巻号一覧
54 巻, 11 号
選択された号の論文の26件中1～26を表示しています
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Review
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Tatsuya Higashi2006 年 54 巻 11 号 p. 1479-1485
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーWith the rapid shift to an aging society in Japan, age-related diseases, such as osteoporosis, dementia and cancer, are sharply increasing. The measurement of steroids related to these diseases in biological fluids and tissues is useful for elucidation of the nature, diagnosis and treatment of such diseases. LC/MS is considered to be the most promising method for this purpose due to its specificity and versatility, but it sometimes does not demonstrate the required sensitivity for trace amounts of steroids, because steroids have a rather low response using either electrospray ionization (ESI) or atmospheric pressure chemical ionization (APCI). To overcome this problem, the author developed detection-oriented derivatization procedures for steroids in LC/MS. For ESI-MS, introduction of a permanently charged moiety is effective. Based on this, 2-hydrazino-1-methylpyridine was developed and used in monitoring prostatic 5α-dihydrotestosterone, a good index for the follow-up of patients affected by prostate cancer under androgen deprivation therapy and salivary dehydroepiandrosterone, which is now often designated as an anti-aging hormone. A proton-affinitive Cookson-type reagent, 4-[2-(6,7-dimethoxy-4-methyl-3-oxo-3,4-dihydroquinoxalyl)ethyl]-1,2,4-triazoline-3,5-dione, was used for the determination of 1α-hydroxyvitamin D3 [1α(OH)D3], a synthetic prodrug of the active form of vitamin D3, in human plasma, and this new LC/positive-APCI-MS method enabled the pharmacokinetic study of 1α(OH)D3 in humans. Electron-capture APCI-MS based on derivatization with 2-nitro-4-trifluoromethylphenylhydrazine was used for the analysis of neurosteroids, which affect brain excitability through action at the neurotransmitter receptors. With this method, the stress-induced rapid biosynthesis of pregnane-type neurosteroids in rat brains was demonstrated.抄録全体を表示PDF形式でダウンロード (362K)
Regular Articles
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Richer Chen, Hirokazu Takahashi, Hirokazu Okamoto, Kazumi Danjo2006 年 54 巻 11 号 p. 1486-1490
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーWe prepared composite particles of acetaminophen (Act) with chitosan (Cht) and hydroxypropylmethylcellulose phthalate (HPMCP) as a carrier using a newly developed 4-fluid nozzle spray-dryer. Cht dissolves in acid solutions and forms a gel, but it is insoluble in alkaline solutions. On the other hand, HPMCP is insoluble in acid solutions, but it dissolves in alkaline solutions. Therefore, we tested a preparation of controlled release composite particles using the characteristics of these carriers. Act and Cht mixtures in prescribed ratios were dissolved in an acid solution. Composite particles of Act and HPMCP in prescribed ratios were dissolved in alkaline solutions. We evaluated the composite particles of the three components (Act, Cht, and HPMCP) by preparing solid dispersions using a 4-fluid nozzle spray-dryer. Observation of particle morphology by scanning electron microscopy (SEM) revealed that the particles from the spray-drying process had atomized to several microns and had all become spherical. We investigated the physical properties of the composite particles by powder X-ray diffraction, differential scanning calorimetry, and dissolution rate analysis to clarify the effects of crystallinity on the dissolution rate. Powder X-ray diffraction peaks and the heat of fusion of Act in the spray-dried samples decreased in proportion to the carrier content, indicating that the drug was amorphous. These results indicate that the Act–Cht–HPMCP system formed a solid dispersion. Furthermore, we investigated the interaction between the drug and the carrier using FT-IR analysis. FT-IR spectroscopy of the Act solid dispersions suggested that the Act carbonyl and Cht amino groups formed a hydrogen bond. On the other hand, interaction by hydrogen bond was observed between the carbonyl group of HPMCP with the amino group of Act. In the three-component Act–Cht–HPMCP system, the 4-fluid nozzle spray-dried preparation with a mixing ratio of 1 : 2.5 : 2.5 obtained sustained release preparation in all pH test solutions.抄録全体を表示PDF形式でダウンロード (385K) -
Katsuko Komatsu, Yorinobu Nagayama, Ken Tanaka, Yun Ling, Shao-Qing Ca ...2006 年 54 巻 11 号 p. 1491-1499
