Amidation-Modified Apelin-13 Regulates PPARγ and Perilipin to Inhibit Adipogenic Differentiation and Promote LipolysisRead the full article
Bioinorganic Chemistry and Applications publishes research in all aspects of bioinorganic chemistry, including bioorganometallic chemistry and applied bioinorganic chemistry, and applications in fields such as medicine and immunology.
Chief Editor, Professor Fanizzi, is based at the Università del Salento. His research interests and current projects are related to the study of transition metals (Platinum in particular), coordination organometallic and bioinorganic chemistry, and the applications of high field NMR Spectroscopy.
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Synthesis, Characterization, and In Vitro Cytotoxicity of Unsymmetrical Tetradentate Schiff Base Cu(II) and Fe(III) Complexes
Unsymmetrical tetradentate Schiff base Fe(III) and Cu(II) complexes were prepared by the coordination of some unsymmetrical tetradentate Schiff base ligands with CuCl2·2H2O or FeCl3·6H2O. The obtained complexes were characterized by ESI-MS, IR, and UV-Vis. The spectroscopic data with typical signals are in agreement with the suggested molecular formulae of the complexes. Their cyclic voltammetric studies in acetonitrile solutions showed that the Cu(II)/Cu(I) and Fe(III)/Fe(II) reduction processes are at (−)1.882–(−) 1.782 V and at (−) 1.317–(−) 1.164 V, respectively. The in vitro cytotoxicity of obtained complexes was screened for KB and Hep-G2 human cancer cell lines. The results showed that almost unsymmetrical tetradentate Schiff base complexes have good cytotoxicity. The synthetic complexes bearing the unsymmetrical tetradentate Schiff base ligands with different substituted groups in the salicyl ring indicate different cytotoxicity. The obtained Fe(III) complexes are more cytotoxic than Cu(II) complexes and relative unsymmetric Schiff base ligands.
Network Pharmacology Reveals Polyphyllin II as One Hit of Nano Chinese Medicine Monomers against Nasopharyngeal Carcinoma
Nasopharyngeal carcinoma (NPC) is a malignant tumor in southern China, and nano Traditional Chinese Medicine (TCM) represents great potential to cancer therapy. To predict the potential targets and mechanism of polyphyllin II against NPC and explore its possibility for the future nano-pharmaceutics of Chinese medicine monomers, network pharmacology was included in the present study. Totally, ninety-four common potential targets for NPC and polyphyllin II were discovered. Gene Ontology (GO) function enrichment analysis showed that biological processes and functions mainly concentrated on apoptotic process, protein phosphorylation, cytosol, protein binding, and ATP binding. In addition, the anti-NPC effects of polyphyllin II mainly involved in the pathways related to cancer, especially in the PI3K-Akt signaling indicated by the Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis. The “drug-target-disease” network diagram indicated that the key genes were SRC, MAPK1, MAPK14, and AKT1. Taken together, this study revealed the potential drug targets and underlying mechanisms of polyphyllin II against NPC through modern network pharmacology, which provided a certain theoretical basis for the future nano TCM research.
Nanoparticles for Oral Cancer Diagnosis and Therapy
Oral cancer is the sixth most common malignant cancer, affecting the health of people with an unacceptably high mortality rate. Despite numerous clinical methods in the diagnosis and therapy of oral cancer (e.g., magnetic resonance imaging, computed tomography, surgery, and chemoradiotherapy), they still remain far from optimal. Therefore, an urgent need exists for effective and practical techniques of early diagnosis and effective therapy of oral cancer. Currently, various types of nanoparticles have aroused wide public concern, representing a promising tool for diagnostic probes and therapeutic devices. Their inherent physicochemical features, including ultrasmall size, high reactivity, and tunable surface modification, enable them to overcome some of the limitations and achieve the expected diagnostic and therapeutic effect. In this review, we introduce different types of nanoparticles that emerged for the diagnosis and therapy of oral cancers. Then, the challenges and future perspectives for nanoparticles applied in oral cancer diagnosis and therapy are presented. The objective of this review is to help researchers better understand the effect of nanoparticles on oral cancer diagnosis and therapy and may accelerate breakthroughs in this field.
