巻号一覧
59 巻, 7 号
選択された号の論文の18件中1～18を表示しています
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Review
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Biswanath Dinda, Sudhan Debnath, Rajarshi Banik原稿種別: Review
2011 年 59 巻 7 号 p. 803-833
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーA compilation of new naturally occurring iridoids and secoiridoids including their glycosides, esters, aglycones, derivatives and dimers reported during mid 2008—2010 is provided with available physical and spectral data: mp, [α]D, UV, IR, circular dichroism (CD), 1H- and 13C-NMR as well as natural source with family and references. The important bioactivity of new and known iridoids and secoiridoids reported during this period is also highlighted.抄録全体を表示PDF形式でダウンロード (2673K)
Regular Articles
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Min Cheol Kim, Hak Cheol Kwon, Su Nam Kim, Hyung Seop Kim, Byung Hun U ...原稿種別: Regular Article
2011 年 59 巻 7 号 p. 834-838
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーFour new plastoquinones, together with two known compounds, sargahydroquinoic acid and sargaquinoic acid, were isolated from the brown alga, Sargassum yezoense collected from the eastern coast of Korea. The structures of these compounds were elucidated based on spectroscopic analyses including NMR and MS. Their structures designated as meroterphenol A (1), B (2), C (3) and D (4) were characterized by a 6-methyl-1,4-benzohydroquinone moiety with an oxygenated diterpenoic acid chain. Meroterphenols A—D showed potent activation effects on peroxisome proliferator-activated receptor gamma (PPARγ).抄録全体を表示PDF形式でダウンロード (539K) -
Lunzhao Yi, Pengfei Zhang, Xiaoyan Ji, Yizeng Liang, Yamin Wang, Zhigu ...原稿種別: Regular Article
2011 年 59 巻 7 号 p. 839-843
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーThe article reports a simple, sensitive and fast LC/MS method for the analysis of L-arginine (L-Arg), asymmetric dimethylarginine (ADMA) and symmetric dimethylarginine (SDMA) in human plasma. The homoarginine was used as the internal standard (IS). The chromatographic separation was achieved on C18 (150 mm×2.1 mm, 5 μm) column with a mobile phase consisting of ammonium acetate (0.25 mmol/l) and methanol (93 : 7, v/v), at a flow rate of 0.2 ml/min. L-Arg, ADMA and SDMA were well separated by LC/MS with selective ion mode (SIM). The method was successfully applied to type 2 diabetes mellitus (T2DM) study. Twenty-one healthy controls and twenty-two T2DM patients before and after treatment two years were investigated. The results indicated that the level of ADMA in T2DM was significantly higher than that in healthy controls. Furthermore, ADMA has important association with the development of cardiovascular diseases.抄録全体を表示PDF形式でダウンロード (593K) -
Nam Sung Ha, Thao Truong-Dinh Tran, Phuong Ha-Lien Tran, Jun-Bom Park, ...原稿種別: Regular Article
2011 年 59 巻 7 号 p. 844-850
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーThe purpose of this study was to investigate the effects of alkalizers in dissolution rate and crystal structure of valsartan (VAL) in Poloxamer 407 (POX)-based solid dispersions (SD). VAL, a poorly-water soluble drug was selected as a model drug because of its low solubility at low pH. The POX-based SDs containing alkalizers (Na2CO3, MgO, meglumine and arginine) were prepared by melting method. The dissolution tests were performed using the United States Pharmacopeia (USP) paddle II method in enzyme-free simulated gastric fluid (pH 1.2) for 2 h. Microenvironmental pH (pHM) was examined potentiometrically by using a surface pH electrode. Dissolution rate of SD incorporating Na2CO3 was drastically increased. The differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) data indicated that crystalline structure of VAL in SD was transformed to amorphous form by the addition of alkalizers but could not explain the differences in the dissolution rates. The molecular interaction between VAL and Na2CO3 was observed in the Fourier transform infrared spectroscopy (FT-IR) spectra by the shift of C=O band from 1732 to 1719 cm−1 and the disappearance of carbonyl group at 1598 cm−1. Furthermore, Na2CO3 efficiently modulated pHM by providing a favorable microenvironment for drug dissolution. A combination of SD method and use of alkalizer is a promising approach to modulate release rate of poorly water-soluble and ionizable drug with an aid of changes of drug crystallinity, molecular interaction and pHM.抄録全体を表示PDF形式でダウンロード (941K) -
