巻号一覧
58 巻, 4 号
選択された号の論文の32件中1～32を表示しています
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Regular Articles
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Shivsagar Ashok Randale, Chandu Somatbhai Dabhi, Avinash Ramrao Tekade ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 443-448
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe purpose of this study was to mask the intensely bitter taste of metoclopramide HCl and to formulate a rapid disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing metoclopramide HCl with aminoalkyl methacrylate copolymer (Eudragit® EPO) in different ratio by the extrusion–precipitation method. Drug–polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.8, taste evaluation in oral cavity and molecular property. The complex having drug–polymer ratio of 1 : 2 shows significant taste masking, confirmed by drug release in SSF and in-vivo taste evaluation; therefore, it was selected for further study. Taste evaluation of DPCs in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) within 10 s, whereas, metoclopramide HCl was rated intensely bitter with a score of +3 for 10 s. Tablets were evaluated for various parameters like tensile strength, wetting time, water absorption ratio, in-vitro disintegration time, and disintegration in oral cavity. The effect of diluents, lubricants and sweetening agent (Xylisorb) on the disintegration time was also evaluated. Tablets of batch F3 containing mannitol and microcrystalline cellulose in the ratio 1 : 1 and 8% w/w crosspovidone showed faster disintegration (within 20 s) than the marketed formulation (180 s). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Tablets of batch F3 also revealed rapid drug release (t90, 90 s) in SGF compared with marketed formulation (t90, 600 s).抄録全体を表示PDF形式でダウンロード (389K) -
Miyako Yoshida, Emi Tokuyama, Mai Hazekawa, Takahiro Uchida原稿種別: Regular Article
2010 年 58 巻 4 号 p. 449-453
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe purpose of this study was to evaluate the effect of various flavoured jellies on the palatability and bitterness of the Kampo medicine ‘Orengedokuto’, using human gustatory sensation testing. In the gustatory sensation test, eight items were evaluated according to the semantic differential (SD) method and four taste intensities (sweetness, astringency, sourness, and bitterness) were determined. Factor analysis of the results identified two main factors ‘Disagreeable taste’ and ‘Agreeable taste and odour’ as predominantly determining the palatability of Orengedokuto. To investigate the influence of jelly odour, evoked images were obtained for five fundamental tastes after smelling jellies. The inhibitory effect of the jelly odour on the bitterness of Orengedokuto was found to be small. When the influence of the various jellies on the disagreeable taste of Orengedokuto was investigated, the bitterness intensities of Orengedokuto mixed with chocolate or strawberry–chocolate jelly were found to be significantly lower than the bitterness of the control. The bitterness intensity of Orengedokuto was found to be significantly and negatively correlated with sweetness intensity using simple linear regression analysis. These results suggest that the sweetness intensity of various jellies inhibits the bitterness intensity of Orengedokuto.抄録全体を表示PDF形式でダウンロード (605K) -
Yoko Sakuda, Akihiko Ito, Masanaho Sasatsu, Yoshiharu Machida原稿種別: Regular Article
2010 年 58 巻 4 号 p. 454-457
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーMedicinal carbon (MC) films, which can be taken more easily than other dosage forms, were prepared using sodium carboxymethyl cellulose (CMC), hydroxypropylmethyl cellulose (HPMC) and alginic acid sodium (ALG) as film base materials. Brilliant blue FCF (BB) was used as a model drug. The films containing MC had sufficient strength and disintegration time, but their ability to adsorb BB was clearly inhibited compared to that of MC in powder form. When ALG was used as the film base, the BB adsorption capacity of MC film was approximately 50% of that of MC powder. In an attempt to improve