巻号一覧
51 巻, 10 号
選択された号の論文の24件中1～24を表示しています
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Regular Articles
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Toshihiro Shimizu, Masae Sugaya, Yoshinori Nakano, Daisuke Izutsu, Yos ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1121-1127
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーLansoprazole fast-disintegrating tablets (LFDT) are a patient-friendly formulation that rapidly disintegrates in the mouth. LFDT consist of enteric-coated microgranules (mean particle size, approximately 300 μm) and inactive granules. In the design of the inactive granules, mannitol was used as a basic excipient. Microcrystalline cellulose, low-substituted hydroxypropyl cellulose (L-HPC), and crospovidone were used as binders and disintegrants. A new grade of L-HPC (L-HPC-33), with a hydroxypropoxy group content of 5.0—6.9%, was developed and it has no rough texture due to a decrease in water absorption. It was clarified that L-HPC-33 could be useful as a binder and disintegrant in rapidly disintegrating tablets. LFDT contain enteric-coated microgranules in tablet form. The enteric-coated microgranule content in LFDT affect qualities such as tensile strength, disintegration time in the mouth, and dissolution behavior in the acid stage and in the buffer stage of LFDT. The 47.4% content of the enteric-coated microgranules was selected to give sufficient tensile strength (not less than 30 N/cm2), rapid disintegration time in the mouth (not more than 30 s), and dissolution behavior in the acid stage and buffer stage similar to current lansoprazole capsules. Compression force affected the tensile strength and the disintegration time in the mouth, but did not affect the dissolution behavior in the acid and buffer stages.抄録全体を表示PDF形式でダウンロード (66K) -
Ioanna Andreadou, Anna Tsantili-Kakoulidou, Eleni Spyropoulou, Theodor ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1128-1131
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーWe have previously reported on the synthesis of novel indole derivatives containing an amine-triazole moiety (1a—d, 2a—c), and their antioxidant activity on in vitro non-enzymatic rat hepatic microsomal lipid peroxidation. Some of the compounds showed protective activity against oxidative injury of ischemic myocardium. In the present paper we investigated the interactions of these derivatives with reactive oxygen species, in order to find a mechanism of their antioxidant capacity and to identify structural characteristics responsible for these properties. These interactions were compared with melatonin, which is also an indole derivative. The antioxidant profiles of the compounds were established by different in vitro protocols as follows: 1) by the interaction of the compounds with the 1,1-diphenyl-2-picrylhydrazyl (DPPH) stable free radical, 2) their scavenging effects on superoxide anions using an enzymic system of xanthine–xanthine oxidase, 3) their inhibitory effects on xanthine oxidase and 4) their ability to scavenge hydroxyl radicals by comparison with dimethyl sulfoxide (DMSO) for ·OH. All compounds were found to interact with DPPH, most of them to be superoxide anion scavengers and to be strong hydroxyl radical scavengers. Derivatives 1a and 1d substituted on the nitrogen of the indolic nucleus were found to have better antioxidant properties than the reference compounds used and melatonin.抄録全体を表示PDF形式でダウンロード (77K) -
Eugene Bratoeff, Elena Ramírez, Eugenio Flores, Norma Valencia, ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1132-1136
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーThe in vitro inhibitory activity of five new progesterone derivatives: 17α-hydroxy-16β-methylpregna-1,4,6-triene-3,20-dione 1; 16β-methyl-17α-toluoyloxypregna-1,4,6-triene-3,20-dione 2; 17α-hydroxy-6-methylenepregn-4-ene-3,20-dione 3; 6-methylene-17α-toluoyloxypregn-4ene-3,20-dione 4 and 17α-(p-bromobenzoyloxy)-6-methylenepregn-4-ene-3,20-dione 5 was determined. These compounds were evaluated as 5α-reductase inhibitors as well as antagonists for the androgen receptor. Compounds 1, 2, 3, 4 and 5 showed the following inhibitory activity for the 5α-reductase enzyme with IC50 values of: 1 (1.65 μM), 2 (10 μM), 3 (19 nM), 4 (100 nM) and 5 (100 nM). The results of this study also showed the effect of increasing concentrations of the novel steroids upon [3H]dihydrotestosterone binding to androgen receptors from male hamster prostate. The Ki values for compounds 1, 2, 3, 4, 5 and dihydrotestosterone showed the following order of affinity for the androgen receptor: 4>5>dihydrotestosterone>2>3>1. The overall data indicated that all synthesized compounds 1, 2, 3, 4 and 5 are inhibitors of the 5α-reductase enzyme present in the hamster prostate. In addition compounds 1, 2, 3, 4 and 5 also presented an affinity for the androgen receptor.抄録全体を表示PDF形式でダウンロード (101K) -
