Reaction of Chalcones with Cellular Thiols. The Effect of the 4-Substitution of Chalcones and Protonation State of the Thiols on the Addition Process. Diastereoselective Thiol Addition

Several biological effects of chalcones have been reported to be associated with their thiol reactivity. In vivo, the reactions can result in the formation of small-molecule or protein thiol adducts. Both types of reactions can play a role in the biological effects of this class of compounds. Progress of the reaction of 4-methyl- and 4-methoxychalcone with glutathione and N-acetylcysteine was studied by the HPLC-UV-VIS method. The reactions were conducted under three different pH conditions. HPLC-MS measurements confirmed the structure of the formed adducts. The chalcones reacted with both thiols under all incubation conditions. The initial rate and composition of the equilibrium mixtures depended on the ratio of the deprotonated form of the thiols. In the reaction of 4-methoxychalcone with N-acetylcysteine under strongly basic conditions, transformation of the kinetic adduct into the thermodynamically more stable one was observed. Addition of S-protonated N-acetylcysteine onto the polar double bonds of the chalcones showed different degrees of diastereoselectivity. Both chalcones showed a Michael-type addition reaction with the ionized and non-ionized forms of the investigated thiols. The initial reactivity of the chalcones and the equilibrium composition of the incubates showed a positive correlation with the degree of ionization of the thiols. Conversions showed systematic differences under each set of conditions. The observed differences can hint at the difference in reported biological actions of 4-methyl- and 4-methoxy-substituted chalcones.     

Estimation of natural gas contribution in indoor 222Rn concentration level in residential houses

Journal of Radioanalytical and Nuclear Chemistry - The effect of natural gas use on indoor radon concentrations was studied in the dwelling of two cities in Cyprus using an AlphaGUARD radon...     

AC electrokinetic isolation and detection of extracellular vesicles from dental pulp stem cells: Theoretical simulation incorporating fluid mechanics

Extracellular vesicles (EVs) are cell-derived nanoscale vesicles involved in intracellular communication and the transportation of biomarkers. EVs released by mesenchymal stem cells have been recently reported to play a role in cell-free therapy of many diseases. However, the demand for better research tools to replace the tedious conventional methods used to study EVs is getting stronger. EVs' manipulation using alternating current (AC) electrokinetic forces in a microfluidic device has appeared to be a reliable and sensitive diagnosis and trapping technique. Given that different AC electrokinetic forces may contribute to the overall motion of particles and fluids in a microfluidic device, EVs' electrokinetic trapping must be examined considering all dominant forces involved depending on the experimental conditions. In this paper, AC electrokinetic trapping of EVs using an interdigitated electrode arrays is investigated. A 2D numerical simulation incorporating the two significant AC electrokinetic phenomena (Dielectrophoresis and AC electroosmosis) has been performed. Theoretical predictions are then compared with experimental results and allow for a plausible explanation of observations inconsistent with DEP theory. It is demonstrated that the inconsistencies can be attributed to a significant extent to the contribution of the AC electroosmotic effect.     

Efficient synthesis of chromeno[4,3-b]pyrano[3,4-e]pyridine-6,8-dione derivatives via multicomponent one-pot reaction under mild reaction conditions in water

10-Methyl-7-aryl-7,12-dihydro-6H,8H-chromeno[4,3-b]pyrano[3,4-e]pyridine-6,8-dione derivatives are significant class of compounds and this is critical to develop methods in water using commercially available and non-toxic catalysts. In this paper, an efficient method is introduced for the synthesis of 10-methyl-7-aryl-7,12-dihydro-6H,8H-chromeno[4,3-b]pyrano[3,4-e]pyridine-6,8-dione derivatives. For the synthesis of the desired products, a multicomponent reaction was designed and performed between 4-hydroxycoumarin, an aldehyde, 6-methyl-2H-pyran-2,4(3H)-dione, and ammonium acetate. The products are obtained under green conditions in water in the presence of a catalytic amount of L-proline (10 mol%). The advantage of this method is no need to any toxic solvent, which is critical from the environmental viewpoint. A possible mechanism was suggested, which confirms the role of L-proline in the reaction as the catalyst.

     

Acceleration of osteogenic differentiation by sustained release of BMP2 in PLLA/graphene oxide nanofibrous scaffold

After about three decades of experience, tissue engineering has become one of the most important approaches in reconstructive medical research to treat non‐self‐healing bone injuries and lesions. Herein, nanofibrous composite scaffolds fabricated by electrospinning, which containing of poly(L‐lactic acid) (PLLA), graphene oxide (GO), and bone morphogenetic protein 2 (BMP2) for bone tissue engineering applications. After structural evaluations, adipose tissue derived mesenchymal stem cells (AT‐MSCs) were applied to monitor scaffold's biological behavior and osteoinductivity properties. All fabricated scaffolds had nanofibrous structure with interconnected pores, bead free, and well mechanical properties. But the best biological behavior including cell attachment, protein adsorption, and support cells proliferation was detected by PLLA‐GO‐BMP2 nanofibrous scaffold compared to the PLLA and PLLA‐GO. Moreover, detected ALP activity, calcium content and expression level of bone‐related gene markers in AT‐MSCs grown on PLLA‐GO‐BMP2 nanofibrous scaffold was also significantly promoted in compression with the cells grown on other scaffolds. In fact, the simultaneous presence of two factors, GO and BMP2, in the PLLA nanofibrous scaffold structure has a synergistic effect and therefore has a promising potential for tissue engineering applications in the repair of bone lesions.     

