Antioxidant activity of phenolic compounds from extracts of Eucalyptus globulus and Melaleuca styphelioides and their protective role on D-glucose-induced hyperglycemic stress and oxalate stress in NRK-49Fcells

Phytochemicals serve as potential therapeutic agents for the prevention and treatment of diseases. In this study, we elucidate the renoprotective activity of compounds isolated from Eucalyptus globulus and Melaleuca styphelioides extracts in glucose- and oxalate-challenged NRK-49F cell model. The antioxidant potential of isolated compounds was evaluated based on their effect on antioxidant enzyme activities and lipid peroxidation levels. The results demonstrated that exposure of NRK-49F cells to glucose and oxalate stress augmented cell damage and attenuated antioxidant enzyme activities. The phytochemicals 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-β-D-glucopyranoside, Cornusiin B and tellimagrandin I treatment restored antioxidant enzyme activity, significantly lowered lipid peroxidation levels and effectively protected cells from glucose and oxalate stress equivalent to the known antioxidant, N-acetyl cysteine. Pterocarinin A significantly reversed cellular damage owing to glucose stress. In conclusion, the compounds isolated from E. globulus and M. styphelioides showed potential cytoprotective and anti-oxidative property against glucose- and oxalate-induced oxidative stress in NRK-49F cells.     

Oxidative macrocyclocondensation of 3,4-diaminofurazan and 4,4′-diamino-3,3′-azofurazan with dibromoisocyanurate. Crystal structures of hexa- and octadiazenofurazan macrocycles

The oxidative cyclocondensation of 3,4-diaminofurazan and 4,4-diamino-3,3-azofurazan with dibromoisocyanurate afforded macrocyclec polydiazenofurazans. The reaction can be directed towards the formation of both the four-membered cycle alone or the three-, six-, and eight-membered macrocycles.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1250–1254, May, 1996.Deceased in 1995.     

Selective inhibition of 6-phosphogluconate dehydrogenase from Trypanosoma brucei

A number of triphenylmethane derivatives have been screened against 6-phosphogluconate dehydrogenase from Trypanosoma brucei and sheep liver. Some of these compounds show good inhibition of the enzymes and also selectivity towards the parasite enzyme. Modelling was undertaken to dock the compounds into the active sites of both enzymes. Using a combination of DOCK 3.5 and FLEXIDOCK a correlation was obtained between docking score and both activity for the enzymes and selectivity. Visualisation of the docked structures of the inhibitors in the active sites of the enzymes yielded a possible explanation of the selectivity for the parasite enzyme.     

Synthesis and Antimicrobial Evaluation of Some Chalcones and Their Derived Pyrazoles, Pyrazolines, Isoxazolines, and 5,6-Dihydropyrimidine-2-(1 H )-thiones

Chalcones were synthesized by a base catalyzed Claisen-Schmidt condensation reaction. Bromination of chalcones afforded the dibromo derivatives. Monobromo derivatives could be obtained by treating the corresponding dibromochalcones with dry benzene in the presence of triethylamine. Pyrazole derivatives were obtained by refluxing of dibromochalcones with phenylhydrazine or 2,4-dinitrophenylhydrazine in dry pyridine. Chalcones were treated with hydrazine hydrate or phenyl hydrazine in ethanol to afford Δ ²-pyrazolines and N-phenyl-Δ ²-pyrazolines. Condensation of chalcones with hydroxylamine hydrochloride or thiourea in ethanolic sodium hydroxide solution gave 4,5-dihydroisoxazoles and 5,6-dihydropyrimidine-2-(1H)-thiones. The prepared compounds were tested for antimicrobial activity against four different bacterial species displaying different degrees of antibacterial activities or inhibitory actions.     

