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Volume 63, Issue 1
Displaying 1-9 of 9 articles from this issue
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Review
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Yasumaru Hatanaka2015 Volume 63 Issue 1 Pages 1-12
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
JOURNAL FREE ACCESS FULL-TEXT HTMLPhotoaffinity labeling has become increasingly important with the development of powerful specific probes that are synthesized by installing a photo-activatable functional group (photophore) on the framework of biological ligands. The present review summarizes the development of diazirine-based photoaffinity labeling by focusing on its application to the structural elucidation of ligand-accepting sites within proteins.Graphical Abstract Fullsize ImageView full abstractDownload PDF (2281K) Full view HTML
Regular Articles
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Aki Hayashi, Mai Kubota, Miki Okamura, Hirokazu Nakayama2015 Volume 63 Issue 1 Pages 13-17
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialLayered double hydroxides (LDHs) have been used commercially as antacids, to stabilize drugs, to allow the controlled release of incorporated drugs, and to act as drug carriers to reduce drug accumulation within the body. Several types of LDH were investigated: nitrate type (LDH-NO3); chloride type (LDH-Cl); and carbonate type (LDH-CO3). Each type was added to an aqueous or methanol (MeOH) solution containing a drug (pravastatin or nateglinide). With pravastatin sodium, the interlayer distance expanded after reaction with LDH-NO3 and LDH-Cl in aqueous solution. In contrast, the interlayer distance of LDH-CO3 increased in methanol with nateglinide. Each drug was intercalated into the interlayer space of LDH by ion exchange. The hygroscopicity of the drug substances, complexes, and physical mixtures were determined at 70% relative humidity. Increases in weight (%) of the complexes were less than those of the physical mixtures, which demonstrates that hygroscopicity was reduced upon complexation with LDH due to the layer of LDH over the drugs.Graphical Abstract Fullsize ImageView full abstractDownload PDF (543K) Full view HTML -
Makoto Mukaida, Kiyohiko Sugano, Katsuhide Terada2015 Volume 63 Issue 1 Pages 18-24
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
JOURNAL FREE ACCESS FULL-TEXT HTMLThe purpose of the present study was to determine the thermodynamic stability orders of co-crystals by co-crystal former (CCF) exchange reactions. Caffeine (CA) was employed as a model drug. The CCF exchange reaction was performed by liquid-assisted grinding using ethanol. When oxalic acid (OX) was added to CA–citric acid co-crystal (CA–CI), CA–CI converted to CA–OX, suggesting that CA–OX is more stable than CA–CI. The stability orders of other co-crystals were determined in the same manner. The stability order of CA co-crystals was determined as CA–OX≈CA–p-hydroxybenzoic acid (HY)>CA–CI>CA–malonic acid>CA–maleic acid. The stability order correlated with the difference in hydrogen bond energy estimated in silico, except for CA–HY. The π–π stacking in CA–HY was suggested as a reason for this discrepancy. The CCF exchange reaction was demonstrated as a useful method to determine the stability order of co-crystals, which can be used for the validation of in silico parameters to predict co-crystal formation.Graphical Abstract Fullsize ImageView full abstractDownload PDF (1234K) Full view HTML -
Liangmian Chen, Akira Kotani, Fumiyo Kusu, Zhimin Wang, Jingjing Zhu, ...2015 Volume 63 Issue 1 Pages 25-32
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
JOURNAL FREE ACCESS FULL-TEXT HTMLFor the determination of seven caffeoylquinic acids [neochlorogenic acid (NcA), cryptochlorogenic acid (CcA), chlorogenic acid (CA), caffeic acid (CfA), isochlorogenic acid A (Ic A), isochlorogenic acid B (Ic B), isochlorogenic acid C (Ic C)] and two flavonoids [luteolin 7-O-glucoside (LtG) and luteolin (Lt)], a three-channel liquid chromatography with electrochemical detection (LC-3ECD) method was established. Chromatographic peak heights were proportional to each concentration, ranging from 2.5 to 100 ng/mL for NcA, CA, CcA, and CfA, and ranging from 2.5 to 250 ng/mL for LtG, Ic B, Ic A, Ic C, and