Synthesis and antimicrobial activities of oximes derived from O-benzylhydroxylamine as FabH inhibitors.

Forty-three oxime derivatives were synthesized by allowing O-benzylhydroxylamines to react with primary benzaldehydes or salicylaldehydes; these products were gauged as potential inhibitors of β-ketoacyl-(acyl-carrier-protein) synthase III (FabH). Among the 43 compounds, 38 are reported herein for the first time. These compounds were assayed for antimicrobial activities against Escherichia coli, Pseudomonas aeruginosa, Pseudomonas fluorescens, Bacillus subtilis, Staphylococcus aureus, and Enterococcus faecalis.

[Expression and clinical significance of Notch1 on the membrane of bone marrow CD38(+)CD138(+) plasma cells in the patients with multiple myeloma].

Objective: To investigate the expression of Notch1 on the membrane of bone marrow CD38(+)CD138(+) plasma cells in the patients with multiple myeloma (MM), and explore the importance of Notch signaling pathway in the formation and progression of MM.

Methods: Thirty three MM patients and 15 healthy controls were enrolled in this study. The expression of Notch1 on the membrane of bone marrow CD38(+)CD138(+) and CD38(+)CD138(-) plasma cells were analyzed by flow cytometry.

[Expression of phosphorylated STAT5 in bone marrow hematopoietic stem cells of patients with paroxysmal nocturnal hemoglobinuria before and after in vitro G-CSF or SCF stimulation].

Objective: To study the expressions of phosphorylated STAT5 (P-STAT5) in CD34(+)CD59(-) and CD34(+)CD59(+) bone marrow cells of the patients with paroxysmal nocturnal hemoglobinuria (PNH) before and after in vitro G-CSF or SCF stimulation, then evaluate the functions of G-CSF and SCF receptors in PNH clone cells.

Methods: Bone marrow mononuclear cells (BMMNC) of 26 PNH patients and 14 normal controls were stimulated in vitro with G-CSF (100 ng/ml) or SCF (100 ng/ml) for 10 min. Before and after these stimulations, the mean fluorescence intensity (MFI) of P-STAT5 in CD34(+)CD59(+) BMMNC and CD34(+)CD59(-) BMMNC were measured by flow cytometry.

Ca+2/calmodulin-dependent protein kinase mediates glucose toxicity-induced cardiomyocyte contractile dysfunction.

(1) Hyperglycemia leads to cytotoxicity in the heart. Although several theories are postulated for glucose toxicity-induced cardiomyocyte dysfunction, the precise mechanism still remains unclear. (2) This study was designed to evaluate the impact of elevated extracellular Ca(2+) on glucose toxicity-induced cardiac contractile and intracellular Ca(2+) anomalies as well as the mechanism(s) involved with a focus on Ca(2+)/calmodulin (CaM)-dependent kinase.

Dimensional crossover of thermal conductance in graphene nanoribbons: a first-principles approach.

First-principles density-functional calculations are performed to investigate the thermal transport properties in graphene nanoribbons (GNRs). The dimensional crossover of thermal conductance from one to two dimensions (2D) is clearly demonstrated with increasing ribbon width. The thermal conductance of GNRs of a few nanometers width already exhibits an approximate low-temperature dependence of T(1.

[Quantity and subtypes of dendritic cells in patients with immune related pancytopenia and their clinical significance].

This study was aimed to investigate the quantity and subtypes of dendritic cells (DC) in patients with immune related pancytopenia (IRP) and to explore the role of DC in pathogenesis of IRP. The quantity of plasmacytoid dendritic cells (pDC, Lin(-)HLA-DR(+) CD123(+) cells) and myeloid dendritic cells (mDC, Lin(-)HLA-DR(+) CD11c(+)cells) in peripheral blood of 65 patients with IRP (37 new diagnosed and 28 remitted) and 17 healthy controls were analyzed by flow cytometry. The results indicated that the ratio of pDC in peripheral blood mononuclear cells (PBMNC) was (0.

[Expressions of miR-21, miR-155 and miR-210 in plasma of patients with lymphoma and its clinical significance].

This study was purposed to investigate the expressions of miR-21, miR-155 and miR-210 in plasma of patients with lymphoma, and explore their role played in diagnosis, evaluation of chemotherapy effect and prognosis of lymphoma. The expressions of miR-21, miR-155 and miR-210 were assayed by RT-PCR in plasma of 54 cases of lymphoma, 10 cases of lymphonode inflammation and 27 cases of normal controls. The results indicated that the expressions of miR-21, miR-155 and miR-210 in plasma of lymphoma patients were higher than those of control group and lymphonode inflammation group (P < 0.

