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Huang B.,Shandong University | Li C.,Shandong University | Chen W.,Shandong University | Liu T.,Shandong University | And 9 more authors.
European Journal of Medicinal Chemistry | Year: 2015

In our arduous efforts to develop new potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs), novel piperidine-linked [1,2,4]triazolo[1,5-a]pyrimidine derivatives were designed, synthesized and evaluated for their antiviral activities in MT-4 cell cultures. Biological results showed that all of the title compounds displayed moderate to excellent activities against wild-type (wt) HIV-1 strain (IIIB) with EC50 values ranging from 8.1 nM to 2284 nM in a cell-based assay. Among them, the most promising analog 7d possessed an EC50 value of 8.1 nM against wt HIV-1, which was much more potent than the reference drugs DDI, 3 TC, NVP and DLV. Additionally, 7d demonstrated weak activity against the double mutant HIV-1 strain (K103N + Y181C), and was more efficient than NVP in a RT inhibition assay. Besides, some measured and calculated physicochemical properties of 7d, like log P and water solubility, as well as the structure-activity relationships (SARs) analysis have been discussed in detail. Furthermore, the binding mode of the active compound 7d was rationalized by molecular simulation studies. © 2015 Elsevier Masson SAS. Source

Shi L.,Shandong University | Shi L.,Peking University | Zhang D.,Shandong Institute for Food and Drug Control | Lin R.,Peking University | And 3 more authors.
Tetrahedron Letters | Year: 2014

A novel and efficient transition metal-free C-H bond halogenation of indole derivatives has been developed. 3-Halogenated (3-Br, 3-I) indoles are highly regioselectively produced by this protocol. Simple and readily available halide salts (TBAB, KI) are employed as the halogen source. The transition metal-free and the mild conditions make this protocol very easy to handle and practical. © 2014 Elsevier Ltd. All rights reserved. Source

Sun P.,Shandong University of Traditional Chinese Medicine | Wei S.,Shandong University of Traditional Chinese Medicine | Wei X.,Shandong Institute for Food and Drug Control | Wang J.,Shandong University of Traditional Chinese Medicine | And 3 more authors.
Neural Plasticity | Year: 2016

Objective. We discuss the influence of anger emotional stress upon VEGF/VEGFR2 and its induced PI3K/AKT/mTOR signal pathway. Methods. We created a rat model of induced anger (anger-out and anger-in) emotional response using social isolation and resident-intruder paradigms and assessed changes in hippocampus' VEGF content, neuroplasticity, and the PI3K/AKT/mTOR signaling pathway. Results. The resident-intruder method successfully generated anger-out and anger-in models that differed significantly in composite aggression score, aggression incubation, open field behavior, sucrose preference, and weight gain. Anger emotional stress decreased synaptic connections and VEGFR2 expression. Anger emotional stress led to abnormal expression of VEGF/VEGFR2 mRNA and protein and disorderly expression of key factors in the PI3K/AKT/mTOR signal pathway. Fluoxetine administration ameliorated behavioral abnormalities and damage to hippocampal neurons caused by anger emotional stress, as well as abnormal expression of some proteins in VEGF/VEGFR2 and its induced PI3K/AKT/mTOR signal pathway. Conclusion. This research provides a detailed classification of anger emotion and verifies its influence upon VEGF and the VEGF-induced signaling pathway, thus providing circumstantial evidence of mechanisms by which anger emotion damages neurogenesis. As VEGFR2 can promote neurogenesis and vasculogenesis in the hippocampus and frontal lobe, these results suggest that anger emotional stress can result in decreased neurogenesis. Copyright © 2016 Peng Sun et al. Source

Chen L.Q.,Nanjing Southeast University | Chen L.Q.,Tianjin Medical University | Wang Y.,Nanjing Southeast University | Qu J.S.,Shandong Institute for Food and Drug Control | And 2 more authors.
Instrumentation Science and Technology | Year: 2015

A convenient and green pre-processing method is presented for determining physiological targets and drugs in biological samples using nanofiber-packed solid-phase extraction instead of a traditional cartridge. Biological samples, including plasma (model target molecule is desloratadine), urine (catecholamines), and saliva (cortisol) were used to characterize sample pre-treatment. Nanofiber-based solid-phase extraction sufficiently isolated the compounds from the complex matrixes. The absolute extraction rates were between 52.3% and 85.7 %. Because the nanofiber-packed solid-phase extraction cartridge is a small, lightweight, portable, convenient, and labor-saving device, this pre-processing method has great potential for further application. Copyright © Taylor & Francis Group, LLC. Source

Miao T.,Shandong University | Li Y.,Shandong University | Zhang D.,Shandong Institute for Food and Drug Control
Journal of Nanoscience and Nanotechnology | Year: 2016

We report the successful synthesis of ultralong polyaniline nanorods (UL-PANI-NRs) via using watersoluble magnetic Fe3O4 nanoparticles as soft templates under the assistance of external magnetic field. It was found that the concentration of Fe3O4 nanoparticles, the aniline concentration and the use of an external magnetic field significantly affect the morphology of the PANI products. The following characterizations including transmission electron microscopy (TEM), Fourier-Transform Infrared Spectroscopy (FTIR), X-ray diffraction (XRD) and thermogravimetric analysis (TGA) were conducted to investigate the electronic structure and composition of as-prepared UL-PANI-NRs. Our preliminary result indicates that complicated polymer structures (such as ultralong rods with vertical branches) may be prepared by water-soluble magnetic Fe3O4 nanoparticles as soft templates under the assistance of alternatively external magnetic fields. Copyright © 2016 American Scientific Publishers All rights reserved. Source

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