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Volume 64, Issue 1
Displaying 1-13 of 13 articles from this issue
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Review
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Youhei Sohma2016 Volume 64 Issue 1 Pages 1-7
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLThe aggregation of peptides/proteins is intimately related to a number of human diseases. More than 20 have been identified which aggregate into fibrils containing extensive β-sheet structures, and species generated in the aggregation processes (i.e., oligomers and fibrils) contribute to disease development. Amyloid-β peptide (designated Aβ), related to Alzheimer’s disease (AD), is the representative example. The intensive aggregation property of Aβ also leads to difficulty in its synthesis. To improve the synthetic problem, we developed an O-acyl isopeptide of Aβ1–42, in which the N-acyl linkage (amide bond) of Ser26 was replaced with an O-acyl linkage (ester bond) at the side chain. The O-acyl isopeptide demonstrated markedly higher water-solubility than that of Aβ1–42, while it quickly converted to intact monomer Aβ1–42 via an O-to-N acyl rearrangement under physiological conditions. Inhibition of the pathogenic aggregation of Aβ1–42 might be a therapeutic strategy for curing AD. We succeeded in the rational design and identification of a small molecule aggregation inhibitor based on a pharmacophore motif obtained from cyclo[-Lys-Leu-Val-Phe-Phe-]. Moreover, the inhibition of Aβ aggregation was achieved via oxygenation (i.e., incorporation of oxygen atoms to Aβ) using an artificial catalyst. We identified a selective, cell-compatible photo-oxygenation catalyst of Aβ, a flavin catalyst attached to an Aβ-binding peptide, which markedly decreased the aggregation potency and neurotoxicity of Aβ.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1278K) Full view HTML
Communication to the Editor
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Fuyuhiko Inagaki, Yasuhiko Okada, Chiaki Matsumoto, Masayuki Yamada, K ...2016 Volume 64 Issue 1 Pages 8-13
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
Advance online publication: November 20, 2015
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Supplementary materialFrom an economic and ecological perspective, the efficient utilization of atmospheric CO2 as a carbon resource should be a much more important goal than reducing CO2 emissions. However, no strategy to harvest CO2 using atmospheric CO2 at room temperature currently exists, which is presumably due to the extremely low concentration of CO2 in ambient air (approximately 400 ppm=0.04 vol%). We discovered that monoethanolamine (MEA) and its derivatives efficiently absorbed atmospheric CO2 without requiring an energy source. We also found that the absorbed CO2 could be easily liberated with acid. Furthermore, a novel CO2 generator enabled us to synthesize a high value-added material (i.e., 2-oxazolidinone derivatives based on the metal catalyzed CO2-fixation at room temperature) from atmospheric CO2.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1100K) Full view HTML
Regular Articles
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Tamami Haraguchi, Takahiro Uchida, Mai Hazekawa, Miyako Yoshida, Masak ...2016 Volume 64 Issue 1 Pages 14-20
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLThe purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor using a bitterness-responsive membrane (C00). The effect of topiramate on the taste characteristics of the foods/drinks themselves was also evaluated by taste sensor outputs. The viscosities of the foods/drinks and the influence of the lactic acid and orotic acid components of yoghurt, the most successful of the tested substances in taste masking, on the bitterness of topiramate were also measured. Yoghurt was predicted to be the most effective of the foods/drinks tested in reducing the acidic bitterness-responsive sensor output of topiramate. The outputs of the astringency sensor, sourness sensor, and saltiness sensor to yoghurt were not reduced by the addition of topiramate. The viscosity and lactic acid and orotic acid components of yoghurt seemed to be the keys in reducing the bitterness of topiramate. Yoghurt is predicted to be the food/drink most capable of reducing the bitterness of topiramate without losing the taste of the food/drink itself.Graphical Abstract Fullsize ImageView full abstractDownload PDF (851K) Full view HTML -