Lt, respectively. The present LC-3ECD method was applied to the quantitative analysis of caffeoylquinic acids and flavonoids in four cultivars of Chrysanthemum morifolium flowers and their sulfur-fumigated products. It was found that 60% of LtG and more than 47% of caffeoylquinic acids were lost during the sulfur fumigation processing. Sulfur fumigation showed a destructive effect on the C. morifolium flowers. In addition, principle component analyses (PCA) were performed using the results of the quantitative analysis of caffeoylquinic acids and flavonoids to compare the “sameness” and “differences” of these analytes in C. morifolium flowers and the sulfur-fumigated products. PCA score plots showed that the four cultivars of C. morifolium flowers were clearly classified into four groups, and that significant differences were also found between the non-fumigated C. morifolium flowers and the sulfur-fumigated products. Therefore, it was demonstrated that the present LC-3ECD method coupled with PCA is applicable to the variation analysis of different C. morifolium flower samples.Graphical Abstract Fullsize ImageView full abstractDownload PDF (871K) Full view HTML -
Long-Bo Li, Wen-Jia Dan, Fang-Fang Tan, Li-Hui Cui, Zhi-Peng Yuan, Wen ...2015 Volume 63 Issue 1 Pages 33-37
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
Advance online publication: October 30, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLThe synthesis of Yanglingmycin and its enantiomer, along with eighteen Yanglingmycin analogues is reported. The structures were confirmed mainly by analyses of NMR spectral data. Antibacterial activity assays showed that Yanglingmycin and some of its analogues exhibited significant antibacterial activities against two important agricultural pathogenic bacteria, Ralstonia solanacearum and Pseudomonas syringae pv. actinidiae, with minimum inhibitory concentration (MIC) values ranging from 3.91 to 15.62 µg/mL. The antibacterial activities exhibited by Yanglingmycin and its analogues are promising, suggesting potential in the development of compounds for novel bactericides.Graphical Abstract Fullsize ImageView full abstractDownload PDF (434K) Full view HTML
Notes
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Maromu Yamada, Kaya Nakamura, Takayuki Kameda, Fumihisa Kobayashi, Ats ...2015 Volume 63 Issue 1 Pages 38-42
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
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Supplementary materialPolycyclic aromatic hydrocarbons (PAHs) are known as carcinogenic and/or mutagenic substances, and are present at high concentration in polluted environments. It has recently been reported that spore-forming bacteria (e.g., Bacillus spp.) can be transported long distances alive in the atmosphere, which raises the possibility that some of the transported bacteria could have adverse effects on human health. There is thus a need for filters that can remove gaseous PAHs from the air that people breathe and that can inhibit bacterial growth on the filters. We focused on metallophthalocyanine derivatives (M-Pc) which are known to adsorb PAHs as well as to inhibit the growth of bacteria as a potential filtering agent. In this study, we developed different types of M-Pc-supported rayon fibers by changing central metals, functional groups, concentrations of M-Pc and rayon types, and evaluated their removal effects by measuring adsorption rates of 3- and 4-ring PAHs with a HPLC and growth curves of Bacillus sp. with a spectrophotometer. The results showed that both the effects depended on functional groups and concentrations of M-Pc, and rayon types. The most effective combination was observed in Fe-Pc with sulfo group supported on cationized rayon fiber at the concentration of 2 to 3.3 wt%. Central metal species of M-Pc were influenced only on the antibacterial properties. This fiber would be applicable to filtering agents and textiles.Graphical Abstract Fullsize ImageView full abstractDownload PDF (539K) Full view HTML -
Shuji Kitagawa, Megumi Fujiwara, Yuta Okinaka, Reiko Yutani, Reiko Ter ...2015 Volume 63 Issue 1 Pages 43-48
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
