2,3,5,6-四溴-吲哚 (31),2,3,6-tribromo-1H-indole (32),3,5,6-tribromo-1-methylindole (33),3,5,6-tribromo -1H-indole (34),2,3,5-tribromo-1-methylindole (35),其中化合物1-9为新化合物,化合物10-15、20和化合物24-30均为首次从该种海藻中得到。对新化合物1-9进行PTP1B酶抑制剂活性筛选,新化合物1、3、7显示强的PTP1B酶抑制活性。 对红藻齐藤凹顶藻Laurencia saitoi乙酸乙酯萃取物进行分离纯化,从中得到单体化合物11个,通过波谱学方法(IR、MS、NMR等)鉴定了他们的结构,分别为:2-hydroxyl-Luzofuranone (1),2-hydroxyl-Luzofuranone B (2),4-hydroxyl-Palisudin C (3),2-bromo-γ-ionone (4),Aplysistatin (5),5-Acetoxypalisadin B (6),Palisadin B (7),Palisadin A (8),Pacifigorgiol (9),豆甾-4-烯-3α,6β-二醇 (10),2, 3, 5, 6-四溴-吲哚 (11),其中化合物1-4为新化合物,所有化合物均为首次从该种海藻中得到。通过MTT法对分离得到的新化合物1-4进行肿瘤细胞毒活性筛选,结果显示4个新化合物对所测肿瘤细胞株均无明显的活性。 对红藻瘤状软骨凹顶藻Chondrophycus papillous乙酸乙酯萃取物进行分离纯化,从中得到单体化合物5个,通过波谱学方法(MS、NMR等)鉴定了他们的结构,分别为邻苯二甲酸二丁酯 (1),邻苯二甲酸二异辛酯 (2),胆甾醇 (3),3,7,11,15-tetramethyl-hexadec-2-en-1-ol (4),4-羟基苯甲醛 (5),所有化合物均为首次从该种海藻中得到。 对海洋放线菌M159乙酸乙酯萃取物进行分离纯化,从中得到单体化合物13个,通过波谱学方法(MS、NMR等)鉴定了他们的结构,分别为:5-(4',6'-dihydroxy-6-methyloctyl)furan-2(5H)-one (A),phenethyl alcohol (1),4-羟基苯甲醛(2),anthranilic acid (3),4-Hydroxy-3-methoxy- phenyl-propionic acid (4),5-(6,7-dihydroxy-6-methyloctyl)furan-2(5H)-one (5),p-Hydroxyphenylethyl alcohol (6),3-Indoleacrylic acid (7),Indol-3-carboxylic acid (8),Adenine cordyceposide (9),腺嘌呤核苷(10),尿嘧啶核苷(11),Thymidine (12),其中化合物A为新化合物。所有化合物均为首次从该株放线菌中得到。 对海洋放线菌L211乙酸乙酯萃取物进行分离纯化,从中得到单体化合物15个,通过波谱学方法(MS、NMR等)鉴定了7个结构,分别为:spatozoate (1),anthranilic acid (2),3-Indolylethanol (3),1-Acetyl-β-carbolin (4),p-Hydroxyphen- ylethyl alcohol (5),Indole-3-acetic acid (6),Indol-3-carboxylic acid (7),所有化合物均为首次从该株放线菌中得到。

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The chemical composition of surface associated metabolites of two Fucus species (Fucus vesiculosus and Fucus serratus) was analysed by means of gas chromatography-mass spectrometry (GC-MS) to describe temporal patterns in chemical surface composition. Method: The two perennial brown macroalgae F. vesiculosus and F. serratus were sampled monthly at Bülk, outer Kiel Fjord, Germany (54°27'21 N / 10°11'57 E) over an entire year (August 2012 - July 2013). Per month and species six non-fertile Fucus individuals were collected from mixed stands at a depth of 0.5 m under mid water level. For surface extraction approx. 50 g of the upper 5-10 cm apical thalli tips were cut off per species. The surface extraction of Fucus was performed according to the protocol of de Nys and co-workers (1998) with minor modifications (see Rickert et al. 2015). GC/EI-MS measurements were performed with a Waters GCT premier (Waters, Manchester, UK) coupled to an Agilent 6890N GC equipped with a DB-5 ms 30 m column (0.25 mm internal diameter, 0.25 mM film thickness, Agilent, USA). The inlet temperature was maintained at 250°C and samples were injected in split 10 mode. He carrier gas flow was adjusted to 1 ml min-1. Alkanes were used for referencing of retention times. For further details (GC-MS sample preparation and analysis) see the related publication (Rickert et al. submitted to PLOS ONE).

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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.