Lixia Wang, Shiwei Yang, Jinli Cao, Shaohua Zhao, Wuwei Wang2016 Volume 64 Issue 1 Pages 21-26
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLThe coacervation between gelatin and sodium alginate for ginger volatile oil (GVO) microencapsulation as functions of mass ratio, pH and concentration of wall material and core material load was evaluated. The microencapsulation was characterized by scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), and thermal gravimetric analysis (TGA). SEM and FT-IR studies indicated the formation of polyelectrolyte complexation between gelatin and sodium alginate and successful encapsulation of GVO into the microcapsules. Thermal property study showed that the crosslinked microparticles exhibited higher thermal stability than the neat GVO, gelatin, and sodium alginate. The stability of microencapsulation of GVO in a simulated gastric and an intestinal situation in vitro was also studied. The stability results indicated that the release of GVO from microcapsules was much higher in simulated intestinal fluid, compared with that in simulated-gastric fluid.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1779K) Full view HTML -
Zhi-Gang Sun, Zhen Li, Dan-dan Yuan, Jun-Fa Gao, Lin Lin, Jie Lin, Min ...2016 Volume 64 Issue 1 Pages 27-33
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
Advance online publication: October 30, 2015
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Supplementary materialWe report a novel ratiometric and reversible fluorescent probe for Cd2+ detection utilizing a 6-(dimethylamino)quinaldine derivative as the fluorophore and a 2-hydrazinopyridine derivative as Cd2+ chelator. This ratiometric fluorescent probe possesses favorable photophysical properties. It shows a large (55 nm) red-shift from 515 nm to 570 nm in the emission spectrum. Moreover, this probe also exhibits an excellent linear relationship of fluorescence intensity ratio (F570/F515) (R2=0.989) vs. Cd2+ concentration in the range of 0–10 µM at physiological pH, which can serve as a “quantitative detecting” probe for Cd2+. Utilizing this sensitive and selective probe, we have successfully detected Cd2+ in living cells.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1285K) Full view HTML -
Mohamed Salah Rezk, Mohammad Abdel-Halim, Adam Keeton, Derek Franklin, ...2016 Volume 64 Issue 1 Pages 34-41
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLTwelve derivatives of the general formula 3-substituted-6-chloroindoles were synthesized and tested for their growth inhibitory effects versus p53+/+ colorectal cancer HCT116 and its p53 knockout isogenic cells; colorectal cancer cell p53−/− SW480; the lung cancer cell line p53−/− H1299; mouse embryonic fibroblasts (MEF) p53+/+ and its p53 knockout isogenic cells. The compounds were also evaluated for their ability to induce p53 nuclear translocation and binding to murine double minute 2 (MDM2) and murine double minute 4 (MDM4). Of these, compound 5a was the most active in inhibiting the growth of cells, with selectivity towards the p53+/+ cell lines, and it showed stronger binding to MDM4 rather than MDM2. The activity profile of compound 5a is strongly similar to that of Nutlin-3.Graphical Abstract Fullsize ImageView full abstractDownload PDF (872K) Full view HTML -
Rehab Mohammad Yusif, Irhan Ibrahim Abu Hashim, Elham Abdelmonem Moham ...2016 Volume 64 Issue 1 Pages 42-51