Protection of Iron-Induced Oxidative Damage in Neuroblastoma (SH-SY5Y) Cells by Combination of 1-(N-Acetyl-6-aminohexyl)-3-hydroxy-2-methylpyridin-4-one and Green Tea Extract
Iron is a crucial trace element and essential for many cellular processes; however, excessive iron accumulation can induce oxidative stress and cell damage. Neurodegenerative disorders, such as Alzheimer’s disease and Parkinson’s disease, have been associated with altered iron homoeostasis causing altered iron distribution and accumulation in brain tissue. This study aims to investigate the protective effect of 1-(N-acetyl-6-aminohexyl)-3-hydroxy-2-methylpyridin-4-one (CM1) in combination with green tea extract (GTE) on iron-induced oxidative stress in neuroblastoma (SH-SY5Y) cells. Cells were cultured in medium with or without ferric chloride loading. Their viability and mitochondrial activity were assessed using MTT and JC-1 staining methods. Levels of the cellular labile iron pool (LIP), reactive oxygen species (ROS), and lipid-peroxidation products were determined using calcein acetoxymethyl ester, 2′,7′-dichlorohydrofluorescein diacetate, and TBARS-based assays, respectively. The viability of iron-loaded cells was found to be significantly increased after treatment with CM1 (10 µM) for 24 h. CM1 co-treatment with GTE resulted in a greater protective effect than their monotherapy. Combination of CM1 and GTE also reduced mitochondrial disruption and LIP content and ROS and TBARS production. In conclusion, the combination of CM1 and GTE exhibits protection against iron-induced oxidative stress in neuroblastoma cells.
Identification of Differentially Expressed Genes and Elucidation of Pathophysiological Relevance of ABCA1 in HaCaT Cells Induced by PM2.5
Objective. In order to investigate the effects of PM2.5 on proliferation, cell cycle, apoptosis, and potential mechanism of human keratinocyte cell line HaCaT. Methods. HaCaT cells were treated with different concentrations of PM2.5 suspension for 24 hours. Cell viability was detected by the CCK-8 method. Cell cycle distribution and apoptosis were detected by flow cytometry. Microarray analyses were used to find out the microarray gene expression profiling; data processing included gene enrichment and pathway analysis. Western blot was conducted to validate the key pathways and regulators in the microarray analysis. Results. The cell activity decreased, and the cell cycle was significantly inhibited with the increase in PM2.5 concentration. Also, by conducting the gene expression microarray assay, we identified 541 upregulated genes and 935 downregulated genes in PM2.5-treated HaCaT cells. Real-time qPCR and western blot confirmed that PM2.5 treatment could induce the expression of ABCA1 while inhibiting that of END1 and CLDN1. Conclusion. Our results showed that PM2.5 could potentially regulate cell apoptosis and cell cycle arrest via ABCA1-, END1-, ID1-, and CLDN1-mediated pathways in human HaCaT cells, which laid a good foundation for follow-up drug intervention and drug development against skin damage caused by PM2.5 exposure.
Preparation and Thermogravimetric and Antimicrobial Investigation of Cd (II) and Sn (II) Adducts of Mercaptopyridine, Amino Triazole Derivatives, and Mercaptothiazoline Organic Ligand Moieties
The solid adducts of SnCl2.(3amt).H2O, SnCl2.2(3amt).H2O, CdCl2.(3amt), CdCl2.2(3amt), SnCl2.(2mct).0.5H2O, SnCl2.2(2mct), CdCl2.(2mct), CdCl2.2(2mct).H2O, SnCl2.(2mcp).1.5H2O, >2.2(2mcp).4H2O, CdCl2.(2mcp), CdCl2.2(2mcp), SnCl2.(4amt).4H2O, SnCl2.2(4amt).1.5H2O, CdCl2.(4amt).H2O, and CdCl2.2(4amt) (where the 3amt, 4amt, 2mct, and 2mcp represent 3-amino-1,2,4-triazole, 4-amino-1,2,4-triazole, 2-mercaptothiazoline, and 2-mercaptopyridine simple organic chelates, respectively) were prepared using a solid-state route and investigated by CHN elemental analysis and infrared spectroscopy. Additionally, we investigated the thermogravimetric characterization and antimicrobial proprieties. It is verified that for 3amt and 4amt adducts, the coordination occurs through nitrogen atom. For 2mct compounds, the coordination occurs through nitrogen (Sn) or sulfur (Cd). For 2mcp adducts, both coordination sites nitrogen and sulfur are involved. By examination of TG curves, it is confirmed that for each hydrated compounds, the first mass loss step is linked with the release of water molecules followed by the release of ligand molecules and sublimation of the metal chloride. Furthermore, it is verified that, considering only the release of ligand molecules (3amp, 4amp, 2mct, or 2mcp), the cadmium adducts are always more stable than the correspondent tin adducts probably due to the formation of cross-linking bonds in these compounds. Finally, of these 16 adducts, 14 showed antimicrobial activities against different bacterial and fungal strains.