199 resultados para 8-hydroxyquinolinate derivatives


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本文对新疆紫草培养细胞的生长及紫革宁衍生物形成的调节与控制进行了研究.结果表朗:在不同时期照射白光、蓝光,对紫草培养细胞生长及紫草宁衍生物的积累均有明显的抑制作用;而第三周照红光一天、第二周以及整个培养过程均照远红光、第19天照紫外光等,都对生产培养基中紫草宁衍生物的积累有促进作用;其中,远红光与紫外光的最佳照射时间长度都为30分钟,且细胞内苯丙氨酸解氨酶的活性与紫草宁衍生物的含量有明显的正相关性.研究了不同照光条件下,紫草培养细胞生长,紫草宁衍生物积累以及苯丙氨酸解氨酶活性变化的动态,基本上找出了它们的变化规律以及它们之间的相互关系. 通过试验发现,紫草细胞培养的适宜温度为25℃,适宜pH值为5.3—5.8:在培养基中加入O,l%-0.30%的活性炭、用磁水器处理培养基等,对紫草宁衍生物的积累有良好的促进作用。 提高培养基中的Cu2+,Mg2+,Zn2+.K+浓度,有利于紫草宁衍生物的积累,而在生产培养基中加入NH:,则显著抑制了紫草宁衍生物的产生;培养基中蔗糖浓度为50g/L时,对紫草细胞生长及紫草宁衍生物的积累最有利,而生产培养基中不加IAA,KT对紫草宁衍生物的积累有利.以密环菌为诱导子,促进了紫草细脆生长及紫草宁衍生物的积累。 此外,对Cu2+、密环菌发酵液处理条件下,紫革宁衍生物积累与苯丙氨 酸解氨酶活性的关系以及不同蔗糖浓度条件下,生长培养基中紫草细胞生长、 紫草宁衍生物的积累,细胞内可溶性糖含量变化的动态进行了研究.

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Kallikrein 8 (KLK8) is a serine protease functioning in the central nervous system, and essential in many aspects of neuronal activities. Sequence comparison and gene expression analysis among diverse primate species identified a human-specific splice for

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In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues, were designed, s

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Several 2-heteroaryl-, 2-heteroarylcarbonylmethyl-, 2-arylcarbonylmethyl, and 2-arylethyl derivatives of S-dihydro(alkyloxy)benzyloxypyrimidines have been synthesized and the anti-HIV activities of these compounds were tested in C8166 cell and against RT

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A series of (E)-N-phenylstyryl-N-alkylacetamides, 5, were synthesized by direct reduction-acetylation of beta-arylnitroolefins, followed by N-alkylation. The title compounds were characterized by H-1-NMR, EIMS and IR analysis. All the synthesized compound

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To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-ethylbenzenesulfonate (4g) and 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-chlorobenzenesulfonate (41) showed the more potent anti-HIV-1 activity with 50% effective concentration (EC50) values of 2.59 and 4.01 mu g/ml, and therapeutic index (TI) values of 31.77 and 24.51, respectively.

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报道了云南8种树蛙的染色体组型, 并对目前所已知的树蛙种类的染色体组型进行了比较。

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Sertoli cells play a central role in the control and maintenance of spermatogenesis. Isolated Sertoli cells of mouse and rat testes have been shown to secrete plasminogen activator (PA) and a plasminogen activator inhibitor type-1 (PAI-1) in culture. In this study, we have investigated the hormonal regulation of PA and PAI-1 activities in cultured monkey Sertoli cells. Sertoli cells (5x10(5) cells/well) isolated from infant rhesus monkey testes were preincubated at 35 degrees C for 16 h in 24-well plates precoated with poly(D-lysine) (5 mu g/cm(2)) in 0.5 mi McCoy's 5a medium containing 5% of fetal calf serum and further incubated for 48 h in 0.5 mi serum-free medium with or without various hormones or other compounds, PA as well as PAI-1 activities in the conditioned media were assayed by fibrin overlay and reverse fibrin autography techniques respectively. The Sertoli cells in vitro secreted only tissue-type PA (tPA), no detectable amount of urokinase-type PA (uPA) could be observed, Monkey Sertoli cells were also capable of secreting PAI-1, Immunocytochemical studies indicated that both tPA and PAI-1 positive staining localized in the Sertoli cells, spermatids and residual bodies of the seminiferous epithelium; Northern blot analysis further confirmed the presence of both tPA and PAI-1 mRNA in monkey Sertoli cells. Addition of follicle-stimulating hormone (FSH) or cyclic adenosine monophosphate (cAMP) derivatives or cAMP-generating agents and gonadotrophin-releasing hormone (GnRH) agonist or phorbol ester (PMA) to the cell culture significantly increased tPA activity. PAI-1 activity in the culture was also enhanced by these reagents except 8-bromo-dibutyryl-cAMP, forskolin and 3-isobutyl-1-methylxanthin (MIX) which greatly stimulated tPA activity, whereas decreased PAI-1 activity, implying that neutralization of PAI-1 activity by tile high level of tPA in the conditioned media may occur. These data suggest that increased intracellular signals which activate protein kinase A (PKA), or protein kinase C (PKC) can modulate Sertoli cell tPA and PAI-1 activities, The concomitant induction of PA and PAI-1 by the same reagents in the Sertoli cells may reflect a finely tuned regulatory mechanism in which PAI-1 could limit the excession of the proteolysis.

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To understand pharmacophore properties of pyranmycin derivatives and to design novel inhibitors of 16S rRNA A site, comparative molecular field analysis (CoMFA) approach was applied to analyze three-dimensional quantitative structure-activity relationship (3D-QSAR) of 17 compounds. AutoDock 3.0.5 program was employed to locate the orientations and conformations of the inhibitors interacting with 16S rRNA A site. The interaction mode was demonstrated in the aspects of inhibitor conformation, hydrogen bonding and electrostatic interaction. Similar binding conformations of these inhibitors and good correlations between the calculated binding free energies and experimental biological activities suggest that the binding conformations of these inhibitors derived from docking procedure were reasonable. Robust and predictive 3D-QSAR model was obtained by CoMFA with q(2) values of 0.723 and 0.993 for cross-validated and noncross-validated, respectively. The 3D-QSAR model built here will provide clear guidelines for novel inhibitors design based on the Pyranmycin derivatives against 16S rRNA A site. (c) 2005 Elsevier B.V. All rights reserved.

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We analyzed n-mers (n=3-8) in the local environment of 8,249,446 human SNPs and compared their distribution with that in the genome reference sequences. The results revealed that the short sequences, which contained at least one CpG dinucleotide, occurred