Artificial Water Channel Promoting Depolymerization of Actin Filaments to Trigger Cancer Cell Apoptosis

A new strategy to design antitumor reagents has been developed based on artificial water channel (AWC)-promoted depolymerization of actin filaments. Its effectivity has been demonstrated in vitro and in vivo by using colorectal cancer as a disease model. The AWC conjugated with acetazolamide (AZA) moiety exhibited targeting behavior and water permeability to induce the depolymerization of the actin and apoptosis of the cancer cells.
Comprehensive Summary
Actin filaments play important physiological functions, which have become potential targets of antitumor drugs. Using chemicals to intervene their polymerization-depolymerization dynamics would generate new strategies for designing antitumor drugs. In this report, an artificial water channel appending acetazolamide moiety, a ligand that can selectively bind to carbonic anhydrase IX, has been prepared. We demonstrated that this conjugate can target colorectal cancer cells overexpressing carbonic anhydrase IX and trigger the depolymerization of actin filaments of the cancer cells by selectively mediating water transmembrane transport. Moreover, the conjugate-promoted actin depolymerization led to tumor cell apoptosis and its high antitumor activity in vitro and in vivo against colorectal cancer. The method described herein represents a new and general strategy for designing antitumor drugs by using artificial channel-mediated selective water transport to promote actin depolymerization.
Unveiling the mutual effects of hydroxyl and dibenzhydryl groups in α‐diimino‐nickel precatalysts for direct synthesis of polyethylene elastomers

The prepared unsymmetrical α-diimine nickel precatalysts demonstrated exceptional performance at higher temperatures (act. 2.4 × 106 g mol−1 h−1 at 100°C, M w = 105 g mol−1, Ð = ≈1.5, branches 97–142/1000C). Excellent tensile strength and strain recovery of polyethylene highlight characteristic properties of thermoplastic elastomers.
The properties and practical applications of polyethylene are closely associated with the polymer molecular weight, polydispersity, degree of branching, and the type of branches and its arrangement within microstructure. In this study, a set of structurally diverse unsymmetrical 1-(2,6-dibenzhydryl-4-hydroxylphenylimino)-2-(2,6-(R)-4-(R1)phenylimino)acenaphthene-nickel dibromide precatalysts (where Ni 2Me [R = Me, R1 = H], Ni 2Et [R = Et, R1 = H], Ni 2iPr [R = iPr, R1 = H], Ni 3Me [R, R1 = Me], Ni 2Et,Me [R = Et, R1 = Me]) has been prepared and studied for ethylene polymerization. Molecular structure analysis of Ni 2Me and Ni 2Et complexes revealed distorted tetrahedral geometries at nickel. The polymerization activities are extremely high for all precatalysts upon activation with either EASC or MMAO aluminum reagents, a trend notably pronounced in the case of the EASC-activated systems, entering activity in the range of 10 million g mol−1 h−1 at 30°C. The Ni 2Me demonstrated exceptional performance at higher temperatures, achieving an activity of 2.4 × 106 g mol−1 h−1 at 100°C and generated high molecular weight polyethylene (M w = 105 g mol−1) with narrow polymer dispersity across all reaction temperatures (Ð ≈ 1.5). High temperature 13C NMR spectra identified 97–142/1000C branches in resulting polyethylene, a feature significantly dependent on the reaction temperature. In terms of mechanical properties, stress–strain analysis indicated that polyethylene synthesized at lower temperatures displayed superior tensile strength compared with that produced at higher reaction temperatures, while a reverse trend was observed in strain recovery analysis. The high strain recovery (up to 72%) of these polyethylene highlights the characteristic properties of thermoplastic elastomers.
Homoselective synthesis of tetrazole derivatives using copper complex anchored on mesoporous KIT‐6 as a reusable, highly efficient, and environmentally green nanocatalyst

The mesoporous KIT-6 was modified using 3,4-diaminobenzophenone, and further, a new complex of copper was immobilized on its surface (KIT-6@DABP@Cu) as an organometallic and nanocatalyst in the selective synthesis of 5-substituted tetrazoles. This catalyst was identified with FT-IR, WDX, AAS, XRD, SEM, TGA, EDX, and BET techniques. KIT-6@DABP@Cu nanocatalyst was demonstrated highly effective and good reusability in the synthesis of 5-substituted tetrazoles.
In this article, the mesoporous silica framework of KIT-6 was synthesized and, then its surface was modified using 3-aminopropyltrimethoxysilane (APTMS). The new KIT-6@DABP@Cu nanocatalyst was then prepared by anchoring the copper complex on modified mesoporous KIT-6. The nanocatalyst was identified using several techniques, including FT-IR, WDX, AAS, SEM, TGA, XRD, EDS, and BET. The physical properties, such as size, shape, and morphology of the nanocatalyst were studied by SEM analysis. The elemental composition of KIT-6@DABP@Cu nanocatalyst was described using wavelength dispersive X-ray spectroscopy (WDX) and EDS. FT-IR spectroscopy was used to characterize the functional groups in the structure of the nanoparticles. The stability of KIT-6@DABP@Cu nanocatalyst was studied by TGA at high temperatures. Also, the surface area, total volume, and average diameter of pores of the nanocatalyst were determined using Brunauer–Emmett–Teller (BET) analysis. The KIT-6@DABP@Cu catalyst was found to be a new, highly effective, and green catalyst for the synthesizing of 5-substituted-tetrazoles using nitriles and sodium azide (NaN3) catalyzed in polyethyleneglycol-400 (PEG-400) as a green solvent. This heterogeneous catalyst showed good recyclability for up to five consecutive cycles without notable loss of its catalytic efficiency.
Complexation behavior of copper and zinc divalent ions towards diisatin malonyl dihydrazone ligand with biological and catalytic assessments

