Isoindoline-based fluorogenic probes bearing a self-immolative linker for the sensitive and selective detection of O-GlcNAcase activity.

O-GlcNAcase (OGA) is implicated in several important biological and disease-relevant processes. Here, we synthesized fluorogenic probes for OGA by grafting GlcNAc directly or using a self-immolative linker to the hydroxyl position of 4-hydroxylisoindoline (BHID), a typical excited-state intramolecular proton transfer (ESIPT) probe. The probe was used for a fluorogenic assay to determine the half maximal inhibitory concentration of a known OGA inhibitor and differentiate between OGA and hexosaminidase when GlcNAc is replaced by GlcNPr, where a propionyl group is used instead of an acetyl group.

Synthesis of Axially Chiral QUINAP Derivatives by Ketone-Catalyzed Enantioselective Oxidation.

QUINAPs have emerged as a pivotal class of axially chiral compounds with remarkable features in the stereoinduction of diverse enantioselective transformations. However, the confined substrate range and extravagant price still pose challenges, limiting their broader utilization. Herein, we describe the first atroposelective oxidation of an N atom using a chiral ketone catalyst, allowing the kinetic resolution of QUINAPOs to give both the unreacted substrates and their corresponding N-oxides with excellent enantioselectivity.

Organocatalytic Direct Asymmetric Indolization from Anilines by Enantioselective [3 + 2] Annulation.

We report the efficient syntheses of chiral tetrahydroindole pyrazolinones by the asymmetric [3 + 2] cascade cyclizations (indolizations) of simple aniline derivatives with pyrazolinone ketimines as 2C synthons. The chiral phosphoric-acid-catalyzed system uses a concerted π-π interaction/dual H-bond control strategy to catalytically direct the asymmetric aniline, which undergoes a highly chemo-, regio-, and enantioselective [3 + 2] cascade annulation, furnishing a series of optically active tetra-hydroindole pyrazolinones with two contiguous chiral aza-quaternary carbon centers in excellent yields with excellent enantioselectivities. This method features a relatively broad substrate scope for amines and 2-naphthylamines and highlights the emerging value of direct chiral indolizations from simple amine sources in organic synthesis.

Asymmetric Organocatalytic Synthesis of 2,3-Allenamides from Hydrogen-Bond-Stabilized Enynamides.

Asymmetric catalytic synthesis of 2,3-allenamides from hydrogen-bond-stabilized enynamides in the presence of quinine-based bifunctional squaramide organocatalysts is described. This protocol forms a variety of 2,3-allenamides in high yields and excellent stereoselectivities, in which the elaborated introduction of intramolecular H-bonds within the N, N-bidentate amide group constitutes one of the keys to this highly enantioselective transformation. The synthetic practicality of this reaction has been demonstrated by the axis-to-center chirality transfer of allenamides to furnish enantiomerically enriched building blocks.

Cavernous hemangiomas of the temporalis muscle with prominent formation of phleboliths: Case report and review of the literature.

Rationale: Hemangiomas are benign tumors characterized by an abnormal proliferation of blood vessels, most often occur in the skin and subcutaneous tissue, intramuscular hemangioma, a distinctive type of hemangioma within the skeletal muscle, account for <1% of all hemangiomas, temporalis muscle is a very uncommon site, cavernous hemangioma of the temporalis muscle with prominent formation of phleboliths is rare reported.

Patient Concerns: A 62-year-old man presented with a slowly increased mass in his right temporal fossa.

Diagnoses: Computed tomography (CT) scan showed the lesion across the zygomatic arch, with many calcified nodules differ in sizes and no erosion to the bone, magnetic resonance imaging (MRI) showed an oval lesion with hypointense and isointense on T2-weighted imaging within the temporal muscle, and preoperation diagnosis was hemangioma.

Co-Adsorption of O and CO on Au : Infrared Photodissociation Spectroscopy and Theoretical Study of [Au O (CO) ] (n=2-6).

The co-adsorption of O and CO on anionic sites of gold species is considered as a crucial step in the catalytic CO oxidation on gold catalysts. In this regard, the [Au O (CO) ] (n=2-6) complexes were prepared by using a laser vaporization supersonic ion source and were studied by using infrared photodissociation spectroscopy in the gas phase. All the [Au O (CO) ] (n=2-6) complexes were characterized to have a core structure involving one CO and one O molecule co-adsorbed on Au with the other CO molecules physically tagged around.

Clinicopathological characteristics and prognosis of patients with adenosquamous lung carcinoma.

