Thermal and structural properties of KPO3·Ln(PO3)3 glasses (Ln=rare earth ion)

Glass transition temperatures T_g and Raman spectra of KPO₃·Ln(PO₃)₃ (Ln=rare earth ion) glasses were measured for all rare earth members (except Pm). From the series behavior of the T_g and Raman data, it is concluded that the coordination number around rare earth ions changes, probably from nine to eight, in the middle of the rare earth series.     

Design and synthesis of potent antitumor 5,4'-diaminoflavone derivatives based on metabolic considerations

Recently, we reported that 5,4'-diaminoflavone (1) exhibits potent and specific growth-inhibitory activity against the estrogen receptor (ER)-positive human breast cancer cell line MCF-7. However, when compound 1 was incubated with S-9 mix, its metabolites were observed. Moreover, addition of S-9 mix to the medium caused the drastic decrease in activity of compound 1. Since the 6-, 8-, and 3'-positions were considered to be metabolized oxidatively in vivo from MO calculations, a series of 5,4'-diaminoflavone derivatives substituted at such putative metabolic positions with various functional groups were synthesized aiming at the metabolically stable derivatives. Among them, 5,4'-diamino-6,8,3'-trifluoroflavone (14d) exhibited strong growth-inhibitory activity against MCF-7 cells even in the presence of S-9 mix. Moreover, orally administered compound 14d completely suppressed the growth of MCF-7 inoculated into nude mice, and the effect was more potent than that of compound 1. In addition to ER-positive breast cancer cells, compound 14d exhibited growth-inhibitory activity against a panel of human cancer cell lines including a part of ER-negative breast, endometrial, ovarian, and liver cancers. From these results, fluorine introduction to the putative metabolic positions of compound 1 was elucidated to be effective in the enhancement of the in vivo antitumor activity, probably due to the block of the metabolic deactivation.     

New cleavable surfactants derived from glucono-1,5-lactone

New amido nonionic cleavable surfactants were synthesized in good yields by the acetalization of glucono-1,5-lactone with octanal, 2-octanone or 2-undecanone, followed by amidation with monoethanolamine, diethanolamine or morpholine. These compounds possessed good water solubilities. The compounds derived from 2-octanone showed higher critical micelle concentrations than the compounds from octanal. For the same hydrophobic chain, both the micelle-forming property and the ability to lower surface tension increased with the change in the terminal amide group in the order diethanolamide<morpholide<monoethanolamide. Interestingly, in spite of their relatively short hydrophobic chains, these compounds showed greater ability to lower surface tension than conventional nonionic surfactants, such as alcohol ethoxylates. Furthermore, their acid-decomposition properties were determined. Their decomposition rates were also compared with that of the corresponding carboxylate type of compound derived from glucono-1,5-lactone.     

Isolation of intact transition protein 2 with three zinc finger motifs from boar late spermatid nuclei

Boar intact transition protein 2, TP2, was isolated from the late spermatid nuclei by chromatography on Fractogel EMD SO3- 650 (M), and HPLCs on Nucleosil 300 7C18, Diol-120 and Chemcosorb 3C18H. CD spectroscopy study showed that TP2 underwent a small but significant zinc dependent secondary structural change. TP2, having three potential zinc finger motifs, was shown to be contain 3 atoms of zinc bound per molecule of the protein by atomic absorption spectroscopy. These results together with the amino acid sequence of TP2 suggest that TP2 is a zinc metalloprotein with three zinc finger structures.     

Nondestructive sizing of a 3D surface crack generated in a railway component using closely coupled probes for direct-current potential drop technique

The direct-current potential drop technique was applied to the quantitative estimation of the size and shape of the crack generated in railway components. First, calibration equations that relate the potential drop to the crack depth and crack length along with its location were derived where the boundary element method was used for the electric potential problem. The crack depth, crack length and its location were then determined by analyzing an inverse problem by using the quasi-Newton method which compared the potential drop obtained by the calibration equations with measurements using a carbon steel specimen containing a crack. Although the values of depths were slightly scattered because depth estimations were sensitive to the crack location and changed with even a minimal change in distance between the crack and probes, the estimations of lengths and locations were adequate.     

Clinical and pathological significance of numerical aberrations of chromosomes 11 and 17 in colorectal neoplasms

Numerical chromosome aberrations by interphase cytogenetic analysis have been reported in a few samples of colorectal neoplasms. No studies have defined a distinct relationship between these aberrations and clinicopathological features. To investigate the chromosome aberrations as a marker of invasiveness or prognosis, we conducted an interphase cytogenetic study using fluorescence in situ hybridization and examined 142 colorectal neoplasms consisting of 15 adenomas and 127 cancers. The target chromosomes were chromosomes 11 and 17. We also evaluated the nuclear DNA content as detected by flow cytometry, analyzed the relationship between the frequency of aneusomy and clinicopathological features, and examined the survival rate in these patients. The loss of chromosome 11 was observed in 31% of adenomas, whereas in cancers DNA aneuploidy was observed in 63% of cases, a gain of chromosome 17 was observed in 63% of cases, and a gain of chromosome 11 was observed in 42% of cases. Numerical chromosome aberrations in diploid DNA were also observed. Increased depth of invasion (>/=T3) and advanced Dukes' stage (>/=B) of malignant tumors were associated with a higher frequency of a gain of chromosome 11 (P < 0.01 and P < 0.05, respectively). Increased depth of invasion (>/=T2) in cancers was associated with a higher frequency of a gain of chromosome 17 (P < 0.05). Multivariate analysis of postoperative survival showed that a loss or gain of chromosome 11 was independently associated with a poor prognosis (P < 0.05). Numerical chromosome aberrations appear prior to the alteration of nuclear DNA content as detected by flow cytometry and influence the progression of colorectal cancers. Aneusomy of chromosome 11 is associated with poor postoperative prognosis of primary colorectal cancers.