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLCarbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0.1 N HCl was investigated and characterized by Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Hence, directly compressed GR tablets of different combinations of PVP and CP with sodium bicarbonate (SB) as an effervescent agent were examined for prolonged gastroretention and sustained release of ranitidine hydrochloride (RHCl) as a model drug. Tablets were evaluated for in vitro buoyancy, bioadhesiveness, swelling, and drug release in 0.1 N HCl. All GR tablets containing PVP–CP combinations achieved more prolonged floating (>24 h) than CP tablets (5.2 h). Their bioadhesiveness, swelling, and drug release were dependent on the PVP molecular weight and its ratio to CP. Drug release profiles of all formulae followed non-Fickian diffusion. Formula containing the PVP K90–CP combination at a respective ratio of 1 : 3 (P90C13) was a promising system, exhibiting good floating and bioadhesive properties as well as sustained drug release. Abdominal X-ray imaging of P90C13 formula, loaded with barium sulfate, in six healthy volunteers showed a mean gastric retention period of 6.8±0.3 h.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1982K) Full view HTML -
Sakura Yoshida, Eriko Hori, Sakiko Ura, Mamoru Haratake, Takeshi Fuchi ...2016 Volume 64 Issue 1 Pages 52-58
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
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Supplementary materialThe intracellular metabolism of selenium in the brain currently remains unknown, although the antioxidant activity of this element is widely acknowledged to be important in maintaining brain functions. In this study, a comprehensive method for identifying the selenium-binding proteins using PenSSeSPen as a model of the selenium metabolite, selenotrisulfide (RSSeSR, STS), was applied to a complex cell lysate generated from the rat brain. Most of the selenium from L-penicillamine selenotrisulfide (PenSSeSPen) was captured by the cytosolic protein thiols in the form of STS through the thiol-exchange reaction (R-SH+PenSSeSPen→R-SSeSPen+PenSH). The cytosolic protein species, which reacted with the PenSSeSPen mainly had a molecular mass of less than 20 kDa. A thiol-containing protein at m/z 15155 in the brain cell lysate was identified as the cystatin-12 precursor (CST12) from a rat protein database search and a tryptic fragmentation experiment. CST12 belongs to the cysteine proteinase inhibitors of the cystatin superfamily that are of interest in mechanisms regulating the protein turnover and polypeptide production in the central nervous system and other tissues. Consequently, CST12 is suggested to be one of the cytosolic proteins responsible for the selenium metabolism in the brain.Graphical Abstract Fullsize ImageView full abstractDownload PDF (801K) Full view HTML
Notes
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Keumja Yun, Trung Thang Khong, Alain Simplice Leutou, Gun-Do Kim, Jong ...2016 Volume 64 Issue 1 Pages 59-62
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
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Supplementary materialCristazine (1), a new class of dioxopiperazine alkaloid, along with previously isolated chetomin (2), neoechinulin A (3), and golmaenone (4), were isolated from the mudflat-sediment-derived fungus Chaetomium cristatum. The structure and absolute stereochemistry of 1 was assigned on the basis of NMR, electron impact (EI)-MS, tandem FAB-MS/MS, and circular dichroism (CD) experiments. Compounds 1–4 displayed potent radical-scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), with IC50 values of 19, 15, 24, and 20 µM, respectively, which were similar to that of the positive control, ascorbic acid (IC50, 20 µM). Compound 1 also displayed cytotoxic activity against human cervical carcinoma (HeLa) cells, with an IC50 value of 0.5 µM.Graphical Abstract Fullsize ImageView full abstractDownload PDF (390K) Full view HTML -
Kohei Tahara, Wakana Hashimoto, Hirofumi Takeuchi2016 Volume 64 Issue 1 Pages 63-67
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
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Supplementary materialThe use of naked unmodified small interfering RNA (N-siRNA) without vector has previously been investigated as a pulmonary therapy. However, little is known regarding stabilities and aerodynamic particle sizes of N-siRNA-containing droplets; nebulizers have not yet been optimized for N-siRNA solutions. Thus, in this study, we investigated the feasibility of inhaled N-siRNA solutions for pulmonary therapy using nebulization. Various nebulizers and N-siRNA concentrations were assessed in terms of siRNA integrity after nebulization, and inhalation properties including aerodynamic particle size were examined. In comparison with ultrasonic-, air-jet-, and vibrating-mesh