This study was aimed to characterize clinicopathological features and prognosis of patients with adenosquamous lung carcinoma (ASC). Among the 2531 patients with lung cancer who underwent surgery between January 2000 and June 2012 in our hospital, 59 were histologically diagnosed as having ASC. The clinicopathological features and follow-up data of ASC patients were collected and analyzed statistically.

Primary natural killer/T cell lymphoma of the cervix: case report and clinicopathological analysis.

Objective: To present pathological and molecular characterizations of a rare case that was diagnosed as nasal-type natural killer (NK)/T cell lymphoma primarily arising in the cervix.

Case Report: An Asian woman was admitted to hospital with a hysteromyoma, and laparotomy was performed. A large tumor of the uterus was found, which was limited to the cervix.

The effect of borneol on the concentration of meropenem in rat brain and blood.

Meropenem is a carbapenem antibiotic with a wide spectrum of activity against both Gram-positive and Gram-negative bacteria. Because of its clinical efficacy, meropenem is an excellent choice for the treatment of serious infections in both adults and children. The knowledge of tissue concentrations of antibiotic in an infection site is valuable for the prediction of treatment outcome.

Prognostic value of serum AFP, AFP-L3, and GP73 in monitoring short-term treatment response and recurrence of hepatocellular carcinoma after radiofrequency ablation.

Purpose: Alpha-fetoprotein (AFP), Lens culinaris agglutinin-reactive fraction of AFP (AFP-L3), and Golgi protein 73 (GP73) levels have been widely used as tumor markers for the diagnosis of hepatocellular carcinoma (HCC). The aim of this study was to investigate whether these tumor markers could be used to monitor short-term treatment response and recurrence of HCC in patients undergoing radiofrequency ablation (RFA).

Methods: Between July 2012 and July 2013, 53 consecutive patients with newly diagnosed HCC were prospectively enrolled in this study.

Effects of arsenic trioxide alone and in combination with bortezomib in multiple myeloma RPMI 8266 cells.

The aim of this study was to detect the efficiency of arsenic trioxide (ATO) alone or together with bortezomib to inhibit proliferation and induce apoptosis in a multiple myeloma (MM) RPMI 8266 cells. Mechanisms of action were also investigated. RPMI 8266 cells were treated with ATO alone and in combination with bortezomib for 24 hours, and cell viability was assessed by modified MTT.

[Identification of serum biomarkers for assessing minimal residual disease in acute leukemia by serum peptide pattern].

Objective: To screen serum biomarkers for minimal residual disease (MRD) monitoring according to differential peptidomics profile in the serum from the patients with acute leukemia (AL) and healthy controls.

Methods: Serum polypeptides from 90 AL patients, 60 healthy controls and 20 patients with benign hematological disorders were enriched by copper chelate magnetic beads, and the peptidomics profile was obtained by matrix assisted laser desorption ionization time of flight mass spectrometry (MALDI-TOF-MS) analysis. And the intensities of differential peptides were calculated to assess MRD level.

[The study on relationship between age and cytogenetic subgroups in 640 patients with de novo acute myeloid leukemia].

Objective: To analyze the cytogenetic characteristics of different age subgroups in patients with acute myeloid leukemia (AML), and to explore the relationship between age and cytogenetics.

Methods: Between January 2004 and December 2011, Bone marrow (BM) samples from 640 patients with de novo AML were analyzed retrospectively. The analyses were performed according to standard culturing and banding techniques, and clonal abnormalities were defined and described according to the International System for Human Cytogenetic Nomenclature (ISCN 2009).

RAD23A negatively regulates RIG-I/MDA5 signaling through promoting TRAF2 polyubiquitination and degradation.

RIG-I/MDA5 plays a pivotal role in innate immunity by detecting intracellular double-stranded RNA (dsRNA) and activating the transcription of type I interferons and proinflammatory factors, but the exactly regulating mechanism of RIG-I/MDA5 signaling remains elusive. In this study, UbL-UBA domain containing protein RAD23A was identified as a negative regulator of RIG-I/MDA5-mediated signaling activation through a small interfering RNA (siRNA)-based screening. Knockdown of RAD23A augmented the expression of RIG-I/MDA5-mediated expression of proinflammatory cytokines and IFN-β whereas ectopic expression of RAD23A showed the converse effect.

Observation of Microvascular Perfusion in the Hegu (LI4) Acupoint Area after Deqi Acupuncture at Quchi (LI11) Acupoint Using Speckle Laser Blood Flow Scanning Technology.

The aim of this study was to investigate the traditional meridian theory using speckle laser blood flow scanning technology to observe microcirculation of the Hegu acupoint area after acupuncture stimulation on distant points. An observational study was conducted to observe the microvascular perfusion of Hegu (LI4) and control points after acupuncturing Quchi (LI11). Thirty healthy volunteers (mean age 31.

