Preparation of thin polymer films with drug release and protein adsorption resistance

Thin polymer films with the ability of both drug release and protein adsorption resistance were formed on silicon substrates and silica particles. The films were made of a block copolymer of poly(N-isopropylacrylamide) (p(AAm)) that can load and release drugs and poly(2-methoxyethyl methacrylate) (p(MEMA)) that can suppress protein adsorption. Aspirin and bovine serum albumin were respectively used as model substances for testing the abilities of the films to load and release drugs and to suppress protein adsorption. The films were immersed in a phosphate buffer saline (pH 7.4) for 100 days to evaluate their water resistance. The experimental results showed that the films have both drug release and protein adsorption resistance and are highly stable against PBS.     

Enantioselective arylative cyclization of allenyl aldehydes with arylboronic acids under Pd(II)-diphosphine catalysis

A Pd(OAc)2-SEGPHOS combination catalyzes the first enantioselective arylative cyclization of allenyl aldehydes with arylboronic acids to provide cis-fused five- and six-membered cyclic homoallylic alcohols. The excellent diastereo- and enantioselectivity and the fact that the reaction proceeds at room temperature in the absence of any additives make the process highly practical.     

Preparation and evaluation of orally rapidly disintegrating tablets containing taste-masked particles using one-step dry-coated tablets technology

In this study, in order to address the problems with manufacturing orally rapidly disintegrating tablets (ODT) containing functional (taste masking or controlled release) coated particles, such as the low compactability of coated particles and the rupture of coated membrane during compression, a novel ODT containing taste-masked coated particles (TMP) in the center of the tablets were prepared using one-step dry-coated tablets (OSDrC) technology. As a reference, physical-mixture tablets (PM) were prepared by a conventional tableting method, and the properties of the tablets and the effect of compression on the characteristics of TMP were evaluated. OSDrC was found to have higher tensile strength and far lower friability than PM, but the oral disintegration time of OSDrC is slightly longer than that of PM following high compression pressure. Consequently, OSDrC approaches the target tablet properties of ODT, whereas PM does not. The deformation of TMP in OSDrC due to compression is slight, and the release rate of acetaminophen (AAP) from OSDrC is the same as from TMP. However, TMP on the surface of PM are considerably deformed, and the release rate of AAP from PM is faster than from TMP. These findings suggest that OSDrC technology is a useful approach for preparing ODT containing functional coated particles. Furthermore, we demonstrate that the elastic recovery of tablets can affect differences in the properties of OSDrC, PM and placebo tablets (PC).     

Artificial Golgi apparatus: globular protein-like dendrimer facilitates fully automated enzymatic glycan synthesis

Despite the growing importance of synthetic glycans as tools for biological studies and drug discovery, a lack of common methods for the routine synthesis remains a major obstacle. We have developed a new method for automated glycan synthesis that employs the enzymatic approach and a dendrimer as an ideal support within the chemical process. Recovery tests using a hollow fiber ultrafiltration module have revealed that monodisperse G6 (MW = 58 kDa) and G7 (MW = 116 kDa) poly(amidoamine) dendrimers exhibit a similar profile to BSA (MW = 66 kDa). Characteristics of the globular protein-like G7 dendrimer with high solubility and low viscosity in water greatly enhanced throughput and efficiency in automated synthesis while random polyacrylamide-based supports entail significant loss during the repetitive reaction/separation step. The present protocol allowed for the fully automated enzymatic synthesis of sialyl Lewis X tetrasaccharide derivatives over a period of 4 days in 16% overall yield from a simple N-acetyl-d-glucosamine linked to an aminooxy-functionalized G7 dendrimer.     

Thermodynamics of the two-dimensional ferromagnetic Heisenberg spin systems

The problem of the title is studied by means of the Green function formalism with decoupling at a stage one-step further than Tyablikov's theory. At low temperatures the specific heat is proportional to the temperature T and the magnetic susceptibility to exp (constant/T)/T.     

Inventories of 239+240Pu, 137Cs, and excess 210Pb in sediment cores from brackish Lake Obuchi, Rokkasho Village, Japan

The aim of this study was to measure the distribution and inventories of ^239+240Pu, ¹³⁷Cs, and excess ²¹⁰Pb (²¹⁰Pb_excess) in sediment core samples from brackish Lake Obuchi, which is in the vicinity of nuclear fuel facilities in Rokkasho Village, Japan. The inventory of the ^239+240Pu activity in the sediment samples from the estuary of a freshwater river, the central point of the lake, and the deepest point in the lake were 0.18, 0.29, and 0.24 kBq·m^–2, respectively. The inventories of ¹³⁷Cs and ²¹⁰Pb_excess in sediments were 0.83–1.2 kBq·m^–2 and 25–30 kBq·m^–2, respectively. The mean ^239+240Pu/¹³⁷Cs and ²¹⁰Pb_excess/¹³⁷Cs activity ratios were 0.23 and 28, respectively. The^239+240Pu/¹³⁷Cs activity ratios were approximately 13–24 times the ratio expected from global fallout. The inventories of ^239+240Pu and ²¹⁰Pb in sediments were higher than the inventory expected from atmospheric fallout, but the ¹³⁷Cs inventory was significantly lower than expected.This revised version was published online in November 2005 with corrections to the Cover Date.     

Remarkable ligand effect on the palladium-catalyzed double carbonylation of aryl iodides

The use of t-Bu3P as a ligand dramatically improved the generality of the double carbonylation of aryl iodides, and Mo(CO)6 was also found to be effective as a CO source in the system.     

Seasonal variation of tropospheric aerosol properties by direct and scattered solar radiation spectroscopy

Long-term characterization of tropospheric aerosol has been carried out at Chiba, Japan, using a compact, stand-alone spectroradiometer under clear-sky conditions between August 2007 and March 2009. The spectra of direct solar radiation, aureole, and scattered solar radiation in various directions are observed in a wavelength range between 350 and 1050 nm with an optical resolution of 10 nm. Radiative transfer calculation using the MODTRAN4 code is employed to retrieve aerosol optical parameters such as aerosol optical depth (AOD), extinction coefficient, single-scattering albedo, scattering phase function, and asymmetry parameter, as well as water vapor column amount. The retrieved value of AOD varies in the range 0.1-0.5, while the water vapor column amount changes from 0.2 to 4 g/cm², showing reasonable agreements with the concurrent measurements with a sunphotometer and a microwave radiometer, respectively. The seasonal variation of the retrieved parameters indicates the major impacts of dust particles in spring, sea salt particles in summer, and anthropogenic fine particles in winter.