A highly enantioselective allylic alkylation of isoquinolinedione derivatives under palladium catalysis was developed in the preparation of quaternary carbon stereocenters. Under standard reaction conditions, excellent yields and enantioselectivities were realized and the products could be transformed into dihydroisoquinolone with vicinal chiral carbon centers or THIQ core structures in short steps with high yields.
View Article and Find Full Text PDFTwo dimensional transition metal dichalcogenides (TMDCs) have attracted much interest and shown promise in many applications. However, it is challenging to obtain uniform TMDCs with clean surfaces, because of the difficulties in controlling the way the reactants are supplied to the reaction in the current chemical vapor deposition growth process. Here, we report a new growth approach called 'dissolution-precipitation' (DP) growth, where the metal sources are sealed inside glass substrates to control their feeding to the reaction.
View Article and Find Full Text PDFCancer metastasis is a major cause of death among women afflicted with breast cancer (BC) and understanding the molecular processes involved is a major focus in BC research. Circular RNAs (circRNAs) have emerged as genomic regulatory molecules in carcinogenesis and metastasis; however, their role in BC is unclear. We characterized a novel circRNA, hsa_circ_0000515, in context of BC.
View Article and Find Full Text PDFPurpose: To assess the efficacy of diffusion kurtosis imaging (DKI) in the prediction of the treatment response to neoadjuvant chemotherapy in patients with locally advanced gastric cancer (LAGC).
Methods: A total of 31 LAGC patients were enrolled in this prospective study. All patients underwent diffusion-weighted MRI examination (with b = 0, 200, 500, 800, 1000, 1500, 2000 s/mm, the subscript denotes the number of signal averages) before and after chemotherapy.
Zhong Nan Da Xue Xue Bao Yi Xue Ban
March 2020
Objectives: To investigate the role of pyruvate kinase isozyme type M2 (PKM2) in regulating the expression of matrix metalloproteinase-1 (MMP-1) in human umbilical vein endothelial cells (HUVECs) under high glucose exposure and the underlying mechanisms.
Methods: HUVECs were exposed to concentration gradient (5.5, 15.
Using a rational design strategy for isoform-selective inhibition of PI3Kα, two series of novel 2,3,4,5-tetra-substituted thiophene derivatives containing either diaryl urea or N-Acylarylhydrazone scaffold were designed and synthesized. The most promising compound 12k was demonstrated to bear nanomolar PI3Kα inhibitory potency with 12, 28, 30, 196-fold selectivity against isoforms β, γ, δ and mTOR. Besides, it also showed good developability profiles in cell-based proliferation against a panel of human tumor cells as well as ADME assays.
View Article and Find Full Text PDFWith the development of research on superwettability materials, superhydrophobic and superoleophilic materials show superior separation ability in oil-water separation due to their excellent oil-water selectivity. However, due to the super wetting ability of the oil to the material, it is difficult to clean and reuse after adsorbing the oil spill. Therefore, how to realize the complete regeneration of superhydrophobic and superoleophilic materials is still a worldwide problem.
View Article and Find Full Text PDFBackground: Ultrasound can produce certain biophysical effects including thermal and non-thermal effects on cells. Sonoporation, the most widely studied non-thermal biological effect of ultrasound, is considered to be the basis for new therapeutic applications. Ultrasound irradiation can increase the permeability of cell membranes through sonoporous effect, which makes molecules like those of drugs, protein, and DNA that normally cannot pass through the cell membranes be able to enter cells.
View Article and Find Full Text PDFVorinostat (SAHA) with great therapeutic potential has been approved by the FDA for the treatment of cutaneous T-cell lymphoma as the first HDACs inhibitor, but the drawbacks associated with hydroxamic acid group (poor stability, easy metabolism, weak binding ability to class IIa isozymes, and poor selectivity) have been exposed during the continuous clinical application. Based on the pharmacophore of HDAC inhibitors, two series of compounds with novel zinc binding group (ZBG) were designed and synthesized, and the antitumor bioactivities were evaluated in four human cancer cell lines (A549, Hela, HepG2, and MCF-7). Among the synthesized compounds, compounds , , , , and exhibited promising inhibitory activities against the selected tumor cell lines, especially compounds and on Hela's cytostatic activity (: IC = 11.