H14[NaP5W30O110] as a heterogeneous recyclable catalyst for the air oxidation of thiols under solvent free conditions

The catalytic oxidation of thiols to the corresponding disulfides using Preyssler's catalyst H(14)[NaP(5)W(30)O(110)] has been studied. These highly selective oxidations gave good yields of the target disulfides.     

Preparation and preliminary evaluation of [<Superscript>67</Superscript>Ga]-tetra phenyl porphyrin complexes as possible imaging agents

[⁶⁷Ga]labeled tetraphenyl porphyrin ([⁶⁷Ga]-TPP) was prepared using freshly prepared [⁶⁷Ga]GaCl₃ and tetraphenyl porphyrin (TPPH₂) for 30–60 min at 25 °C (radiochemical purity: >97 ± 1% ITLC, >98 ± 0.5% HPLC, specific activity: 13–14 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 24 h. The partition coefficient was calculated for the compound (log P 1.89). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT imaging up to 24 h. A detailed comparative pharmacokinetic study performed for ⁶⁷Ga cation and [⁶⁷Ga]-TPP. The complex is mostly washed out from the circulation through kidneys and can be an interesting tumor imaging/targeting agent due to low liver uptake and rapid excretion through the urinary tract.     

Complexation of 4′-Nitrobenzo-15-crown-5 with Zn<Superscript>2+</Superscript>, Mn<Superscript>2+</Superscript>, Cr<Superscript>3+</Superscript> and Sn<Superscript>4+</Superscript> Cations in Acetonitrile–Ethanol Binary Mixtures

The complexation reactions of 4′-nitrobenzo-15-crown-5 (4′NB15C5) with Zn²⁺, Mn²⁺, Cr³⁺ and Sn⁴⁺ cations were studied in acetonitrile–ethanol (AN–EtOH) binary solvent mixtures at different temperatures by the electrical conductometry method. The stability constants of the resulting 1:1 complexes were determined from computer fitting of the conductance versus mole ratio data. The results show that the selectivity order of 4′NB15C5 for the metal cations in the AN–EtOH (mol-%AN=76) binary solvent at 298.15 K is: Cr³⁺>Mn²⁺≈Zn²⁺>Sn⁴⁺, but the selectivity order changes with the composition of the mixed solvents. A nonlinear relationship was observed between the stability constants (log ₁₀ K _f) of these complexes and the composition of the AN–EtOH binary solvents. The corresponding thermodynamic parameters (DH_c^o, DS_c^o)(\Delta H_{\mathrm{c}}^{\mathrm{o}}, \Delta S_{\mathrm{c}}^{\mathrm{o}}) were obtained from the temperature dependence of the stability constants using van’t Hoff plots. The results show that the values and also the sign of these parameters are influenced by the nature and composition of the mixed solvents.     

Mercury selenide nanorods: Synthesis and characterization via a simple hydrothermal method

HgSe nanorods have been synthesized through a simple hydrothermal reduction approach. The nanorods formed were ≈45 nm average diameter and ≈3 μm nm in length. X-ray diffraction characterization suggested that the product consists of cubic phase pure HgSe. The as-prepared products were also characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). An X-ray energy dispersive spectroscopy (EDX) study further confirmed the composition and purity of the product. The synthesis procedure is simple and uses less toxic reagents than the previously reported methods. The results showed that the capping agent CTAB (cetyltrimethylammoniumbromide) plays a crucial role in the process. Other factors, such as the reaction time, temperature, different capping agent and the reductant type also have an influence on the morphology of the final products to some extent.     

Application of dimeric cyclopalladated complex of tribenzylamine as an efficient catalyst in the Heck cross-coupling reaction

The activity of [Pd{C₆H₄(CH₂N(CH₂Ph)₂)} (μ-Br)]₂ complex was investigated in the Heck-Mizoroki C-C cross-coupling reaction. This complex is an active and efficient catalyst for the Heck reaction of aryl iodides, bromides and even chlorides and also arenesulfonyl chlorides. The cross-coupled products were produced in excellent yields in short reaction time using a catalytic amount of [Pd{C₆H₄(CH₂N(CH₂Ph)₂) (μ-Br)]₂ complex in NMP at 130 °C.