Structural basis of tolvaptan binding to the vasopressin V receptor.

The vasopressin V receptor (VR) is a validated therapeutic target for autosomal dominant polycystic kidney disease (ADPKD), with tolvaptan being the first FDA-approved antagonist. Herein, we used Gaussian accelerated molecular dynamics simulations to investigate the spontaneous binding of tolvaptan to both active and inactive VR conformations at the atomic-level. Overall, the binding process consists of two stages.

Exosomes combined with biosynthesized cellulose conduits improve peripheral nerve regeneration.

Peripheral nerve injury is one of the more common forms of peripheral nerve disorders, and the most severe type of peripheral nerve injury is a defect with a gap. Biosynthetic cellulose membrane (BCM) is a commonly used material for repair and ligation of nerve defects with gaps. Meanwhile, exosomes from mesenchymal stem cells can promote cell growth and proliferation.

Defluorinative Alkylation of Trifluoromethylbenzimidazoles Enabled by Spin-Center Shift: A Synergistic Photocatalysis/Thiol Catalysis Process with CO

We describe a catalytic strategy for direct single C(sp)-F bond alkylation of trifluoromethylbenzimidazoles under a photoinduced thiol catalysis process. The CO radical anion (CO) proved to be the most efficient single-electron reductant to realize such a transformation. The spin-center shift of the generated radical anion intermediate is the key step in realizing C-F bond activation under mild conditions with high efficiency.

Risk Factors for Recurrence of Chronic Subdural Hematoma: A Single Center Experience.

Objective: Chronic subdural hematoma (CSDH) is a common form of intracranial hemorrhage with a substantial recurrence rate. We aimed to investigate the predictive factors for the postsurgical recurrence of CSDH.

Methods: We retrospectively reviewed the medical records of patients with CSDH who underwent surgery in West China Hospital between January 2012 and June 2018.

Risk assessment and genomic characterization of Zika virus in China and its surrounding areas.

Background: Zika virus (ZIKV) has emerged as a global pathogen causing significant public health concerns. China has reported several imported cases where ZIKV were carried by travelers who frequently travel between China and ZIKV-endemic regions. To fully characterize the ZIKV strains isolated from the cases reported in China and assess the risk of ZIKV transmission in China, comprehensive phylogenetic and genetic analyses were performed both on all ZIKV sequences of China and on a group of scientifically selected ZIKV sequences reported in some of the top interested destinations for Chinese travelers.

Viability, biofilm formation, and MazEF expression in drug-sensitive and drug-resistant strains circulating in Xinjiang, China.

Background: Tuberculosis (TB) caused by (MTB) is one of the most common chronic infectious amphixenotic diseases worldwide. Prevention and control of TB are greatly difficult, due to the increase in drug-resistant TB, particularly multidrug-resistant TB. We speculated that there were some differences between drug-sensitive and drug-resistant MTB strains and that 3,6,9 toxin-antitoxin systems (TASs) were involved in MTB viability.

[Effects of hypoxia preconditioning on serum NGB and S-100B in patients with intracranial aneurysm surgery].

Objective: To study the clinical effects of hypoxia preconditioning (HPC) and its effects on serum neuroglobin (NGB) and S-100B level in the patients undergoing intracranial aneurysm surgery.

Methods: Forty patients scheduled to intracranial aneurysm surgery were randomly.divided into 2 groups: HPC group (n= 20) and control group (n= 20).

Association of polymorphisms in the DCDC2 gene with developmental dyslexia in the Han Chinese.

Background: Genetic association studies on populations of European origin have identified the DCDC2 gene as a susceptibility locus for developmental dyslexia. Here, we sought to investigate the association of DCDC2 polymorphisms with developmental dyslexia in children of Han Chinese origin.

Methods: We undertook a case-control genetic association study on 76 dyslexic children and 79 non-dyslexic matched controls.

Design and diversity-oriented synthesis of novel 1,4-thiazepan-3-ones fused with bioactive heterocyclic skeletons and evaluation of their antioxidant and cytotoxic activities.