this adsorption ability, two saccharides, sorbitol (SOR) and maltitol (MT), were separately added to MC at a mixing ratio of 1 : 1 by weight. When ALG was the film base, MC films containing SOR or MT showed rapid adsorption profiles and had greatly increased capacities for BB adsorption compared with films containing MC alone. SOR was superior to MT as an additive, though both gave MC-containing films a BB adsorption capacity almost equal to that of MC powder after 24 h, and physical mixtures tended to have better BB adsorption capacities than pre-treatment mixture. In addition, both SOR and MT tended to increase vertical strength of films, but neither additive in either type of mixture had a clear effect on disintegration time. When CMC or HPMC was used as the film base, on the other hand, the addition of SOR or MT caused hardly any improvement in adsorption ability. The above results demonstrate that ALG is useful as a film base material for the preparation of MC films, and that MC films with sufficient strength and adsorption capacities equal to those of MC powders can be produced using a physical mixture of MC and SOR on an ALG base.抄録全体を表示PDF形式でダウンロード (253K) -
Yukako Ito, Tomohiro Maeda, Keizo Fukushima, Nobuyuki Sugioka, Kanji T ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 458-463
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーAscorbic acid (AA) loaded self-dissolving micropiles (SDMP) were prepared using chondroitin sulfate as the base for the percutaneous administration of AA. AA solution was added to dense solution of chondroitin solution, glue, and array tip, 1.0 cm2, containing 100 SDMPs of which length was 500 μm and basal diameter was 300 μm, were prepared. Two kinds of AA array tips containing 1344.2±1.7 μg (high content ones) and 638.7±4.3 μg (low content ones) were used. In vitro dissolution study showed that more than 90% of AA were released from both SDMP array tips within 5 min. Stability experiment showed that 99.2—99.4% of AA was detected in SDMP array tips when stored at 23 °C for 1 week. When in vitro permeation experiments were performed after AA SDMP array was inserted to the isolated rat abdominal skin, extremely high amounts of AA, 1285.3±369.0 μg (95.3%) for high content SDMP tip and 405.6±84.3 μg (65.8%) for low content SDMP tip, were permeated for 6 h into the receptor compartment due to the break down of the skin barrier function. When AA SDMP array tip was administered to the rat skin under anesthetized condition with the different contact times, 10, 20 and 30 min, the permeated amount of AA was dependent on both the AA content in SDMP array tips and the contact time. When AA SDMP was contact to the skin for 30 min, permeated amounts of AA were 146.8±22.9 μg (10.9%) for high content-SDMP tip and 61.2±18.2 μg (9.6%) for low content SDMP tip. These results suggest the usefulness of SDMP array tip for the percutaneous absorption of AA.抄録全体を表示PDF形式でダウンロード (545K) -
Yi Lu, Jui-Hsin Su, Chiung-Yao Huang, Yung-Chun Liu, Yao-Haur Kuo, Zhi ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 464-466
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTwo new cembranoids, namely granosolides C (1) and D (2), along with one known cembranoid 4, were isolated from the soft coral Sinularia granosa. Chemical investigation of Sinularia querciformis also afforded one new cembranoid, querciformolide E (3), along with four known cembranoids 4—7. The structures of these compounds were elucidated on the basis of their spectroscopic data. Both 4 and 5 were shown to significantly inhibit the accumulation of the pro-inflammatory inducible nitric oxide synthase protein in lipopolysaccharide-stimulated RAW264.7 macrophage cells.抄録全体を表示PDF形式でダウンロード (274K) -
Dong-Qing Fei, Qiu-Hong Wu, Shi-Gang Li, Kun Gao原稿種別: Regular Article
2010 年 58 巻 4 号 p. 467-469
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTwo new asymmetric eremophilane-type sesquiterpene dimers, ligulamulienin A (1) and B (2), were isolated from the rhizomes of Ligularia muliensis. Their structures were determined based on their spectroscopic data, including IR, EI-MS, HR-electrospray ionization (ESI)-MS, 1D and 2D-NMR spectroscopy. The cytotoxicity of compounds 1 and 2 was measured in in vitro human carcinoma (MGC-803), human hepatoma (HEP-G2), and murine sarcoma (S-180) cell lines.抄録全体を表示PDF形式でダウンロード (188K) -