Synthesis, biological evaluation, and molecular docking studies of 1,3,4-thiadiazol-2-amide derivatives as novel anticancer agents.

A series of 1,3,4-thiadiazol-2-amide derivatives (5a-5y) have been designed and synthesized, and their biological activities were also evaluated as potential antiproliferation and FAK inhibitors. Among all the compounds, 5h showed the most potent activity in vitro, which inhibited the growth of MCF-7 and B16-F10 cell lines with IC(50) values of 0.45 and 0.

Promising oxonitridosilicate phosphor host Sr3Si2O4N2: synthesis, structure, and luminescence properties activated by Eu2+ and Ce3+/Li+ for pc-LEDs.

A novel oxonitridosilicate phosphor host Sr(3)Si(2)O(4)N(2) was synthesized in N(2)/H(2) (6%) atmosphere by solid state reaction at high temperature using SrCO(3), SiO(2), and Si(3)N(4) as starting materials. The crystal structure was determined by a Rietveld analysis on powder X-ray and neutron diffraction data. Sr(3)Si(2)O(4)N(2) crystallizes in cubic symmetry with space group Pa ̅3, Z = 24, and cell parameter a = 15.

PRAME Gene Expression in Acute Leukemia and Its Clinical Significance.

Objective: To investigate the expression of the preferentially expressed antigen of melanoma (PRAME) gene in acute leukemia and its clinical significance.

Methods: The level of expressed PRAME mRNA in bone marrow mononuclear cells from 34 patients with acute leukemia (AL) and in 12 bone marrow samples from healthy volunteers was measured via RT-PCR. Correlation analyses between PRAME gene expression and the clinical characteristics (gender, age, white blood count, immunophenotype of leukemia, percentage of blast cells, and karyotype) of the patients were performed.

TET2 Expression in Bone Marrow Mononuclear Cells of Patients with Myelodysplastic Syndromes and Its Clinical Significances.

Objective: To investigate the expression of TET2 mRNA and protein in the bone marrow mononuclear cells (BMMNC) of patients with myelodysplastic syndrome (MDS) and its clinical significance.

Methods: The expression of TET2 mRNA and protein in bone marrow mononuclear cells (BMMNC) of 32 patients with MDS and 20 healthy donors was examined by qPCR and Western blot.

Results: The expression of TET2 mRNA in BMMNC was down-regulated in MDS patients compared with the donor group [(0.

Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.

A series of pyrazolyl-thiazolinone derivatives (E1-E36) have been designed and synthesized and their biological activities were also evaluated as potential EGFR and HER-2 kinase inhibitors. Thirty-four of the 36 compounds were reported for the first time. Among them, compound 2-(5-(4-bromophenyl)-3-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-one (E28) displayed the most potent inhibitory activity (IC(50)=0.

[EPOR and TPOR expressions on CD34+ CD59- and CD34+ CD59+ bone marrow cells from patients with paroxysmal nocturnal hemoglobinuria].

Objective: To study the expressions of erythropoietin receptor (EPOR) and thrombopoietin receptor (TPOR) on CD34+ CD59- and CD34+ CD59+ bone marrow (BM) cells from patients with paroxysmal nocturnal hemoglobinuria (PNH).

Methods: (1) The expressions of EPOR and TPOR on CD34+ CD59- and CD34+ CD59- BM cells from 26 PNH patients and 16 normal controls were examined by flow cytometry (FCM). (2) The mRNA expression of the EPOR and the TPOR in BM mononuclear cells (BMMNC) from 25 PNH patients and 13 normal controls were examined by RT-PCR.

[Effect of CD8+ effector T cells on the hematopoiesis pathway damage in the patients with severe aplastic anemia].

Objective: To investigate the quantity and the pathway to damage hematopoietic cells of CD8+CD25+ and CD8+ HLA-DR+ effector T cells in peripheral blood (PB) of severe aplastic anemia(SAA) patients and explore the immunopathogenesis of SAA.

Methods: The quantity of CD8+ CD25+ and CD8+ HLA-DR+ cells in PB and the expressions of perforin, granzyme B, tumor necrosis factor-beta (TNF-beta) and FasL in 29 SAA (14 untreated and 15 recovered) patients and 12 normal controls were analyzed by flow cytometry.

Results: The fraction of CD8+ CD25+ T cells in CD8+ T cells was (3.

[Research of cyclopentolate 1% on the effect of cycloplegia for Chinese hyperopic children].

Objective: To investigate the peak time of refractive error obtained by Cyclopentolate Hydrochloride 1.0% (Cyclopentolate 1.0% for short) and Cyclopentolate 1.

[Protective role of pericardial tissue on injured myocardium in rats].

Objective: To define the protective role of pericardial tissue and identify the subcellular population with potential contribution to cardiac protection after injury in a rat model.