Anshu Dandia, Meha Sati, Kapil Arya, Rekha Sharma, André Loupy原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1137-1141
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーMicrowave activation coupled with dry media technique as a green chemistry procedure has been applied to synthesis of a series of some new title compounds. They have been obtained by the reaction of in situ synthesized 1,3-dihydro-3-[2-(phenyl/4-fluorophenyl)-2-oxoethylidene)-indol-2(1H)-one (4a, b) with substituted aminobenzenethiols (5a—d). The key intermediates 4a, b were also prepared in one step by this improved technique by reacting isatin and substituted acetophenones (2a, b). The results obtained under microwave irradiation when compared with that following conventional method demonstrate the versatility of the process. The title compounds 7a—e have also been screened for their antifungal and antitubercular activity, 7a and 7e showing maximum inhibition of growth of Alternaria alternata and Fusarium oxysporium and 7b, c, e revealing significant antitubercular activity.抄録全体を表示PDF形式でダウンロード (76K) -
Tenji Konishi, Kiyonori Yamazoe, Masahiro Kanzato, Takao Konoshima, Ya ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1142-1146
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーThree new diterpenoids, excoecarins V1—V3 (1—3) and a new flavanone glycoside (7) were isolated from the fresh stem of Excoecaria agallocha L. Their structures were elucidated as: 2α,3α,18-trihydroxy-3β,20-epoxybeyer-15-ene (1), ent-2,3-secokaur-16-en-2,3-dioic acid (2), ent-3,4-seco-16α-hydroxyatis-4(19)-en-3-oic acid (3), and 3,5,7,3′,5′-pentahydroxy-2R,3R-flavanonol 3-O-α-L-rhamnopyranoside (7) on the basis of spectroscopic data, chemical evidence, and/or X-ray analysis.抄録全体を表示PDF形式でダウンロード (102K) -
Hiroaki Hayashi, Shui-Li Zhang, Tomoko Nakaizumi, Kumiko Shimura, Misa ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1147-1152
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーA new prenylated flavanone, licoleafol, and a new prenylated dihydrostilbene, uralstilbene, together with four known compounds, 8-dimethylallyleriodictyol, sophoraflavanone B, gancaonin R, and 6-dimethylallyleriodictyol, were isolated from the leaves of Glycyrrhiza uralensis collected in Kazakhstan. HPLC analysis of the leaves of Glycyrrhiza plants collected in Kazakhstan showed that both G. uralensis-specific and Glycyrrhiza glabra-specific compounds were detected in the leaves of the morphologically intermediate-type plants, suggesting that the intermediate-type plant is a hybrid of G. glabra and G. uralensis. In addition, HPLC profiles of leaf extracts from offspring of intermediate-type plants were divided into the three types: the G. uralensis type, G. glabra type, and the intermediate type. From these results, it appears likely that the intermediate-type plant back-crosses with G. glabra and G. uralensis to generate a G. glabra-type plant and a G. uralensis-type plant, respectively.抄録全体を表示PDF形式でダウンロード (195K) -
Henry Rapoport, Yuewu Chen, Rafat M. Mohareb, Jin Hee Ahn, Tae Bo Sim, ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1153-1156
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーEnantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total synthesis of (+)-4′-deoxycarbapentostatin nucleoside.抄録全体を表示PDF形式でダウンロード (70K) -
Masafumi Goto, Yuuichiro Yamamoto, Masamitsu Sumimoto, Nobuhiro Tsurud ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1157-1162
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーSquare-planar complexes with the formula [Pt(L2)(L1)](X)2·nH2O, where L1 is S-2-aminomethylpyrrolidine (S-pyrda) or 2-aminomethylpiperidine (pipda) and L2 is diammine (X=Cl), cyclobutane-1,1-dicarboxylato (cbdca) (X=none), 2,2′-bipyridine (bpy) (X=NO3), or 1,10-phenanthroline (phen) (X=Cl), were prepared and the nature of the coordination of L1 was examined by 1H-NMR spectroscopy and X-ray crystallography. These 2-aminomethylazacycloalkane derivatives form five-membered chelate rings condensed with an azacycloalkane ring in cis- or trans-configurations. The 1H-NMR spectrum of complexes with S-pyrda as L1 were consistent with cis-condensed rings in an S(N) conformation with any of L2 group. However, 1H-NMR spectra of the complexes with pipda as L1 indicated trans-fused successive rings for the diammine and cbdca as L2, but spectra for bpy and phen as L2 were consistent with a conformation having cis-fused successive rings. X-Ray crystallography data for the two complexes with pipda as L1 and cbdca (1) and bpy (2) as L2 confirms the different coordination behavior in the solid state.抄録全体を表示PDF形式でダウンロード (141K) -
Ten New Lycopodium Alkaloids Having the Lycopodane Skeleton Isolated from Lycopodium serratum THUNB.Hiromitsu Takayama, Kazuaki Katakawa, Mariko Kitajima, Kentaro Yamaguc ...原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1163-1169
