Determination and mathematical modelling of budesonide solubility in N-methyl-2-pyrrolidone + water mixtures from T = 293.2 to 313.2 K

The solubilities of budesonide (BDS) in binary aqueous mixtures of N-methyl-2-pyrrolidone at temperatures ranging from 293.2 to 313.2 K were determined and mathematically correlated by three cosolvency models, i.e. Jouyban–Acree model, Jouyban–Acree–van’t Hoff model and modified Wilson model. The solubilities were measured using the shake-flask method and the models wereused to fit the solubility data of BDS in the solvent mixtures. The obtained mean relative deviations (MRDs %) for cosolvency models trained using whole data points varied between 5.0% and 31.0%. Solubilities were also predicted by the generally trained version of the Jouyban–Acree model with the MRD of 37.0%. Furthermore, the apparent thermodynamic properties of dissolution process of BDS in all the mixed solvents were calculated according to van’t Hoff and Gibbs equations. Dissolution of BDS in these mixed solvents is an endothermic process.     

Screening of several biological activities induced by different sesquiterpene lactones isolated from Centaurea behen L. and Rhaponticum repens (L.) Hidalgo

This study aims to evaluate the in vitro cytotoxic, in vitro and in ovo anti-angiogenic effects and antimicrobial activity of sesquiterpene lactones (SLs) from two plants Centaurea behen and Rhaponticum repens (L.). Five SLs, including cynaropicrin (1), 4β,15-dehydro-3-dehydrosolstitialin A (2), aguerin B (3), janerin (4), cebellin E (5), and a flavone hispidulin (6) were isolated from C. behen (compounds 1–3) and R. repens (compounds 4–6). Cynaropicrin (1) and aguerin B (3) were characterised by strong cytotoxic activities against A2780 cells with IC₅₀ values of 1.15 and 1.62 μg mL^?1, respectively, comparable to that of doxorubicin (IC₅₀ = 1.17 μg mL^?1). The anti-angiogenic study showed the remarkable inhibitory effect of cynaropicrin (1) and aguerin B (3) on the proliferation and migration of HUVECs. In addition, cynaropycrin and aguerin B exhibited significant angio-inhibitory effects in CAM assay. These findings may be useful for the development of novel chemotherapeutic agents for the treatment of cancer.     

N-Bromo Reagent Mediated Oxidation of Urazoles to Their Corresponding Triazolinediones under Mild and Heterogeneous Conditions

Various N-bromo reagents [HMTAB, DABCO-bromine, DPTBE, and TBCA] were used as effective oxidizing agents for the oxidation of urazoles and bisurazoles to their corresponding triazolinediones under mild and heterogeneous conditions at room temperature with good to excellent yields. Also the oxidation of some new 4-phenylurazole derivatives with these reagents is discussed.     

Phase-dependent heat current of granular Josephson junction for different geometries

We theoretically investigate the phase-dependent heat transport of a temperature-biased granular Josephson junction in the presence of a perpendicular magnetic field. We illustrate the influence of geometry of the junction on the thermal current. The use of granular Josephson junction rather than bulk one makes significant changes in the heat current behavior. The heat current diffraction pattern of the rectangular, circular and annular geometries with no trapped fluxons demonstrates similar to the current of s-wave superconducting junction. By increasing the number of trapped fluxon, the pattern of current behaves such as d-wave superconducting junction. The feasibility of using granular superconductors, with different geometries, controlled by the magnetic field provides an appropriate tool to obtain the desired result for a specific application.     

Improved antibacterial properties of an Mg‐Zn‐Ca alloy coated with chitosan nanofibers incorporating silver sulfadiazine multiwall carbon nanotubes for bone implants

Bacteria‐caused infection remains an issue in the treatment of bone defects by means of Mg‐Zn‐Ca alloy implants. This study aimed to improve the antibacterial properties of an Mg‐Zn‐Ca alloy by coating with chitosan‐based nanofibers with incorporated silver sulfadiazine (AgSD) and multiwall carbon nanotubes (MWCNTs). AgSD and MWCNTs were prepared at a weight ratio of 1:1 and then added to chitosan at varying concentrations (ie, 0, 0.25, 0.5, and 1.5 wt.%) to form composites. The obtained composites were ejected in nanofiber form using an electrospinning technique and coated on the surface of an Mg‐Zn‐Ca alloy to improve its antibacterial properties. A microstructural examination by scanning electron microscopy (SEM) revealed the diameter of chitosan nanofiber ejected increased with the concentration of AgSD‐MWCNTs. The incorporation of AgSD‐MWCNTs into the chitosan nanofibers was confirmed by Fourier transform infrared spectroscopy (FTIR). Examination of the antibacterial activity shows that chitosan nanofibers with AgSD‐MWCNTs can significantly inhibit the growth and infiltration of Escherichia coli and Staphylococcus aureus. Biocompatibility assay and cell morphology observations demonstrate that AgSD‐MWCNTs incorporated into nanofibers are cytocompatible. Taken together, the results of this study demonstrate the potential application of electrospun chitosan with AgSD‐MWCNTs as an antibacterial coating on Mg‐Zn‐Ca alloy implants for bone treatment.     

(Benzyl isocyanide)gold(I) pyrimidine‐2‐thiolate complex: Synthesis and biological activity

The reaction of [(Me₂S)AuCl] with an equimolar amount of benzyl isocyanide (PhCH₂NC) ligand led to the formation of complex [(PhCH₂NC)AuCl] ( 1 ). The solid‐state structure of 1 was determined using the X‐ray diffraction method. Through a salt metathesis reaction, the chloride ligand in 1 was replaced by pyrimidine‐2‐thiolate (SpyN^?) to afford the complex [(PhCH₂NC)Au(η¹‐S‐Spy)] ( 2 ), which was characterized spectroscopically. The cytotoxic activities of 1 and 2 were evaluated against three human cancer cell lines: ovarian carcinoma (SKOV3), lung carcinoma (A549) and breast carcinoma (MCF‐7). Complex 2 showed higher cytotoxicity than cisplatin against SKOV3 and MCF‐7 cancer cell lines. It showed a strong anti‐proliferative activity with IC₅₀ of 7.80, 6.26 and 6.14 μM, compared with that measured for cisplatin which was 7.62, 12.36 and 11.47 μM, against A549, SKOV3 and MCF‐7 cell lines, respectively. The induction of cellular apoptosis by 2 was also studied on MCF‐7 cell line. Our results indicated that 2 could induce apoptosis in cancerous cells in a dose‐dependent manner.     

Synthesis of ZnO nanostructures with controlled morphology and size in ionic liquids

Nanostructured ZnO has been synthesized by a hydrothermal route, using different ionic liquids (ILs) as the morphology templates. The morphology of ZnO changes from rod-like to star-like and flower-like in different ILs. A 3D nano/micro structure ZnO with unique flower-like morphology has been synthesized via the assembly of dicationic IL and [Zn(OH)₄]²⁻. The flower-like pattern was obtained in the presence of IL 1. The flower-like ZnO structure has a hexagonal prism, with a hexagonal pyramid on the tip, and diameter of ~444 nm. While the ZnO prepared in IL 2, shows uniform rod-like shape with a diameter of 91 nm, star-like morphology consisting of nanorods with diameter of ~109 nm was formed in IL 3. The XRD, SEM, and PL spectra have been employed for characterization of the synthesized ZnO nano structures.