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Volume 51, Issue 6
Displaying 1-27 of 27 articles from this issue
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Regular Articles
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Kenji Mori, Seiji Tokumoto, Hiroyuki Kubo, Naruhito Higo, Iwao Nozawa, ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 617-619
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSFew studies have been reported on the design of topical formulations consisting of electrodes and active drugs for electroporation as a means to increase skin permeability of the drugs, although many studies were reported for the effect of this physical means using aqueous drug solutions. We, therefore, designed a prototypic reservoir and matrix topical formulations that are suitable for electroporation in the present study. Plate-plate Ag electrodes and sodium diclofenac were used as model electrodes and the drug, respectively. The in vitro skin permeations of the drug obtained from the reservoir and matrix formulations were slightly higher than that from an aqueous suspension. This may be due to slightly higher electric field in the skin barrier for the presently designed formulations than that for the aqueous suspension. The present feasibility test suggests that these reservoirs and matrix formulations are useful prototypic topical formulations for electroporation application to improve the drug permeability through skin.View full abstractDownload PDF (85K) -
Norihito Shimono, Toshihito Takatori, Masumi Ueda, Masaaki Mori, Yasuh ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 620-624
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSA multiparticulate chitosan-dispersed system (CDS), which is composed of the drug reservoir and the drug release-regulating layer, was developed for drug delivery. The drug release-regulating layer is a mixture of water-insoluble polymer and chitosan powder. The drug is released from CDS pellets in all regions of the gastrointestinal tract (from the stomach to the colon). CDS pellets containing chitosan powder were designed to dissolve chitosan powder partly in the release-regulating layer in the stomach and release part of drug. After passing through the stomach, the drug is released from CDS pellets at a constant speed in the small intestine. In the large intestine, CDS pellets were designed to disintegrate the remaining chitosan powder at an accelerated speed and the remaining drug in CDS pellets is released. The drug release rate can be controlled with the thickness of the chitosan-dispersed water-insoluble layer. Furthermore, for colon-specific drug delivery, an additional outer enteric coating is necessary to prevent drug release from CDS pellets in the stomach, because the chitosan-dispersed water-insoluble layer dissolves gradually under acidic conditions. The resulting enteric-coated CDS (E-CDS) pellets were found to permit colon-specific drug delivery. In this study, the multiparticulate CDS was adopted not only for colon-specific drug delivery but also for sustained drug release.View full abstractDownload PDF (339K) -
Eiko Toyota, Haruo Sekizaki, Kunihiko Itoh, Kazutaka TanizawaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 625-629
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESS3-Formyl-4-hydroxyphenylguanidine hydrochloride and its Schiff base copper(II), zinc(II), and iron(III) chelates were synthesized and their inhibitory activity against bovine β-trypsin were determined. Syntheses of Schiff base metal chelates were carried out from 3-formyl-4-hydroxyphenylguanidine, various L-amino acids, and divalent metal acetate. Their structures were established on the basis of spectroscopic evidence and elemental analysis. The inhibitory activity of these chelates against bovine β-trypsin was determined. The guanidine-containing copper(II) and zinc(II) chelates behaved as potent competitive inhibitors of trypsin. However, similar inhibitory activity was not observed for guanidine-containing iron(III) chelates. The inhibition constants (Ki values, ca. 10−5 M) of guanidine-containing Schiff base copper(II) and zinc(II) chelates were slightly lower than those (ca. 10−6 M) of the corresponding amidine-containing Schiff base chelates with regard to bovine trypsin.View full abstractDownload PDF (78K) -
Takanori Miyashita, Masanori Baba, Shiro Shigeta, Kenya Mori, Kazuo Sh ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 630-634
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSA series of novel 10-thiaisoalloxazine derivatives bearing an alkoxymethyl or benzyloxymethyl moiety at the N-1 position has been synthesized through the bromination of 1-substituted-5-hydroxyuracils and subsequent condensation with aminobenzenethiol in a one-pot reaction. Contrary to the previous report, the formation of intermediary 5,6-diethoxy-5-hydroxy-5,6-dihydrouracil seems to be not the necessary factor for the formation of the thiaisoalloxazines, since the reaction proceeds in tetrahydrofuran (THF) or acetonitrile far more smoothly than in ethanol. The anti-human immunodeficiency virus (HIV)-1 activity of the resulted thiaisoalloxazine derivatives was evaluated in lymphocyte cells based on the inhibitory activity against the viral-induced cytopathic activity. Among the derivatives, compounds 6, 7, and 8 bearing an alkoxymethyl moiety at the N-1 position exhibited modest inhibitory activity towards the cytotopathic effect of HIV-1.View full abstractDownload PDF (78K) -
Makoto Ichikawa, Manabu Udayama, Kazuhiko Imamura, Sumihiro Shiraishi, ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 635-639
