Unexpected hydrazinolysis behaviour of 1-chloro-4-methyl-5H-pyridazino[4,5-b]indole and a convenient synthesis of new [1,2,4]-triazolo[4',3':1,6]pyridazino[4,5-b]indoles

Reaction of the title compound with hydrazine in the presence of air gives the 1-unsubstituted parent system via oxidative dehydrazination of the 1-hydrazino intermediate. The latter can be obtained in high yield by carrying out the hydrazinolysis step under inert gas, and it is smoothly converted into [1,2,4]-triazolo[4',3':1,6]pyridazino[4,5- b]indoles.     

Tungsten Oxide Nanoplates; the Novelty in Targeting Metalloproteinase-7 Gene in Both Cervix and Colon Cancer Cells

In this study, we synthesized tungsten oxide (WO₃) nanoplates, both crystallographic phases and the morphology of the samples were determined by powder x-ray diffraction and the scanning electron microscopy, respectively. The obtained data clarified that, the all prepared WO₃·H₂O samples were composed of large quantity of nanoplates. The cytotoxicity patterns of nanoplates were checked on both normal and cancer mammalian cell lines. Both nanoplates cytotoxicity did not exceed the 50 % inhibitory concentration (IC50) on the all normal tested cells even by using concentrations up to 1 mg/ml. In addition, orthorhombic tungsten oxide nanoplate was more potent against both Caco2 and Hela cells by showing inhibition percentages in cellular viability 64.749 and 72.27, respectively, and with cancer selectivity index reached 3.2 and 2.6 on both colon and cervix cancer, respectively. The anticancer effects of nanoplates were translated to alteration in both pro-apoptotic and anti-apoptotic genes expressions. Tungsten oxide nanoplates down regulated the expression of B cell lymphoma 2 (Bcl-2) and metalloproteinase-7 (MMP7) genes. In addition, orthorhombic tungsten oxide nanoplates showed more potentiation in IL2 and IL8 induction (40.43 pg/ml) and upregulation of TNF-α gene expression but with lower folds than Escherichia coli lipopolysaccharide (LPS) induction.     

Different Chromatographic Methods for the Simultaneous Determination of Vitamin E and Vinpocetine in Their Combined Dosage Form and in the Presence of the Alkaline-Induced Degradation Product of Vinpocetine

JPC – Journal of Planar Chromatography – Modern TLC - Accurate, selective, and sensitive thin-layer chromatography (TLC)—densitometry and reversed-phase high-performance liquid...     

Development of metal oxide incorporated Al-Zn-Sn sacrificial anodes processed by stir casting and heat treatment

Aluminum sacrificial anodes are currently the first choice for cathodic protection in numerous applications. The galvanic performance of aluminum-based sacrificial anodes is considerably enhanced by addition of certain alloying elements called activators. Recent researches proved that incorporation of specific metal oxides like MnO₂, CeO₂, RuO₂, and IrO₂ into the aluminum matrix could enhance the galvanic efficiency of aluminum anodes; however, the mechanism by which metal oxides improve galvanic properties of aluminum is still subject to discussion. The present work investigates the effect of incorporating commercially available low-cost manganese dioxide concentrate into Al-5Zn-0.1Sn sacrificial anodes in different volume fractions. It also studies the influence of heat treatment on anode’s galvanic performance by performing solution treatment at 3 different temperatures (250 °C, 400 °C, 550 °C). The electrochemical testing results proved an increase in efficiency of anodes incorporated with metal oxides and solution treated at 550 °C. The SEM imaging and EDX elemental mapping declared that the presence of SiO₂ particles in the anode matrix which might cause effective and uniform corrosion of Al anodes and decreased non-coulombic losses.

Graphical abstract

     

In Silico Mining of Terpenes from Red-Sea Invertebrates for SARS-CoV-2 Main Protease (Mpro) Inhibitors