Chuanzhu Gao, Shaohua Gou, Gang Xu原稿種別: Regular Article
2011 年 59 巻 7 号 p. 851-854
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーEight platinum(II) compounds with a new chiral ligand, 2-(((1R,2R)-2-aminocyclohexylamino)methyl)phenol (HL), were designed, prepared and spectrally characterized. All compounds showed better aqueous solubility than cisplatin and oxaliplatin. In vitro cytotoxicity of these compounds against human HepG-2, MCF-7, A549 and HCT-116 cell lines was evaluated. Results indicated that all compounds showed cytotoxicity against A549 and HepG-2 cell lines. Particularly, compounds B1 and B8, which have CF3SO3− and (CH3)3COCH2COO− as leaving groups, respectively, exhibited better cytotoxicitiy than that of carboplatin in these two cell lines.抄録全体を表示PDF形式でダウンロード (491K) -
Carlos Andres Coy Barrera, Ericsson David Coy Barrera, Diana Susana Gr ...原稿種別: Regular Article
2011 年 59 巻 7 号 p. 855-859
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーA novel seco-limonoid, rel-(1S,5R,9S,7R,8S,9R,10S,11R,13S,14R,15R,17R)-11,19-dihydroxy-7-acetoxy-7-deoxoichangin (raputiolide) (1), and two novel quinolone alkaloids N-methyl-2-phenoxyquinolin-4(1H)-one (heptaphyllone A) (2) and 6-methylbenzofuro[2,3-b]quinolin-4(1H)-one (heptaphyllone B) (3), along with the known seco-limonoid ichangin (4), were isolated from Raputia heptaphylla PITTIER (Rutaceae) stem bark. Five known alkaloids, N-methyl-8-methoxyflindersine (5), skimmianine (6), kokusaginine (7), dictamnine (8) and flindersiamine (9), were also isolated from R. heptaphylla leaves. Their structures were established on the basis of full spectroscopic data interpretation supported by data from the pertinent literature. seco-Limonoid 1 configuration was determined by enhanced nuclear Overhauser effect spectroscopy (NOESY) experiments and density functional theory (DFT) molecular modeling. The antileishmanial effect of the isolated compounds was evaluated on Leishmania Viannia panamensis (promastigotes and amastigotes). Whereas alkaloids 2—3, 6—8 and limonoid 4 exhibited no significant parasitocide activity against internalized L. (V.) panamensis amastigotes, limonoid 1 and alkaloid 5 had leishmanicidal activity on intracellular amastigotes (EC50: 8.7 μg/ml) and promastigotes (EC50: 14.3 μg/ml), respectively.抄録全体を表示PDF形式でダウンロード (710K) -
Shin-ichi Fujiwara, Takashi Amisaki原稿種別: Regular Article
2011 年 59 巻 7 号 p. 860-867
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーHuman serum albumin (HSA) binds with drugs and fatty acids (FAs). This study was initiated to elucidate the relationship between the warfarin binding affinity of HSA and the positions of bound FA molecules. Molecular dynamics simulations of 11 HSA-warfarin-myristate complexes were performed. HSA-warfarin binding free energy was then calculated for each of the complexes by the molecular mechanics-Poisson–Boltzmann surface area (MM-PBSA) method. The results indicated that the magnitude of the binding free energy was smaller in HSA-warfarin complexes that had 4 or more myristate molecules than in complexes with no myristate molecules. The unfavorable effect on the HSA-warfarin binding affinity was caused sterically by the binding of a myristate molecule to the FA binding site closest to the warfarin binding site. On the other hand, the magnitude of HSA-warfarin binding free energy was largest when 3 myristate molecules were bound to the high-affinity sites. The strongest HSA-warfarin binding was attributable to favorable entropic contribution related to larger atomic fluctuations of the amino acid residues at the warfarin binding site. In the binding of 2 myristate molecules to the sites with the highest and second-highest affinities, allosteric modulation that enhanced electrostatic interactions between warfarin and some of the amino acid residues around the warfarin binding site was observed. This study clarified the structural and energetic properties of steric/allosteric effects of FAs on the HSA-warfarin binding affinity and illustrated the approach to analyze protein–ligand interactions in situations such that multiple ligands bind to the other sites of the protein.