Experimental Investigation on Shear Behavior of the Interface between Early-Strength Self-Compacting Shrinkage-Compensating High-Performance Concrete and Ordinary Concrete Substrate.

To improve interface bonding stress, early-strength self-compacting shrinkage-compensating high-performance concrete (ESS-HPC) was selected as an excellent strengthening material to investigate by direct shear test. Tests on seventeen Z-type specimens were carried out considering the ESS-HPC and ordinary concrete substrate (OCS) compressive strength grade, the ESS-HPC curing age, the OCS surface roughness, and the ratio of steel shear dowels as the variables. A bond stress-slip model of the interface was proposed via statistical fitting.

SPA: a peptide antagonist that acts as a cell-penetrating peptide for drug delivery.

Although cell-penetrating peptides (CPPs) has been proven to be efficient transporter for drug delivery, ideal peptide vectors for tumor therapy are still being urgently sought. Peptide antagonists have attracted substantial attention as targeting molecules because of their high tumor accumulation and antitumor activity compared with agonists. SPA, a derivative of substance P, is a potent antagonist that exhibits antitumor activity.

Establishment of a fluorescent PCR melting curve method for detecting asthma susceptibility using gene SNP typing.

To develop a detection method for single nucleotide polymorphisms (SNPs) of bronchial asthma (BA) susceptibility genes (, and ) based on fluorescence PCR melting curves. Peripheral blood samples from 33 patients with BA were collected. DNA was extracted, and positive plasmids were constructed.

Evaluation of Serum α-Fetoprotein Levels During Different Infection Phases of CHB Patients.

Background: Chronic hepatitis B patients carry a high risk of developing hepatocellular carcinoma (HCC). α-Fetoprotein (AFP) is one of the most commonly used and reliable biomarkers for HCC. However, the AFP level during different phases of CHB is not well understood.

Application of a C-C Bond-Forming Conjugate Addition Reaction in Asymmetric Dearomatization of β-Naphthols.

A C-C bond-forming conjugate reaction was successfully applied to the enantioselective dearomatization of β-naphthols. A C(sp2)-C(sp3) bond is formed by using propargylic ketones as reactive partners. Good to excellent Z/E ratios and ee values were obtained by employing an in situ generated magnesium catalyst.

Anti-cancer small molecule JP-8g exhibits potent in vivo anti-inflammatory activity.

Spirooxindoles are a class of compounds with diverse biological activity. Previously, we identified a series of spirooxindole-pyranopyrimidine compounds that exhibited broad-spectrum anti-cancer activity. In this study, we evaluated one of these compounds, JP-8g, on mouse models and found that it showed potent in vivo anti-inflammatory activity.

Design of an acid-activated antimicrobial peptide for tumor therapy.

Antimicrobial peptides have received increasing attention as potential antitumor drugs due to their new mode of action. However, the systemic toxicity at high concentration always hampers their successful utilization for tumor therapy. Here, we designed a new type of acid-activated antimicrobial peptide AMitP by conjugating antimicrobial peptide MitP to its anionic binding partner MitPE via a disulfide linker.

Enantioselective 1,3-dipolar cycloaddition of methyleneindolinones and N,N'-cyclic azomethine imines.

A new chiral bis-phosphoric acid 3l bearing triple axial chirality was synthesized and applied to effect a highly enantioselective 1,3-dipolar cycloaddition reaction between N,N'-azomethine imines and methyleneindolinones for the creation of chiral spiro[pyrazolidin-3,30-oxindoles] in excellent yields and selectivities. MS experiment and DFT calculation studies prompted us to propose a dual H-bond donor activation mode of bis-phosphoric acid which is different from the traditional phosphoric acid catalysis.

Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists.

Recently we reported the synthesis and structure-activity study of endomorphin-1 (EM-1) analogues containing novel, unnatural α-methylene-β-aminopropanoic acids (Map). In the present study, we describe new EM-1 analogues containing Dmt(1), (R/S)-βPro(2), and (ph)Map(4)/(2-furyl)Map(4). All of the analogues showed a high affinity for the μ-opioid receptor (MOR) and increased stability in mouse brain homogenates.

Membrane active antimicrobial activity and molecular dynamics study of a novel cationic antimicrobial peptide polybia-MPI, from the venom of Polybia paulista.

As the frequent emergence of the resistant bacteria, the development of new agents with a new action mode attracts a great deal of interest. It is now widely accepted that antimicrobial peptides (AMPs) are promising alternatives to conventional antibiotics. In this study, antimicrobial peptide polybia-MPI and its analogs were synthesized and their antibacterial activity was studied.

Asymmetric inverse-electron-demand hetero-Diels-Alder reaction for the construction of bicyclic skeletons with multiple stereocenters by using a bifunctional organocatalytic strategy: an efficient approach to chiral macrolides.

