共查询到20条相似文献,搜索用时 31 毫秒
1.
2.
A.K. Banerjee B.J. Broughton T.S. Burton M.P.L. Caton A.J. Christmas E.C.J. Coffee K. Crowshaw M.A. Heazell K.A.J. Stuttle G.L. Watkins 《Prostaglandins & other lipid mediators》1978,16(4):541-554
The synthesis and gastrointestinal pharmacology of some 11-deoxyprostaglandin E1 analogues are described with results analysed for selectivity from side effects. 11-Deoxygenation reduced potency relative to PGE2 but, as has been reported for natural PGs, 15- or 16-methyl analogues were more potent than the unsubstituted parent compound in the order 16-methyl > 15-methyl > 16, 16-dimethyl. The results suggest that a complex interaction between C-15 and C-16 in methyl analogues affects their profile of activity, but that none of the modifications studied conferred a substantial potency or selectivity advantage over PGE2. 相似文献
3.
Lu Y Prudent M Qiao L Mendez MA Girault HH 《Metallomics : integrated biometal science》2010,2(7):474-479
Copper-β-amyloid 16 (Aβ16) complexes were investigated by electrospray ionization mass spectrometry (ESI-MS). Copper(i) and (ii) complexes were formed on-line in a microchip electrospray emitter by using a sacrificial copper electrode as the anode in positive ionization mode. In the presence of ascorbic acid in the peptide solution, the amount of Cu(i)-Aβ16 generated electrochemically was even higher. A kinetic model is proposed to account for the generation of copper complexes. The structure of Cu(i)-Aβ16 was investigated by tandem mass spectrometry (MS/MS), and the binding site of Cu(i) to Aβ16 was identified at the His13, His14 residues. Cu(ii)-Aβ16 was also investigated by MS/MS and, based on the unusual observations of a-ions, the two binding residues of His13 and His14 of Aβ16 to Cu(ii) were also confirmed. This approach provides direct information on Cu(i)-Aβ16 complexes generated in solution from metallic copper and gives evidence that both His13 and His14 are involved in the coordination of both Cu(i)- and Cu(ii)-Aβ16 complexes. 相似文献
4.
《基因组学与应用生物学》2016,(4)
TYRO3、AXL和MER受体是受体酪氨酸激酶亚家族之一,广泛地表达在哺乳动物神经、免疫、生殖、血液等系统多种细胞中,促进细胞存活、增殖和分化。本研究利用基因芯片技术筛选基因敲除的TYRO3~(~(-/-))AXL~(-/-)MER~(-/-)小鼠骨髓细胞中差异性表达的m RNA,并进行生物信息学分析。与正常小鼠骨髓细胞相比,TYRO3~(-/-)AXL~(-/-)MER~(-/-)小鼠骨髓细胞中差异表达基因探针共1 363条,其中表达上调的基因探针499条、下调的基因探针864条。GO功能富集分析发现上调的基因主要参与免疫反应,下调的基因主要参与造血。KEGG Pathway富集分析发现上调的基因主要参与细胞粘附分子和抗原呈递等信号通路。Real-time PCR验证5个差异基因,与芯片中表达变化趋势一致。因此TYRO3、AXL和MER受体共同参与调控机体的免疫反应和血细胞分化。 相似文献
5.
(S)-(?)-Vertinolide 1 was synthesized via the tetronic acid derivative 6 from (S)-(?)-tetrahydro-2-methyl-5-oxo-2-furancarboxylic acid 3. (±)-Vertinolide was also synthesized from (±)-3. 相似文献
6.
Protein aggregation is associated with fatal neurodegenerative diseases, including Alzheimer's and Parkinson's. Mapping out kinetics along the aggregation pathway could provide valuable insights into the mechanisms that drive oligomerization and fibrillization, but that is beyond the current scope of computational research. Here we trace out the full kinetics of the spontaneous formation of fibrils by 48 Aβ16-22 peptides, following the trajectories in molecular detail from an initial random configuration to a final configuration of twisted protofilaments with cross-β-structure. We accomplish this by performing large-scale molecular-dynamics simulations based on an implicit-solvent, intermediate-resolution protein model, PRIME20. Structural details such as the intersheet distance, perfectly antiparallel β-strands, and interdigitating side chains analogous to a steric zipper interface are explained by and in agreement with experiment. Two characteristic fibrillization mechanisms—nucleation/templated growth and oligomeric merging/structural rearrangement—emerge depending on the temperature. 相似文献
7.
O. M. Selivanova E. Yu. Gorbunova L. G. Mustaeva E. I. Grigorashvili M. Yu. Suvorina A. K. Surin O. V. Galzitskaya 《Biochemistry. Biokhimii?a》2016,81(7):755-761
A method for the synthesis and high purification of fragments of Aβ(1-42) peptide has been elaborated. We have synthesized the amyloidogenic fragment Aβ(16-25) predicted by us and studied the process of its aggregation by electron microscopy and X-ray analysis. Electron microscopy images show that the peptide forms a film, which is not characteristic of amyloid fibrils. At the same time, according to the X-ray diffraction data, its preparations display the presence of two main reflections (4.6-4.8 and 8-12 Å) characteristic of cross-β structure of amyloid fibrils. Thus, the fragment Aβ(16-25) that we predicted is a promising object not only for studying the process of polymerization of the peptides/proteins, but also for using it as a nanomaterial to study a number of biological processes. 相似文献
8.
