Novel biaryloxazolidinone derivatives with broad-spectrum antibacterial activity, favorable drug-like profiles and in vivo efficacy against linezolid-resistant Staphylococcusaureus.

The emergence of multidrug-resistant bacteria along with a declining pipeline of clinically useful antibiotics has led to the urgent need for the development of more effective antibacterial agents to treat drug-resistant bacteria. We previously discovered compound OB-158 with potent antibacterial activity but exhibited poor oral bioavailability. Herein, a systematic structural optimization of OB-158 to improve pharmacokinetic profiles yielded 26 novel biaryloxazolidinone analogues, and their activities against Gram-positive S.

Cerebral Venous Thrombosis Presenting as a Ring-Enhancing Lesion on MR imaging: A Case Report and Critical Review.

Cerebral venous thrombosis (CVT) is a rare form of venous thromboembolism. The presentation of symptoms is highly variable in this disease. The findings on MRI vary depending on the age of the thrombus within the vessel.

Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.

A series of novel oxazolidinone derivatives with nitrogen-containing fused heterocyclic moiety were designed and synthesized in this article. Their antibacterial activities were measured against S. aureus, MRSA and MSSA by MIC assay.

Cancer-associated fibroblasts induce immunotherapy resistance in hepatocellular carcinoma animal model.

Hepatocellular carcinoma is known to be a common predominant cancer in adults, especially in eastern countries. Immune response and cancer-associated fibroblasts (CAFs) have significant influences on tumor development. However, the interaction between CAFs and immunotherapy is unclear in hepatocellular carcinoma.

Polymorphisms of genes related to vitamin D metabolism and transportation and its relationship with the risk of osteoporosis: protocol for a multicentre prospective cohort study in China.

Introduction: Osteoporotic fracture is one of the most common causes of disability and a major contributor to medical care costs in many regions of the world. The polymorphisms of genes related to vitamin D metabolism and transportation are associated with variation in bone mineral density and the risk of osteoporosis.

Methods And Analysis: The China Community-based Cohort of Osteoporosis study is an observational, longitudinal, multicentre, prospective cohort study for middle-aged and older permanent residents of China, which has been ongoing in six cities since 2016.

Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.

In this article, a series of novel oxazolidinone derivatives containing a piperidinyl moiety was designed and synthesized. Their antibacterial activities were measured against S. aureus, MRSA, MSSA, LREF and VRE by MIC assay.

Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.

A series of novel biaryloxazolidinone derivatives containing amide and acrylamide structure were designed, synthesized and evaluated for their antibacterial activity. Most compounds generally exhibited potent antibacterial activity with MIC values of 1 μg/mL against S. aureus, MRSA, MSSA, LREF and VRE pathogens, using linezolid and radezolid as positive controls.

Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.

We previously discovered a series of novel biaryloxazolidinone analogues bearing a hydrazone moiety with potent antibacterial activity. However, the most potent compound OB-104 exhibited undesirable chemical and metabolic instability. Herein, novel biaryloxazolidinone analogues were designed and synthesized to improve the chemical and metabolic stability.

Tetrahydrocurcumin protects against spinal cord injury and inhibits the oxidative stress response by regulating FOXO4 in model rats.

It has been reported that tetrahydrocurcumin has hypoglycemic, hypolipidemic, anti-metastasis, anticancer and anti-depressant pharmacological effects, and its antioxidative, hypoglycemic and hypolipidemic properties are better than those of curcumin. The present study assessed whether tetrahydrocurcumin exerts a neuroprotective effect against spinal cord injury (SCI) and investigated the underlying mechanisms. In a rat model of SCI, tetrahydrocurcumin enhanced the average Basso-Beattie-Bresnahan scores, inhibited water accumulation in the spinal cord and decreased inflammatory factors.

Computer-assisted engineering of programmed drug releasing multilayer nanomedicine via indomethacin-mediated ternary complex for therapy against a multidrug resistant tumor.

Nanomedicine with programmed drug release can give full play to the synergistic effect of multi-component system in complicated tumor environment. However, the construction of these programmed drug delivery systems often depends on the sophisticated materials design and synthesis. In this study, we successfully designed an indomethacin (IND)-mediated ternary complex system based on a PEG cleavable polyethyleneimine (PEI), indomethacin (IND) and benzene ring containing chemotherapeutic drugs (such as paclitaxel (PTX), doxorubicin and docetaxel).

Glutamate dehydrogenase inhibits tumor growth in gastric cancer through the Notch signaling pathway.

Glutamate dehydrogenase (GDH) is a key enzyme in glutaminolysis and can regulate allosteric functions. Immunohistochemical study found that GDH expressed in gastric cancer cell cytoplasm and membrane, and a few located in the nucleus, ranging from light yellow to tan to sepia. According to the analysis by Kaplan Meier survival curve and the Log-Rank test, the median survival of GDH high expression in patients was 51.

Image Fusion: A Novel Approach in Gamma Knife Surgery Treating Trigeminal Neuralgia.

Objective: Finding accurate locations for radiosurgical targets in trigeminal neuralgia (TN) remains challenging. This study provides a novel approach of image fusion used in locating radiosurgical targets for gamma knife surgery (GKS) in the treatment of TN.