[Anti-leukemic effect of scutellaria extract SBX and its mechanisms].

This study was aimed to explore the anti-leukemic effect of scutellaria extract SBX in human leukemia cell lines and its mechanism. The leukemia cell lines, including HL-60, NB4, U937, K562 and Jurkat, were cultured in vitro and proliferative inhibition of these cell lines was detected by CellTiter-Glo Luminescent Cell Viability Assay in order to screen the most sensitive cell line. The effect of SBX on cell cycle was analyzed by flow cytometry and the protein expressions determined by Protein Pathway Array respectively.

Silencing of the COPS3 gene by siRNA reduces proliferation of lung cancer cells most likely via induction of cell cycle arrest and apoptosis.

The COPS3 gene has stimulating effect on cell proliferation and progression of osteosarcomas and related cells. However, the features of COPS3 and its potential application as a therapeutic target in other cancers has not yet been studied. In this study, therefore, the effect of COPS3 silencing via COPS3 siRNA on lung cancer cell proliferation was examined.

Acceleration of diabetic wound healing by low-dose radiation is associated with peripheral mobilization of bone marrow stem cells.

In this study we investigated the effect of repeated low-dose radiation exposure (75 mGy X ray) on skin wound healing in a rat model of diabetes. A skin wound was made on the backs of diabetic and age-matched control rats 60 days after diabetes was induced by a single injection of streptozotocin. Rats with skin wounds were immediately treated with whole-body radiation daily for 5, 10 or 15 days with a 2-day break every 5 days.

[Differential expression genes in various phases of chronic myeloid leukemia by cDNA microarray].

The aim of this study was to explore the mechanism underlying the blast crisis of chronic myeloid leukemia. Analysis of gene expression profiles of chronic myeloid leukemia patients in chronic phase and blast crisis were analyzed by using cDNA microarray representing 4096 genes for finding the differential expression genes. The results indicated that 74 differential expression genes were identified in at least 3 gene chips in blast crisis compared with chronic phase, among them 52 genes were down-regulated and 22 genes were up-regulated in blast crisis.

[Construction of shRNA eukaryotic expression vectors of pkm2 gene and their effect on drug resistant cell line of acute promyelocytic leukemia].

This study was aimed to construct the shRNA eukaryotic expression vectors of M2-pyruvate kinase gene (pkm2) and to investigate the effects of pkm2 gene interference on the drug resistance of acute promyelocytic leukemia (APL) cells in vitro. Three specific shRNAs of pkm2 gene were designed and cloned into PBSU6 vector containing a U6 promotor. The constructed plasmids were identified and proved by the restriction sequence analysis.

Combined IFN-gamma-endostatin gene therapy and radiotherapy attenuates primary breast tumor growth and lung metastases via enhanced CTL and NK cell activation and attenuated tumor angiogenesis in a murine model.

Background: Gene-radiotherapy, a combination of gene therapy and radiotherapy, is a new paradigm for cancer treatment, with the potential to simultaneously improve local and systemic breast cancer control. The aim of this study was to evaluate antitumor effect of interferon (IFN)-gamma-endostatin-based gene-radiotherapy in a murine metastatic breast tumor model, and to elucidate possible mechanisms involved.

Methods: Murine mammary adenocarcinoma 4T1 cells transfected with pEgr-IFN-gamma and pEgr-endostatin plasmids were irradiated (2-20 Gy).

[The methylation pattern and clinical significance of Zonula occludens-1 gene promoter in acute leukemia].

Objective: To investigate the methylation status of Zonula occludens-1 (ZO-1) gene promoter and discuss its role in the pathogenesis and progression of acute leukemia (AL) as a general gene marker.

Methods: The methylation pattern in promoter region of ZO-1 gene was detected with methylation specific PCR in AL cell lines HL60, Molt4 and NK92 as well as in 121 clinical bone marrow samples including 81 cases of AL and 40 non malignant cases.

Results: The promoter region of ZO-1 gene was completely methylated in HL60, Molt4 and NK92 cells; but it was unmethylated in 40 non malignant bone marrow samples.

Low-dose radiation and its clinical implications: diabetes.

Induction of hormesis and adaptive response by low-dose radiation (LDR) has been extensively indicated. Adaptive response induced by LDR was not only resistant to damage caused by a subsequently high-dose radiation, but also cross-resistant to other non-radiation challenges, such as chemicals. Mechanisms by which LDR induces the preventive effect on radiation- or chemical-induced tissue damage include induced or up-regulated expression of protective proteins, such as heat shock proteins and antioxidants.