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent for the COVID-19 pandemic, which generated more than 1.82 million deaths in 2020 alone, in addition to 83.8 million infections. Currently, there is no antiviral medication to treat COVID-19. In the search for drug leads, marine-derived metabolites are reported here as prospective SARS-CoV-2 inhibitors. Two hundred and twenty-seven terpene natural products isolated from the biodiverse Red-Sea ecosystem were screened for inhibitor activity against the SARS-CoV-2 main protease (M^pro) using molecular docking and molecular dynamics (MD) simulations combined with molecular mechanics/generalized Born surface area binding energy calculations. On the basis of in silico analyses, six terpenes demonstrated high potency as M^pro inhibitors with ΔG_binding ≤ −40.0 kcal/mol. The stability and binding affinity of the most potent metabolite, erylosides B, were compared to the human immunodeficiency virus protease inhibitor, lopinavir. Erylosides B showed greater binding affinity towards SARS-CoV-2 M^pro than lopinavir over 100 ns with ΔG_binding values of −51.9 vs. −33.6 kcal/mol, respectively. Protein–protein interactions indicate that erylosides B biochemical signaling shares gene components that mediate severe acute respiratory syndrome diseases, including the cytokine- and immune-signaling components BCL2L1, IL2, and PRKC. Pathway enrichment analysis and Boolean network modeling were performed towards a deep dissection and mining of the erylosides B target–function interactions. The current study identifies erylosides B as a promising anti-COVID-19 drug lead that warrants further in vitro and in vivo testing.     

Fabricated wearable and flexible chip composed strain of gallium and silver metals composites assembled on graphene inside PDMS matrix

With a view to creating a specific unique chip, its wearable, flexible and conductor.utilizing conventional physical methods like grafting and assembling metals (silver, copper, and gallium indium alloy) on graphene as composite, then immersed inside PDMS matrix. However, there is an incompatibility between liquid gallium and graphene sheet. So we used the abridge of metallic nanoparticles as silver and copper as a boundary barrier to its different charges to maximize interfacial surface interaction in between amorphous carbon and liquid gallium. to evaluate the chip conduct during the fabrication process we utilize various characterization such as electrochemical EIS and CVT to justify conductivity besides electrochemical reaction and oxidation and reduction, addition to measure the dielectric constant (?) of a composite at a different range of frequencies which is equal to 3.73 compared to PDMS 2.69.moreover its thermal stability (DSC) of prepared composite and tensile stress as an inductor for enforcement and enhancement physical properties, as well as, surface Morphology techniques characterize using TEM IR, and UV absorption.     

The Profile of Plasma Free Amino Acids in Type 2 Diabetes Mellitus with Insulin Resistance: Association with Microalbuminuria and Macroalbuminuria

Applied Biochemistry and Biotechnology - Altered plasma levels of branched-chain amino acids (BCAAs) and aromatic amino acids (AAAs) may predict the development of insulin resistance and other type...     

Bioconvection in oxytactic microorganism-saturated porous square enclosure with thermal radiation impact

This investigation addresses bioconvection of oxytactic microorganisms in a porous square enclosure by thermal radiation impact. The bioconvection flow and heat transfer in porous media are formulated based on Darcy model of Boussinesq approximation. Appropriate transformations lead to the non-dimensionalized governing partial differential equations. Galerkin finite element method for the resulting equations is computed. The role of relevant parameters on the streamlines, isotherms, isoconcentrations of oxygen and microorganisms and average Nusselt number is analysed in the outputs. It is revealed that the flow intensity of bioconvection is pronounced with larger Rayleigh number and reduced with radiation parameter. Furthermore, the temperature distribution is affected significantly with Rayleigh number. Radiation parameter serves to fasten the heat transfer in the enclosure. Oxygen density is enhanced with Rayleigh number and radiation parameter. The profile of motile isoconcentrations is boosted with Rayleigh number. The stability of microorganisms is improved with the radiation parameter.

     

Steam-Induced Coarsening of Single-Unit-Cell MFI Zeolite Nanosheets and Its Effect on External Surface Brønsted Acid Catalysis

Commonly used methods to assess crystallinity, micro-/mesoporosity, Brønsted acid site density and distribution (in micro- vs. mesopores), and catalytic activity suggest nearly invariant structure and function for aluminosilicate zeolite MFI two-dimensional nanosheets before and after superheated steam treatment. Yet, pronounced reaction rate decrease for benzyl alcohol alkylation with mesitylene, a reaction that cannot take place in the zeolite micropores, is observed. Transmission electron microscopy images reveal pronounced changes in nanosheet thickness, aspect ratio and roughness indicating that nanosheet coarsening and the associated changes in the external (mesoporous) surface structure are responsible for the changes in the external surface catalytic activity. Superheated steam treatment of hierarchical zeolites can be used to alter nanosheet morphology and regulate external surface catalytic activity while preserving micro- and mesoporosity, and micropore reaction rates.