View Article and Find Full Text PDFThe B(CF)-catalyzed chemoselective hydrosilylation of α,β- and α,β,γ,δ-unsaturated ketones into the corresponding non-symmetric ketones in mild reaction conditions is developed. Nearly 55 substrates including those bearing reducible functional groups such as alkynyl, alkenyl, cyano, and aromatic heterocycles are chemoselectively hydrosilylated in good to excellent yields. Isotope-labeling studies revealed that hexafluoro-2-propanol also served as a hydrogen source in the process.
View Article and Find Full Text PDFAnn Palliat Med
February 2021
The coronavirus disease 2019 (COVID-19) is a new infectious disease, firstly appeared in Wuhan city and has rapidly spread to 114 countries outside China, which is receiving worldwide attention. As two important means of examination, computed tomography (CT) and real-time reverse transcription polymerase chain reaction (RT-PCR) have always been controversial in the clinical diagnosis of COVID-19 pneumonia. Here, we report a family cluster case of a father and a son diagnosed as COVID-19 at our hospital, and described the clinical manifestations, laboratory results, CT changes, diagnosis and treatment strategy of these two patients.
View Article and Find Full Text PDFTwo-dimensional (2D) transition metal dichalcogenides (TMDCs) have attracted great attention due to their physical and chemical properties that make them promising in electronics and optoelectronics. Because of the difficulties in controlling concentrations of solid precursors and spatially nonuniform growth dynamics, it is challenging to grow 2D TMDCs over large areas with good uniformity and reproducibility so far, which significantly hinders their practical use. Here we report a vertical chemical vapor deposition (VCVD) design with gaseous precursors to grow monolayer TMDCs with a uniform density and high quality over the whole substrate and with excellent reproducibility.
View Article and Find Full Text PDFBackground And Objective: Long-acting nociceptive-selective regional anesthesia has remained an elusive clinical goal. We aspired to identify a novel compound that would produce nociceptive-selective regional anesthesia through the transient receptor potential vanilloid 1 (TRPV1) channels.
Methods: We designed and synthesized a novel compound (LL-a) that penetrates the cell membrane through TRPV1 channels and binds to voltage-gated sodium channels.
Porcine deltacoronavirus (PDCoV) is a novel enteropathogenic coronavirus that causes watery diarrhea in piglets. Little is known regarding the alteration of the gut microbiota in PDCoV-induced diarrhea piglets. In this study, 5-day-old piglets were experimentally infected with PDCoV strain CH-01, and all piglets developed typical clinical disease, characterized by acute and severe watery diarrhea.
View Article and Find Full Text PDFTo improve CO adsorption performance of nanoparticle absorbents, a novel tertiary amine functionalized nano-SiO (NS-NR) was synthesized based on the 3-aminopropyltrimethoxysilane (KH540) modified nano-SiO (NS-NH) via methylation. The chemical structure and performances of the NS-NR were characterized through a series of experiments, which revealed that NS-NR can react with CO in water and nanofluid with low viscosity revealed better CO capture. The CO capture mechanism of NS-NR was studied by kinetic models.
View Article and Find Full Text PDFJ Diabetes Investig
September 2020
Aims/introduction: Non-coding ribonucleic acids (ncRNAs) have recently been shown to be involved in various biological processes. However, most of these ncRNAs are of unknown function or without annotation. This study first investigated the whole transcriptome profiles of placentas to identify the potential functions that ncRNAs exerted in gestational diabetes mellitus (GDM).
View Article and Find Full Text PDFThe development of Portunus trituberculatus egg cells is directly related to the nutritional status of the fertilized egg, which affects the key production stages of offspring hatching. Vitellogenin plays a key role in the nutrient supply required for the development of the egg cells. The c-Jun N-terminal kinase (JNK) is an important member of the mitogen-activated protein kinase (MAPK) superfamily and plays an important role in cell proliferation, transformation, differentiation, and apoptosis.
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