Ke Pan, Masanori Inagaki, Nagisa Ohno, Chiaki Tanaka, Ryuichi Higuchi, ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 470-474
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTwenty-one galactocerebrosides (1—21), including sixteen new compounds (3—7, 9—17, 19, 21), were identified from a cerebroside molecular species obtained from the chloroform/methanol extract of pyloric caeca dissected from the starfish Protoreaster nodosus. The structures of these galactocerebrosides were determined on the basis of chemical and spectroscopic evidences. Especially, one-pot GC-MS analysis following methanolysis and periodate oxidation of these galactocerebrosides gave efficient structural information of ceramide moiety rapidly in minute amounts.抄録全体を表示PDF形式でダウンロード (439K) -
Xiaoyin Chen, Zonghua Wang, Feifei Zhang, Lingyan Zhu, Yanhui Li, Yanz ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 475-478
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe electrochemical behaviors of rutin at a poly(p-aminobenzene sulfonic acid) modified glassy carbon electrode (PABSA/GC) have been investigated. Rutin can generate a pair of well-defined redox peaks at the PABSA/GC located at 0.440 V (Epa) and 0.396 V (Epc) (vs. saturated calomel electrode (SCE)), respectively. The results indicate that the reaction involves two electrons transfer, accompanied by two protons and the electrochemical process is controlled by adsorption. The electrochemical parameters of rutin on the modified electrode were calculated with the results of the charge transfer coefficient (α), the number of electron transfer (n) and the electrode reaction rate constant (ks) as 0.61, 2.08 and 2.18 s−1, respectively. Under the selected conditions, the oxidation peak current was linear to the rutin concentration over the range of 2.5×10−7—1.0×10−5 M with a detection limit of 1.0×10−7 M. The proposed method has been successfully applied to the determination of compound rutin tablets with no interference from the coexisting ascorbic acid.抄録全体を表示PDF形式でダウンロード (360K) -
Bahira Hegazi, Hanan Ahmed Mohamed, Kamal Mohamed Dawood, Farid Abdel- ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 479-483
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーBenzo[d]imidazole 3 and 1,2,4-triazin-5(2H)-one 6 were prepared by the reaction of starting ethyl (3-hydroxy-1H-inden-2-yl)(oxo)-acetate 2 with o-phenylenediamine and thiosemicarbazide respectively. Reaction of 1,4-dihydro-1-phenylindeno[1,2-c]pyrazole-3-carbohydrazide 8 with phenylisothiocyanate gave thiosemicarbazide 9, and its reaction with chloroacetic acid or phenacylbromides led to the formation of thiazolidinone-4-one 10 or 1,3-thiazoles 12a, b. The reactivity of hydrazide 8 towards fluorinated aldehyde, phthalic anhydride, and hydrazonoyl chlorides 15a, b was studied to give fluorinated hydrazones, imide bis-hydrazones 13—16. The newly synthesized compounds were screened for their cytotoxic activities and compounds 6, 8, 9 and 10 were found the most potentially cytotoxic. The detailed synthesis, spectroscopic and biological data are reported.抄録全体を表示PDF形式でダウンロード (353K) -
Tomoyoshi Fuchise, Hideki Kishimura, Zhi-hong Yang, Mareshige Kojoma, ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 484-487
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーAtlantic cod trypsin-catalyzed peptide synthesis has been studied by using p-amidino- and p-guanidinophenyl esters of N-(tert-butyloxycarbonyl)amino acid as acyl donor components. The reaction temperature was optimized at 0 °C. The method was shown to be successful as effectively for synthesizing the peptide and useful for preparing dipeptide between D-amino acid with D-amino acid and β-amino acid with β-amino acid, respectively. The enzymatic hydrolysis of the resulting products was negligible.抄録全体を表示PDF形式でダウンロード (222K) -