Methods: Myocardial infarction (MI) was created by the ligation of left anterior descending artery (LAD) in rats while the pericardial sac was either completely removed (-PC, n = 10) or surgically closed after ligation (+PC, n = 8). The follow-up functional and structure benefits were analyzed by echocardiography and 2,3,5- triphenyl-2H-tetrazolium, chloride(TTC) and bromodeoxyuridine (BrdU) staining.

Design, synthesis and biological evaluation of N-phenylsulfonylnicotinamide derivatives as novel antitumor inhibitors.

A series of novel N-phenylsulfonylnicotinamide derivatives (1-24) have been synthesized and evaluated as potential EGFR tyrosine kinase (TK) inhibitors. Among all the compounds, compound 10 (5-bromo-N-(4-chlorophenylsulfonyl)nicotinamide) showed the most potent growth inhibitory activity against EGFR TK and antiproliferative activity of MCF-7 cancer cell line in vitro, with IC(50) value of 0.09 and 0.

Urotensin upregulates transforming growth factor-β1 expression of asthma airway through ERK-dependent pathway.

Airway smooth muscle cells (ASMCs) play a key role in the process of asthma airway remodeling. Urotensin II (UII) and transforming growth factor (TGF)-β are potent mitogens for ASMCs proliferation. The study was aimed to determine whether UII-upregulated TGF-β-mediated ASMCs proliferation and extracellular signal-regulated kinase (ERK) was required for such an effect.

Expression of N-methyl-d-aspartate receptor 1 and its phosphorylated state in basal ganglia of a neonatal piglet hypoxic-ischemic brain injury model: a controlled study of (1)H MRS.

Excitatory amino acids (EAAs) and excitotoxicity medicated by receptors of these amino acids play an important role in hypoxic-ischemic brain injury (HIBI), but most studies were ex vivo experiments, the mechanism in vivo is not well understood. We sought to study the expression of N-methyl-d-aspartate receptor 1 (NR1) and phosphorylated N-methyl-d-aspartate receptor 1 (P-NR1) in basal ganglia in a piglet model of HIBI and to investigate the correlation between Glx(Glu/Gln) value measured by magnetic resonance spectroscopy (MRS) and NR1/P-NR1 expression. Multi-voxel (1)H MRS was applied to detect change in Glx in basal ganglia of the newborn piglets in vivo.

[STAT5 phosphorylation levels of erythropoietin and thrombopoietin receptors in CD34(+)CD59(-) and CD34(+)CD59(+) bone marrow cells of patients with paroxysmal nocturnal hemoglobinuria].

Objective: To study the STAT5 phosphorylation levels of erythropoietin receptor (EPOR) and thrombopoietin receptor (TPOR) in CD34(+)CD59(-) and CD34(+)CD59(+) bone marrow cells of the patients with paroxysmal nocturnal hemoglobinuria (PNH).

Methods: The bone marrow mononuclear cells (BMMNC) were extracted from 23 PNH patients treated at our department from April 2010 to February 2011 and 11 normal controls. The mean fluorescence intensity (MFI) of phosphorylated STAT5 (P-STAT5) in CD34(+)CD59(+) cells and CD34(+)CD59(-) cells with or without the stimulation of 10 U/ml EPO and 50 U/ml TPO were examined by flow cytometry.

[Case-control study on influence factors of birth defects].

Objective: To investigate the influence factors of birth defects.

Methods: The congenital malformational fetuses born from 13 week of gestation to 7 days after birth were selected as the study group between April 1st, 2009 and March 31st, 2010. The health born fetuses were set as control in the same period.

Synthesis, antibacterial activities and molecular docking studies of Schiff bases derived from N-(2/4-benzaldehyde-amino) phenyl-N'-phenyl-thiourea.

A series of novel Schiff base derivatives have been designed and synthesized, and their biological activities were also evaluated as potential inhibitors of FabH. These compounds were assayed for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus. Compounds with potent antibacterial activities were tested for their E.

[Value of MRI in the diagnosis of cerebral abscess caused by Candida albicans in premature infants].

Objective: To explore the value of serial magnetic resonance imaging (MRI) in the diagnosis of cerebral abscess caused by Candida albicans in premature infants.

Methods: The clinical data of 8 premature infants with central nervous system invasive fungal infection (IFI) were retrospectively studied. The infants underwent serial cerebral MRI scans (T1WI, T2WI and DWI).

Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells.

A series of oxadiazole derivatives containing 1,4-benzodioxan (4a-4s) have been first synthesized for their potential immunosuppressive activity. Among the compounds, compound 4i showed the most potent biological activity against RAW264.7 cells (inhibition=37.