The cell-penetrating peptide TAT(48-60) induces a non-lamellar phase in DMPC membranes.

Cell-penetrating peptides (CPPs) are short polycationic sequences that can translocate into cells without disintegrating the plasma membrane. CPPs are useful tools for delivering cargo, but their molecular mechanism of crossing the lipid bilayer remains unclear. Here we study the interaction of the HIV-derived CPP TAT (48-60) with model membranes by solid-state NMR spectroscopy and electron microscopy. The peptide induces a pronounced isotropic (31)P NMR signal in zwitterionic DMPC, but not in anionic DMPG bilayers. Octaarginine and to a lesser extent octalysine have the same effect, in contrast to other cationic amphiphilic membrane-active peptides. The observed non-lamellar lipid morphology is attributed to specific interactions of polycationic peptides with phosphocholine head groups, rather than to electrostatic interactions. Freeze-fracture electron microscopy indicates that TAT(48-60) induces the formation of rodlike, presumably inverted micelles in DMPC, which may represent intermediates during the translocation across eukaryotic membranes.     

Mössbauer study on thermal decomposition of some hydroxy iron(III) carboxylates

Thermal decomposition of some hydroxy iron(III) carboxylates, i.e., iron(III) lactate, Fe(CH₃CHOHCOO)₃, iron(III) tartrate, Fe₂(C₄H₄O₆)₃ and iron(III) citrate, Fe(C₆H₅O₇) · 5H₂O has been studied in static air atmosphere in the temperature range 298–773 K employing Mössbauer, infrared spectroscopies and themogravimetric methods. The compounds directly decompose to -Fe₂O₃ without undergoing reduction to iron(II) intermediates. An increase in particle size of -Fe₂O₃ has been observed with increasing decomposition temperature. The thermal stability follows the sequence: iron(III) tartrate > iron(III)citrate > iron(III)lactate.     

Monofluoroalkene-Isostere as a 19F NMR Label for the Peptide Backbone: Synthesis and Evaluation in Membrane-Bound PGLa and (KIGAKI)3

Solid-state ¹⁹F NMR is a powerful method to study the interactions of biologically active peptides with membranes. So far, in labelled peptides, the ¹⁹F-reporter group has always been installed on the side chain of an amino acid. Given the fact that monofluoroalkenes are non-hydrolyzable peptide bond mimics, we have synthesized a monofluoroalkene-based dipeptide isostere, Val-Ψ[(Z)-CF=CH]-Gly, and inserted it in the sequence of two well-studied antimicrobial peptides: PGLa and (KIGAKI)₃ are representatives of an α-helix and a β-sheet. The conformations and biological activities of these labeled peptides were studied to assess the suitability of monofluoroalkenes for ¹⁹F NMR structure analysis.     

Mild Organic Ammonium Tribromide–Mediated Regioselective Ring Opening of Epoxides with Alcohols,Water, Acetic Anhydride,and Amines Under Solvent-Free Reaction Conditions

Organic ammonium tribromide (OATB), N-methylpyrrolidine-2-one hydrotribromide (MPHT) was found to be an efficient catalyst for the regioselective ring opening of epoxides with various nucleophiles under solvent free conditions. This procedure occurs under neutral and mild reaction conditions with out adding any additive and afforded high yields of products.

Synthesis of ferrites: Thermal analysis of some transition metal tris(maleato)ferrates(III)

Thermal analysis of some transition metal ferrimaleate precursors, M₃[Fe(mal)₃]₂·xH₂O (M=Mn, Co, Ni, Cu) has been studied in static air atmosphere from ambient to 600°C. Various physico-chemical techniques, i.e. TG, DTG, DTA, XRD, IR, Mössbauer spectrometry, have been employed to characterize both the intermediates and final products. After dehydration the anhydrous precursors undergo decomposition to yield an iron(II) intermediate, M[Fe^II(mal)₂] (M=Mn, Co, Ni, Cu) in the temperature range 160-275°C. A subsequent oxidative decomposition of iron(II) species leads to the formation of -Fe₂O₃ and MO in the successive stages. Finally a solid-state reaction occurs between the oxides above 400°C resulting in the formation of transition metal ferrites, MFe₂O₄. The ferrites have been obtained at much lower temperature and in less time than in the conventional ceramic method.This revised version was published online in November 2005 with corrections to the Cover Date.     