《Bioscience, biotechnology, and biochemistry》2013,77(10):1709-1711
For use as the internal standards in a quantitative analysis of natural jasmonic acid (JA) and methyl jasmonate (JAMe) by gas chromatography-mass spectrometry-selected ion monitoring, (±)-2-(2,3–2H2)JA and its methyl ester, (±)-2-(2,3–2H2)JAMe, were efficiently prepared from 2-(2–pentyl)-2-cyclopentenone through catalytic semi-deuteriogenation of acetylenic intermediates with deuterium gas in pyridine. 相似文献
9.
1903年10月22日,乔治·威尔斯·比德尔(G.W.Beadle)出生于美国内布拉斯加州一户农民家庭,1926年和1927年先后获内布拉斯加林肯大学理科学士和硕士学位。尔后,他到康奈尔大学,在遗传学大师爱默生(Emerson)领导的“玉米小组”攻读博士学位,从事玉米细胞遗传学研究。1931年获博士学位后,他又到加州理工学院,在遗传学大师摩尔根(Morgan)领导的“蝇室”从事果蝇细胞遗传学研究。1936年,他到哈佛大学任助理教授,1937~1946年任斯坦福大学教授,1946年回到加州理工学院任教授和生物学系主任,1961~1968年任芝加哥大学校长。比德尔和泰特姆(Tatum)以… 相似文献
10.
目的:探究干扰素γ诱导蛋白16(IFI16)在多发性骨髓瘤(MM)中的生物学功能。方法:将人多发性骨髓瘤细胞(RPMI-8266)分为Control组(未转染的细胞)、NC-sh组(转染阴性对照shRNA慢病毒的细胞)、IFI16-sh组(转染IFI16 shRNA慢病毒的细胞)、NC-OE组(转染阴性对照过表达慢病毒的细胞)和IFI16-OE组(转染IFI16过表达慢病毒的细胞)。使用Lipofectamine 2000进行细胞转染,培养48 h后收集细胞。通过MTT法和集落形成实验检测细胞增殖。通过Annexin V-FITC和PI染色法检测细胞凋亡。通过Transwell检测细胞侵袭。通过qRT-PCR检测IFI16、Bcl-2、Bax、成纤维细胞生长因子(FGF)1、FGF2的m RNA水平。通过Western blot检测IFI16的蛋白表达水平。将裸鼠随机分为NC-sh组和IFI16-sh组,每组6只。NC-sh组和IFI16-sh组裸鼠分别皮下注射转染NC-sh和IFI16-sh的RPMI-8266细胞悬液。35 d后测量肿瘤体积和肿瘤重量。采用ELISA法检测Th1细胞... 相似文献
11.
Xinbo Zhou Wei Chen Cheng Xu Shiyong Fan Yunde Xie Wu Zhong Lili Wang Song Li 《Bioorganic & medicinal chemistry letters》2010,20(8):2605-2608
A series of novel, potent PPARα/γ dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC50 value of 0.012 ± 0.002 and 0.032 ± 0.01 μM, respectively, for hPPARα and hPPARγ in transactivation assay. Additionally, compound 2b demonstrated good glucose and lipid lowering effect in genetic diabetic (db/db) mice. 相似文献
12.
Victor M. Rosas-García Isabel del Carmen Sáenz-Tavera Verónica Janeth Rodríguez-Herrera Benjamín Raymundo Garza-Campos 《Journal of molecular modeling》2013,19(4):1459-1471
We studied hydrated calcium oxalate and its ions at the restricted Hartree–Fock RHF/6-31G* level of theory. Performing a configurational search seems to improve the fit of the HF/6-31G* level to experimental data. The first solvation shell of calcium oxalate contains 13 water molecules, while the first solvation shell of oxalate ion is formed by 14 water molecules. The first solvation shell of Ca(II) is formed by six water molecules, while the second shell contains five. At 298.15 K, we estimate the asymptotic limits (infinite dilution) of the total standard enthalpies of hydration for Ca(II), oxalate ion and calcium oxalate as ?480.78, –302.78 and –312.73 kcal mol?1, resp. The dissociation of hydrated calcium oxalate is an endothermic process with an asymptotic limit of +470.84 kcal mol?1. Figure
CaC2O4(H2O)16 and C2O4 2-(H2O)14 相似文献
13.
Mugunthan G Ramakrishna K Sriram D Yogeeswari P Ravindranathan Kartha KP 《Bioorganic & medicinal chemistry letters》2011,21(13):3947-3950
A series of galactose-derived aryl enones were synthesised and screened against Mycobacterium tuberculosis H37Rv. Preliminary results were promising with MIC values in the range 1.56-12.5 μg/mL. 相似文献
14.