We have performed the first bifunctional organocatalytic highly enantioselective inverse-electron-demand hetero-Diels-Alder reaction of cyclic ketones with enones to afford densely functionalized bicyclic skeletons that contain three stereocenters (up 82% yield, 10:1 d.r., and 97% ee).

A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map).

A new class of endomorphin-1 (EM-1) analogues were synthesized by introduction of novel unnatural α-methylene-β-amino acids (Map) at position 3 or/and position 4. Their binding and functional activity, metabolic stability, and antinociceptive activity were determined and compared. Most of these analogues showed high affinities for the μ-opioid receptor and an increased stability in mouse brain homogenates compared with EM-1.

A new chiral 2-(ethylthio)-thiazolone analogue shows strong antitumor activities by inducing cancer cell apoptosis and inhibiting angiogenesis.

Our initial study showed the potent cytotoxic effects of a series of new chiral 2-(ethylthio)-thiazolone analogues we synthesized. In the present study, we used computer prediction and found that nitro functionality and the modification of substituents R could further improve their activities in the presence of the nitro group. Compound 1s with nitro, naphthyl, ethyl groups, and a chiral center was predicted to be the most effective.

The dimerization interface of the glycoprotein Ibβ transmembrane domain corresponds to polar residues within a leucine zipper motif.

Experiments with the transmembrane (TM) domains of the glycoprotein (GP) Ib-IX complex have indicated that the associations between the TM domains of these subunits play an important role in the proper assembly of the complex. As a first step toward understanding these associations, we previously found that the Ibβ TM domain dimerized strongly in Escherichia coli cell membranes and led to Ibβ TM-CYTO (cytoplasmic domain) dimerization in the SDS-PAGE assay, while neither Ibα nor IX TM-CYTO was able to dimerize. In this study, we used the TOXCAT assay to probe the Ibβ TM domain dimerization interface by Ala- and Leu-scanning mutagenesis.

Cellular uptake of transportan 10 and its analogs in live cells: Selectivity and structure-activity relationship studies.

Transportan 10 (TP10) is an amphipathic cell-penetrating peptide with high translocation ability. In order to obtain more details of structure-activity relationship of TP10, we evaluated the effects of structure and charge on its translocation ability. Our results demonstrated that disrupting the helical structure or Arg substitution could remarkably decrease the cellular uptake of TP10.

Novel cytotoxity exhibition mode of polybia-CP, a novel antimicrobial peptide from the venom of the social wasp Polybia paulista.

Antimicrobial peptide polybia-CP was purified from the venom of the social wasp Polybia paulista. It has an amphipathic sequence ILGTILGLLKSL-NH(2) and possesses potent antimicrobial activity against both Gram-positive and Gram-negative bacteria. In this study we synthesized polybia-CP, studied its cytotoxity on tumor cells and proposed its possible mechanism.

Primary hyperparathyroidism presenting as intractable nausea and vomiting.

Primary hyperparathyroidism (PHPT) is characterized by inappropriate secretion of parathyroid hormone (PTH). The proportion of PHPT with asymptomatic or nontypical symptoms is continuously increasing. PHPT typically affects elderly women, and it is characterized by few symptoms or complications.

Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.

The molecular docking of a series of endomorphin analog with the mu opioid receptor was performed. The successive molecular dynamics of several proposed ligand-receptor complexes inserted into the phospholipid bilayer were carried out to optimize the complex and explore the conformational changes. Meaningful differences of their binding modes were detected and the involvement of some essential residues in ligand binding was also identified.

Computational study of the heterodimerization between mu and delta receptors.

A growing body of evidence indicated that the G protein coupled receptors exist as homo- or hetero-dimers in the living cell. The heterodimerization between mu and delta opioid receptors has attracted researchers' particular interests, it is reported to display novel pharmacological and signalling regulation properties. In this study, we construct the full-length 3D-model of mu and delta opioid receptors using the homology modelling method.

Gene expression and function study of fusion immunotoxin anti-Her-2-scFv-SEC2 in Escherichia coli.

The whole sec2 DNA fragment was obtained by polymerase chain reaction with total genomic DNA extracted from Staphylococcus aureus. The newly discovered gene contains 717 bp (GenBank Accession number AY450554) and encodes 239 amino acids in accordance with the protein sequence reported in GenBank. The sec2 gene was fused to anti-Her-2 scFv gene with a DNA linker at the upstream to construct the fusion gene of immunotoxin which was subcloned to expression vector pET-32a(+) and expressed efficiently in Escherichia coli.

Exercise interventions: defusing the world's osteoporosis time bomb.

Osteoporosis is a major public health problem, affecting millions of people worldwide. The associated health care costs are growing in parallel with increases in elderly populations, and it is expected that the number of osteoporotic fractures will double over the next 50 years. The best way to address osteoporosis is prevention.