Analysis of glycolytic intermediates in Saccharomyces cerevisiae using anion exchange chromatography and electrospray ionization with tandem mass spectrometric detection

The purpose of this study is to selectively and quantitatively analyze several glycolytic intermediates in cells of Saccharomyces cerevisiae using high-performance anion exchange chromatography (HPAEC) coupled to electrospray ionization tandem mass spectrometry for the analysis. A sodium hydroxide gradient is used to separate the glycolytic compounds and after the column sodium hydroxide is reduced by proton exchange with a membrane device prior to introduction to the mass spectrometer. The detection limits for 10 μl samples are down to the 0.4–5 pmol range. This corresponds for the intracellular metabolites to a range of 2–20 nmol per gram biomass dry weight (DW). Standard addition did reveal some influence of the sample matrix on the measured concentrations. Separation and analysis is hardly affected by the high sulfate and phosphate concentrations (1 mM) in the fermentation medium and by the intracellular matrix. Validation of the glucose-6-phosphosphate LC–MS–MS analysis results with enzymatic analysis showed an excellent agreement between the two methods. The suitability of the method was clearly shown by analyzing a series of steady state S. cerevisiae samples from a carbon limited aerobic chemostat culture.     

Inner-sphere oxidation of ethylenediaminetetraacetatocobaltate(II) by N-bromosuccinimide

Summary The kinetics of oxidation of [Co^II(EDTA)]^2- (EDTA = ethylenediaminetetraacetate) by N-bromosuccinimide (NBS) in aqueous solution obey the equation: Rate = k ₂ K ₃[Co^II]_T[NBS]/{1 + [H⁺]/K ₂ + K ₃[NBS]} where k ₂ is the rate constant for the electron-transfer process, K ₂ the equilibrium constant for the dissociation of [Co^II(EDTAH)(H₂O)]^– to [Co^II(EDTA)(OH)]^3– and K ₃ the pre-equilibrium formation constant. The activation parameters are reported. It is proposed that electron transfer proceeds via an inner-sphere mechanism with the formation of an intermediate which slowly generates hexadentate[Co^III(EDTA)]^–.Abstracted from the M.Sc. thesis of Eman S. H. Khaled.     

A Comparative Study of Fluorescein Isothiocyanate-Encapsulated Silica Nanoparticles Prepared in Seven Different Routes for Developing Fingerprints on Non-Porous Surfaces

Preparation of fluorescein isothiocyanate (FITC)-encapsulated silica nanoparticles (F-SiNPs) via seven different approaches to be used as developing agents for fingerprints detection is presented in this report. In this study, the suitability of each synthesis route toward incorporation of the selected fluorophore into silica matrix and its efficiency in fingerprints detection were systematically studied. The composition of the particles was designed to examine the hydrophobic and dipole-dipole interactions between the silicate backbone and both of the fluorescent reporter molecules and the fingerprint residues. F-SiNPs were prepared with two conventional sol-gel approaches; the Stöber method and the water in oil reverse microemulsion (WORM) method. The alkoxysilane precursor, tetraethoxyorthosilicate (TEOS) and its binary mixtures with phenyltriethoxysilane (PTEOS) or 3-aminopropyl triethoxysilane (APTES) have been used in preparing the F-SiNPs to study the effect of nanoparticles composition on fingerprints development. In addition, FITC was conjugated with APTES so it can be covalently bonded to the silica matrix and to be compared with non-covalently FITC-doped SiNPs. Moreover, the enhancement effect of introducing polyvinylpyrrolidone (PVP) onto the surface of the less hydrophobic F-SiNP on fingerprints detection on different non-porous surfaces was also investigated. The mean diameters of the F-SiNPs were between 4.1?±?0.6 and 110.4?±?31.1 nm as obtained from the TEM size measurement for the nanoparticles prepared by the WORM and Stöber methods, respectively. The obtained results clearly highlight the advantages of using a mixture of TEOS and PTEOS alkoxysilane precursors in preparing F-SiNPs with remarkable encapsulation efficiency and clear detection of fingerprints due to efficient embedding of the fluorophore inside the silica network even without conjugation. It was also observed that both the Stöber and WORM methods can be used in preparing the F-SiNPs developing agents and that PVP coated particles did not show any significant enhancement in fingerprints visualization.     