抄録全体を表示PDF形式でダウンロード (2114K) -
Masatomo Ito, Tatsuya Suzuki, Naoki Wakiyama, Hiroshi Teramoto, Etsuo ...原稿種別: Regular Article
2011 年 59 巻 7 号 p. 868-873
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーA nondestructive transmittance near-infrared (NIR) method for detecting off-centered cores in dry-coated (DC) tablets was developed as a monitoring system in the DC tableting process. Caffeine anhydrate was used as a core active pharmaceutical ingredient (API), and DC tablets were made by the direct compression method. NIR spectra were obtained from these intact DC tablets using the transmittance method. The reference assay was performed with HPLC. Calibration models were generated by partial least squares (PLS) regression and principal component regression (PCR) utilizing external validations. Hierarchical cluster analysis (HCA) of the results confirmed that NIR spectroscopy correctly detected off-centered cores in DC tablets. We formulated and used the Centering Index (CI) to evaluate the precision of core alignment and generated an NIR calibration model that could correctly predict this index. The principal component (PC) 1 loading vector of the final calibration model indicated that it could specifically detect the misalignment of tablet cores. The model also had good linearity and accuracy. The CIs of unknown sample tablets predicted by the final calibration model and those calculated through the HPLC analysis were closely parallel with each other. These results demonstrate the validity of the final calibration model and the utility of the transmittance NIR spectroscopic method developed in this study as a monitoring system in DC tableting process.抄録全体を表示PDF形式でダウンロード (782K)
Notes
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Humaira Yasmeen Gondal, Muhammad Iqbal Choudhary, Ahmed Abbas Khan原稿種別: Note
2011 年 59 巻 7 号 p. 874-875
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーMicrobial transformation of (+)-isomenthol (1) by various strains of fungi was investigated. Fusarium lini has successfully converted compound 1 into a new metabolite, 5α-hydroxyisomenthol (2), and a known metabolite, 1α-hydroxyisomenthol (3), whereas incubation with Rhizopus stolonifer only yielded metabolite 3. The transformed metabolites were structurally characterized on the basis of their spectral data.抄録全体を表示PDF形式でダウンロード (452K) -
Kazuya Otake, Satoru Azukizawa, Kenji Takahashi, Masaki Fukui, Michiko ...原稿種別: Note
2011 年 59 巻 7 号 p. 876-879
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリー2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and protein-tyrosine phosphatase 1B (PTP-1B) inhibitory activities. PPARγ agonist activity of 14 was comparable to that of rosiglitazone, and PTP-1B inhibitory activity was about 10-fold weaker than that of ertiprotafib, a PTP-1B inhibitor. Compound 14 showed high oral absorption in rats and potent hypoglycemic effects in KK-Ay mice. In conclusion, 14 would be an excellent lead compound for a new type of anti-diabetic drug with triple actions.抄録全体を表示PDF形式でダウンロード (500K) -
Kazunori Motoshima, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita原稿種別: Note
2011 年 59 巻 7 号 p. 880-884
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーWe discovered inhibitors of the restriction enzymes EcoRI, BamHI and HindIII by screening our library of compounds with a phenethylphenylphthalimide skeleton, based on α-glucosidase inhibitors and liver X receptor antagonists derived from thalidomide. Structural development afforded the potent restriction enzyme inhibitors 25 and 26.抄録全体を表示PDF形式でダウンロード (613K) -