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーA comparative study of the pharmacologically active constituents of 24 rhubarb samples, which were identified genetically as Rheum tanguticum, 3 intraspecies groups of R. palmatum and R. officinale, was conducted using reversed-phase high performance liquid chromatography (HPLC) methods. Thirty compounds belonging to anthraquinones, anthraquinone glucosides, dianthrones, phenylbutanones, stilbenes, flavan-3-ols, procyanidins, galloylglucoses, acylglucoses, gallic acid, and polymeric procyanidins were analyzed quantitatively. The drug samples derived from the same botanical source showed similar chromatographic profiles, and the comparable specific shape that appeared in the 10-directed radar graphs constructed on the basis of the results of quantitative analysis indicated the relationship between chemical constituent patterns and genetic varieties of rhubarb samples.抄録全体を表示PDF形式でダウンロード (816K) -
Hongyi Qi, Li Li, Chunyan Huang, Wenmin Li, Chunjie Wu2006 年 54 巻 11 号 p. 1500-1507
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe purpose of this study was to systematically optimize an ophthalmic thermosensitive poloxamer analogs gel containing puerarin that was a free flowing liquid below the room temperature and could shift to a gel with an eligible gel strength and bioadhesive force in physiological condition (dilution by the simulated tear fluid and at 35.0 °C). A two-factor, five-level central composite design (CCD) was employed to the optimization procedure. The effect of formulation variables (the w/v concentration of poloxamer 407 (X1) and poloxamer 188 (X2)) on a number of response variables (the gelation temperature before (Y1) and after (Y2) the simulated tear fluid diluted, the difference between them (Y3)) was systemically investigated. A second order polynomial equation was fitted to the data. The resulting equation and response surface plots were used to predict the responses in the optimal region. Finally, 21.0% (w/v) poloxamer 407 and 5.0% (w/v) poloxamer188 were chosen as the optimal poloxamer gel matrix. The influence of the other ingredients on the physicochemical properties of the formulation was also investigated. Hydroxypropyl-β-cyclodextrin (HPCD) enhanced the gelation temperature and reduced the gel strength and the bioadhesive force, while puerarin and benzalkonium chloride (BC) had a comparatively smaller influence. All the isotonicity agents studied had the gelation temperatures lowered, and the gel strengths and the bioadhesive forces enhanced. But only sodium chloride appears to be a promising isotonicity agent for the poloxamer gel containing puerarin, HPCD and BC.抄録全体を表示PDF形式でダウンロード (969K) -
Michiko Kumon, Masahiko Suzuki, Akira Kusai, Etsuo Yonemochi, Katsuhid ...2006 年 54 巻 11 号 p. 1508-1514
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe effect of lactose carrier surface property on the inhalation profile of dry powder inhaler (DPI) was evaluated using a micronized drug (Compound A) by inverse gas chromatography (IGC). Mechanofusion with magnesium stearate (Mg-St) or sucrose stearate increased the fine particle fraction (FPF), considered to be due to decrease in the interaction between Compound A and the lactose carrier. The effect of Compound A concentration on FPF was smaller in mechanofusion-processed lactose compared to intact lactose, especially when processed with Mg-St. The relationship between the IGC parameters of the lactose and FPF was also investigated. FPF increased as both the dispersive component of the surface energy and acidity similarity between the lactose carriers and Compound A increased. Although further investigation is necessary, it could be suggested that acidity similarity decreases the interaction between Compound A and lactose, thus contributing to the increase in the FPF. In conclusion, (1) mechanofusion with Mg-St or sucrose stearate could be an effective method to improve FPF of a DPI drug formulation; (2) IGC would be a valuable method to investigate the interaction between a drug and the DPI carrier; and (3) a relationship between surface acidity and inhalation profile was suggested.抄録全体を表示PDF形式でダウンロード (1754K) -
Jun Chiba, Shin Iimura, Yoshiyuki Yoneda, Yuichi Sugimoto, Takao Horiu ...2006 年 54 巻 11 号 p. 1515-1529
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーA novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50=1.6 nM each) and moderate lipophilicity (Log D=2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.抄録全体を表示PDF形式でダウンロード (427K) -
