Visible-Light-Driven, Radical-Triggered Tandem Cyclization of o-Hydroxyaryl Enaminones: Facile Access to 3-CF /CF-Containing Chromones.

A practical and straightforward synthetic route to construct a variety of 3-CF/CF-containing chromones via photoredox catalysis was developed. This novel protocol features a visible-light-induced radical-triggered tandem cyclization.

Mineralocorticoid Receptor Deficiency in Macrophages Inhibits Atherosclerosis by Affecting Foam Cell Formation and Efferocytosis.

Mineralocorticoid receptor (MR) has been considered as a potential target for treating atherosclerosis. However, the cellular and molecular mechanisms are not completely understood. We aim to explore the functions and mechanisms of macrophage MR in atherosclerosis.

Boronate affinity-based surface molecularly imprinted polymers using glucose as fragment template for excellent recognition of glucosides.

Rapid and efficient extraction of bioactive glycosides from complex natural origins poses a difficult challenge, and then is often inherent bottleneck for their highly utilization. Herein, we propose a strategy to fabricate boronate affinity based surface molecularly imprinted polymers (MIPs) for excellent recognition of glucosides. d-glucose was used as fragment template.

The association between expression of IFIT1 in podocytes of MRL/lpr mice and the renal pathological changes it causes: An animal study.

Renal damage is the major cause of SLE associated mortality, and IFIT1expression was elevated in SLE cases in accordance of previous studies. Therefore, we conducted an animal study to identify the role of IFIT1 expression in renal pathological changes.18 female MRL/lpr mice and same number of female BALB/c mice were enrolled in present study.

Diastereoselective Intramolecular [3 + 2]-Annulation of Donor-Acceptor Cyclopropane with Imine-Assembling Hexahydropyrrolo[3,2-c]quinolinone Scaffolds.

An intramolecular [3 + 2]-annulation of amide-linked donor-acceptor cyclopropane with in situ-generated imine is described. As a result, diverse hexahydropyrrolo[3,2-c]quinolinones, as the tricyclic core of martinellines, were efficiently assembled in good to excellent yield (up to 93%) with a good diastereomeric ratio (up to 98:2).

Alkaloids from piper longum protect dopaminergic neurons against inflammation-mediated damage induced by intranigral injection of lipopolysaccharide.

Background: Alkaloids from Piper longum (PLA), extracted from P. longum, have potent anti-inflammatory effects. The aim of this study was to investigate whether PLA could protect dopaminergic neurons against inflammation-mediated damage by inhibiting microglial activation using a lipopolysaccharide (LPS)-induced dopaminergic neuronal damage rat model.

Hollow molecular imprinted polymers towards rapid, effective and selective extraction of caffeic acid from fruits.

Rapid and selective extraction and enrichment of trace bioactive analytes from complex matrices were of significant importance for efficient and accurate quantification. Here, novel hollow molecular imprinted polymers (HMIPs) were prepared using caffeic acid (CA) as template, 4-vinylpyridine (4-VP) as functional monomer, and FeO@SiO as sacrificial support. Fourier transform infrared spectrometer (FT-IR), transmission electron microscopy (TEM), nitrogen adsorption and thermo-gravimetric analysis (TGA) were used to verify the successful synthesis of HMIPs.

Fetal bovine serum influences the stability and bioactivity of resveratrol analogues: A polyphenol-protein interaction approach.

Fetal bovine serum (FBS) is a universal growth supplement of cell and tissue culture media. Herein, the influences of FBS on the stability and antioxidant activity of 21 resveratrol analogues were investigated using a polyphenol-protein interaction approach. The structure-stability relationships of resveratrol analogues in FBS showed a clear decrease in the stability of hydroxylated resveratrol analogues in the order: resorcinol-type>pyrogallol-type>catechol-type.

An Epigenetic Compound Library Screen Identifies BET Inhibitors That Promote HSV-1 and -2 Replication by Bridging P-TEFb to Viral Gene Promoters through BRD4.

The human HSV-1 and -2 are common pathogens of human diseases. Both host and viral factors are involved in HSV lytic infection, although detailed mechanisms remain elusive. By screening a chemical library of epigenetic regulation, we identified bromodomain-containing protein 4 (BRD4) as a critical player in HSV infection.