This study has achieved the design and diversity-oriented synthesis of novel 1,4-thiazepine derivatives embedded with carbazole, pyrazole or isoxazole motif via microwave-assisted multicomponent reactions under solvent-free condition, thus providing a green and facile access to 1,4-thiazepine derivatives with prominent features of high structural diversity, short reaction time, high yields and environmental friendliness. More importantly, these novel compounds have been subjected to the test of in vitro antioxidant and cytotoxic activities, resulting in the finding that these 1,4-thiazepine derivatives not only have significant antioxidant activity, but also exhibit remarkably selective cytotoxicity to carcinoma cell line HCT 116.

Antitumor constituents from the leaves of Carya cathayensis.

This study aimed to find cytotoxic chemical constituents from Carya cathayensis leaves (LCC) by using various chromatographic procedures. Identification of the chemical constituents was carried out by various spectroscopic techniques and classical chemical methods. The cytotoxic activity of the constituents was assayed on HeLa and HepG2 cell lines by staining with 3-(4,5-dimethylthiahiazol-2-y1)-2,5-di-phenytetrazolium bromide (MTT).

A novel biosynthetic hybrid scaffold seeded with olfactory ensheathing cells for treatment of spinal cord injuries.

Background: Implantation of tissue-engineered scaffolds is one of the most promising therapeutic strategies for inducing nerve regenerations following spinal cord injuries. In this paper, we report a novel bioengineered hybrid scaffold comprised of three major extracellular matrix (ECM) proteins.

Methods: ECM-scaffolds (ECM-S) were prepared by gelling fibrinogen, fibronectin and laminin using fresh rat plasma.

Synthesis of isoxazolo[5,4-b]pyridines by microwave-assisted multi-component reactions in water.

A series of new polycyclic-fused isoxazolo[5,4-b]pyridines were obtained by a one-pot tandem reaction under microwave irradiation in water. Without any use of additional reagent or catalyst, the synthetic protocol represents a green one and makes this methodology suitable for library synthesis in drug discovery efforts.

A new mild base-catalyzed Mannich reaction of hetero-arylamines in water: highly efficient stereoselective synthesis of beta-aminoketones under microwave heating.

A new mild base-catalyzed Mannich reaction of aromatic aldehydes with 1,2-diphenylethanone and hetero-arylamines including pyridin-2-amine and pyrimidin-2-amine is described. In this reaction, a series of new beta-aminoketones were stereoselectively synthesized in water by controlling the steric hindrance of the substrates under microwave heating. This method has the advantages of a short synthetic route, operational simplicity, increased safety for small-scale high-speed synthesis, and minimal environmental impact.

An efficient and chemoselective synthesis of benzo[e][1,4]thiazepin-2(1H,3H,5H)-ones via a microwave-assisted multi-component reaction in water.

A new and efficient strategy for the synthesis of benzo[e][1,4]thiazepin-2(1H,3H,5H)-ones via a microwave-assisted multi-component reaction in aqueous media is described.

Microwave-assisted combinatorial synthesis of new 3-pyrimidin-5-ylpropanamides via a solvent-dependent chemoselective reaction.

A series of new 3-pyrimidin-5-ylpropanamides was selectively synthesized via a microwave-assisted, chemoselective reaction of arylidene-Meldrum's acid, 6-hydroxypyrimidin-4(3H)-one, and structurally diverse amines including (S or R)-1-phenylethanamine, cyclohexanamine, and cyclopentanamine depended on nature of solvents. In this reaction, the utilization of HOAc as a solvent leads to 3-pyrimidin-5-ylpropanamides, whereas water as reaction media results in the spiro[5.5]undecane-1,5,9-triones from same starting materials.

In situ expression and significance of B7 costimulatory molecules within tissues of human gastric carcinoma.

Aim: To explore the role and significance of costimulatory molecules B7H1,B7H2 and ICOS within tissues of human gastric carcinoma and the possible mechanisms in tumor escape.

Methods: mRNA expressions of costimulatory molecules including B7H1,B7H2,ICOS and B7-1 in tissues of human gastric carcinoma were investigated by in situ hybridization using digoxigenin-labeled oligonucleotide-probes. The tissue of chronic gastric ulcer was used as a control.