Methods: Magnetic resonance imaging (MRI) scans were performed before frame fixation, and computed tomography (CT) scans were performed following frame fixation.

Downregulation of miR-218 by nicotine promotes cell proliferation through targeting CDK6 in non-small cell lung cancer.

Background: Nicotine, an important component of tobacco, is a major risk factor of lung cancer, but the mechanism through which nicotine promotes lung cancer development remains unclear.

Methods: Eighty patients with lung cancer were enrolled in this study, 34 of whom did not smoke and the others did. The expression of miR-218 and CDK6 messenger RNA (mRNA) was measured using quantitative reverse transcription polymerase chain reaction (qRT-PCR).

A case report: acute pancreatitis associated with tacrolimus in kidney transplantation.

Background: Tacrolimus has been widely used for immunosuppressive therapy in solid organ transplantation (SOT) and allo-geneic stem cell transplantation (allo-SCT) over the past 2 decades. Pancreatitis caused by tacrolimus was rarely reported in kidney transplantation previously.

Case Presentation: Here we presented a case of a 45-year-old male who underwent kidney transplantation and received immunosuppressive therapy of tacrolimus, on day + 67 after transplantation he developed acute pancreatitis with extremely high blood concentration of tacrolimus.

A Systematic Review of Neuroprotective Efficacy and Safety of DL-3-N-Butylphthalide in Ischemic Stroke.

DL-3-n-butylphthalide (NBP) is widely used as a neuroprotective drug for ischemic stroke in China. There is, however, no established evidence on its efficacy and safety for patients with ischemic stroke. We, therefore, conducted a systematic review and meta-analysis.

Circulating NK cell subsets and NKT‑like cells in renal transplant recipients with acute T‑cell‑mediated renal allograft rejection.

Emerging evidence indicates that natural killer (NK) cells and NKT‑like cells may affect allograft outcomes following solid organ transplantation. However, the roles of these cells in allograft acceptance and dysfunction are controversial. To assess the changes in NK cell and CD3+CD56+ NKT‑like cell frequency and phenotype in renal allograft recipients and to explore their associations with acute T‑cell‑mediated renal allograft rejection (ACR), longitudinal changes in NK and NKT‑like cell frequency and phenotype were characterized using flow cytometry and immunohistochemistry in the peripheral blood and kidney allograft tissues in 142 recipients undergoing kidney transplantation.

A Clinical Comparative Analysis of Retroperitoneal Laparoscopic Tuberculous Nephrectomy and Open Tuberculous Nephrectomy.

This study aimed to investigate the efficacy and safety of retroperitoneal laparoscopic tuberculous nephrectomy (RLTN) and open tuberculous nephrectomy (OTN). One hundred fifty-eight patients treated with RLTN were enrolled in the RLTN group. One hundred patients treated with OTN were enrolled in the control group.

Differentiation of glioblastoma from solitary brain metastases using radiomic machine-learning classifiers.

This study aimed to identify the optimal radiomic machine-learning classifier for differentiating glioblastoma (GBM) from solitary brain metastases (MET) preoperatively. Four hundred and twelve patients with solitary brain tumors (242 GBM and 170 solitary brain MET) were divided into training (n = 227) and test (n = 185) cohorts. Radiomic features extraction was performed with PyRadiomics software.

Quantification of Microsurgical Anatomy in Three-Dimensional Model: Transfrontal Approach for Anterior Portion of the Thalamus.

The thalamus located in the deep site of cerebrum with the risk of internal capsule injury during operation. The purpose of this study was to compare the anatomy for exposure and injury using simulative surgical corridor of 3-dimensional model. The 3-dimensional anatomy model of thalamus in cerebrum was created based on magnetic resonance imaging performed for 15 patients with trigeminal neuralgia.

Chromatin accessibility changes are associated with enhanced growth and liver metastasis capacity of acid-adapted colorectal cancer cells.

The acidic extracellular microenvironment, namely acidosis, is a biochemical hallmark of solid tumors. However, the tumorigenicity, metastatic potential, gene expression profile and chromatin accessibility of acidosis-adapted colorectal cancer cells remain unknown. The colorectal cancer cell SW620 was cultured in acidic medium (pH 6.

CD4+ T Cell Immune Response to VP1 and VP3 in BK Virus Infected Recipients of Renal Transplantation.

Objective: To investigate the characteristics of BK virus (BKV) specific cellular immune response in the recipients who have early infection with BKV after renal transplantation.

Methods: The recipients of renal allografts (n = 30) were divided into groups of BK virus nephropathy (BKVN), viruria, and viremia. The BKV load was observed with real-time fluorescence quantitative polymerase chain reaction in urine and blood every three months.

[The usage of comprehensive geriatric assessment in elderly patients with acute myeloid leukemia: a multicenter, prospective study].

To evaluate the feasibility and potential value of comprehensive geriatric assessment (CGA) in elderly (≥60 years) patients with newly diagnosed acute myeloid leukemia (AML) in China. The CGA results of 83 newly diagnosed AML (non-APL) patients from 16 hospitals in Beijing and Tianjin between March 2016 and December 2017 were prospectively collected and analyzed. The clinical data, treatment and follow-up information were also collected.