Hiroki Tsumoto, Ryo Taguchi, Kohfuku Kohda原稿種別: Regular Article
2010 年 58 巻 4 号 p. 488-494
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーProtein nitration at tyrosine residues proceeds to form 3-nitrotyrosine; this product is today used as a biomarker of nitrative stress. We have developed an efficient method with which to identify nitrated peptides and to quantify protein nitration levels in different biological samples by a combination of the chemical derivatization of nitrotyrosine-containing peptides and mass spectrometry. Our strategy includes: 1) the protection of both N-terminal amines and ε-amines of lysine residues by acetylation with 13C0/13C4– or D0/D6–acetic anhydride; 2) the reduction of nitrotyrosine to aminotyrosine with sodium hydrosulfite; and 3) the derivatization of aminotyrosine with 1-(6-methyl[D0/D3]nicotinoyloxy)succinimide. The utility of our method is demonstrated with nitrotyrosine-containing angiotensin II and bovine serum albumin as the model compounds.抄録全体を表示PDF形式でダウンロード (706K) -
Kazusa Nishiyama, Atsushi Yamada, Miki Takahashi, Tomoharu Takeuchi, K ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 495-500
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTo search for the endogenous glyco-epitope in Caenorhabditis elegans, we synthesized labeled Galβ1-3Fuc and Galβ1-4Fuc and examined their binding affinity for C. elegans galectin LEC-6 using frontal affinity chromatography analysis. We developed a new strategy for synthesizing the labeled saccharides, in which the labeling unit, the 2-aminopyridine moiety, is coupled with a spacer unit derived from D-mannitol. Our results indicate that Galβ1-4Fuc is the endogenous glyco-epitope present in C. elegans N-glycans.抄録全体を表示PDF形式でダウンロード (483K) -
Sherine Nabil Khattab原稿種別: Regular Article
2010 年 58 巻 4 号 p. 501-506
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーA new family of sulfonate ester-type coupling reagents is described which differs in its leaving group. The sulfonate ester coupling reagents ethyl 2-cyano-2-(naphthalen-2-ylsulfonyloxyimino)acetate (NpsOXY), and ethyl 2-cyano-2-(tosyloxyimino)acetate (TsOXY) are more efficient alternatives to the benzotriazole sulfonate esters in terms of racemization suppression and coupling effectiveness. Both oxyma and its related sulfonate esters can be handled with a considerably lower risk than the explosive benzotriazole and its derivatives. 2-Oxopyridin-1(2H)-yl naphthalene-2-sulfonate (NpsOPy) and 2-oxopyridin-1(2H)-yl 4-methylbenzenesulfonate (TsOPy) sulfonate esters derived from 1-hydroxypyridin-2(1H)-one were also successfully used as new coupling reagents requiring a longer preactivation time during the coupling process. An improvement in yield and almost comparable optical purity to that of the 1-hydroxy-benzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) analogues was observed.抄録全体を表示PDF形式でダウンロード (198K) -
Cai-Xia Dong, Kyoko Hayashi, Jung-Bum Lee, Toshimitsu Hayashi原稿種別: Regular Article
2010 年 58 巻 4 号 p. 507-510
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThree polysaccharides including a neutral polysaccharide (RN), an acidic polysaccharide (RA) and a pectic polysaccharide (RP) were isolated from aerial part of Portulaca oleracea L. and evaluated for their anti-herpes simplex virus type 2 (HSV-2) and anti-influenza A virus (IFV-A). RN was found to consist of glucose (Glc), mannose (Man) and arabinose (Ara) with small amounts of galactose (Gal), and identified to be an arabinoglucomannan. RA was mainly composed of Gal and Ara with a small proportion of glucuronic acid (GlcA). It was characterized as a type II arabinogalactan (AGII), which consisted of a 1,3-, 1,6- and 1,3,6-linked galactopyranosyl (Galp) and non-reducing terminal and 1,5-linked arabinofuranosyl (Araf) residues. RP was deduced to be a pectin, which consisted of a predominant amount of galacturonic acid (GalA) with small amounts of Gal, rhamnose (Rha) and Ara. The GalA residues were found to be highly methyl-esterified and partially acetylated. Results of antiviral tests showed that only RP had anti-HSV-2 activity. Furthermore, its anti-HSV-2 target was elucidated to be the step of virus penetration into host cells. No marked virucidal activity of RP was observed.抄録全体を表示PDF形式でダウンロード (182K) -