Shigeki Sano, Yoshinori Okubo, Atsushi Handa, Michiyasu Nakao, Syuji K ...原稿種別: Note
2011 年 59 巻 7 号 p. 885-888
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーIsoliquiritigenin [ILG, (E)-1] was readily prepared via the Horner–Wadsworth–Emmons reactions using β-ketophosphonates 5a, b. An improved protocol for the synthesis of (E)-1 via the Claisen–Schmidt condensation was also presented.抄録全体を表示PDF形式でダウンロード (705K) -
Structures of Oleanane-Type Triterpene Saponins, Perennisosides VIII, IX, X, XI, and XII, from the Flowers of Bellis perennisToshio Morikawa, Xuezheng Li, Eriko Nishida, Seikou Nakamura, Kiyofumi ...原稿種別: Note
2011 年 59 巻 7 号 p. 889-895
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーFive new triterpene saponins perennisosides VIII (1), IX (2), X (3), XI (4), and XII (5) were isolated from the MeOH-eluated fraction of the methanolic extract from the flowers of Bellis perennis. The MeOH-eluted fraction of the methanolic extract from the flowers of B. perennis was found to inhibit gastric emptying in olive oil-loaded mice at a dose of 200 mg/kg, per os (p.o.). The stereostructures of 1—5 were elucidated on the basis of chemical and spectroscopic evidence.抄録全体を表示PDF形式でダウンロード (586K) -
Hairin Taha, A. Hamid A. Hadi, Noraziah Nordin, Ibrahim A. Najmuldeen, ...原稿種別: Note
2011 年 59 巻 7 号 p. 896-897
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーPseuduvarines A (1) and B (2), two new dioxoaporphine alkaloids with an amino moiety, were isolated from the stem bark of Pseuduvaria rugosa and their structures were elucidated by combination of 2D-NMR spectroscopic analysis. Pseuduvarines A (1) and B (2) showed cytotoxicity against MCF7, HepG2, and HL-60 (1: IC50, 0.9, 21.7, and >50.0 μM, respectively, 2: IC50 >50.0, 15.7, and 12.4 μM, respectively).抄録全体を表示PDF形式でダウンロード (475K) -
Miwa Kubo, Naoki Shima, Kenichi Harada, Hideaki Hioki, Yoshiyasu Fukuy ...原稿種別: Note
2011 年 59 巻 7 号 p. 898-901
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーTwo new prenylated C6–C3 compounds, cycloillicinone (1) and 4-allyl-2-methoxy-6-(2-methylbut-3-en-2-yl)phenol (2), were isolated from the twigs of Illicium anisatum, and their structures were determined by 2D-NMR methods. Cycloillicinone (1) is a unique prenylated C6–C3 that is appended with an additional geranyl unit. Compound 2 was found to show moderate neurite-outgrowth promoting activity in primary cultured rat cortical neurons at a concentration of 10 μM.抄録全体を表示PDF形式でダウンロード (1003K) -
Zhimin Zhao, Katsuyoshi Matsunami, Hideaki Otsuka, Takakazu Shinzato, ...原稿種別: Note
2011 年 59 巻 7 号 p. 902-905
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーFrom the 1-BuOH-soluble fraction of a MeOH extract of leaves of Tarenna gracilipes, collected in Okinawa, six further new cycloartane glycosides, named tareciliosides H—M (1—6), were isolated. Their structures were established through a combination of spectroscopic analyses.抄録全体を表示PDF形式でダウンロード (471K) -
Norihiro Tada, Yoko Matsusaki, Tsuyoshi Miura, Akichika Itoh原稿種別: Note
2011 年 59 巻 7 号 p. 906-908
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーHydroxycarboxylic acids were converted to the corresponding carbonyl compounds under aerobic photo-oxidative conditions in the presence of FSM-16 under visible light irradiation by a fluorescent lamp. This synthetic protocol is the first example of FSM-16 functioning as a photocatalyst by visible light.抄録全体を表示PDF形式でダウンロード (523K) -
Naonobu Tanaka, Shohei Suto, Jun'ichi Kobayashi原稿種別: Note
2011 年 59 巻 7 号 p. 909-912
発行日: 2011/07/01
公開日: 2011/07/01
ジャーナル フリーTwo new steroidal alkaloids possessing a cevanine-type skeleton, veramadines A (1) and B (2), were isolated from the aerial parts of Veratrum maackii var. japonicum. The structures of 1 and 2 were elucidated on the basis of their spectroscopic data.抄録全体を表示PDF形式でダウンロード (780K)
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