Tacrines as Therapeutic Agents for Alzheimer's Disease. V. Recent Developments

Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy. Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. Thus, the drug was withdrawn from the clinics administration. Since then, many publications have described non‐hepatotoxic tacrines, and in addition, important efforts have been made to design multitarget tacrines by combining their cholinesterase inhibition profile with the modulation of other biological targets involved in AD.     

Concentration of sodium ion as the determining factor for the association of dansyl amino acids with the teicoplanin molecule in reversed-phase liquid chromatography

The mechanism of the binding of D,L dansyl amino acids to teicoplanin was investigated. Na+ was used as an indicator of the interactions between the solutes and teicoplanin. The number (n) of sodium ions, Na+, excluded from the solute-teicoplanin interface when analyte transfer occurred was determined. A thermodynamic study and enthalpy-entropy compensation were performed to further explore the interaction mechanism. From these results, it was shown that teicoplanin was balanced between 2 conformational states characterized by distinct enantioselective properties. This approach indicates that liquid chromatography (LC) is a useful tool to extract physicochemical and molecular information from retention data. Thus, LC can be used as a complementary technique with the conventional techniques of molecular interaction analysis.     

The order-interval hypergraph of a finite poset and the König property

We study the hypergraph H(P) whose vertices are the points of a finite poset and whose edges are the maximal intervals in P (i.e. sets of the form I = {{v ε P: p ν q}}, p minimal, q maximal). We mention resp. show that the problems of the determination of the independence number , the point covering number τ, the matching number v and the edge covering number p are NP-complete. For interval orders we describe polynomial algorithms and prove the König property (v = τ) and the dual König property (a = p). Finally we show that the (dual) König property is preserved by product.     

The Uncountable Lattice of All Subfunctors of the Functor of Rational Representations

In set theory the cardinality of the continuum \(|{\mathbb R}|\) is the cardinal number of some interesting sets, like the Cantor set or the transcendental numbers. We will prove that the cardinal number of all subfunctors of the functor of rational representations \(k \otimes_{{\mathbb Z}} R_{{\mathbb Q}}\), taking values on odd order groups over the field k of characteristic 2, is equal to \(|{\mathbb R}|\). When the characteristic q?>?0 of the field k is not necessarily even, we will present a formula giving the dimension of the evaluations S _C,k(G), of the simple functor S _C,k, at any group G of order prime to q and being associated to a suitable cyclic group C.     

Quantitative study of fluorescence excitation and emission spectra of bean leaves

A quantitative and comprehensive knowledge of leaf fluorescence is required for the interpretation of fluorescence signals at the canopy level and also for the modelling of leaf and canopy fluorescence. In this work we present full range fluorescence excitation and emission spectra of intact leaves, expressed in units of apparent spectral fluorescence yield, from both the adaxial and the abaxial sides of the leaves, and for both front-side and back-side geometries. Emission spectra were measured for incident radiations in the blue and the green spectral range. The red/far-red fluorescence ratio depended on the measurement geometry and on the excitation wavelength. Excitation spectra were measured for emissions at 687 and 760 nm. When the abaxial side was illuminated, the measured spectra always had a larger intensity compared to adaxial side that is explained by the higher scattering of the spongy tissues. At 760 nm, the spectra had the same shape for front-side and back-side geometry, indicating that scattering predominated. At 687 nm, the shape of the spectra was very different for front-side and back-side geometry due to re-absorption of red fluorescence within the leaf. The comparison of excitation spectra measured from the adaxial or the abaxial side revealed differences in carotenoid absorption.     

Linear forms in logarithms and the mathematical method of diophantine equations: applications in chemistry and physics

Journal of Mathematical Chemistry - In this paper, we established the bound of n in term of p of the following equation $${\mathcal {F}}_n=2^p\quad {\text {with}}\quad n,p\ge 0 $$ where...     

Developing imprinted polymer nanoparticles for the selective separation of antidiabetic drugs

In this study, new molecularly imprinted polymer (MIP) nanoparticles are designed for selective recognition of different drugs used for the treatment of type 2 diabetes mellitus, i.e. sitagliptin (SG) and metformin (MF). The SG‐ and MF‐imprinted polymer nanoparticles are synthesized by free‐radical initiated polymerization of the functional monomers: methacrylic acid and methyl methacrylate; and the crosslinker: ethylene glycol dimethacrylate. The surface morphology of resultant MIP nanoparticles is studied by atomic force microscopy. Fourier transform infrared spectra of MIP nanoparticles suggest the presence of reversible, non‐covalent interactions between the template and the polymer. The effect of pH on the rebinding of antidiabetic drugs with SG‐ and MF‐imprinted polymers is investigated to determine the optimal experimental conditions. The molecular recognition characteristics of SG‐ and MF‐imprinted polymers for the respective drug targets are determined at low concentrations of SG (50–150 ppm) and MF (5–100 ppm). In both cases, the MIP nanoparticles exhibit higher binding response compared to non‐imprinted polymers. Furthermore, the MIPs demonstrate high selectivity with four fold higher responses toward imprinted drugs targets, respectively. Recycled MIP nanoparticles retain 90% of their drug‐binding efficiency, which makes them suitable for successive analyses with significantly preserved recognition features.     

Instability of the magnetohydrodynamics system at vanishing Reynolds number

The aim of this note is to study the dynamo properties of the magnetohydrodynamics system at vanishing R _m . Improving the analysis in Gérard-Varet (SIAM J Math Anal 37(3):815–840, 2006), we shall establish a generic Lyapunov instability result.     

Benzochromenopyrimidines: Synthesis,Antiproliferative Activity against Colorectal Cancer and Physicochemical Properties

Ten new differently substituted 3-benzyl-5-aryl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidin-4,6,11-triones 3 were synthesized by a simple and cost-efficient procedure in a one-pot, three-component reaction from readily available ethyl 2-amino-4-aryl-5,10-dioxo-5,10-dihydro-4H-benzo[g]chromene-3-carboxylates, benzylamine and triethyl orthoformate under solvent- and catalyst-free conditions. All the new compounds were screened for their antiproliferative activity against two colorectal-cancer-cell lines. The results showed that the compounds 3-benzyl-5-phenyl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3a) and 3-benzyl-5-(3-hydroxyphenyl)-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3g) exhibited the most potent balanced inhibitory activity against human LoVo and HCT-116 cancer cells.