3 research outputs found
Fikri Mülkiyet Hukuku 1-2 Ders slaytları
Additional file 1: File S1. Studied structures in the SAR map.zip
Presentation_1_Spinacetin Suppresses the Mast Cell Activation and Passive Cutaneous Anaphylaxis in Mouse Model.PDF
<p>We previously reported the anti-inflammatory and anti-asthmatic activities of the extract of the Inula japonica Thunb. Aiming for discovery of a novel anti-inflammatory compound, we isolated spinacetin from the extract and investigated its in vitro and in vivo anti-inflammatory effect and the related mechanism. Effect of spinacetin on the Syk signaling pathway was studied in bone marrow-derived mast cells (BMMCs), and that on the nuclear factor-κB (NF-κB) and mitogen-activated protein kinases (MAPKs) was investigated in Rat basophilic leukemia (RBL)-2H3 cells and human mast cell line (HMC-1). The in vivo anti-inflammatory activity was assessed with passive cutaneous anaphylaxis (PCA) reaction assay. Spinacetin significantly inhibited the release of histamine, and production of inflammatory mediators such as leukotriene C<sub>4</sub> (LTC<sub>4</sub>) and interlukin-6 (IL-6) in IgE/Ag stimulated BMMCs. Analysis of the signaling pathways demonstrated that spinacetin inhibited activation of Syk, linker of activated T cells (LAT), phospholipase Cγ (PLCγ), cytosolic phospholipase A<sub>2</sub> (cPLA<sub>2</sub>), MAPKs, Akt/NF-κB, and intracellular Ca<sup>2+</sup> mobilization but with no effect on Fyn and Lyn. On the other hand, spinacetin suppressed IgE/Ag-induced activation of RBL-2H3 cells with inhibition against phosphorylation of extracellular signal regulated-protein kinase (ERK), c-Jun-NH<sub>2</sub>-terminal kinase (JNK), p38 MAPKs, PLCγ, translocation of cPLA<sub>2</sub>, and Akt/IκBα/NF-κB signal. However, spinacetin had no effect on PMA and A23187-induced activation of HMC-1. Furthermore, oral administration of spinacetin dose-dependently attenuated IgE/Ag-mediated PCA reaction in mouse model. Taken together, spinacetin showed the activities in preventing inflammatory processes, which might be at least partially attributed to the abolishment of Syk-dependent activation of IgE/Ag-mediated mast cells.</p
Structurally Diverse Cytotoxic Dimeric Chalcones from <i>Oxytropis chiliophylla</i>
Ten isomeric cyclobutane- and cyclohexene-containing
chalcone dimers,
oxyfadichalcones A–G, were isolated from the aerial parts of <i>Oxytropis chiliophylla</i>. These included six new compounds
and three pairs of enantiomers that are being reported from natural
sources for the first time. The relative configurations were elucidated
by spectroscopic data analysis, while the absolute configurations
were determined by comparing the experimental and calculated electronic
circular dichroism spectra. Quantitative LC-MS analysis of the main
dimers from different parts of the plant revealed their characteristic
accumulation in the viscous secretion and provided supporting evidence
for the hypothesized photochemical biosynthesis. In addition, the
cytotoxic activities of all isolates against the PC-3 human prostate
cancer cell line are reported