Advance online publication: November 15, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLWhite petrolatum is a mixture of solid and liquid hydrocarbons and its structure can be affected by shear stress. Thus, it might also induce changes in its rheological properties. In this study, we used polarization microscopy to investigate how different mixing methods affect the structure of white petrolatum. We used two different mixing methods, mixing using a rotation/revolution mixer and mixing using an ointment slab and an ointment spatula. The extent of the fragmentation and dispersal of the solid portion of white petrolatum depended on the mixing conditions. Next, we examined the changes in the structure of a salicylic acid ointment, in which white petrolatum was used as a base, induced by mixing and found that the salicylic acid solids within the ointment were also dispersed. In addition to these structural changes, the viscosity and thixotropic behavior of both test substances also decreased in a mixing condition-dependent manner. The reductions in these parameters were most marked after mixing with a rotation/revolution mixer, and similar results were obtained for spreadability. We also investigated the effects of mixing procedure on the skin accumulation and permeation of salicylic acid. They were increased by approximately three-fold after mixing. Little difference in skin accumulation or permeation was detected between the two mixing methods. These findings indicate that mixing procedures themselves affect the utility and physiological effects of white petrolatum-based ointments. Therefore, these effects should be considered when mixing is required for the clinical use of petrolatum-based ointments.Graphical Abstract Fullsize ImageView full abstractDownload PDF (3285K) Full view HTML -
Yukiko Yamashita-Higuchi, Sachiko Sugimoto, Katsuyoshi Matsunami, Masa ...2015 Volume 63 Issue 1 Pages 49-53
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
JOURNAL FREE ACCESS FULL-TEXT HTMLFrom the EtOAc-soluble fraction of a MeOH extract of the leaves of Glochidion acuminatum, six new compounds along with five known ones were isolated. The structures of the new compounds were elucidated to be two gallates, a p-hydroxybenzoate and an (S)-2-(4-hydroxycyclohex-1-en-1-yl)acetate of a nitrile-containing phenolic glucoside, methyl 2-(2-hydroxyphenyl)acetate β-D-glucopyranoside, and (S)-methyl 2-[4-sulfooxycyclohex-1-en-1-yl]acetate on the basis of spectroscopic evidence.Graphical Abstract Fullsize ImageView full abstractDownload PDF (479K) Full view HTML -
Hideyuki Sato, Kumiko Ogawa, Yoshiki Kojo, Hiroki Suzuki, Takahiro Miz ...2015 Volume 63 Issue 1 Pages 54-58
Published: January 01, 2015
Released on J-STAGE: January 01, 2015
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Supplementary materialThe main purpose of the present study was to evaluate the physicochemical stability of cyclosporine A (CsA)-loaded glycerol monooleate-based dry emulsion (DE). DE formulations containing 5–25% CsA (DE5–25) were stored at 25°C/60% relative humidity for 4 weeks, and freeze-dried solid dispersion formulations containing 5–30% CsA (FD5–30) were also prepared as reference formulations. Even after the storage, no significant changes were observed in the appearance of any formulations. In the dissolution study, both DE and FD exhibited marked enhancement of solubility and there was at least 2.0-fold improvement in the initial dissolution rate of DE formulations compared with that of FD formulations. After storage, DE5, DE15 and FD5 maintained relatively high solubility, with 10% reduction compared with the initial state. However, the solubility of DE25 gradually decreased during storage, as evidenced by 76% reduction of the dissolution amount. No significant changes were seen in DE5–25 using powder X-ray diffraction, although thermal analysis revealed moderate changes in crystallinity in DE25 after storage, possibly leading to the decreased dissolution. Furthermore, particle size distributions of micelles in DE5 and DE15 were almost unchanged after storage for 4 weeks. From these findings, it appears that the physicochemical stability of CsA-loaded DE might vary depending on the manufacturing method and that further optimization could improve physical properties and stability.Graphical Abstract Fullsize ImageView full abstractDownload PDF (485K) Full view HTML
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