One-pot synthesis of water-soluble, β-cyclodextrin-based polyrotaxanes in a homogeneous water system and its use in bio-applications.

A small, nano-sized, water-soluble polyrotaxane (PR) was synthesized using a highly efficient one-pot synthesis strategy in a homogeneous water system, formed from β-cyclodextrin-(COOH), poly(propylene glycol)bis(2-aminopropyl ether) (PPG, 2 kDa) and a mono-(6-azido-6-desoxy)-β-cyclodextrin stopper via room temperature click chemistry. β-cyclodextrin-(COOH) and PR were characterized by one- and two-dimensional NMR as well as by high resolution transmission electron microscopy (HR-TEM). The number of carboxyl groups in one PR was determined by H NMR.

Disturbance of redox status enhances radiosensitivity of hepatocellular carcinoma.

Aims: High constitutive expression of Nrf2 has been found in many types of cancers, and this high level of Nrf2 also favors resistance to drugs and radiation. Here we investigate how isoliquiritigenin (ISL), a natural antioxidant, inhibits the Nrf2-dependent antioxidant pathway and enhances the radiosensitivity of HepG2 cells and HepG2 xenografts.

Results: Treatment of HepG2 cells with ISL for 6 h selectively enhanced transcription and expression of Keap1.

A chemometric-assisted method for the simultaneous determination of malachite green and crystal violet in water based on absorbance-pH data generated by a homemade pH gradient apparatus.

An attractive method of generating second-order data was developed by a dropping technique to generate pH gradient simultaneously coupled with diode-array spectrophotometer scanning. A homemade apparatus designed for the pH gradient. The method and the homemade apparatus were used to simultaneously determine malachite green (MG) and crystal violet (CV) in water samples.

Homocysteine Triggers Inflammatory Responses in Macrophages through Inhibiting CSE-H2S Signaling via DNA Hypermethylation of CSE Promoter.

Hyperhomocysteinemia (HHcy) is an independent risk factor of atherosclerosis and other cardiovascular diseases. Unfortunately, Hcy-lowering strategies were found to have limited effects in reducing cardiovascular events. The underlying mechanisms remain unclear.

[Study on mineral elements distribution in soil of Angelica sinensis producing regions and its relationship with altitude and soil types].

Objective: To investigate the distribution characteristics of mineral elements in the soil of Angelica sinensis producing regions and its relationship with altitude and soil types.

Methods: The contents of 15 mineral elements in 103 batches of soil from 13 counties were determined by ICP-MS or AAS. Pearson correlation analysis, partial correlation analysis and systematical cluster analysis were used to analyze the data.

The Prevalence and Incidence of Latent Tuberculosis Infection and Its Associated Factors among Village Doctors in China.

Background: China is a high tuberculosis (TB) burden country. More than half of acute TB cases first seek medical care in village doctors' clinics or community health centers. Despite being responsible for patient referral and management, village doctors are not systematically evaluated for TB infection or disease.

Analytic known-plaintext attack on a phase-shifting interferometry-based cryptosystem.

We demonstrate a new analytic approach to a known-plaintext attack (KPA) on an optical cryptosystem based on the phase-shifting interferometry (PSI) technique. With the proposed analytic attack method, an opponent can access the exact decryption keys and obtain perfect attack results. This demonstration, to the best of our knowledge, shows for the first time that the optical cryptosystem based on the PSI technique is vulnerable to KPA.

Synthesis and evaluation of selegiline derivatives as monoamine oxidase inhibitor, antioxidant and metal chelator against Alzheimer's disease.

A series of compounds with monoamine oxidase inhibition and biometal chelation activities were designed, synthesised and evaluated as agents against Alzheimer's disease. The in vitro assay shows that most target compounds exhibit good MAO-B activities with submicromolar IC50 values and antioxidant activity (1.49-5.

[Application of entropy-weight TOPSIS model in synthetical quality evaluation of Angelica sinensis growing in Gansu Province].

Objective: To investigate the establishment and application methods of entropy-weight TOPSIS model in synthetical quality evaluation of traditional Chinese medicine with Angelica sinensis growing in Gansu Province as an example.

Methods: The contents of ferulic acid, 3-butylphthalide, Z-butylidenephthalide, Z-ligustilide, linolic acid, volatile oil, and ethanol soluble extractive were used as an evaluation index set. The weights of each evaluation index were determined by information entropy method.