Optical properties,structural, and DFT studies of Pd(II) complexes with 1-phenyl-1H-tetrazol-5-thiol,X-ray crystal structure of [Pd(κ1-S-ptt)2(κ2-dppe)] complex

Seven tetrazole-thione complexes, [Pd₂(κ²-ptt)₄]( 1 ), trans-[Pd(k¹-S-ptt)₂(PPh₃)₂] ( 2 ), trans-[Pd(k¹-S-ptt)₂(SPPh₃)₂] ( 3 ), trans-[Pd(k¹-S-ptt)₂(OPPh₃)₂] ( 4 ), [Pd(k¹-N-ptt)₂(k²-dppe)] ( 5a ), [Pd(k¹-S-ptt)₂(k²-dppe)] ( 5b ), [Pd(k¹-S-ptt)₂(k²-dppeS₂)] ( 6 ), and [Pd(k¹-S-ptt)₂(k²-dppeO₂)] ( 7 ), were prepared from 1-phenyl-1H-tetrazole-5-thiol (Hptt), with substituted phosphines. These complexes were investigated by CHNS analysis; infrared (IR), nuclear magnetic resonance (NMR) (¹H and ³¹P), and ultraviolet–visible (UV–Vis) spectroscopy; and single-crystal X-ray data for 5b . In Complex 1 , the ptt⁻ ligand adopted μ²- k-N, k-S bridging mode to afford a dimeric complex, whereas in Complexes 2–4 , 6 , and 7 , the ptt⁻ was covalently coordinated via sulfur atom of the thiol group as a solo product. In contrast, in Complex 5 , the ptt⁻ ligand was bonded in a monodentate fashion through a deprotonated tetrazole ring nitrogen atom in isomer 5a or via a thiolato sulfur atom in isomer 5b . These linkage isomers were clearly shown in the ³¹P-{¹H} NMR. To explain the adoption of the ligand binding modes in Complexes 5a and 5b , geometry optimization calculations were carried out on two isomers. Very small differences of all molecular parameters were found between 5a and 5b isomers. This confirms the reason for obtaining two isomers. Also, theoretical studies are made for all compounds, and excellent agreement is obtained with experimental data. The direct band gap (Eg) values are equal to 2.88, 2.85, and 2.45 eV for Complexes 1 , 2 , and 4 , respectively, revealing a semiconductor nature. The inhibition activity of Complexes 1–3 , 5 , and 8 were evaluated versus the growth of four types of bacteria in vitro. The complexes showed a good activity compared with free ligand and a standard antibiotic.     

Structural characterization,thermal investigation and biological activity of metal complexes containing Schiff Base ligand (Z)‐3‐(1‐((4,6‐dimethyl‐1H‐pyrazolo[3,4‐b] pyridin‐3‐yl)imino)ethyl)‐4‐hydroxy‐6‐methyl‐2H‐pyran‐2‐one

A new series of metal complexes containing Co(II), Pd(II), Fe(III) chloride and Cu(II) salts (chloride, bromide, sulphate and perchlorate) have been prepared with Schiff base ligand ( HL ). The synthesized compounds were elucidated using elemental analyses, spectral techniques, molar conductance, magnetic measurements and thermogravimetric studies. The analytical data established (1 M:1 L) stoichiometry for complexes ( 1 ), ( 2 ), ( 4 ), ( 6 ) and ( 7 ) as well as (1 M:2 L) and (2 M:3 L) stoichiometry for complexes ( 5 ) and ( 3 ), respectively. As a result, the ligand HL coordinates in complexes ( 1 ), ( 2 ), ( 4 ), ( 6 ) as a monobasic tridentate ONN moiety via the oxygen atom of the deprotonated phenolic OH, the nitrogen atoms of the azomethine and the imine group in pyrazolopyridine ring. While, it behaves as a neutral bidentate in complexes ( 3 , 7 ), chelates via oxygen and nitrogen atoms of enolic OH and azomethine groups. Also, in complex ( 5 ) Cu²⁺ ion binds via NO sits of two ligand molecules in its monobasic and neutral forms. The magnetic moment and electronic spectral data proposed octahedral structure for complexes ( 2 , 3 and 7 ) as well as triagonal bipyramidal and square pyramidal geometry for complexes ( 1 and 4 ), while, chelates ( 5 ) and ( 6 ) possess square planar geometry. TG/DTG studies confirmed the chemical formula for these complexes and established the thermal decomposition processes ended with the formation of metal or metal oxides contaminated with carbon residue. An axial electron spin resonance spectra were suggested for Cu(II) complexes pointing to ²B_1g as a ground state with hyperfine structure for complex ( 4 ). In vitro antibacterial and antioxidant activities were performed for HL ligand and its metal complexes. The biological studies indicate that complex ( 3 ) has better antibacterial activity compared to the ligand and the other complexes.     

5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation

A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, ¹H-NMR, and ¹³C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.