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーTen new alkaloids, lycoposerramines-F (1), -G (2), -H (3), -I (4), -J (5), -K (6), -L (7), -M (8), -N (9), and -O (10), having lycopodine-related structures, were isolated from the club moss Lycopodium serratum THUNB. and their structures were elucidated on the basis of spectroscopic analysis and/or chemical transformation.抄録全体を表示PDF形式でダウンロード (126K) -
Naoyuki Suzuki, Sakura Yasaki, Akito Yasuhara, Takao Sakamoto原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1170-1173
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーThe sequential Sonogashira reaction and the cyclization reaction of various 2-iodoanilines and terminal alkynes in the presence of a palladium catalyst and tetrabutylammonium fluoride (TBAF) gave the corresponding 2-substituted indoles in good yields.抄録全体を表示PDF形式でダウンロード (58K) -
Rong-Tao Li, Quan-Bin Han, Ai-Hua Zhao, Han-Dong Sun原稿種別: Regular Article
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1174-1176
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーTwo novel octanortriterpenoids, micranoic acids A (1) and B (2), along with three known compounds, kadsuric acid (3), 3β-hydroxy-lanost-9(11),24(25)-dien-26-oic acid (4) and schizandronic acid (5), were isolated from the leaves and stems of Schisandra micrantha. The structures of 1 and 2 were determined by 1D and 2D NMR spectroscopic analysis. Micranoic acids A and B represent a new group of triterpenes in which the entire C-17 side chain has lost. This is the first report of octanortriterpenoids isolated from the family Schisandraceae.抄録全体を表示PDF形式でダウンロード (64K)
Notes
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Kazuo Okumura, Yutaka Nakamura, Seiji Takeuchi, Isao Kato, Yoshinori F ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1177-1182
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーThe key intermediate to squalamine, (5α,7α,24R)-7,24-dihydroxy-cholestan-3-one, was synthesized from the 3-O-acetyl-24R,25-dihydroxy derivative of desmosterol via 10 steps in 16% overall yield and squalamine was also prepared via two further steps in 7.4% total yield from the desmosterol derivative.抄録全体を表示PDF形式でダウンロード (96K) -
Shuji Kitagawa, Ai Ikarashi原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1183-1185
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーUsing excised guinea pig dorsal skin, we examined the effects of three surfactants, anionic sodium dodecylsulfate (SDS), cationic n-dodecyltrimethylammonium bromide and non-ionic n-dodecyl-β-D-maltoside, all of which commonly have an n-dodecyl group, on in vitro skin permeation of the cationic drug ketotifen. All these three surfactants increased the skin permeation of ketotifen. Among the surfactants tested, anionic SDS had the largest enhancement effects, and significantly increased the permeation at concentrations over 1 mM. The enhancement effect of the same anionic surfactant on the permeation of anionic salicylate was smaller and similar to that of cationic n-dodecyltrimethylammonium. The enhancement effects of SDS on ketotifen permeation were more marked than those of the cationic surfactant but differed from previous findings of their effects on other drugs permeation. Analysis of the retention of ketotifen in the skin suggested that SDS-induced increase in the transfer of hydrophilic ketotifen to the skin is the main reason for the marked increase in skin permeation.抄録全体を表示PDF形式でダウンロード (52K) -
Ryuichiro Suzuki, Yoshihito Okada, Toru Okuyama原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1186-1188
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーA new flavone C-glycoside, chrysoeriol 6-C-β-fucopyranoside (1), and a known flavone C-glycoside (2) were isolated from the style of Zea mays L. These structures were elucidated on the basis of spectroscopic analysis. Compound 1 exhibited glycation inhibitory activity.抄録全体を表示PDF形式でダウンロード (56K) -
Fumihiro Nagashima, Wakana Kasai, Masuo Kondoh, Makiko Fujii, Yoshiter ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1189-1192
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーTwo new ent-kaurene-type and a new rearranged ent-kaurene-type diterpenoids possessing cytotoxicity against a human leukemia cell line have been isolated from the New Zealand liverwort Jungermannia species, together with previously known ent-kaurene-type diterpenoids. Their structures were established based on extensive NMR techniques.抄録全体を表示PDF形式でダウンロード (76K) -
Pendyala Muralidhar, Nallamothu Krishna, Muthyala Muralikrishna Kumar, ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1193-1195