Biocatalytic synthesis of C3 chiral building blocks by chloroperoxidase-catalyzed enantioselective halo-hydroxylation and epoxidation in the presence of ionic liquids.

The optically active C3 synthetic blocks are remarkably versatile intermediates for the synthesis of numerous pharmaceuticals and agrochemicals. This work provides a simple and efficient enzymatic synthetic route for the environment-friendly synthesis of C3 chiral building blocks. Chloroperoxidase (CPO)-catalyzed enantioselective halo-hydroxylation and epoxidation of chloropropene and allyl alcohol was employed to prepare C3 chiral building blocks in this work, including (R)-2,3-dichloro-1-propanol (DCP*), (R)-2,3-epoxy-1-propanol (GLD*), and (R)-3-chloro-1-2-propanediol (CPD*).

β2-Glycoprotein I-Dependent Anti-Cardiolipin Antibodies Associated With Periodontitis in Patients With Systemic Lupus Erythematosus.

Background: It was reported that patients with systemic lupus erythematosus (SLE) exhibited increased levels of anticardiolipin (anti-CL) antibodies, a class of antiphospholipid antibodies associated with thrombosis. β2-glycoprotein I (β2GPI) has been considered as the actual target antigen for anti-CL antibodies. This study investigates the association of periodontal infection with anti-CL antibodies in patients with SLE.

Design, synthesis, and biological evaluation of benzoselenazole-stilbene hybrids as multi-target-directed anti-cancer agents.

To identify novel multi-target-directed drug candidates for the treatment of cancer, a series of benzoselenazole-stilbene hybrids were synthesised by combining the pharmacophores of resveratrol and ebselen. The biological assay indicated that all of the hybrids exhibited antiproliferative activities against four human cancer cell lines and demonstrated good TrxR inhibitory activities. The mechanism of cell apoptosis was investigated in G2/M cell cycle arrest induced by compound 6e and the apoptosis of the human liver carcinoma Bel-7402 cell line.

The modulation of nicotinic acetylcholine receptors on the neuronal network oscillations in rat hippocampal CA3 area.

γ oscillations are associated with higher brain functions such as memory, perception and consciousness. Disruption of γ oscillations occur in various neuro-psychological disorders such as schizophrenia. Nicotinic acetylcholine receptors (nAChR) are highly expressed in the hippocampus, however, little is known about the role on hippocampal persistent γ oscillation.

Dual functional cholinesterase and MAO inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of homoisoflavonoid derivatives.

Because of the complexity of Alzheimer's disease (AD), the multi-target-directed ligand (MTDL) strategy is expected to provide superior effects for the treatment of AD, instead of the classic one-drug-one-target strategy. In this context, we focused on the design, synthesis and evaluation of homoisoflavonoid derivatives as dual acetyl cholinesterase (AChE) and monoamine oxidase (MAO-B) inhibitors. Among all the synthesized compounds, compound 10 provided a desired balance of AChE and hMAO-B inhibition activities, with IC50 value of 3.

In silico design of human IMPDH inhibitors using pharmacophore mapping and molecular docking approaches.

Inosine 5'-monophosphate dehydrogenase (IMPDH) is one of the crucial enzymes in the de novo biosynthesis of guanosine nucleotides. It has served as an attractive target in immunosuppressive, anticancer, antiviral, and antiparasitic therapeutic strategies. In this study, pharmacophore mapping and molecular docking approaches were employed to discover novel Homo sapiens IMPDH (hIMPDH) inhibitors.

Induction of haemeoxygenase-1 improves FFA-induced endothelial dysfunction in rat aorta.

Background: The induction of haemeoxygenase-1 (HO-1) exerts beneficial effects in the setting of endothelial dysfunction in obesity. High free fatty acid (FFA) levels are a common feature of obesity and are the primary cause of endothelial dysfunction. The objective of our study was to explore the effects of HO-1 induction on FFA-induced endothelial dysfunction in rats.

Highly specific enrichment of N-glycoproteome through a nonreductive amination reaction using Fe3O4@SiO2-aniline nanoparticles.

A novel method based on the conjunction of aldehydes from oxidized glycopeptides to aniline groups on magnetic nanoparticles via nonreductive amination is reported for the highly selective enrichment of N-glycopeptides. For the first time, a nonreductive amination reaction has been introduced into N-glycoproteome extraction, and correspondingly a new type of aniline-functionalized nanoparticle has been designed and synthesized.