nebulizers, N-siRNA integrity was not affected by nebulization. Thus, in further experiments, performances of N-siRNA aerosols with different nebulizers and N-siRNA concentrations were evaluated and screened using an aerodynamic particle sizer (APS) which employed the time-of-flight principle or a cascade impactor. Mean mass aerodynamic diameters of N-siRNA-containing droplets from vibrating-mesh nebulizers tended to decrease with increasing N-siRNA concentrations, reflecting the influence of N-siRNA solutions on surface tension, as indicated by contact angles. These data indicate the utility of APS instruments for investigating the nebulized characteristics of expensive drugs including siRNAs and may facilitate the development of N-siRNA inhalation formulations.Graphical Abstract Fullsize ImageView full abstractDownload PDF (603K) Full view HTML -
Satoshi Tanida, Tsuyoshi Kurokawa, Hideyuki Sato, Kazunori Kadota, Yui ...2016 Volume 64 Issue 1 Pages 68-72
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLThe main purpose of this study was to investigate the solubilization enhancement properties of an amphipathic graft copolymer, Soluplus®, on test compounds. Micellization of Soluplus® in solution was characterized by evaluating the changes in the surface activity, turbidity, and thermodynamic behavior. To assess the feasibility of Soluplus® as a polymeric carrier of solid dispersions, freeze-dried samples of ipriflavone were prepared, and the physicochemical properties of the carrier plus ipriflavone were evaluated in terms of solubility, dissolution, and crystallinity. The surface tension of the solution decreased depending on the polymer concentration, and gradual turbidity increase was observed. Isothermal titration calorimetry was used to measure the thermal reaction accompanying the micellization of Soluplus® and indicated that a colloidal micelle formation improved solubility. The prepared formulations, particularly at a ratio of ipriflavone : Soluplus®=1 : 10 (w/w) exhibited a dramatically improved solubility of ipriflavone that was ca. 70-fold higher than that of untreated ipriflavone. The solubilization mechanism of Soluplus® was partially elucidated and suggested that its strategic application could improve the solubility of hydrophobic compounds.Graphical Abstract Fullsize ImageView full abstractDownload PDF (600K) Full view HTML -
Zhong-liu Zhou, Wen-Qing Yin, Ya-Mei Yang, Chun-Hong He, Xiao-Na Li, C ...2016 Volume 64 Issue 1 Pages 73-77
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLBased on bioactive screening results, two new iridoid glycosides, named rotunduside G (1) and rotunduside H (2), were isolated from the rhizomes of Cyperus rotundus, together with four known ones, negundoside (3), nishindaside (4), isooleuropein (5) and neonuezhenide (6). Their structures were elucidated on the basis of spectroscopic methods and from literature values. In mice models of despair, 1 and 2 showed significant antidepressant activity.Graphical Abstract Fullsize ImageView full abstractDownload PDF (534K) Full view HTML -
Yoshiaki Amakura, Morio Yoshimura, Sara Morimoto, Takashi Yoshida, Ats ...2016 Volume 64 Issue 1 Pages 78-82
Published: January 01, 2016
Released on J-STAGE: January 01, 2016
JOURNAL FREE ACCESS FULL-TEXT HTMLGentian root extract is used as a bitter food additive in Japan. We investigated the constituents of this extract to acquire the chemical data needed for standardized specifications. Fourteen known compounds were isolated in addition to a mixture of gentisin and isogentisin: anofinic acid, 2-methoxyanofinic acid, furan-2-carboxylic acid, 5-hydroxymethyl-2-furfural, 2,3-dihydroxybenzoic acid, isovitexin, gentiopicroside, loganic acid, sweroside, vanillic acid, gentisin 7-O-primeveroside, isogentisin 3-O-primeveroside, 6′-O-glucosylgentiopicroside, and swertiajaposide D. Moreover, a new compound, loganic acid 7-(2′-hydroxy-3′-O-β-D-glucopyranosyl)benzoate (1), was also isolated. HPLC was used to analyze gentiopicroside and amarogentin, defined as the main constituents of gentian root extract in the List of Existing Food Additives in Japan.Graphical Abstract Fullsize ImageView full abstractDownload PDF (678K) Full view HTML
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