Cu2+ and Zn2+ complexes of malonyl dihydrazone derivative are synthesized and characterized.
The antimicrobial (bacteria and fungi) and anticancer potential of M-complexes and their ligand are examined. Their binding to ctDNA is examined via UV–Visible spectroscopy and hydrodynamic measurements. Cu2+ and Zn2+ complexes have more biological reactivity over their free ligand based the role of metal ion of the Tweedy's chelation theory. Their catalytic reactivity was examined in the epoxidation of 1,2-cyclohexene with H2O2, in which they assigned high catalytic performance.
According to the interesting reactivity of arylhydrazones in coordination chemistry and biological assays, malonyl dihydrazone ligand of diisatin derivative (H2Lm) was reacted with Cu2+ and Zn2+ ions forming two complexes of dinuclear homoleptic mode (CuLm and ZnLm, respectively). Demonstration of their chemical structures was confirmed through various spectroscopic ways alongside the elemental analyses (EA), conductivity measurements, and magnetic characteristics.
Their bio-performance was recorded based on their inhibited potential of the growing ability of some common bacteria, fungi, and human cancer/normal cell lines. The biological studies appointed the role and job of M2+ ion = Cu2+ or Zn2+ in its chelated MLm complex to perform the bio-reactivity over the free ligand, H2Lm. Moreover, their interacted modes with ctDNA (i.e., calf thymus DNA) were examined via the viscometry and spectrophotometric titration. Because the two chelates (CuLm and ZnLm) represented an attractive job for the inhibited action against the current microorganisms and the human cancer/normal strains' growth over the free H2Lm ligand, CuLm and ZnLm complexes displayed a distinguished interaction with ctDNA more than that of their uncoordinated H2Lm ligand. From the values of binding constant (K b) and Gibb's free energy ( ∆Gb≠$$ \Delta {G}_b^{\ne } $$), CuLm assigned more bio-action within ctDNA more than ZnLm H2Lm ligand, referring to the role of Cu2+ ion with more electronegativity to enhance the reactivity of CuLm over their free H2Lm ligand and ZnLm.
The catalytic behavior of CuLm and ZnLm was given within the epoxidation of 1,2-cyclohexene (an example of unsaturated hydrocarbons) homogeneously using hydrogen peroxide (the oxidant). Their catalytic action was optimized through various temperatures, solvents, time, and type of M2+ ion in the catalyst.
Advances in Electrochemical Biosensors for the Detection of Common Oral Diseases
[ASAP] “Three-in-One” Multifunctional Hollow Nanocages with Colorimetric Photothermal Catalytic Activity for Enhancing Sensitivity in Biosensing
Significant Effect of 2nd Sphere Interactions on the Reductive Activation of O2 by non‐heme Iron(II) Complexes – Application to the Electroassisted Oxidation of Thioanisole

2nd sphere hydrogen bonds within non-heme iron complexes significantly improves the potential of the reductive O2 activation process, by generating stabilizing interactions within the Fe/O2 adduct. O2 can be activated at a much more favorable potential, which we took advantage of to achieve the electroassisted oxidation of thioanisole by O2.
Abstract
New mononuclear non-heme FeII complexes derived from a well-known pentadentate amine/pyridine ligand were synthesized. The new ligand bears an additional OH group on one pyridyl aimed at developing second sphere hydrogen bonds. Two binding modes of the ligand were observed that can be selectively obtained through the choice of the counterion: the OH group develops an intramolecular H-bond with the 6th exogenous ligand in the classical mode, or an intermolecular one with the unbound triflate counterion in the alternative mode. The complexes were studied by cyclic voltammetry in the reductive activation of O2. The addition of an H-bond improves the O2 activation potential with a gain of 90 mV in the classical case and 220 mV in the alternative one. The difference is ascribed to the development of stabilizing H-bonds within the FeIII-peroxo intermediate with the proximal O atom of peroxo (classical mode) or the distal one (alternative mode). Ultimately, the complex in the alternative mode activates O2 at −0.5 V vs SCE (500 mV gain compared to free O2). We took advantage of this significantly reduced energetic cost to carry out and achieve the electroassisted oxidation of thioanisole by O2 at −0.5 V vs SCE.