Toshio Morikawa, Fengming Xu, Hisashi Matsuda, Masayuki Yoshikawa2006 年 54 巻 11 号 p. 1530-1534
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーA new flavanol, erycibenin D, and two new flavans, erycibenins E and F, were isolated from the stems of Erycibe expansa originating in Thailand. The structures of new flavonoids were elucidated on the basis of chemical and physicochemical evidence. In addition, the inhibitory activities of the isolated constituents from E. expansa on lipopolysaccharide-activated nitric oxide production in mouse peritoneal macrophages were examined. Among the principal constituents, two isoflavones, clycosin (IC50=13 μM) and erythrinin B (18 μM), and two rotenoids, deguelin (26 μM) and rotenone (27 μM), were found to show potent inhibitory activity.抄録全体を表示PDF形式でダウンロード (199K) -
Fumihiko Saitoh, Takafumi Mukaihira, Hidemitsu Nishida, Tsutomu Satoh, ...2006 年 54 巻 11 号 p. 1535-1544
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーWe have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved in a similar fashion to the N,O-spiro acetal synthesis. Consequently, FXa inhibitory activity was increased and more active compounds could be found (M58163: IC50=0.61 nM, M58169: IC50=0.58 nM). Additionally, the absolute configuration could be determined by X-ray crystallography analysis (M58169: (R)-config.).抄録全体を表示PDF形式でダウンロード (326K) -
Seikou Nakamura, Toshiyuki Murakami, Junko Nakamura, Hisanori Kobayash ...2006 年 54 巻 11 号 p. 1545-1550
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThree new cucurbitane-type triterpene called karavilagenins A, B, and C and five new cucurbitane-type triterpene glycosides called karavilosides I, II, III, IV, and V were isolated from the dried fruit of Sri Lanka Momordica charantia L. (Cucurbitaceae) together with two known cucurbitane-type triterpenes, 19(R)-methoxy-5β,19-epoxycucurbita-6,23-dien-3β,25-diol and 5,19-epoxycucurbita-6,23-diene-3,25-diol, and nine known cucurbitane-type triterpene glycosides, goyaglycosides-b, -c, and -d, and momordicosides F1, F2, G, I, K, and L. The structures of karavilagenins and karavilosides were elucidated on the basis of chemical and physicochemical evidence.抄録全体を表示PDF形式でダウンロード (323K) -
Tsutomu Warashina, Tadataka Noro2006 年 54 巻 11 号 p. 1551-1560
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThirty-two new 13,14-seco and 13,14:14,15-disecopregnane glycosides were obtained from the roots of Cynanchum sublanceolatum (Asclepiadaceae). These glycosides were confirmed to be possessing five known compounds, cynajapogenin A, glaucogenin-A, 13-hydroxycynajapogenin A, 2α-hydroxyanhydrohirundigenin, atratogenin A and one new pregnane, 13-epi-cynajapogenin A, as their aglycones, using both spectroscopic and chemical methods.抄録全体を表示PDF形式でダウンロード (232K) -
Abolghasem Jouyban2006 年 54 巻 11 号 p. 1561-1566
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーA numerical method is proposed for predicting solubility of drugs in water–PEG 400 mixtures based on the Jouyban–Acree cosolvency model. The accuracy of the proposed method is evaluated by computing mean percentage deviation (MPD) and compared with that of log-linear model of Yalkowsky. The overall MPDs of the Jouyban–Acree model and the most accurate version of Yalkowsky's model are 39.8 (±46.7) % and 175.8 (±266.4) %, respectively, and the mean difference is statistically significant (p<0.0005). The proposed method produces acceptable residual distribution and the probability of solubility prediction with residual log of solubility <0.5 unit is 0.86. The applicability of the proposed method could be extended for predicting the solubility of drugs in water–PEG 400 mixtures at various temperatures. The impact of various log P values computed using different software is also studied and the results of ANOVA revealed that there are no significant differences between the accuracy of the predicted solubilities employing various log P values.抄録全体を表示PDF形式でダウンロード (204K) -
Natsuko Murata, Shiho Fujimori, Yoshitatsu Ichihara, Yoshio Sato, Take ...2006 年 54 巻 11 号 p. 1567-1570