Construction of LRET-based nanoprobe using upconversion nanoparticles with confined emitters and bared surface as luminophore.

Upconversion nanoparticles (UCNPs) are promising energy donors for luminescence resonance energy transfer (LRET) and have widely been used to construct nanoprobes. To improve the LRET efficiency, which is currently a limiting factor for UCNPs-based bioassay, we herein propose a strategy to construct LRET-based nanoprobe using UCNPs with confined emitters and bared surface as the luminophore, with Ca(2+) as the proof-of-concept target. The sandwich-structure upconversion nanoparticles (SWUCNPs) are designed with a core-inner shell-outer shell architecture, in which the emitting ions (Ln(3+)) are precisely located in the inner shell near the particle surface, which is close enough to external energy acceptors.

Protective effects of drag-reducing polymers on ischemic reperfusion injury of isolated rat heart.

Drag-reducing polymers (DRPs) are blood-soluble macromolecules that can increase blood flow and reduce vascular resistance. The purpose of the present study was to observe the effect of DRPs on ischemic reperfusion (I/R) injury of isolated rat hearts. Experiments were performed on isolated rat hearts subjected to 30 min of ischemia followed by 90 min of reperfusion in Langendorff preparations.

[Epidemiological characteristics of human avian influenza A (H7N9) virus infection in China].

Objective: To investigate the epidemiological characteristics of human infections with avian influenza A (H7N9) in China and to provide scientific evidence for the adjustment of preventive strategy and control measures.

Methods: Demographic and epidemiologic information on human cases were collected from both reported data of field epidemiological investigation and the reporting system for infectious diseases.

Results: A total of 433 cases including 163 deaths were reported in mainland China before June 4, 2014.

Pyruvate carboxylase is critical for non-small-cell lung cancer proliferation.

Anabolic biosynthesis requires precursors supplied by the Krebs cycle, which in turn requires anaplerosis to replenish precursor intermediates. The major anaplerotic sources are pyruvate and glutamine, which require the activity of pyruvate carboxylase (PC) and glutaminase 1 (GLS1), respectively. Due to their rapid proliferation, cancer cells have increased anabolic and energy demands; however, different cancer cell types exhibit differential requirements for PC- and GLS-mediated pathways for anaplerosis and cell proliferation.

Decreased vascular endothelial growth factor expression is associated with cell apoptosis in low-dose aspirin-induced gastric mucosal injury.

Background: The use of low-dose aspirin (LDA) has emerged as an important cause of gastrointestinal ulcers. The aim of this study was to investigate the association between LDA-induced gastric mucosal injury and the expression of vascular endothelial growth factor (VEGF) and cell apoptosis in elderly Chinese patients.

Methods: A total of 136 patients aged 60 to 80 years with LDA-induced (100 mg/d for at least 1 month) gastric mucosal injury and 48 age-matched healthy subjects were enrolled in this study.

Radiosensitization to X-ray radiation by telomerase inhibitor MST-312 in human hepatoma HepG2 cells.

Aims: Previous studies in malignant cells have shown that irradiation-induced upregulation of telomerase activity, not only protected damaged telomeres, but also contributed to DNA damage repair by chromosomal healing and increased resistance to irradiation. The purpose of the present study was to investigate the radiosensitizing effect of telomerase inhibitor MST-312 and the corresponding mechanism in the human hepatoma cell line HepG2.

Main Methods: Cell proliferation, telomerase activity, cell cycle distribution, DNA damage and repair, expression of p53, mitochondrial membrane potential, and cell apoptosis were measured with the MTT assay, real-time fluorescent quantitative PCR, flow cytometry, immunofluorescence, western blots, JC-1 staining, and Hoechst 33258 staining, respectively.

Matrine inhibits the invasive properties of human glioma cells by regulating epithelial‑to‑mesenchymal transition.

Matrine is reported to be effective in tumor therapies; however, the anti‑metastatic effect and molecular mechanism(s) of matrine on glioma remain poorly understood. Therefore, the purpose of this study was to assess the effects of matrine on glioma and the associated mechanism(s). In the study, we demonstrated that matrine inhibited the proliferation of glioma cells.