Enhance the oral insulin delivery route using a modified chitosan-based formulation fabricated by microwave.

Chitosan (Cs) was subjected to ball milling and subsequently functionalized with Dinitro salicylic acid (Cs-DNS) to enhance the efficacy of oral insulin delivery. The hydrodynamic spherical particle sizes exhibited 33.29 ± 5.08 nm for modified Cs-DNS NPs. Irrespective of insulin entrapment, zeta potential measurements revealed positively charged Cs-DNS NPs (+ 35 ± 3.5 mV). The entrapment performance (EP%) was evaluated in vitro, and insulin release patterns at various pH levels. The EP% for Cs-DNS NPs was 99.3 ± 1.6. Cs- DNS NPs retained a considerable amount of insulin (92 %) in an acidic medium, and significant quantities were released at increasing pH values over time. In vivo investigations, the diabetic rats which taken insulin-incorporated NPs had lower serum glucose levels (SGL) after 3 h to (39.4 ± 0.6 %) for Cs- DNS NPs. For insulin-incorporated Cs- DNS NPs, the bioavailability (BA%) and pharmacological availability (PA%) were 17.5 ± 0.31 % and 8.6 ± 0.8 %, respectively. The assertion above highlights the significance and effectiveness of modified chitosan in promoting insulin delivery, decreasing SGL levels, and guaranteeing safety.

Metal Chelates of Sulfafurazole Azo Dye Derivative: Synthesis, Structure Affirmation, Antimicrobial, Antitumor, DNA Binding, and Molecular Docking Simulation.

A series of divalent and one trivalent metal chelates of the azo ligand resulting from coupling of sulfafurazole diazonium chloride with resorcinol have been designed and synthesized. Structure investigation of the isolated chelates have been achieved by applying spectroscopic and analytical tools which collaborated to assure the formation of the metal chelates in the molar ratios of 1L: 1M for Ni(II), Co(II), and Fe(III) chelates, where Cu(II) and Zn(II) complexes formed in the ratio 2L : 1M. The geometrical arrangement around the metal canters was concluded from UV-Vis spectra to be octahedral for all metal chelates. The attachment of the ligand to the metal ions took place through the azo group nitrogen and o-hydroxyl oxygen through proton displacement leading to the ligand being in monobasic bidentate binding mode. Antimicrobial and antitumor activities of the interested compounds have been evaluated against alternative microorganisms and cancer cells, respectively, in a trial to investigate their extent of activity in addition to docking studies. The mode of interaction of the compounds with SS-DNA has been examined by UV-Vis spectra and viscosity studies.

Synthesis of new Cu(II)-benzohydrazide nanometer complexes, spectral, modeling, CT-DNA binding with potential anti-inflammatory and anti-allergic theoretical features.

New nanometer Cu(II)-benzohydrazide complexes were synthesized and characterized. Mono negative tetra-dentate mode is the general feature proposed for all coordinating ligands. Variable structural forms were established, square-planer, tetrahedral and octahedral arrangements around copper centers. XRD and TEM studies displayed a nanometer size for crystalline compounds. TGA analysis of new complexes showed low thermal stability due to the presence of crystal water molecules. Kinetic parameters were calculated using two comparative methods for assertion. ESR study was performed on three chosen complexes to estimate essential spectral parameters and assert on proposed geometries. Gaussian09 software program and applying DFT/B3LYP method was used for optimizing all structures to give the best arrangement for atoms. Essential indexes were extracted from log files as well as other indexes were computed based on frontier energy gaps. Potential theoretical anti-inflammatory, antitumor and anti-allergic studies were executed using Autodock 4.2 tools. Essential energies were calculated over docking complexes corresponding to 5HN1, 5AV1 and 4H1L protein receptors for three pathogens (inflammation, liver cancer and allergy, respectively). H2L5 ligand displays significant activity towards inflammation and allergy diseases. Such potential feature will give a well insight about their biological attitude in future experimentation.

Synthesis of Pyrazolone Derivatives and Their Nanometer Ag(I) Complexes and Physicochemical, DNA Binding, Antitumor, and Theoretical Implementations.

Four pyrazolone derivatives and their corresponding silver complexes were synthesized and characterized. Based on elemental analysis, 1 : 2 (M : L) molar ratio was suggested for all inspected complexes. 1H, 13C NMR, mass, UV-Vis, TGA, and IR were the spectral tools used for describing the formulae. Moreover, XRD patterns and SEM pictures were used to evaluate the particle sizes which appeared strongly in nanometer range. CT-DNA study is the major consideration in this study, to test the interacting ability of all synthesized cationic complexes towards cell DNA. Each binding constant was computed and correlated with the Hammett sigma constant. Antitumor activity was examined upon three carcinoma cell lines (MCF-7, HepG2, and HCT116). The high efficiency was recorded towards MCF-7 (breast carcinoma) cell line. Kinetic studies yield essential parameters to assert on the rule of metal atom on thermal feature of organic compounds. Molecular modeling was implemented to optimize the structures of compounds. Also, molecular docking was achieved to obtain a clear view about proposed drug behavior within the affected cells. This was achieved through comparing the calculated internal energy values of all docking complexes. All the tested compounds displayed a significant interaction with breast cancer protein (strong matching with practical result) followed by DNA polymerase protein.