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーWe synthesized 9α-fluoromedroxyprogesterone acetate (FMPA) in order to test whether it is a more potent anti-angiogenic agent than medroxyprogesterone acetate (MPA), which has been widely used as a therapeutic agent for breast and endometrium cancers. FMPA was previously synthesized in 10 steps (total yield: 1%). An efficient synthesis of FMPA has been achieved in 6 steps (total yield: 12%). We examined the anti-tumor effect of FMPA, complexed with dimethyl-β-cyclodextrin (DM-β-CyD), on rat mammary carcinomas induced by 7,12-dimethylbenz[a]anthracene (DMBA). FMPA showed great anti-tumor effect on DMBA-induced rat mammary carcinomas.抄録全体を表示PDF形式でダウンロード (183K) -
Akichika Itoh, Tomohiro Kodama, Yukio Masaki, Shinji Inagaki2006 年 54 巻 11 号 p. 1571-1575
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーFSM-16, a mesoporous silica, was found to catalyze oxidative photo-decarboxylation of α-hydroxy carboxylic acid, phenyl acetic acid derivatives and N-acyl-protected α-amino acids to afford the corresponding carbonyl compounds. Furthermore, FSM-16 proved to be re-usable by re-calcination at 450 °C after the reaction.抄録全体を表示PDF形式でダウンロード (165K) -
Takafumi Arao, Kei Sato, Kazuhiro Kondo, Toyohiko Aoyama2006 年 54 巻 11 号 p. 1576-1581
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーFunction of a new N-heterocyclic carbene ligand based on the concept of a chiral mimetic is described. With (4R,5R)-4,5-diphenyl-1,3-dialkyl-4,5-dihydro-3H-imidazol-1-ium tetrafluoroborates as N-heterocyclic carbene precursors, Rh-catalyzed enantioselective arylation (up to 27% ee) of aromatic aldehydes with arylboronic acids and Pd-catalyzed enantioselective intramolecular α-arylation (up to 66% ee) of N-(2-bromoaryl)-N-alkyl-2-arylpropanamides are investigated.抄録全体を表示PDF形式でダウンロード (200K) -
Jun Wu, Si Zhang, Minyi Li, Yuan Zhou, Qiang Xiao2006 年 54 巻 11 号 p. 1582-1585
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーFour new mexicanolides with a Δ14,15 double bond, named xylogranatins A and D (1—4), were isolated from the fruit of a Chinese mangrove Xylocarpus granatum, together with two known 8,9,30-phragmalin ortho esters, xyloccensins P and Q. Their structures were elucidated on the basis of spectroscopic data, especially 2D NMR techniques including HSQC, HMBC and NOESY.抄録全体を表示PDF形式でダウンロード (320K)
Notes
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Palanivelu Manoj Kumar, Chandrabose Karthikeyan, Narayana Subbiah Hari ...2006 年 54 巻 11 号 p. 1586-1591
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーIn the present paper, quantitative structure activity relationship (QSAR) approach was applied to understand the affinity and selectivity of a novel series of triaryl imidazole derivatives towards glucagon receptor. Statistically significant and highly predictive QSARs were derived for glucagon receptor inhibition by triaryl imidazoles using QuaSAR descriptors of molecular operating environment (MOE) employing computer-assisted multiple regression procedure. The generated QSAR models revealed that factors related to hydrophobicity, molecular shape and geometry predominantly influences glucagon receptor binding affinity of the triaryl imidazoles indicating the relevance of shape specific steric interactions between the molecule and the receptor. Further, QSAR models formulated for selective inhibition of glucagon receptor over p38 mitogen activated protein (MAP) kinase of the compounds in the series highlights that the same structural features, which influence the glucagon receptor affinity, also contribute to their selective inhibition.抄録全体を表示PDF形式でダウンロード (197K) -
Hai-Long Yuan, Ming Yang, Xian-Yi Li, Rong-Hui You, Yi Liu, Jun Zhu, H ...2006 年 54 巻 11 号 p. 1592-1594
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーFrom the ethanol extract of the seeds of Herpetospermum caudigerum wall, one new lignan compound 1, was isolated and characterized along with three known compounds 2, 3 and 4. The structure elucidation of the isolated new compound was performed on the basis of spectroscopic and chemical evidence. The structures of known compounds were determined by comparison of spectral data and physical data with those previously reported. The activity inhibiting hepatitis b virus was evaluated. Preliminary studies showed that compound 1 and 2 displayed promising inhibitory potential against hepatitis b virus.抄録全体を表示PDF形式でダウンロード (93K) -
Jun-Rong Yang, Zheng An, Zhi-Hong Li, Song Jing, Hai-Lin Qina2006 年 54 巻 11 号 p. 1595-1598
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThree new natural sesquiterpene coumarins, isofeterin (1), lehmannolol (3), sinkianone (4), and one known compound, lehmannolone (2), were isolated from the roots of Ferula teterrima and Ferula sinkiangensis. Their chemical structures were established on the basis of spectroscopic analysis, including X-ray crystallography and CD spectrum measurements for determining the absolute configuration of compound 2.抄録全体を表示PDF形式でダウンロード (179K) -