Yasuyoshi Agata, Yasunori Iwao, Atsuo Miyagishima, Shigeru Itai原稿種別: Regular Article
2010 年 58 巻 4 号 p. 511-515
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーA mechanistic mathematical model was designed to predict dissolution patterns under non-sink conditions. Sulfamethoxazole was used as a model drug, and its physico-chemical properties such as solubility, density, and intrinsic dissolution rate constant etc., were investigated in order to apply these experimental values to the proposed model. Dissolution tests were employed as a way of validating the mathematical model, and it was found that the predictions given by the model were surprisingly accurate for all particle sizes. In addition, a simulation focused on forecasting the fraction of the drug that was dissolved at a certain time point when various initial particle diameters were used was also particularly valuable. Therefore, these results demonstrated that the model enables dissolution profiles to be analyzed under non-sink conditions.抄録全体を表示PDF形式でダウンロード (300K) -
Ramin Ghahremanzadeh, Fatemeh Fereshtehnejad, Ayoob Bazgir原稿種別: Regular Article
2010 年 58 巻 4 号 p. 516-520
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーA simple and one-pot synthesis of new chromeno[2,3-d]pyrimidine-triones by a three-component condensation reaction of barbituric acids, aldehydes and cyclohexane-1,3-diones in refluxing ethanol in the presence of p-toluenesulfonic acid (p-TSA) for 3—10 h is reported. Two cyclohexane-1,3-diones, four barbituric acids and six substituted aldehydes were chosen for the library validation. Prominent among the advantages of this new method are operational simplicity, good yields and easy work-up procedures employed.抄録全体を表示PDF形式でダウンロード (237K) -
Bui Huu Tai, Vu Thi Huyen, Tran Thu Huong, Nguyen Xuan Nhiem, Eun-Mi C ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 521-525
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe new pyrano-pyrone, (+)-8-epi-9-deoxygoniopypyrone (1) and (+)-9-deoxygoniopypyrone (2) were isolated from a chloroform extract of Goniothalamus tamirensis leaves. Their absolute stereostructures were discussed and confirmed by using infrared (IR), Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR-MS), one (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) spectra, Mosher's method, and comparison with the known compounds leiocapin A (3), deoxygoniopypyrone A (4), and (−)-8-epi-9-deoxygoniopypyrone (5). At concentrations of 2.67 μM, compounds 1 and 2 significantly increased the growth of osteoblastic MC3T3-E1 cells and caused a significant elevation of collagen content, alkaline phosphatase activity, and nodule mineralization in the cells (p<0.05). Our data suggest that the enhancement of osteoblast function by 1 and 2 may result in the prevention of osteoporosis.抄録全体を表示PDF形式でダウンロード (387K) -
Suresh Thareja, Ganesh Rajendra Kokil, Saurabh Aggarwal, Tilak Raj Bha ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 526-532
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーProtein tyrosine phosphatase 1B (PTP 1B), a cytosolic PTP involved in down-regulation of receptor tyrosine kinase activity following stimulation of the insulin or leptin receptors. Thus, PTP 1B inhibitors could potentially ameliorate insulin resistance and normalize plasma glucose and insulin levels without inducing hypoglycemia, and could therefore be a major advancement in the treatment of type 2 diabetes. A three-dimensional quantitative structure–activity relationship (3D-QSAR) study has been performed on a novel class of sulphonamides using self-organizing molecular field analysis (SOMFA) to correlate their chemical structures with their observed PTP 1B inhibitory activities. The master grid obtained for the various SOMFA models indicates electrostatic and shape potential contributions that can be mapped back onto structural features relating to the trends in inhibitory activities. On the basis of the spatial arrangement, steric and electrostatic factors should appropriately be taken into account for development of new potent inhibitors of PTP 1B for the management of type 2 diabetes.抄録全体を表示PDF形式でダウンロード (916K) -
Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takayuki Suzuki, Te ...原稿種別: Regular Article
2010 年 58 巻 4 号 p. 533-545
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーIn the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human β3-, β2-, and β1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5-methylthiazol-4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3-ylacetanilide (36h) derivatives showed potent agonistic activity at the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model.抄録全体を表示PDF形式でダウンロード (856K)
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Mehdi Mohammadi, Maryam Yousefi, Zohreh Habibi, Abbas Shafiee原稿種別: Notes
2010 年 58 巻 4 号 p. 546-548
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe aerial parts of several Angelica species of the Apiaceae as natural medicine, are rich sources of various coumarins with biological, to a lesser extent, toxicological activities. From the chloroform extract of the aerial parts of Angelica urumiensis MOZAFF. two new coumarins (1, 2), together with six known coumarins and two known flavonoids were isolated. On the basis of comprehensive spectroscopic analyses, including electron ionization-mass spectra (EI-MS), 1H-NMR, 13C-NMR, 1D nuclear Overhauser effect (NOE), distortionless enchancement by polarization transfer (DEPT), H, H correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple bond correlation (HMBC), rotating frame Overhauser enhancement spectroscopy (ROESY) spectra and comparison with spectral data of known compounds, the structure of new compounds were established as pyranocoumarin dimmer (1) and (+)-8,9-dihydro-8-(2-hydroxypropan-2-yl)-2-oxo-2H-furo[2,3-h]chromen-9-yl-3-methylbut-2-enoate (2). The eight known compounds (3—10) were isosamidin, laserpitin, pteryxin, isolaserpitin, cis-khellactone, angelicin, genkwanin and salvigenin, respectively. These known structures are isolated from the aerial parts of A. urumiensis for the first time. Antioxidant activities of the two new coumarins were evaluated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and exhibited a moderate antioxidant activity.抄録全体を表示PDF形式でダウンロード (110K) -
Jian-Feng Liu, Kang-Ping Xu, Fu-Shuang Li, Jian Shen, Chang-Ping Hu, H ...原稿種別: Notes
2010 年 58 巻 4 号 p. 549-551
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーA new flavonoid, 6-(2-hydroxy-5-carboxyphenyl)-apigenin (1), together with two new natural products, 3-(4-hydroxyphenyl)-6,7-dihydroxy coumarin (2), 1-methoxy-3-methylanthraquinone (3) and four known compounds, were isolated from Selaginella tamariscina (BEAUV.) SPRING. The structures of the new isolated compounds were elucidated on the basis of 1D and 2D NMR as well as ESI-HR-MS spectroscopic analysis.抄録全体を表示PDF形式でダウンロード (201K) -
Jing Zhang, Sheng-Xin Yang, Xiao-Bo Yang, Min-Yi Li, Gang Feng, Jian-Y ...原稿種別: Notes
2010 年 58 巻 4 号 p. 552-555
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTwo new mexicanolides, named xylomexicanolides A and B, were isolated from the seeds of an Indian mangrove, Xylocarpus moluccensis, together with four known limonoids, khayasin, angolensic acid methyl ester, khayasin T, and 2′S-methylbutanoylproceranolide. The structures of these limonoids were established on the basis of spectroscopic data. The 13C-NMR data of khayasin were reported for the first time. Khayasin was found to exhibit marked insecticidal activity against the fifth instar larvae of Brontispa longissima (GESTRO) at a concentration of 10 mg/l.抄録全体を表示PDF形式でダウンロード (205K) -
Hiroshi Ishii, Hiroaki Todo, Kenji Sugibayashi原稿種別: Notes
2010 年 58 巻 4 号 p. 556-561