Structure elucidation, protein profile and the antitumor effect of the biological active substance extracted from sea cucumber Holothuria polii.

Holothuria polii (Delle Chiaje, 1823) (Holothuriidae) is a sea cucumber inhabiting Mediterranean Sea coast of Egypt. The bioactive compound of its tegument has antifungal, antibacterial and antiparasitic effects. The present study aims to elucidate the structure of the bioactive material of H. polii for pharmacological and chemotaxonomic purposes. Furthermore, the study demonstrates its efficacy as a cytotoxic agents against two tumor cell lines HCT116 (colon adenocarcinoma cell line) and MCF7 (breast adenocarcinoma cell line). The biological active compound of the ethanol extract has been characterized by means of infrared (IR), proton-nuclear magnetic resonance ((1)H NMR), ultraviolet-visible (UV-Vis) and mass spectra. Protein profile was carried out using sodium dodecyl sulfate polyacrylamide gel electrophoresis. Cytotoxic activity was carried out according to sulforhodamine-B assay. IR, (1)H NMR, UV-Vis and mass spectra showed that the extracted bioactive material is a nonsulfated hexaosides called bivittoside. This glycoside is composed of aglycone and a glycosidic chain (carbohydrate chain) enclosed with six sugar units, including xylose, glucose, 3-O-methylglucose and quinovose. There were no traces of dissolved proteins. The preliminary cytotoxic assay of bivittoside exhibited significant cytotoxic activity against two types of cultured tumor cell lines of HCT116 and MCF7. The half-maximal inhibitory concentration was 17.4 µg/ml and 18 µg/ml for MCF7 and HCT116, respectively. Although H. polii belongs to the genus Holothuria, the lacking of sulfate group and the fact that it contains up to six monosaccharides make it different from this genus. The present study suggests separation of H. polii from its genus to a new one. On the other hand, results support the hypothesis that H. polii bioactive compound has an antitumor effect.

A comparative study of solid and liquid inner contact benzalkonium chloride ion-selective electrode membranes.

A comparative study was made between two designs of benzalkonium ion (Bz)-selective electrodes: a silver-coated (solid contact) called electrode A and a PVC membrane (liquid inner contact) called electrode B based on benzalkonium-phosphomolybdate (Bz-PM) as ion-exchanger complex. Electrode A has a linear dynamic range from 2.0×10(-8) to 1.0×10(-2) mol L(-1), with a Nernstian slope of 60±0.3 mV/decade and a detection limit of 2.0×10(-8) mol L(-1). Electrode B shows linearity over the concentration range from 2.0×10(-7) to 1.0×10(-2) mol L(-1), with a Nernstian slope of 55±1.2 mV/decade and a limit of detection of 1.5×10(-7) mol L(-1). Electrode A showed better performance than electrode B. The detection limit of benzalkonium chloride (BzCl) was effectively improved by a solid contact ion-selective electrode (SC-ISE), rather than the traditional liquid inner contact electrode that gives lower detection limits because of diminished ion fluxes. The present electrodes show clear discrimination of BzCl from several inorganic, organic ions, sugars and some common drug excipients. The sensors were applied efficiently for determination of BzCl in its pharmaceutical preparations (eye, ear and nasal drops) using standard addition and the calibration curve methods.

UV-vis, IR and (1)H NMR spectroscopic studies of some Schiff bases derivatives of 4-aminoantipyrine.

Five Schiff bases derived from 4-aminoantipyrine and benzaldehyde derivatives (I) are prepared and their UV-vis, IR, (1)H NMR and fluorescence spectra are investigated and discussed. The electronic absorption spectra of the hydroxy 4-aminoantipyrine Schiff bases Ib and Ie as well as the fluorescence spectra of Ie are studied in the organic solvents of different polarity. The UV-vis absorption spectra of 4-aminoantipyrine Schiff bases Ib, Id and Ie are investigated in aqueous buffer solutions of varying pH and utilized for the determination of pK(a) and DeltaG of the ionization process. The reactions of the hydroxy compounds Ib and Ie with Ni(II) and Cu(II) ions are also studied. The results of spectral studies are supported by some molecular orbital calculations using an atom superposition and electron delocalization molecular orbital theory for a compound Ib.