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーChemical examination of the marine sponge Iotrochota baculifera of the Indian Ocean furnished a sphingolipid (1), a new glycosphingolipid (iotroridoside-B, 2) and a four-component mixture of sphingolipids (3a—d) with two new components. Structure elucidation was carried out by spectral and chemical methods.抄録全体を表示PDF形式でダウンロード (60K) -
Chisako Yamagami, Hiromi Tachikawa原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1196-1200
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーWe recently proposed a new hydrogen-accepting parameter, SHA, for monosubstituted (di)azines on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, SHA values for monosubstituted thiophenes and furans were calculated and the results were applied to the analysis of relationships between log P (P: 1-octanol/water partition coefficient) and log k (k: retention factor obtained by reversed phase HPLC). The SHA parameter was found to work effectively as a hydrogen-bonding parameter in a range of heteroaromatic compounds.抄録全体を表示PDF形式でダウンロード (66K) -
Jun Wu, Si Zhang, Jianshe Huang, Qiang Xiao, Qingxin Li, Lijuan Long, ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1201-1203
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーFrom the aerial parts of Acanthus ilicifolius, a new aliphatic alcohol glycoside (ilicifolioside C) and two new (Z)-4-coumaric acid glycosides, (Z)-4-coumaric acid 4-O-β-D-glucopyranoside and (Z)-4-coumaric acid 4-O-β-D-apiofuranosyl-(1″→2′)-O-β-D-glucopyranoside were isolated. The structural elucidations were based on the analyses of spectroscopic data. Z-Form 4-coumaric acid glycosides were first isolated from plant.抄録全体を表示PDF形式でダウンロード (69K) -
Chen Xie, Nigel C. Veitch, Peter J. Houghton, Monique S. J. Simmonds原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1204-1207
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーA new flavone C-glycoside, apigenin 6-C-α-L-arabinopyranosyl-8-C-β-L-arabinopyranoside, has been isolated from Viola yedoensis together with the known compounds, apigenin 6,8-di-C-α-L-arabinopyranoside, apigenin 6-C-α-L-arabinopyranosyl-8-C-β-D-glucopyranoside (isoschaftoside), apigenin 6-C-β-D-glucopyranosyl-8-C-α-L-arabinopyranoside (schaftoside), apigenin 6-C-β-D-glucopyranosyl-8-C-β-L-arabinopyranoside (neoschaftoside), apigenin 6,8-di-C-β-D-glucopyranoside (vicenin-2), apigenin 6-C-α-L-arabinopyranosyl-8-C-β-D-xylopyranoside, apigenin 6-C-β-D-xylopyranosyl-8-C-α-L-arabinopyranoside, luteolin 6-C-β-D-glucopyranoside (isoorientin) and luteolin 6-C-α-L-arabinopyranosyl-8-C-β-D-glucopyranoside (isocarlinoside). The structures were determined by spectroscopic methods and new or revised 1H- and 13C-NMR spectral assignments are proposed for some compounds.抄録全体を表示PDF形式でダウンロード (72K) -
Consolacion Y. Ragasa, Jerome Ganzon, Joy Hofileña, Benjie Tamb ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1208-1210
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーA new cassane-type diterpene isovouacapenol E (1) was isolated from the leaves of Caesalpinia pulcherrima, together with the known compounds caesaldekarin A (3), spathulenol (4), caryophyllene oxide (5), phytol, and sitosterol. The structure of 1 was elucidated by spectral data interpretation.抄録全体を表示PDF形式でダウンロード (56K) -
Mariko Kitajima, Akiko Urano, Noriyuki Kogure, Hiromitsu Takayama, Nor ...原稿種別: Note
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1211-1214
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーThree new gelsedine-type oxindole alkaloids, GS-1, GS-2, and GS-3, and one new iridoid, GSIR-1, were isolated from the stems and leaves of cultivated Carolina jasmine (Gelsemium sempervirens AIT. f.) and their structures were determined by spectroscopic analysis.抄録全体を表示PDF形式でダウンロード (69K)
Communicatins to the Editor
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Makiko Nishida, Hitoshi Yoshimitsu, Masafumi Okawa, Tuyoshi Ikeda, Tos ...原稿種別: Communication to the Editor
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1215-1216
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーTwo new 15,16-seco-cycloartane glycosides (1, 2) were isolated from Cimicifuga Rhizome. Their structures were determined by spectroscopic analysis.抄録全体を表示PDF形式でダウンロード (49K) -
Naganori Numao, Hisashi Fujii, Yoshiyuki Fukazawa, Kazuyoshi Tanaka原稿種別: Communication to the Editor
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1217-1219
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーA frequency (or sequence)-dependent rule seems to be conserved in a simple and concerted interaction of various human proteins.抄録全体を表示PDF形式でダウンロード (78K) -
Makoto Yamada, Shin-ichi Watanabe, Osamu Hoshino, Miyuki Ishizaki, Mai ...原稿種別: Communication to the Editor
専門分野: [not specified]
2003 年 51 巻 10 号 p. 1220-1221
発行日: 2003年
公開日: 2003/10/01
ジャーナル フリーAllyl aryl ethers can be easily cleaved by the use of 10% Pd/C under the mild and basic conditions.抄録全体を表示PDF形式でダウンロード (54K)
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