Target-guided isolation of polar antioxidants from Abelmoschus esculentus (L). Moench by high-speed counter-current chromatography method coupled with wavelength switching and extrusion elution mode.

An off-line two-dimensional high-speed counter-current chromatography strategy combined with the wavelength switching technique and extrusion elution mode was successfully developed and applied to the isolation of polar antioxidants from Abelmoschus esculentus (L).Moench. Target-guided by the result of 2,2-diphenyl-1-picrylhydrazyl screening assay, four antioxidants were obtained with purities over 90% through orthogonal high-speed counter-current chromatography separation.

Isolation of α-Amylase Inhibitors from Kadsura longipedunculata Using a High-Speed Counter-Current Chromatography Target Guided by Centrifugal Ultrafiltration with LC-MS.

In this study, a high-speed counter-current chromatography (HSCCC) separation method target guided by centrifugal ultrafiltration with high-performance liquid chromatography-mass spectrometry (CU-LC-MS) was proposed. This method was used to analyze α-amylase inhibitors from Kadsura longipedunculata extract. According to previous screening with CU-LC-MS, two screened potential α-amylase inhibitors was successfully isolated from Kadsura longipedunculata extract using HSCCC under the optimized experimental conditions.

Online coupling solid-phase ligand-fishing with high-performance liquid chromatography-diode array detector-tandem mass spectrometry for rapid screening and identification of xanthine oxidase inhibitors in natural products.

Screening and analysis of bioactive compounds from natural products is challenging work due to their complexity. This study presents the first report on hyphenation of solid-phase ligand-fishing using immobilized xanthine oxidase microcolumn (IXOM) and high-performance liquid chromatography-diode array detector-tandem mass spectrometry (HPLC-DAD-MS/MS) for screening and identification of XO inhibitors from complex mixtures. Solid-phase ligand-fishing system was hyphenated with the HPLC system via four-port switching valve and a six-port injection valve as an interface for transferring effluents from IXOM to HPLC, and collecting chromatograms from LFMC (ligand-fishing microextraction column) and C18 column in a run by only one DAD.

Development of pristane induced mice model for lupus with atherosclerosis and analysis of TLR expression.

Objectives: This study was designed to establish a murine model of lupus with atherosclerosis, and to investigate the expression of Toll-like receptors (TLRs) in the aorta and kidney.

Methods: The 9-week-old female ApoE-/- and C57BL/6 mice were randomly divided into a ApoE-/- pristane treated group (group A), ApoE-/- control group (group B), C57BL/6 pristane treated group (group C) and C57BL/6 control group (group D). Each mouse was given either a single intraperitoneal injection of 0.

A gas-diffusion microfluidic paper-based analytical device (μPAD) coupled with portable surface-enhanced Raman scattering (SERS): facile determination of sulphite in wines.

A novel facile method for on-site determination of sulphite in wine using a gas-diffusion microfluidic paper-based analytical device (μPAD) combined with surface-enhanced Raman spectroscopy (SERS) was explored. The inexpensive and disposable μPAD was realized by sandwiching the ZnO-paper disc and integrating gas-diffusion separation and gas preconcentration on a paper-based platform. Through extensive condition optimization, the SERS signal at a shift of 620 cm(-1) and the concentration of SO2 showed good linearity in the range of 5-300 μg mL(-1).

In-vivo absorption of pinocembrin-7-O-β-D-glucoside in rats and its in-vitro biotransformation.

Pinocembrin-7-O-β-D-glucoside (PCBG), a flavonoid isolated from Penthorum chinense Pursh., has significant liver-protecting effects. The pharmacokinetics of PCBG and its major metabolite pinocembrin (PCB) in rats were investigated in this study.

Enantioselective extraction of phenylsuccinic acid in aqueous two-phase systems based on acetone and β-cyclodextrin derivative: Modeling and optimization through response surface methodology.

A novel aqueous two-phase system (ATPS) composed of β-cyclodextrin (β-CD) derivative and acetone was developed for enantioselective extraction of racemic phenylsuccinic acid (PSA). Binodal curves, tie-lines, and critical points for the investigated ATPS were determined and the experimental tie-lines data were successfully correlated by Othmer-Tobias, Bancroft, and Setschenow-type equations. ATPS containing sulfobutyl ether-β-CD (SBE-β-CD) exhibited better enantioselectivity than that using carboxymethyl-β-CD (CM-β-CD).