Microbial synthesis of gold nanoparticles: Current status and future prospects

Gold nanoparticles have been employed in biomedicine since the last decade because of their unique optical, electrical and photothermal properties. Present review discusses the microbial synthesis, properties and biomedical applications of gold nanoparticles. Different microbial synthesis strategies used so far for obtaining better yield and stability have been described. It also includes different methods used for the characterization and analysis of gold nanoparticles, viz. UV–visible spectroscopy, Fourier transform infrared spectroscopy, X ray diffraction spectroscopy, scanning electron microscopy, ransmission electron microscopy, atomic force microscopy, electron dispersive X ray, X ray photoelectron spectroscopy and cyclic voltametry. The different mechanisms involved in microbial synthesis of gold nanoparticles have been discussed. The information related to applications of microbially synthesized gold nanoparticles and patents on microbial synthesis of gold nanoparticles has been summarized.     

Physico-chemical studies on thermal analysis of cobalt hexa(formato)ferrate(III) decahydrate

Thermal decomposition of cobalt hexa(formato)ferrate(III) decahydrate, Co₃[Fe(HCOO)₆]₂. 10H₂O, has been studied up to 973 K in static air atmosphere, employing TG, DTG, DSC, XRD, ESR, Mössbauer and infrared spectroscopic techniques. Dehydration occurs in two stages in the temperature range of 340–430 K. Immediately after the removal of the last water molecule the anhydrous complex undergoes decomposition till -Fe₂O₃ and cobalt carbonate are formed at 588 K. In the final stage of remixing of cations, a solid state reaction between -Fe₂O₃ and cobalt carbonate leads to the formation of CoFe₂O₄ at a temperature (953 K) much lower than for the ceramic method. A saturation magnetization value of 2310 Gauss of ferrite (CoFe₂O₄) shows its potential to function at high frequencies.     

Daily requirements of Fe,Co and Se during infancy

The daily intakes of trace elements by infants showing optimal pattern of growth are used as the basis to estimate the requirements of Fe, Co and Se during infancy. Since milk is the only food and source of nutrition in the first few months of life, the requirements of these elements are calculated from their average concentrations in human milk and the volume of milk required to supply sufficient amount of energy for maintenance and healthy growth of infants. The concentrations of the three elements in human milk were determined, using the technique of neutron activation followed by radiochemical separation.     

Synthesis,Electrochemical and Antimicrobial Studies of Me6-Dibenzotetraazamacrocyclic Complexes of Ni(II) and Cu(II) Metal Ions

Russian Journal of Electrochemistry - Me6-dibenzotetraaza[14] annulene type macrocyclic complexes of Ni(II) and Cu(II) have been synthesized by template method and characterized by employing...     

Novel glitazones as PPARγ agonists: molecular design,synthesis, glucose uptake activity and 3D QSAR studies

Background

An alarming requirement for finding newer antidiabetic glitazones as agonists to PPARγ are on its utmost need from past few years as the side effects associated with the available drug therapy is dreadful. In this context, herein, we have made an attempt to develop some novel glitazones as PPARγ agonists, by rational and computer aided drug design approach by implementing the principles of bioisosterism. The designed glitazones are scored for similarity with the developed 3D pharmacophore model and subjected for docking studies against PPARγ proteins. Synthesized by adopting appropriate synthetic methodology and evaluated for in vitro cytotoxicity and glucose uptake assay. Illustrations about the molecular design of glitazones, synthesis, analysis, glucose uptake activity and SAR via 3D QSAR studies are reported.

Results

The computationally designed and synthesized ligands such as 2-(4-((substituted phenylimino)methyl)phenoxy)acetic acid derivatives were analysed by IR, ¹H-NMR, ¹³C-NMR and MS-spectral techniques. The synthesized compounds were evaluated for their in vitro cytotoxicity and glucose uptake assay on 3T3-L1 and L6 cells. Further the activity data was used to develop 3D QSAR model to establish structure activity relationships for glucose uptake activity via CoMSIA studies.

Conclusion

The results of pharmacophore, molecular docking study and in vitro evaluation of synthesized compounds were found to be in good correlation. Specifically, CPD03, 07, 08, 18, 19, 21 and 24 are the candidate glitazones exhibited significant glucose uptake activity. 3D-QSAR model revealed the scope for possible further modifications as part of optimisation to find potent anti-diabetic agents.

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