Gold Nanoparticles Downregulate IL-6 Expression/Production by Upregulating microRNA-26a-5p and Deactivating the RelA and NF-κBp50 Transcription Pathways in Activated Breast Cancer Cells.

MicroRNAs (miRNAs) are involved in the modulation of pathogenic genes by binding to their mRNA sequences' 3' untranslated regions (3'UTR). Interleukin-6 (IL-6) is known to promote cancer progression and treatment resistance. In this study, we aimed to explore the therapeutic effects of gold nanoparticles (GNP) against IL-6 overexpression and the modulation of miRNA-26a-5p in breast cancer (BC) cells. GNP were synthesized using the trisodium citrate method and characterized through UV-Vis spectroscopy, dynamic light scattering (DLS), and transmission electron microscopy (TEM). To predict the binding of miR-26a-5p in the IL-6 mRNA's 3'UTR, we utilized bioinformatics algorithms. Luciferase reporter clone assays and anti-miRNA-26a-5p transfection were employed to validate the binding of miR26a-5p in the IL-6 mRNA's 3'UTR. The activity of RelA and NF-κBp50 was assessed and confirmed using Bay 11-7082. The synthesized GNP were spherical with a mean size of 28.3 nm, exhibiting high stability, and were suitable for BC cell treatment. We found that miR-26a-5p directly regulated IL-6 overexpression in MCF-7 cells activated with PMA. Treatment of MCF-7 cells with GNP resulted in the inhibition of IL-6 overexpression and secretion through the increase of miR26a-5p. Furthermore, GNP deactivated NF-κBp65/NF-κBp50 transcription activity. The newly engineered GNP demonstrated safety and showed promise as a therapeutic approach for reducing IL-6 overexpression. The GNP suppressed IL-6 overexpression and secretion by deactivating NF-κBp65/NF-κBp50 transcription activity and upregulating miR-26a-5p expression in activated BC cells. These findings suggest that GNP have potential as a therapeutic intervention for BC by targeting IL-6 expression and associated pathways.

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review.

Chalcone derivatives are considered valuable species because they possess a ketoethylenic moiety, CO-CH=CH-. Due to the presence of a reactive α,ß-unsaturated carbonyl group, chalcones and their derivatives possess a wide spectrum of antiproliferative, antifungal, antibacterial, antiviral, antileishmanial, and antimalarial pharmacological properties. Recent developments in heterocyclic chemistry have led to the synthesis of chalcone derivatives, which had been biologically investigated toward certain disease targets. The major aspect of this review is to present the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010-2021). Based on a review of the literature, many chalcone-heterocycle hybrids appear to exhibit promise as future drug candidates owing to their similar or superior activities compared to those of the standards. Thus, this review may prove to be beneficial for the development and design of new potent therapeutic drugs based on previously developed strategies.

An unexpected single crystal structure of nickel(II) complex: Spectral, DFT, NLO, magnetic and molecular docking studies.

This work explores the study of a synthesized nickel complex as a possible inhibitor against the main protease (Mpro) of the recent emerging coronavirus disease (COVID-19). Overall, the template reaction of 3-acetyl-2-hydroxy-6-methyl-4H-pyran-4-one with nickel(II) chloride hexahydrate in N,N-dimethylformamide (DMF) medium leads to the formation of neutral nickel complex. This resulting complex is formulated as [Ni(DHA)2(DMF)2] on the basis of FT-IR, UV-Vis., single-crystal X-ray diffraction analysis, magnetic susceptibility and CV measurements as well as DFT quantum chemical calculations. Its single crystal suggests was found to be surrounded by the both pairs of molecules of DHA and DMF through six oxygen atoms with octahedral coordination sphere. The obtained magnetic susceptibilities are positive and agree with its paramagnetic state. In addition to the experimental investigations, optimized geometry, spectroscopic and electronic properties were also performed using DFT calculation with B3LYP/6-31G(d,p) level of theory. The nonlinear optical (NLO) properties of this complex are again examined. Some suitable quantum descriptors (EHOMO, ELUMO, Energy gap, Global hardness), Milliken atomic charge, Electrophilic potion and Molecular Electrostatic Potential) have been elegantly described. Molecular docking results demonstrated that the docked nickel complex displayed remarkable binding energy with Mpro. Besides, important molecular properties and ADME pharmacokinetic profiles of possible Mpro inhibitors were assessed by in silico prediction.

