巻号一覧
62 巻, 6 号
選択された号の論文の16件中1～16を表示しています
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Communication to the Editor
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Meiling Zhang, Mingjie Deng, Jianshe Ma, Xianqin Wang2014 年 62 巻 6 号 p. 505-507
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLHydrogen sulfide (H2S) is the second leading cause of toxin-related deaths in the operational site. Its main target organs of toxic effects are the central nervous system and respiratory system. In this study, we developed a serum metabonomic method, based on gas chromatography-mass spectrometry (GC/MS), to evaluate the effect of acute poisoning by hydrogen sulfide on rats. Pattern recognition analysis, including both principal component analysis (PCA) and partial least squares-discriminate analysis (PLS-DA), revealed that acute hydrogen sulfide poisoning induced metabolic perturbations. Compared to the control group, the level of urea, glucose, glyceryl stearate in rat serum of the poisoning group increased after two hours, and the level of glucose, docosahexaenoic acid, glyceryl stearate and arachidonic acid in rat serum of the poisoning group increased after 48 h, while the l-valine, galactose, l-tyrosine levels decreased. Our results indicate that metabonomic methods based on GC/MS may be useful to elucidate acute hydrogen sulfide poisoning through the exploration of biomarkers.抄録全体を表示PDF形式でダウンロード (417K) HTML形式で全画面表示
Regular Articles
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Younghee Kim, Jiwon Son, Juhyeon Kim, Du-Jong Baek, Yong Sup Lee, Eun ...2014 年 62 巻 6 号 p. 508-518
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLA series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 µm against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia.抄録全体を表示PDF形式でダウンロード (739K) HTML形式で全画面表示 -
Zhibin Liang, Enming Du, Lipeng Xu, Yewei Sun, Gaoxiao Zhang, Pei Yu, ...2014 年 62 巻 6 号 p. 519-523
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLPancreatic β-cell dysfunction and death are important feature of diabetes mellitus. Beta-cell protection has demonstrated clinical benefits in the treatment of this disease. In the present study, andrographolide derivatives with nitric oxide (NO)-releasing capability were synthesized and their protective effects against tert-butyl hydroperoxide (t-BHP) induced cell damage were investigated in RIN-m cells. Compound 6b was found to release a moderate amount of NO and was more potent than its natural parent andrographolide in inhibiting cell apoptosis. These findings suggested that andrographolide derivatives with NO-releasing capacity may be a potential therapy for diabetes.抄録全体を表示PDF形式でダウンロード (702K) HTML形式で全画面表示 -
Synthesis and in Vitro Evaluation of 1,3,4-Thiadiazol-2-yl Urea Derivatives as Novel AChE InhibitorsXiao-jian Xue, Yu-bin Wang, Peng Lu, Hai-feng Shang, Jin-xiong She, Li ...2014 年 62 巻 6 号 p. 524-527
発行日: 2014/06/01
公開日: 2014/06/01
[早期公開] 公開日: 2014/04/03ジャーナル フリー HTML1,3,4-Thiadiazole and urea group were hybridized to form new molecular skeleton and 11 compounds were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. Most of them showed comparable effects in inhibition of AChE, especially compound 6b which exhibited activity with IC50 value 1.17 µm, as strong as galanthamine. This information offered by our research would be valuable for further investigation of structure–activity relationship (SAR) and useful in future research of AChE inhibitors.抄録全体を表示PDF形式でダウンロード (365K) HTML形式で全画面表示 -
Rie Nishikawa-Shimono, Yoshinori Sekiguchi, Madoka Kawamura, Daisuke W ...2014 年 62 巻 6 号 p. 528-537
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLSynthesis and structure–activity relationship of a novel series of isoquinoline CRTH2 antagonists bearing a methylene linker between the isoquinoline and benzamide moieties were described. Optimization focusing on the substituents of the benzamide portion in the right hand part of the molecule led to the identification of TASP0412098 (9l), which is a potent, selective CRTH2 antagonist (binding affinity: IC50=2.1 nm, functional activity: IC50=12 nm). Compound 9l, which was orally bioavailable in mice and guinea pigs, showed in vivo efficacy after oral administration in a bronchial asthma model of guinea pigs.抄録全体を表示PDF形式でダウンロード (953K) HTML形式で全画面表示 -
Naozumi Ohnishi, Hiromasa Tomida, Yousuke Ito, Kohei Tahara, Hirofumi ...2014 年 62 巻 6 号 p. 538-544
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTML
電子付録A novel in vitro release test methodology for a liposome formulation was developed using a column-switching high-performance liquid chromatography (HPLC) system. Doxorubicin (DXR) liposome formulations were used as a model. A DXR liposome formulation was dispersed into a release medium, and the dispersion fluid was directly injected at predetermined time points into the column-switching HPLC system. To evaluate the release profile, this system can be used for determining the released and encapsulated DXR in the liposome formulation separately. Comparison with a conventional in vitro release test methodology by dialysis revealed that the methodology developed by column-switching HPLC had no rate-limiting process of membrane permeation of the drug (which is occasionally observed in the dialysis method). The in vitro release profiles of DXR liposome formulations were well characterized using the method developed by column-switching HPLC, and different in vitro release characteristics were revealed. The developed method did not require a large amount of sample or a complicated pretreatment. In addition, the developed column-switching HPLC system was applicable for characterization of the encapsulation profile of liposome formulations.抄録全体を表示PDF形式でダウンロード (782K) HTML形式で全画面表示 -
Eun-Sol Ha, In-hwan Baek, Wonkyung Cho, Sung-Joo Hwang, Min-Soo Kim2014 年 62 巻 6 号 p. 545-551
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLThe aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.抄録全体を表示PDF形式でダウンロード (2382K) HTML形式で全画面表示 -
Takashi Ishizu, Hiroyuki Tsutsumi, Yoshifumi Kinoshita, Hironori Mukai ...2014 年 62 巻 6 号 p. 552-558
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLAn aqueous solution of equimolecular amounts of gallated catechin (−)-epigallocatechin-3-O-gallate (EGCg) and caffeine afforded a crude precipitate by creaming, which crystallized slowly for about three months at 10°C to give a colorless block crystal. The crystal was determined to be a 2 : 2 complex of EGCg and caffeine by X-ray crystallographic analysis. The 2 : 2 complex was formed with the cooperative effect of three intermolecular interactions, π–π and CH–π interactions, and intermolecular hydrogen bonds. Upon formation of the 2 : 2 complex, a caffeine molecule was captured by a hydrophobic space formed by the aromatic rings A, B, and B′ rings of two EGCg molecules. Judging from the entropy value, the shift value in the chemical shift of proton signals in 1H-NMR spectra, the NT1 value, and nuclear Overhauser effects (NOEs), it was thought that the structure of complexes of EGCg and caffeine in aqueous solution were the same as their crystal structure.抄録全体を表示PDF形式でダウンロード (1356K) HTML形式で全画面表示 -
Keisuke Kikuchi, Hiroaki Todo, Kenji Sugibayashi2014 年 62 巻 6 号 p. 559-567
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLTwo unique pressure-sensitive adhesive (PSA) tapes (PSA-A, -B) with different adhesive properties of commercial PSAs were prepared and evaluated for their usefulness as a pretreatment material prior to the application of transdermal therapeutic systems or topical drug formulations and also as a peeling agent against excess layers of the stratum corneum. In the present study, in vitro permeation experiments were conducted using vertical type diffusion cells and excised hairless rat or porcine skin from which the stratum corneum had been stripped several times with PSAs. The results obtained revealed that PSA-A and -B had higher stripping or peeling effects than those of the marketed PSAs. Marked changes were observed in skin barrier function before and after stripping using PSAs, and the enhancement effect on the skin permeation of drugs achieved by stripping the stratum corneum was markedly different between the PSAs. PSA-A, in particular, markedly improved skin permeation and the skin concentration of topically applied chemical compounds because it removed many layers of the stratum corneum when skin was stripped only a few times. In contrast, when PSA-B was used to pretreat the skin surface, the extent of skin permeation and concentration of drugs was safely increased because only a few layers of the stratum corneum were removed, even with repeated stripping. The enhancement effect achieved by PSA-B was not as high as that by PSA-A. Thus, stripping with PSA-A can be used as a penetration enhancement tool, whereas PSA-B can be used as a peeling material against excess layers of the stratum corneum.抄録全体を表示PDF形式でダウンロード (1973K) HTML形式で全画面表示 -
Fei Qi, Satoshi Fudo, Saburo Neya, Tyuji Hoshino2014 年 62 巻 6 号 p. 568-577
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTML
電子付録Information on many protein crystal structures has recently become available due to developments in crystallographic techniques. Even for a single kind of protein, several and sometimes many crystal structures are available. Human immunodeficiency virus type 1 (HIV-1) protease is one of the most extensively studied viral proteins, and about six hundred crystal structures have been determined. In this work, we examined the structural diversity of HIV-1 protease, classifying crystal structures into several groups from the viewpoint of similarity in atom geometry. Using 499 crystal structures downloaded from the Protein Data Bank (PDB), cluster analysis was applied to the whole body of HIV-1 protease and also to a limited number of residues at the binding pocket. As a consequence of clustering with regard to the whole body, 499 crystal structures were separated into 6 groups. It was found that a major factor for this separation is the space group of the crystals and that the space group strongly depends on the agents used in the protein crystallization. Amino acid mutation is a minor factor for separation in clustering. In cluster analysis for a limited number of residues at the binding pocket, crystal structures were not distinctly separated, and no clear factor linked to the separation was clarified. The results suggest that amino acid mutations have little effect on the coordinates of the main-chain atoms of HIV-1 protease. Hence, the changes in drug efficacy or substrate fitness caused by mutations are mainly due to the physicochemical features of amino acid side chains.抄録全体を表示PDF形式でダウンロード (1313K) HTML形式で全画面表示 -
Daisuke Horita, Hiroaki Todo, Kenji Sugibayashi2014 年 62 巻 6 号 p. 578-585
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLThe hair follicle-plugging method was used to analyze the effects of EtOH on skin permeation pathways. Methods: In vitro permeation experiments were performed on 4 model drugs [isosorbide mononitrate (ISMN), ionized lidocaine (ionized LC), fluorescein (FL), and fluorescein isothiocyanate (FITC)-dextran 4 kDa (FD-4)] using excised pig ear skin. The skin permeations of ionized LC, FL, and FD-4 were decreased by hair follicle-plugging. Hair follicle-plugging prevented the skin permeation of FL and FD-4 in EtOH-pretreated skin, but did not prevent that of ISMN. On the other hand, the effect of hair follicle-plugging on the permeation of ionized LC was different among the pretreatment conditions. These results indicate that the EtOH pretreatment greatly affected the aqueous pathway in the stratum corneum and hair follicles.抄録全体を表示PDF形式でダウンロード (910K) HTML形式で全画面表示 -
Masahiro Kimura, Mitsuno Shindo, Toshiyuki Moriizumi, Noriko Tagawa, A ...2014 年 62 巻 6 号 p. 586-590
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTML
電子付録Salusin-β has been detected in numerous mammalian tissues and has been shown to have various effects on the cardiovascular system. In this study, we showed that salusin-β exhibited potent antibacterial activity against Gram-positive microorganisms such as Bacillus subtilis NBRC 3513, Bacillus megaterium ATCC 19213, Staphylococcus aureus NBRC 12732, and Staphylococcus epidermidis NBRC 12933. A cytoplasmic membrane-depolarizing assay using the DiSC3(5) dye revealed that the addition of 4 nmol/mL of salusin-β caused the leakage of fluorescence dye from Staphylococcus aureus NBRC 12732. The antimicrobial potency and circular dichroism (CD) spectroscopy of five analogs related to salusin-β were examined to determine structure-function relationships in its N- and C-terminal regions. The results obtained suggest that the N-terminal sequences of the salusin-β molecule are important for the expression of the potent antimicrobial activity of this peptide. A profile corresponding to that of the α-helix conformation was observed in the salusin-β solution.抄録全体を表示PDF形式でダウンロード (520K) HTML形式で全画面表示 -
Ayman El-Faham, Muhammad Farooq, Sherine Nabil Khattab, Ahmed Mohamed ...2014 年 62 巻 6 号 p. 591-599
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTML
電子付録Series of Schiff bases of valproic acid hydrazide, N-valproylglycine hydrazide and N-valproyl-4-aminobenzoyl hydrazide derivatives were synthesized and characterized by IR, NMR (1H- and 13C-NMR) and elemental analysis. The prepared compounds were evaluated in transgenic zebrafish embryos (Tg: flil-1: enhanced green fluorescent protein (EGFP)) for antiangiogenic activity and in HepG2 liver carcinoma cell line for anti cancer activity. The Schiff bases of N-valproylglycine hydrazide derivatives were most potent in term of suppressing angiogenic blood vessels formation and anticancer activity at very low concentration, followed by the Schiff bases of valproic acid hydrazide derivatives which exhibited moderate activity, while the Schiff bases of N-valproyl-4-aminobenzoyl hydrazide derivatives, ethyl 4-(2-propylpentanamido)benzoate (VABE) and N-(4-(hydrazinecarbonyl)phenyl)-2-propylpentanamide (VABH) in contrast exhibited pro-angiogenic activity and weaker anticancer activity which mean that these derivatives targeted a common signaling pathway in term of affecting the blood vessels formation.抄録全体を表示PDF形式でダウンロード (716K) HTML形式で全画面表示 -