Hamad Hassan Issa, Sue-Ming Chang, Yu-Liang Yang, Fang-Rong Chang, Yan ...2006 年 54 巻 11 号 p. 1599-1601
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーTwo new sesquiterpene lactones, spicatolide C (1) and spicatocadinanolide A (2), have been isolated along with the known piptocarphol isomers (3, 4) and one eudismane type sesquiterpene (5) from the EtOAc extract of the aerial parts of Pseudoelephantopus spicatus. The structures and the relative stereochemistries of the new metabolites were determined by spectroscopic methods.抄録全体を表示PDF形式でダウンロード (158K) -
Yutaka Aoyagi, Yoshinao Takahashi, Haruhiko Fukaya, Koichi Takeya, Rit ...2006 年 54 巻 11 号 p. 1602-1604
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーIsetexane diterpene analogues were semisynthesized from demethylsalvicanol isolated from Perovskia abrotanoides (Labiatae). The structure and cytotoxic activity relationships (SAR) of the natural parent diterpene, demethylsalvicanol, and its semisynthetic analogues were studied by using P388 murine leukemia cells.抄録全体を表示PDF形式でダウンロード (105K) -
Zong-Tsi Chen, Shwu-Woan Lee, Chiu-Ming Chen2006 年 54 巻 11 号 p. 1605-1607
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーA new sulfated cucurbitacin, cucurbitacin B 2-sulfate (1) and a new cucurbitacin glucoside, cucurbitacin G 2-O-β-D-glucopyranoside (2) together with two known cucurbitacin glucosides, arvenin I and arvenin III were isolated from the root bark of Helicteres angustifolia. The structures of these compounds were established on the basis of spectroscopic and chemical evidence. These four compounds taste of strong bitterness. Compound 1 is a first sulfated cucurbitacin found in plants.抄録全体を表示PDF形式でダウンロード (81K) -
Toshifumi Dohi, Koji Morimoto, Naoko Takenaga, Akinobu Maruyama, Yasuy ...2006 年 54 巻 11 号 p. 1608-1610
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe facile and clean direct cyanating reaction of pyrroles and thiophenes has been achieved using a recyclable hypervalent iodine(III) reagent 1b by a simple solid-liquid separation of the products and the reagent.抄録全体を表示PDF形式でダウンロード (79K) -
Kohei Gotoh, Teruhisa Yamamoto, Mitsuhiro Yoshimatsu2006 年 54 巻 11 号 p. 1611-1615
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe scandium-catalyzed reactions of α-organosulfanyl and organoselanyl-α-fluoroacetates 1—2, acetamides 3—4 and acetonitrile 5 with soft nucleophiles proceeded to give the products 6a—b, 7a—c, 8a—c, 9a—e in good to high yields. We also successfully performed the scandium-catalyzed intramolecular cyclization reactions and obtained the unique 5-methylene-2-oxotetrahydropyrans 16—17.抄録全体を表示PDF形式でダウンロード (148K) -
Takeshi Isoda, Kazuhiko Hayashi, Satoshi Tamai, Toshio Kumagai, Yoshim ...2006 年 54 巻 11 号 p. 1616-1619
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe tandem and stepwise Staudinger/aza-Wittig reactions of several azides were examined in detail. The tandem reaction method (Method I) exhibited superior results in the yield of the corresponding isothiocyanates bearing an electron-withdrawing group than the conventional stepwise method (Method II) which involves the sequential treatment of the azides with triphenylphosphine and then carbondisulfide. The mechanistic consideration for both reaction methods was proposed on the basis of the 1H-NMR analyses.抄録全体を表示PDF形式でダウンロード (123K)
Communications to the Editor
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Hiroki Nakayama, Akichika Itoh2006 年 54 巻 11 号 p. 1620-1621
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーBenzyl alcohols and allylic alcohols were found to be oxidized to the corresponding aldehydes in the presence of a catalytic amount of iodine under irradiation of a fluorescent lamp.抄録全体を表示PDF形式でダウンロード (92K) -
Masahiro Anada, Masahiko Tanaka, Kanami Suzuki, Hisanori Nambu, Shunic ...2006 年 54 巻 11 号 p. 1622-1623
発行日: 2006年
公開日: 2006/11/01
ジャーナル フリーThe use of dirhodium(II) catalysts in the 1,4-hydrosilylation of α,β-unsaturated ketones and aldehydes was explored. Dirhodium(II) tetrakis(perfluorobutyrate), Rh2(pfb)4, proved to be the catalyst of choice for this process, providing the corresponding silyl enol ethers in high yields.抄録全体を表示PDF形式でダウンロード (99K)
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