Synthesis and characterization of nickel-doped ceria nanoparticles with improved surface reducibility.

Nickel-doped ceria nanoparticles (Ni0.1Ce0.9O2-x NPs) were fabricated from Schiff-base complexes and characterized by various microscopic and spectroscopic methods. Clear evidence is provided for incorporation of nickel ions in the ceria lattice in the form of Ni3+ species which is considered as the hole trapped state of Ni2+. The Ni0.1Ce0.9O2-x NPs exhibit enhanced reducibility in H2 as compared to conventional ceria-supported Ni particles, while in O2 the dopant nickel cations are oxidized at higher valence than the supported ones.

Crystal structure of bis-(2-{[(3-bromo-prop-yl)imino]-meth-yl}phenolato-κ(2) N,O)copper(II).

In the title compound, [Cu(C10H11BrNO)2], the asymmetric unit consists of one-half of the mol-ecule, the other half being generated by an inversion centre. Hence the Cu(II) cation is symmetrically coordinated by two bidentate Schiff base anions in a slightly distorted square-planar environment with Cu-O and Cu-N bond lengths of 1.8786 (19) and 2.009 (2) Å, respectively. In the crystal, individual mol-ecules are packed in alternating zigzag layers parallel to (001). Weak C-H⋯π inter-actions exist between the mol-ecules.

Bis[µ-(3-acetyl-2-hy-droxy-6-methyl-4H-pyran-4-one-κ(3)O:O',O'')]diaqua-tetra-kis-(pyridine-κN)dicopper(II) diperchlorate.

In the centrosymmetric binuclear cation of the title compound, [Cu(C(8)H(7)O(4))(H(2)O)(C(5)H(5)N)(2)](2)(ClO(4))(2), the Cu(II) atoms are bridged by a pair of two dehydro-acetate anions in a bis-/monodentate mode. The distorted octa-hedral N(2)O(4) coordination sphere of the metal cation is completed by two pyridine N atoms and one O atom of a water mol-ecule. The complex cations and the perchlorate counter anions are arranged in layers parallel to (100). O-H⋯O hydrogen bonds between the coordinating water mol-ecules and the perchlorate anions constitute ribbons parallel to [10-1]. C-H⋯O hydrogen bonds are also observed.

catena-Poly[[[(pyridine-κN)copper(II)]-µ-3-{1-[(2-amino-eth-yl)imino]-eth-yl}-6-methyl-2-oxo-2H-pyran-4-olato-κN,N,O:O] perchlorate].

In the title compound, {[Cu(C(10)H(13)N(2)O(3))(C(5)H(5)N)]ClO(4)}(n), the Cu(II) atom has an N(3)O(2) coordination sphere. The complex contains two different ligands, viz. a pyridine mol-ecule and a Schiff base mol-ecule, resulting from the condensation of ethyl-enodiamine with dehydro-acetic acid. The Cu(II) atom exhibits a square-pyramidal geometry: three of the four donors of the pyramid base belong to the Schiff base ligand (an N atom from the amine group, a second N atom from the imine group and the O atom of the pyran-one residue) and the fourth donor is the pyridine N atom. The coordination around the metal ion is completed by a longer axial bond to the pyran-one O atom of an adjacent Schiff base, so forming a one-dimensional polymer. The complex has a +1 charge that is compensated by a perchlorate ion. The crystal packing, which can be described as alternating chains of cations and tetra-hedral perchlorate anions along the a axis, is stabilized by inter-molecular N-H⋯O, C-H⋯O and C-H⋯N hydrogen-bonding interactions.