Roles of adriamycin and adriamycin dimer in antitumor activity of the polymeric micelle carrier system

Adriamycin (ADR) dimer was prepared and its antitumor activity was evaluated with mouse colon adenocarcinoma 26 (C 26). As compared with original ADR, the dimer did not show significant antitumor activity, either in vitro or in vivo. Furthermore, polymeric micelles containing varied ratios of the dimer to the original ADR were prepared. Polymeric micelles with a higher dimer/ADR ratio (9.7) showed significant antitumor activity, but the effective dose shifted higher. Effective doses were found to largely depend on the concentration of the original ADR, rather than that of the dimer at the tumor sites. Therefore, it was presumed that the original ADR played a major role in antitumor activity, and the dimer played a supplementary role to contribute selective delivery of ADR to the tumor sites.     

Multiple binding of inhibitors in the complex formed by bovine trypsin and fragments of a synthetic inhibitor, 4-[4-(N,N- dimethylcarbamoxylmethoxycarbonylmethyl)phenoxycarbonylphenyl+ ++] guanidinium methanesulfonate (FOY-305)

The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity data were collected to 1.8 A resolution. The structure was solved by molecular replacement methods, and refined to an R-factor = 18.0% for 14364 reflections by the restrained least-squares method. The final difference Fourier maps revealed that hydrolyzed inhibitor fragments bind with the protein at multiple sites around the active center of trypsin. The structural feature in the crystalline state probably corresponds to a statistical average of several complexes which would be formed between the inhibitor and trypsin during the binding and releasing process in solution.     

Decomposition of Pt-intercalated hydrotalcite-like nanocomposites to produce micro/mesoporous catalysts

Platinum intercalated into a hydrotalcite-like solid, Mg0.74Al0.26(OH)2(NO3)0.26, was found to catalytically reduce interlayer nitrate (NO3-) to N2/N2O so as to give rise to a large surface area micro/mesoporous structure at lower temperature of ca. 300 degrees C, compared to 500 degrees C required for the decomposition of the pristine hydrotalcite phase.     

Photoreaction of N-(ω-indol-3-ylalkyl)phthalmides: intramolecular oxetane formation of the aromatic imide system.

Photoreaction of N-(ω-indol-3-ylalkyl)phthalimides ($\text{1a}$ and $\text{1c}$) gave oxeto[2,3-b]indoles ($\text{3a}$ and $\text{3c}$), the first example of oxetane formation of the aromatic imide carbonyl in the Paterno-Buchi reaction.     

Visible light photoelectrochemical activity of K4Nb6O17 intercalated with photoactive complexes by electrostatic self-assembly deposition

Electrostatic self-assembly deposition (ESD) results in the intercalation of Ru(bpy)₃²⁺ or methylene blue (MB) into the niobate layered oxide right after the cations come into contact with [Nb₆O₁₇]⁴⁻ nanosheets. Monolayers can be obtained by the exfoliation of proton exchanged K₄Nb₆O₁₇ (KNbO) in an aqueous tetrabutylammonium (TBA) solution as revealed by the atomic force microscopy micrographs. UV-vis spectra show that intercalated films are able to absorb in the visible light range. Heat-treatment of Ru(bpy)₃²⁺ resulted in the red-shift in the absorption spectra, which was assigned to the enhancement in the interaction between the complex molecules and [Nb₆O₁₇]⁴⁻ host layer. Intercalated niobate layered oxides are able to produce photocurrent as a result of the electron transfer from the excited guest molecule to the host layer under visible light illumination. Ru(bpy)₃²⁺ intercalated niobate layered oxide shows photocatalytic activity under visible light illumination to produce H₂ from water-methanol solution.     

Studies on the constituents of Juglans species. I. Structural determination of (4S)- and (4R)-4-hydroxy-alpha-tetralone derivatives from the fruit of Juglans mandshurica MAXIM. var. sieboldiana MAKINO

Four enantiomerically pure new alpha-tetralones, (4S)- and (4R)-5-hydroxy-4-methoxy-alpha-tetralones and (4S)- and (4R)-5,8-dihydroxy-4-methoxy-alpha-tetralones were isolated, together with five known ones, (4S)- and (4R)-4,8-dihydroxy-alpha-tetralones, (4S)-4,8-dihydroxy-5-methoxy-alpha-tetralone and (4S)- and (4R)-4-hydroxy-alpha-tetralones, from the fruit of Juglans mandshurica MAXIM. var. sieboldiana MAKINO. Their structures were established on the basis of spectral analysis. To the best of our knowledge, this is the first isolation of the (4R)-4-hydroxy-alpha-tetralone derivative from Juglans species.     

Edge-Defined Film-Fed (EFG) Growth of Rare-Earth Orthovanadates REVO4 (RE=Y,Gd): Approaches to Attain High-Quality Shaped Growth

In spite of their superior laser and polarizer properties rare-earth orthovanadates (REVO₄) single crystals have not been adopted yet into extensive industrial applications because of crystal growth difficulties. The main problems of CZ technique are compositional change and diameter instability. This work presents the first attempt to apply the edge-defined film-fed growth (EFG) technique by which well-shaped REVO₄crystals have been grown directly. The capillary properties of YVO₄ and GdVO₄ melt have been measured. The applicability of shaped growth for rare-earth orthovanadate family was approved by successful EFG growth of transparent rod-like macro-defect-free single crystals of YVO₄ and GdVO₄. We address two main approaches to enhance the quality of EFG crystals: (i) meniscus and crystal shape stability dependence on die top shape and (ii) the strategy of effective operating control. Concave die top was found to be the best choice for high-quality EFG growth of REVO₄ along [001] direction. The spectral analysis of weight signal from growing crystal was shown to be a useful feedforward clue to prevent crystallinity degradation at a very early stage. A reasonable stability of the EFG process was achieved using [211], [101], [001] and [100] pulling directions.