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーEffects of thermodynamic activity and the state (solution/suspension) of triamcinolone acetonide (TA) on skin permeation and concentration were physicochemically and kinetically analyzed. Permeation of TA through a silicone membrane, hairless rat skin (full-thickness skin or stripped skin) or a three-dimensional cultured human skin model (LSE-high) was determined and a permeability coefficient (P), partition coefficient (K) , diffusion coefficient (D) and steady-state flux (J) were calculated. The resulting J values proportionally increased with an increase in the TA activity in the drug solution and similar P, K and D values were obtained independent of the TA state (solution/suspension) in all membranes except for full-thickness hairless rat skin. On the other hand, the TA permeation through full-thickness hairless rat skin with the 1000 μg/ml suspension was higher than that expected judging by the thermodynamic acidity of TA. Higher D and P values were also obtained in the skin permeation of TA from the 1000 μg/ml suspension. Morphological observation of the skin surface by scanning electron microscope (SEM) showed the presence of TA solids in the hair follicles after application of the TA suspension. These results suggest that dissolved TA may be permeated predominantly through the stratum corneum, but that solid TA may be passed through the hair follicles to enter the dermis. The present physicochemical and kinetic analysis provides useful information to develop topical steroid formulations.抄録全体を表示PDF形式でダウンロード (1093K) -
Wimal Herath, Ikhlas Ahmad Khan原稿種別: Notes
2010 年 58 巻 4 号 p. 562-564
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe yeast culture, Rhodotorula mucilaginosa (ATCC 20129) transformed flutamide (1) to three metabolites: 4-nitro-3-(trifluoromethyl)aniline (2), 2-methyl-N-[4-amino-3-(trifloromethyl)phenyl]propanamide (3) and N-[4-amino-3-(trifluoromethyl)phenyl]acetamide (4). The structures were established by spectroscopic methods.抄録全体を表示PDF形式でダウンロード (100K) -
Min Wu, Ping Wu, Haihui Xie, Liangxiong Xu, Yueming Jiang, Xiaoyi Wei原稿種別: Notes
2010 年 58 巻 4 号 p. 565-567
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーFurther chemical investigation of the whole plants of Gentiana loureirii led to the isolation and characterization of three new compounds, cyclic 4-O-β-D-glucopyranosylcaffeic acid dimer (1), a new α-tetralone, 4-hydroxy-6-methyl-α-tetralone 4-O-β-D-glucopyranoside (2), and 3β,30-dihydroxy-12-ursen-28-oic acid 28-O-β-D-glucopyranosyl ester (3), along with five known compounds. To the best of our knowledge, compound 1 is the first cyclic phenolic acid glycoside dimer.抄録全体を表示PDF形式でダウンロード (217K) -
Takashi Kikuchi, Masatoshi Nihei, Hisashi Nagai, Hidekuni Fukushi, Kei ...原稿種別: Notes
2010 年 58 巻 4 号 p. 568-571
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーAlbanol A (1), isolated from the root bark extract of Morus alba (mulberry), was evaluated for the cytotoxic and apoptosis-inducing activities in human leukemia (HL60) cells, and for the inhibitory activity in human DNA topoisomerases (Topo) I and II. This compound showed potent cytotoxic activity (IC50 1.7 μM) on the cells, and potent inhibitory activity on topoisomerase II (IC50 22.8 μM). In addition, albanol A induced early apoptosis which was detected by observing the membrane phospholipid exposure in flow cytometry. Western blot analysis showed that albanol A markedly reduced the levels of procaspases-3, 8, and 9, while being increased the levels of cleaved caspases-3, 8, and 9. The Bax/Bcl-2 ratio was significantly increased by albanol A treatment. Furthermore, albanol A induced caspase-2 activation. These results suggested that albanol A induces apoptotic cell death in HL60 via both the cell death receptor pathway by stimulation of death receptor, and the mitochondrial pathway by Topo II inhibition through caspase-2 activation. Therefore, albanol A may be a promising lead compound for developing an effective drug for treatment of leukemia.抄録全体を表示PDF形式でダウンロード (681K) -
Hiroyuki Tsutsumi, Takashi Sato, Takashi Ishizu原稿種別: Notes
2010 年 58 巻 4 号 p. 572-574
