Increasing the solubility of drugs through cyclodextrin complexation

The bioavailability of pharmaca which dissolve in water only with difficulty is very limited. The cyclodextrins /CDs/, and primarily -CD and -CD, were successfully applied to increase the dissolution characteristics and hence the bioavailability of drugs: furosemide, hydrochlorothiazide, mebendazole, metronidazole, spironolactone, tofisopam, vinpocetine base, etc. From these pharmaca, products were made by mixing, kneading, grinding, freeze-drying, spray-embedding and precipitation.The more important factors on which the dissolution and bioavailability of the drugs depend are concluded.     

High-throughput,multiparameter analysis of single cells

Heterogeneity of cell populations in various biological systems has been widely recognized, and the highly heterogeneous nature of cancer cells has been emerging with clinical relevance. Single-cell analysis using a combination of high-throughput and multiparameter approaches is capable of reflecting cell-to-cell variability, and at the same time of unraveling the complexity and interdependence of cellular processes in the individual cells of a heterogeneous population. In this review, analytical methods and microfluidic tools commonly used for high-throughput, multiparameter single-cell analysis of DNA, RNA, and proteins are discussed. Applications and limitations of currently available technologies for cancer research and diagnostics are reviewed in the light of the ultimate goal to establish clinically applicable assays.

A PDMS-based biochip with integrated sub-micrometre position control for TIRF microscopy of the apical cell membrane

A poly(dimethylsiloxane) (PDMS)-based biochip with an integrated pressure controlled positioning system with sub-micrometre precision was realized. The biochip was easy and cheap to manufacture and enabled positioning in a wet environment. It allowed the application of total internal reflection fluorescence (TIRF) microscopy at the dorsal cell membrane, which is not adhering to a support. Specifically, the chip enabled TIRF microscopy at the apical membrane of polarized epithelial cells. Thereby, the device allowed us for the first time to monitor individual fusion events of GPI-GFP bearing vesicles at the apical membrane in live Madin-Darby canine kidney II (MDCK II) cells. Moreover, a mapping of fusion sites became feasible and revealed that the whole apical membrane is fusion competent. In total, the biochip offers an all-in-one solution for apical TIRF microscopy and contributes a novel tool to study trafficking processes close to the apical plasma membrane in polarized epithelial cells.     

Fluorogenic tagging of peptides via Cys residues using thiol-specific vinyl sulfone affinity tags

Fluorescent tagging of Cys-containing peptides is presented herein. The procedure follows a two-step sequential reaction scheme using thiol specific bifunctional chemical reporters and fluorogenic labels. Vinyl-sulfone bearing chemical reporters have been synthesized and demonstrated to selectively modify cysteine under physiological conditions in the presence of other nucleophilic amino acids. Bifunctional chemical reporters decorated with a terminal alkyne moiety, suitable for modification with azide containing fluorogenic labels were also synthesized. Such fluorogenic (turn on) labels in combination with these new vinyl-sulfone tags can be used generally in fluorescent modulation schemes of thiol-bearing biomolecules.     

Memory of chirality in the phthalimide photocyclization of adamantane dipeptides

Upon sensitized irradiation of N-phthalimido dipeptides containing l- or d-phenylalanine, enantioselective cyclization to diazamacrocycles takes place (ee >99%). The high optical purity of the products was explained by the memory of chirality effect. The chirality is preserved owing to the axial chirality of the biradical intermediate formed. An insight into the origin behind the enantioselective cyclization of the intermediate was given by density functional calculations. The very high enantiomeric excess in this type of photocyclization establishes it as a new method for the enantioselective synthesis of different large aza-heterocycles.     

Frequency assignment in a SDMA satellite communication system with beam decentring feature

In satellite communication, Spatial Division Multiple Access (SDMA) has become one of the most promising techniques that can accommodate continuing increase in the number of users and traffic demands. The technology is based on radio resource sharing that separates communication channels in space. It relies on adaptive and dynamic beam-forming technology and well-designed algorithms for resource allocation among which frequency assignment is considered. This paper studies static Frequency Assignment Problem (FAP) in a satellite communication system involving a satellite and a number of users located in a service area. The objective is to maximize the number of users that the system can serve while maintaining the signal to interference plus noise ratio of each user under a predefined threshold. Traditionally, interference is treated as fixed (binary interferences or fixed minimal required separation between frequencies) . In this paper, the interference is cumulative and variable. To solve the problem, we work on both discrete and continuous optimizations. Integer linear programming formulations and greedy algorithms are proposed for solving the discrete frequency assignment problem. The solution is further improved by beam decentring algorithm which involves continuous adjustment of satellite beams and deals with non-linear change of interference.     

Measurements of the D(sJ) resonance properties

We report measurements of the properties of the D(+)(sJ)(2317) and D(+)(sJ)(2457) resonances produced in continuum e(+)e(-) annihilation near sqrt[s]=10.6 GeV. The analysis is based on an 86.9 fb(-1) data sample collected with the Belle detector at KEKB. We determine the masses to be M(D(+)(sJ)(2317))=2317.2+/-0.5(stat)+/-0.9(syst) MeV/c(2) and M(D(+)(sJ)(2457))=2456.5+/-1.3(stat)+/-1.3(syst) MeV/c(2). We observe the radiative decay mode D(+)(sJ)(2457)-->D(+)(s)gamma and the dipion decay mode D(+)(sJ)(2457)-->D(+)(s)pi(+)pi(-) and determine their branching fractions. No corresponding decays are observed for the D(sJ)(2317) state. These results are consistent with the spin-parity assignments of 0(+) for the D(sJ)(2317) and 1(+) for the D(sJ)(2457).     

Mimicking a Superoxide Dismutase (SOD) Enzyme by copper(II) and zinc(II)-complexes

Mimicking the Superoxide Dismutase Enzyme (SOD), several imidazolato-bridged copper(II)-zinc(II) complexes were prepared, characterised by IR spectroscopy and their SOD enzyme activity was determined. 2,2′-Bipyridine, 2,2′:6′,2″-terpyridine and tris(2-aminoethyl)amine molecules were used on both metal sides, as coordinating ligands. The complex, containing the 2,2′:6′,2″-terpyridine ligand on copper side has the smallest SOD activity, which indicates the importance of the rigidity of the copper complex in SOD activity.     

Chemical nonhomogeneity of the electro-slag remelting steel measured by EPMA

The chemical and structural homogeneity of the electro-slag remelting (ESR) alloyed structural Cr-Ni-Mo steel (18H2N4MA) is investigated with electron probe microanalysis. The level of nonhomogeneity is expressed in terms of microsegregation coefficients (C_max/C_min of an investigated element) [1]. Microsegregation coefficients are higher for molybdenum than for chromium and vary from 1.5 to 2.05 for Mo and from 1.13 to 1.3 for Cr. Both at low (< 350 kg/h) and high (> 400 kg/h) melting rates, the increase of microsegregation is more pronounced for both elements investigated.