Alkyl Ammonium Ion Selectivity of Hexahomotrioxacalix[3]arene Triamide Derivative having the Intramolecular Hydrogen-Bonding Group

The lower rim functionalized hexahomotrioxacalix[3]arene triamide 4 with cone-conformation was synthesized from triol 1 by a stepwise reaction. The different extractability for alkali metal ions, transition metal ions, and alkyl ammonium ions from water into dichloromethane is discussed. Due to the strong intramolecular hydrogen bonding between the neighboring NH and CO groups in triamide 4, its affinity to metal cations was weakened. Triamide 4 shows a single selectivity to n-BuNH ₃ ⁺ . The anion complexation of triamide 4 was also studied by ¹H NMR titration experiments. Triamide 4 binds halides through the intermolecular hydrogen bonding among the NH hydrogens of amide in a 1:1 fashion in CDCl₃. The association constants calculated from these changes in chemical shifts of the amide protons are K _a = 223 M^?1 for Cl^? and K _a = 71.7 M^?1 for Br^?. Triamide 4 shows a preference for Cl^? complexation than Br^? complexation.     

Depigmenting activity and low cytotoxicity of alkoxy benzoates or alkoxy cinnamte in cultured melanocytes

To obtain effective and safe topical depigmenting agents, we synthesized hydroxybenzoates, alkoxybenzoates, and 3,4,5-trimethoxycinnamate containing a thymol moiety and screened then for high-level inhibitory activity against melanin synthesis in cultured melanocytes. Eight compounds were tested for their depigmenting effect and cytotoxicity using a murine melanocyte cell line. We found that 3,4,5-trialkoxybenzoates and 3,4,5-trimethoxycinnamate, synthesized by conjugating 3,4,5-trialkoxybenzoic acids and 3,4,5-trimethoxycinnmic acid with thymol, showed a potent depigmenting effect and low cytotoxicity. Compound 4h, 5-methyl-2-(methylethyl)phenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate, showed the most potent depigmenting effect (IC50=10 microM) with low cytotoxicity (IC50=200 microM).     

The characteristics of integrins expression in decidualized human endometrial stromal cell induced by 8-Br-cAMP in in vitro

Integrins are heterodimeric glycoproteins that have been found to undergo dynamic temporal and spatial changes in the endometrium during the menstrual cycle and in early pregnancy. Specificity of integrins is known to be different in human endometrial stromal cells and decidual cells. These shifts of integrins suggested to play an important role in embryo implantation and can be modulated by progesterone, cAMP derivatives, and cytokines. The mechanisms of decidualization and its precise physiological role are still not clearly understood and in vitro systems could provide an alternative that overcomes limitations of studying such complex biological phenomena in vivo at the time of implantation. This study was undertaken to establish an in vitro model system for human decidualization using 8-bromo-cAMP and to investigate the characteristics of stromal integrin expression in vitro by 8-Br-cAMP. Endometrial stromal cells were isolated and cultured, and then were induced to decidualize by 0.5 mM 8-Br-cAMP for 15 days. Immunofluorescence staining and flow cytometric analyses of the integrin subunits (alpha1, alpha4, alpha5, alpha6, beta1 and alphavbeta3) were performed at day 9. In the presence of 8-Br-cAMP, the staining intensity of alphavbeta3 was significantly higher than control and measurements for alpha1, alpha4, alpha5, alpha6, and beta1 were similar. Immunofluorescent localization of the integrins reflected the differences obtained from the flow cytometric analyses described above. In summary, the expression of alphavbeta3 integrin increased in stromal cells in vitro decidualized by 8-Br-cAMP and this up-regulation of alphavbeta3 integrin expression during decidualization might influence on human implantation.     

Spectrophotometric determination of dissociation constants for propionic acid and 2,5-dinitrophenol at elevated temperatures

Using the temperature dependence of pK_a for acetic acid, the pK_a for 2,5-dinitrophenol have been spectrophotometrically determined in acetate buffer at elevated temperatures under the saturation vapor pressures. For 2,5-dinitrophenol $$pK_a = - 33.206 + 2106.7/T + 5.495\ln T$$ where T is in Kelvin. Similarly, pK_a values of propionic acid were obtained at temperatures from 25°C to 175°C producing $$pK_a = - 43.703 + 2128.6/T + 7.2686\ln T$$ From this result, several thermodynamic functions of propionic acid were calculated and compared with those obtained from emf measurement.     

A remark on nilpotent Lie Algebras

Letf(n) denoted the number of essential parameters which are needed to classifyn-dimensional nilpotent Lie Algebras over the complex number field. Then $f(2n) \geqslant \tfrac{{n(n2 - 7)}}{6} - 2$ .