Katsuhiro Okuda, Keisuke Nishikawa, Hiroshi Fukuda, Yoshiharu Fujii, M ...2014 年 62 巻 6 号 p. 600-607
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLThe activity of cis-cinnamic acid (cis-CA), one of the allelochemicals, in plants is very similar to that of indole-3-acetic acid (IAA), a natural auxin, and thus cis-CA has long been believed to be an analog of auxin. We have reported some structure–activity relationships studies by synthesizing over 250 cis-CA derivatives and estimating their inhibitory activities on root growth inhibition in lettuce. In this study, the compounds that showed low- or no-activity on root growth inhibition were recruited as candidates suppressors against cis-CA and/or auxin and tested for their activity. In the presence of cis-CA, lettuce root growth was inhibited; however, the addition of some cis-CA derivatives restored control-level root growth. Four compounds, (Z)-3-(4-isopropylphenyl)acrylic acid, (Z)-3-(3-butoxyphenyl)acrylic acid, (Z)-3-[3-(pentyloxy)phenyl]acrylic acid, and (Z)-3-(naphthalen-1-yl)acrylic acid were selected as candidates for a cis-CA selective suppressor they allowed the recovery of root growth from inhibition by cis-CA treatment without any effects on the IAA-induced effect or elongating activity by themselves. Three candidates significantly ameliorated the root shortening by the potent inhibitor derived from cis-CA. In brief, we have found some cis-CA selective suppressors which have never been reported from inactive cis-CA derivatives for root growth inhibition. cis-CA selective suppressors will play an important role in elucidating the mechanism of plant growth regulation.抄録全体を表示PDF形式でダウンロード (578K) HTML形式で全画面表示
Notes
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Toshihiro Murata, Mari Nakano, Toshio Miyase, Fumihiko Yoshizaki2014 年 62 巻 6 号 p. 608-612
発行日: 2014/06/01
公開日: 2014/06/01
[早期公開] 公開日: 2014/03/15ジャーナル フリー HTML
電子付録An extract of whole plants of Pycnanthemum flexuosum showed an inhibitory effect on hyaluronidase activity. From an 80% acetone extract of aerial parts, 3-[(3E)-4-phenylbut-3-enoylamino]propionic acid, 3-O-β-d-glucuronopyranosyl-echinocystic acid 28-O-β-d-xylopyranosyl-(1→3)-[3,4-diacetyl-β-d-xylopyranosyl-(1→4)]-α-l-rhamnopyranosyl-(1→2)-α-l-arabinopyranosyl ester, vanillic acid 1-O-[(5-O-syringoyl)-β-d-apiofuranosyl]-(1→2)-β-d-glucopyranoside, and (4S,5R)-4-hydroxy-5-phenyl-tetrahydrofuran-2-one were isolated together with 30 known compounds. Six known compounds were isolated from an 80% acetone extract of roots, and eritrichin was revealed as a hyaluronidase inhibitor in P. flexuosum.抄録全体を表示PDF形式でダウンロード (453K) HTML形式で全画面表示 -
Taku Yamashita, Leila Hafsi, Eri Masuda, Hirofumi Tsujino, Tadayuki Un ...2014 年 62 巻 6 号 p. 613-615
発行日: 2014/06/01
公開日: 2014/06/01
ジャーナル フリー HTMLNeuroglobin (Ngb) is the third member of the vertebrate globin family, and the structure was solved as a typical globin fold with a b-type heme. Although it has been proposed that Ngb could be involved in neuroprotection against oxidative stress, the protective mechanism has not been fully identified yet. In order to clarify functions under hypoxic condition, in this study, we focused on the scavenger activity of human Ngb (hNgb) against superoxide. The activity of hNgb for superoxide was evaluated to be 7.4 µm for IC50, the half maximal inhibitory concentration. The result indicates that hNgb can be an anti-oxidant, and the value was almost the same as that of ascorbic acid. In addition, we characterized oxidation states of a heme iron in superoxide-treated hNgb with spectroscopic measurements. Superoxide-treated hNgb in the ferric form was readily converted to the oxygenated ferrous form, and the result suggested that ferric hNgb could scavenge superoxide by change of an oxidation state in a heme iron. Moreover, mutational experiments were performed, and the each variant mutated at 46 and 55 positions suggested a disulfide bond between Cys46 and Cys55 could be essential to be sensors for oxidative stress with the direct binding of superoxide. As a consequence, we concluded that redox changes of the heme iron and the disulfide bond could regulate neuroprotective functions of hNgb, and it suggests that hNgb can afford protection against hypoxic and ischemic stress in the brain.抄録全体を表示PDF形式でダウンロード (508K) HTML形式で全画面表示
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