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe single crystal of (−)-gallocatechin-3-O-gallate (GCg) was prepared using a solution containing an equimolecular amount of GCg and (−)-epigallocatechin-3-O-gallate (EGCg) in water. The crystal structure of GCg determined by X-ray crystallographic analysis was monoclinic with the space group P21 at 223 K. Offset π–π interactions formed between the A and A rings, B and B rings, and gallate and gallate rings of GCg, and five intermolecular hydrogen bonds formed between GCgs, GCg and water. The B ring of GCg bonded to C2 was in the axial position and the gallate ring of GCg bonded to C3 was in the pseudoaxial position with respect to the C ring of GCg.抄録全体を表示PDF形式でダウンロード (423K) -
Yingni Pan, Toshio Morikawa, Kiyofumi Ninomiya, Katsuya Imura, Dan Yua ...原稿種別: Notes
2010 年 58 巻 4 号 p. 575-578
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーFour new acylated phenylethanoid oligoglycosides, kankanosides J1 (1), J2 (2), K1 (3), and K2 (4), were isolated from stems of Cistanche tubulosa (Orobanchaceae) together with isocampneoside I (5). Their structures were elucidated on the basis of chemical and physicochemical evidence. Among them, 3—5 were found to inhibit D-galactosamine-induced cytotoxicity in primary cultured mouse hepatocytes.抄録全体を表示PDF形式でダウンロード (201K) -
Yong-Xia Tan, Ting Gong, Chao Liu, Ruo-Yun Chen, De-Quan Yu原稿種別: Notes
2010 年 58 巻 4 号 p. 579-581
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーFive new 2-arylbenzofuran derivatives wittifurans A—C, F and G (1—5) have been isolated from the stem bark of Morus wittiorum. Their structures were determined on the basis of spectroscopic analysis. Compounds 1, 3—5 were evaluated for their antioxidant and anti-inflammatory activities respectively.抄録全体を表示PDF形式でダウンロード (226K) -
Investigation on the Interaction of Prulifloxacin with Human Serum Albumin: A Spectroscopic AnalysisYa-Bei Huang, Shi-Jun Wang, Yan-Qin Zi, Zhang Yu, Xiao-Yan Gao, Ying-C ...原稿種別: Notes
2010 年 58 巻 4 号 p. 582-586
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーThe interaction between prulifloxacin (PUFX) and human serum albumin (HSA) was investigated under simulated physiologic conditions with fluorescence spectra. The fluorescence quenching process of HSA may be mainly governed by a static quenching mechanism. The apparent binding constant Kb between PUFX and HSA at different temperatures were 2.08±1.04, 2.74±0.50, and 4.98±1.61×108 l/mol. The thermodynamic parameters, with a negative value of ΔG0, revealed that the binding is a spontaneous process. A binding distance R of 1.19 nm between donor and acceptor was obtained from the Fŏrster energy transfer theory.抄録全体を表示PDF形式でダウンロード (321K) -
Yukiko Matsuo, Yoshihiro Mimaki原稿種別: Notes
2010 年 58 巻 4 号 p. 587-590
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーA new neolignan, (7R,8R)-5-O-demethylbilagrewin (1), together with four known lignans (2—5), were isolated from the heartwood of Santalum album (Santalaceae). The structure of 1 was determined by analysis of extensive spectroscopic data. The isolated compounds and derivatives were evaluated for their cytotoxic activities against HL-60 human promyelocytic leukemia cells and A549 human lung adenocarcinoma cells. Compounds 1 and 2 exhibited cytotoxicity against HL-60 cells with IC50 values of 1.5±0.02 and 4.3±0.13 μM, and against A549 cells with IC50 values of 13.6±0.32 and 19.9±1.27 μM, respectively. The aldehyde group of 1 and 2 was revealed to be a structural requirement for the appearance of cytotoxicity in this type of lignans. These tumor cell deaths were shown to be mediated through induction of apoptosis.抄録全体を表示PDF形式でダウンロード (709K)
Communicatins to the Editor
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Jun-ichi Matsuo, Takaya Hoshikawa, Shun Sasaki, Hiroyuki Ishibashi原稿種別: Communications to the Editor
2010 年 58 巻 4 号 p. 591-592
発行日: 2010/04/01
公開日: 2010/04/10
ジャーナル フリーTrialkylamine-mediated intramolecular cyclization of pent-4-enoyl chlorides was studied. Substitution with a tertiary alkyl group at the 2-position gave cyclopent-2-en-1-ones, while substitution with an aromatic group gave enol esters, which were formed by O-acylation of initially formed 3-chlorocyclopentanones with ketenes.抄録全体を表示PDF形式でダウンロード (285K)
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