The 13C.n.m.r spectra of water-soluble and -insoluble glucans synthesized by enzymes isolated from six strains of Streptococcus mutans are interpreted. The glucans are shown to be composed primarily of α(1→3)- and α-(1→6)-linked glucosyl residues, and the relative abundance of each linkage is estimated from peak areas. Treatment of water-insoluble glucans with dextranase is found to result in water-soluble and -insoluble products, the former enriched in α-(1→6)-linkages and the latter in α-(1→3)-linkages. The structural conclusions arrived at by 13C-n.m.r. spectroscopy are consistent with data from methylation analysis and 1H-n.m.r. spectroscopy. 相似文献
15.
《Prostaglandins, Leukotrienes and Medicine》1984,13(2):219-226
CL 115,129, the corresponding carboxylic acid and major metabolite of CL 115,347 (d,1-15-deoxy-16-hydroxy-16(α/β)-vinyl-prostaglandin E2 methyl ester), a potent orally and transdermally long acting antihypertensive agent, infused at 0.1 μg/kg/min into the left renal artery of sodium pentobarbital anesthetized beagle dogs increased urinary volume, sodium (Na+), potassium (K+) and chloride (Cl−) excretion of the left kidney 289, 201, 101 and 229%, respectively, over the 30 min vehicle-treated control periods. At 0.3 μg/kg/min CL 115,129 caused a 475 and 336% increase in urinary volume and Na , respectively. ℓ-Prostaglandin E2 (ℓ-PGE2) infused at 0.1 μg/kg/min into the left renal artery increased urinary volume, Na+, K+ and Cl− excretion of the left kidney of anesthetized beagle dogs 416, 234, 112 and 255%, respectively, over the control. Both CL 115,129 and ℓ-PGE2 did not affect the systemic arterial blood pressure or the electrolyte excretion of the contralateral kidney. It is concluded that in contrast to other conventional vasodilators, which may cause severe water and electrolyte retention, CL 115,347, via its metabolite CL 115,129, may cause diuresis and natriuresis in many clinical settings when used as an antihypertensive. 相似文献
16.
Terpene derivatives converted by microbial biotransformation constitute an important resource for natural pharmaceutical, fragrance, and aroma substances. In the present study, the monoterpene α-phellandrene was biotransformed by 16 different strains of microorganisms (bacteria, fungi, and yeasts). The transformation metabolites were initially screened by TLC and GC/MS, and then further characterized by NMR spectroscopic techniques. Among the six metabolites characterized, 6-hydroxypiperitone, α-phellandrene epoxide, cis-p-menth-2-en-1-ol, and carvotanacetone, which originated from (-)-(R)-α-phellandrene, are reported for the first time in this study. Additionally, the substrate and the metabolite 5-p-menthene-1,2-diol were subjected to in vitro antibacterial and anticandidal tests. The metabolite showed moderate-to-good inhibitory activities (MICs=0.125 to >4?mg/ml) against various bacteria and especially against Candida species in comparison with its substrate (-)-(R)-α-phellandrene and standard antimicrobial agents. 相似文献
17.
18.
从实验室保藏的菌株中筛选获得Candida sp.PT2A,并通过18S rRNA鉴定为安大略假单胞菌Candida on-tarioensis。对C.ontarioensis不对称还原合成(R)-2-氯-1-(3-氯苯基)乙醇的发酵产酶条件和转化条件进行优化,确定了最适的发酵产酶条件和转化条件:温度30℃,初始pH 6.5,摇床转速180 r/min,菌体质量浓度200 g/L。采用2-氯-1-(3-氯苯基)乙酮质量浓度为10 g/L时,还原反应72 h,(R)-2-氯-1-(3-氯苯基)乙醇的e.e.值为99.9%,产率为99%;底物质量浓度提高至30 g/L时,产率下降为84.3%。采用十六烷基三甲基溴化铵(CTAB)对C.ontarioensis细胞进行通透性处理(CTAB g/L,4℃下处理20 min),在30 g/L底物下反应24 h,产物的e.e.和产率分别达到99.9%和97.5%。 相似文献
19.
Isotope-assisted vibrational circular dichroism (VCD) investigations have been used to probe the site specific local structure of an amyloid peptide for the first time. A seven residue peptide, NH2-KLVFFAE-COOH, which represents the Aβ(16–22) fragment of the Alzheimer’s amyloid β peptide, was used for these investigations. 13C labels were introduced separately at the carbonyl group of leucine (residue 17), alanine (residue 21) and also at both sites together. Since VCD spectra provide structure dependent signs, band shapes and frequencies, the isotope-assisted VCD spectroscopy revealed information on site specific secondary structure of the polypeptide. Isotope dilution VCD experiments provided a means to distinguish between parallel and anti-parallel nature of the β-sheet structure formed by the Aβ(16–22) fragment. The current results establish the usefulness of isotope-assisted VCD analysis in determining the site specific secondary structure of amyloid peptides. 相似文献