Synthesis of DPIE [2-(1,2-Diphenyl-1H-indol-3-yl)ethanamine] Derivatives and Their Regulatory Effects on Pro-Inflammatory Cytokine Production in IL-1β-Stimulated Primary Human Oral Cells

Interleukin-1 beta (IL-1β) has diverse physiological functions and plays important roles in health and disease. In this report, we focus on its function in the production of pro-inflammatory cytokines, including IL-6 and IL-8, which are implicated in several autoimmune diseases and host defense against infection. IL-1β activity is markedly dependent on the binding affinity toward IL-1 receptors (IL-1Rs). Several studies have been conducted to identify suitable small molecules that can modulate the interactions between 1L-1β and 1L-1R1. Based on our previous report, where DPIE [2-(1,2-Diphenyl-1H-indol-3-yl)ethanamine] exhibited such modulatory activity, three types of DPIE derivatives were synthesized by introducing various substituents at the 1, 2, and 3 positions of the indole group in DPIE. To predict a possible binding pose in complex with IL-1R1, a docking simulation was performed. The effect of the chemicals was determined in human gingival fibroblasts (GFs) following IL-1β induction. The DPIE derivatives affected different aspects of cytokine production. Further, a group of the derivatives enabled synergistic pro-inflammatory cytokine production, while another group caused diminished cytokine production compared to DPIE stimulation. Some groups displayed no significant difference after stimulation. These findings indicate that the modification of the indole site could modulate IL-1β:IL1R1 binding affinity to reduce or enhance pro-inflammatory cytokine production

Preparation, Characterization, and Catalytic Properties of Pd-Graphene Quantum Dot Catalysts

In this study, Pd-graphene quantum dot (Pd-GQD) catalysts were prepared by depositing Pd nanoparticles onto functionalized GQD surfaces, and their morphology and elemental composition were characterized using transmission electron microscopy, X-ray photoelectron spectroscopy, and Raman spectroscopy. The as-prepared Pd-GQD was subsequently employed as a catalyst for the Heck and decarboxylative cross-coupling reactions and was found to exhibit higher catalytic activity than other reference systems. The expanded substrate scope of various substituted aryl iodides further proved that the GQD is an effective support for preparing new heterogeneous catalysts with improved catalytic performances

Preparation, Characterization, and Catalytic Properties of Pd-Graphene Quantum Dot Catalysts

In this study, Pd-graphene quantum dot (Pd-GQD) catalysts were prepared by depositing Pd nanoparticles onto functionalized GQD surfaces, and their morphology and elemental composition were characterized using transmission electron microscopy, X-ray photoelectron spectroscopy, and Raman spectroscopy. The as-prepared Pd-GQD was subsequently employed as a catalyst for the Heck and decarboxylative cross-coupling reactions and was found to exhibit higher catalytic activity than other reference systems. The expanded substrate scope of various substituted aryl iodides further proved that the GQD is an effective support for preparing new heterogeneous catalysts with improved catalytic performances

Synthesis of Terminal Allenes via a Copper-Catalyzed Decarboxylative Coupling Reaction of Alkynyl Carboxylic Acids

Synthesis of terminal allenes via a copper-catalyzed decarboxylative coupling reaction was developed. Aryl alkynyl carboxylic acid, paraformaldehyde, and dicyclohexylamine were reacted with CuI (20 mol %) in diglyme at 100 °C for 2 h to produce the terminal allene in moderate to good yields. The method showed good functional group tolerance

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Developmentally regulated GTP-binding protein 2 (DRG2) was first identified in the central nervous system of mice. However, the physiological function of DRG2 in the brain remains largely unknown. Here, we demonstrated that knocking out DRG2 impairs the function of dopamine neurons in mice. DRG2 was strongly expressed in the neurons of the dopaminergic system such as those in the striatum (Str), ventral tegmental area (VTA), and substantia nigra (SN), and on neuronal cell bodies in high-density regions such as the hippocampus (HIP), cerebellum, and cerebral cortex in the mouse brain. DRG2 knockout (KO) mice displayed defects in motor function in motor coordination and rotarod tests and increased anxiety. However, unexpectedly, DRG2 depletion did not affect the dopamine (DA) neuron population in the SN, Str, or VTA region or dopamine synthesis in the Str region. We further demonstrated that dopamine release was significantly diminished in the Str region of DRG2 KO mice and that treatment of DRG2 KO mice with l-3,4-dihydroxyphenylalanine (L-DOPA), a dopamine precursor, rescued the behavioral motor deficiency in DRG2 KO mice as observed with the rotarod test. This is the first report to identify DRG2 as a key regulator of dopamine release from dopamine neurons in the mouse brain. © 2019 by the authors. Licensee MDPI, Basel, Switzerland.1