Preparation of functionalized graphene oxide/polypropylene nanocomposite with significantly improved thermal stability and studies on the crystallization behavior and mechanical properties

Autophagy is a major degradative process responsible for the disposal of cytoplasmic proteins and dysfunctional organelles via the lysosomal pathway During the autophagic process, cells form double-membraned vesicles called autophagosomes that sequester disposable materials in the cytoplasm and finally fuse with lysosomes In the present study, we investigated the inhibition of autophagy by a synthesized compound, MHY1485, in a culture system by using Ac2F rat hepatocytes Autophagic flux was measured to evaluate the autophagic activity Autophagosomes were visualized in Ac2F cells transfected with AdGFP-LC3 by live-cell confocal microscopy In addition, activity of mTOR, a major regulatory protein of autophagy, was assessed by western blot and docking simulation using AutoDock 42 In the result, treatment with MHY1485 suppressed the basal autophagic flux, and this inhibitory effect was clearly confirmed in cells under starvation, a strong physiological inducer of autophagy The levels of p62 and beclin-1 did not show significant change after treatment with MHY1485 Decreased co-localization of autophagosomes and lysosomes in confocal microscopic images revealed the inhibitory effect of MHY1485 on lysosomal fusion during starvation-induced autophagy These effects of MHY1485 led to the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time- dependent manner Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound The significance of this study is the finding of a novel inhibitor of autophagy with an mTOR activating effect

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Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion.

Synthesis, spectroscopic characterization, antimicrobial evaluation and molecular docking study of novel triazine-quinazolinone based hybrids

Complexes of iron(III) and chromium(III) salen and salophen Schiff bases with bridging 1,3,5‐triazine derived multidirectional ligands

Boronate affinity materials have been widely used for selective capture of cis-diols such as nucleosides. Adsorbents with features of low binding pH and high adsorption capacity are highly desired. However, most reported materials only possess one of the two features. We have synthesized a 1,3,5-triazine-containing binary boronic acid by reacting cyanuric chloride with 3-aminophenylboronic acid, and the product was then grafted onto attapulgite (a fibrous aluminum-magnesium silicate). The resulting functionalized attapulgite exhibit low binding pH (5.0) and display high adsorption capacity (19.5 ± 1.1 mg⋅g−1 for adenosine). The material exhibits high selectivity for cis-diols even in the presence of a 1000-fold excess of interferences. It was applied to the selective extraction of nucleosides from human urine. Typical features of the method include (a) limits of detection in the range from 4 to 17 ng⋅mL−1, (b) limits of quantification between 13 and 57 ng⋅mL−1, (c) relative standard deviations of ≤9.1 %, and (d) recoveries of nucleosides from spiked human urine between 85.0 and 112.9 %. In our perception, the material and method offer a promising strategy for selective capture of cis-diols in the areas of proteomics, metabolomics and glycomics.

Binary boronic acid-functionalized attapulgite with high adsorption capacity for selective capture of nucleosides at acidic pH values

An efficient, “green” approach to aryl amination of cyanuric chloride using acetic acid as solvent

Acetic acid is an inexpensive and environmentally friendly solvent for facile, clean and high-yielding aryl amination of cyanuric chloride with aromatic amines, including nitroanilines. Aryl amination in acetic acid medium and isolation protocol are greatly simplified as compared to previously reported procedures. Under proper conditions, it is possible to attach the same or different aniline residues in a controlled way to obtain in excellent yields symmetrical and unsymmetrical 1,3,5-triazine derivatives, respectively.

An Efficient, “Green” Approach to Aryl Amination of Cyanuric Chloride Using Acetic Acid as Solvent.

Selective modification of bifunctional heterocyclic compounds containing amino and thioamide groups in acetic acid medium

In acetic acid medium, 2-chloro-4,6-dimorpholin-4-yl-[1,3,5]triazine undergoes amination by bifunctional heterocyclic compounds containing both amino and thioamide groups. The reactions are high-yielding and selective; the thioamide functions are unaffected under the requisite conditions. The reactions do not proceed in satisfactory yields in other solvents and, thus, require acetic acid. The resulting thioamides, consisting of multiple biologically relevant residues, are easily alkylated at the sulfur (thiolthione) centers to furnish new thioethers in subsequent steps.

Kirill A. Kolmakov

Papers

An efficient, “green” approach to aryl amination of cyanuric chloride using acetic acid as solvent

An Efficient, “Green” Approach to Aryl Amination of Cyanuric Chloride Using Acetic Acid as Solvent.

Selective modification of bifunctional heterocyclic compounds containing amino and thioamide groups in acetic acid medium

Selective Modification of Bifunctional Heterocyclic Compounds Containing Amino and Thioamide Groups in Acetic Acid Medium.