Temporal and Spatial Expression of LGR5 After Acute Spinal Cord Injury in Adult Rats.

Leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5), a well-characterized marker of stem cell and cancer stem cells (CSCs), is best known as a transmembrance receptor for increases canonical Wnt signaling amplitude. In addition, in some types of human cancers, LGR5 has been found to be overexpressed. However, the distribution and function of LGR5 in spinal cord injury (SCI) are still unknown.

Eplerenone inhibits atrial fibrosis in mutant TGF-β1 transgenic mice.

The purpose of the present study was to study the impacts of eplerenone (EPL), an antagonist of mineralocorticoid receptors (MR), on atrial fibrosis in a mouse model with selective fibrosis in the atrium, and to explore the possible mechanisms. Using mutant TGF-β1 transgenic (Tx) mice, we first demonstrated that EPL inhibited atrial fibrosis specifically and decreased macrophage accumulation in the atria of these mice. Results from immunohistochemistry and western blotting showed that EPL attenuated protein expression of fibrosis-related molecules such as connective tissue growth factor (CTGF) and fibronectin in the atria of Tx mice.

The Expression of VHL (Von Hippel-Lindau) After Traumatic Spinal Cord Injury and Its Role in Neuronal Apoptosis.

The VHL (Von Hippel-Lindau) gene is a tumor suppressor gene, which is best known as an E3 ubiquitin ligase that negatively regulates the hypoxia inducible factor. The inactivation of VHL gene could result in the abnormal synthesis of VHL protein, which is in contact with the development and occurrence of renal clear cell carcinoma. However, the expression and possible function of VHL in central nervous system (CNS) is still unclear.

Breast cancer risk prediction using a polygenic risk score in the familial setting: a prospective study from the Breast Cancer Family Registry and kConFab.

Purpose: This study examined the utility of sets of single-nucleotide polymorphisms (SNPs) in familial but non-BRCA-associated breast cancer (BC).

Methods: We derived a polygenic risk score (PRS) based on 24 known BC risk SNPs for 4,365 women from the Breast Cancer Family Registry and Kathleen Cuningham Consortium Foundation for Research into Familial Breast Cancer familial BC cohorts. We compared scores for women based on cancer status at baseline; 2,599 women unaffected at enrollment were followed-up for an average of 7.

Point Mutations in Exon 1B of APC Reveal Gastric Adenocarcinoma and Proximal Polyposis of the Stomach as a Familial Adenomatous Polyposis Variant.

Gastric adenocarcinoma and proximal polyposis of the stomach (GAPPS) is an autosomal-dominant cancer-predisposition syndrome with a significant risk of gastric, but not colorectal, adenocarcinoma. We mapped the gene to 5q22 and found loss of the wild-type allele on 5q in fundic gland polyps from affected individuals. Whole-exome and -genome sequencing failed to find causal mutations but, through Sanger sequencing, we identified point mutations in APC promoter 1B that co-segregated with disease in all six families.

Non-covalent interaction between dietary stilbenoids and human serum albumin: Structure-affinity relationship, and its influence on the stability, free radical scavenging activity and cell uptake of stilbenoids.

Dietary stilbenoids are associated with many benefits for human health, which depend on their bioavailability and bioaccessibility. The stilbenoid-human serum albumin (HSA) interactions are investigated to explore the structure-affinity relationship and influence on the stability, free radical scavenging activity and cell uptake of stilbenoids. The structure-affinity relationship of the stilbenoids-HSA interaction was found as: (1) the methoxylation enhanced the affinity, (2) an additional hydroxyl group increases the affinity and (3) the glycosylation significantly weakened the affinity.

Germline polymorphisms in an enhancer of PSIP1 are associated with progression-free survival in epithelial ovarian cancer.

Women with epithelial ovarian cancer (EOC) are usually treated with platinum/taxane therapy after cytoreductive surgery but there is considerable inter-individual variation in response. To identify germline single-nucleotide polymorphisms (SNPs) that contribute to variations in individual responses to chemotherapy, we carried out a multi-phase genome-wide association study (GWAS) in 1,244 women diagnosed with serous EOC who were treated with the same first-line chemotherapy, carboplatin and paclitaxel. We identified two SNPs (rs7874043 and rs72700653) in TTC39B (best P=7x10-5, HR=1.