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSWe developed a rapid and simple HPLC method combined with solid-phase extraction (SPE) for quantitative analysis of (+)-pseudoephedrine (PEP) and (−)-ephedrine (EP) in Japanese herbal (Kampo) medicines such as Kakkon-to, Sho-seiryu-to, Goshaku-san and Bofu-tsusho-san. SPE was performed on TOYOPAK IC-SP M containing propylsulfonic groups. Determination of PEP and EP was carried out using ion-pair reversed-phase HPLC with sodium dodecyl sulfate. N-Benzyldiethylamine was used as an internal standard. The analytical procedure was validated with regard to specificity, linearity, accuracy, and precision. These data suggest that the analytical method developed in this study is useful for quantitative analysis of PEP and EP in various formulations of Kampo medicine containing Ephedra herb.View full abstractDownload PDF (105K) -
Hidemichi Mitome, Masakazu Shinohara, Hiroaki Miyaoka, Yasuji YamadaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 640-645
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESS3α,7α-Dihydroxy-5-epiaragusterol A (3) was synthesized from bile acid (cholic acid) as a new steroidal nuclear analogue of antitumor marine steroid aragusterol A. 7α-Hydroxyaragusterol A (4) was also derived from xestokerol B. The in vitro anti-proliferative activity of each of these analogues toward KB cells as well as in vivo anti-tumor activity of 5-epiaragusterol A (2) previously synthesized by the authors and 3 were assessed.View full abstractDownload PDF (120K) -
Wimal Herath, Julie Rakel Mikell, Daneel Ferreira, Ikhlas Ahmad KhanArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 646-648
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSSeveral microorganisms showed the ability to transform the harman alkaloids, harmaline (1), harmalol (2) and harman (5). Harmaline (1) and harmalol (2) were converted by Rhodotorula rubra ATCC 20129 into the tryptamines, 2-acetyl-3-(2-acetamidoethyl)-7-methoxyindole (3) and 2-acetyl-3-(2-acetamidoethyl)-7-hydroxyindole (4), respectively. Harman (5) was biotransformed by Cunninghamella echinulata NRRL 3655 into 6-hydroxyharman (6) and harman-2-oxide (7).View full abstractDownload PDF (64K) -
Masafumi Goto, Katsutoshi Tanaka, Masamitsu Sumimoto, Hiromasa Mori, H ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 649-653
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSA series of ternary complexes comprised of platinum(II), 2,2′-dipyridine, and N-(ω-phenylalkyl)-1,2-ethanediamine was prepared by varying the number (n) of methylene chain carbons between the phenyl group and one of the amino groups of 1,2-ethanediamine. NMR measurements indicated that intramolecular stacking occurred for n=1 and intermolecular stacking occurred for n=3 for several of the aryl sulfonates.View full abstractDownload PDF (112K) -
Jing Tao, Toshio Morikawa, Shin Ando, Hisashi Matsuda, Masayuki Yoshik ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 654-662
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSThree new arborinane-type triterpene glycosides, rubianosides II, III, and IV, a new arborinane-type triterpene, rubianol-g, and a new anthraquinone, rubianthraquinone, were isolated from a Chinese natural medicine, the roots of Rubia yunnanensis. The structures of the new constituents including their absolute configurations were determined on the basis of chemical and physicochemical evidence. The inhibitory effects of the isolated constituents on nitric oxide production in lipopolysaccharide-activated macrophages were examined. Among them, a cyclic peptide constituent, RA-XII and its aglycon, RA-V (deoxybouvadin), potently inhibited overproduction of nitric oxide and induction of inducible nitric oxide synthase. In addition, an anthraquinone constituent, 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone, was found to show inhibitory effects on the release of β-hexosaminidase in RBL-2H3 cells.View full abstractDownload PDF (156K) -
Ken-ichi Izutsu, Annie Rimando, Nobuo Aoyagi, Shigeo KojimaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 663-666
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSThe effect of sodium tetraborate (Na2B4O7, borax) on the thermal property of frozen aqueous sugar and polyol solutions was studied through thermal analysis. Addition of borax raised the thermal transition temperature (glass transition temperature of maximally freeze-concentrated solutes; Tg′) of frozen sucrose solutions depending on the borax/sucrose concentration ratios. Changes in the Tg′ of frozen mono- and disaccharide solutions suggested various forms of complexes, including those of a borate ion and two saccharide molecules. Borax exerted the maximum effect to raise the oligosaccharide and dextran Tg′s at borax/saccharide molar ratios of approximately 1—2 (maltose and maltooligosaccharides), 2 (dextran 1060), 5 (dextran 4900), and 10 (dextran 10200). Further addition of borax lowered Tg′s of the saccharide solutions. Borax also raised Tg and Tg′ temperatures of frozen aqueous glycerol solutions. The decreased solute mobility in frozen solutions by the borate-polyol complexes suggested higher collapse temperature in the freeze-drying process and improved stability of biological systems in frozen solutions.View full abstractDownload PDF (79K) -
Toshiaki Saitoh, Kentaro Shikiya, Yoshie Horiguchi, Takehiro SanoArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 667-672
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSImproved synthesis of four stereoisomeric chiral 1,3-dimethyl-1,2,3,4-tetrahydroisoquinolines (1a, b, ent-1a, b) was achieved via the super acid-induced cyclization of chiral N-[1-methyl-2-(phenylsulfinyl)ethyl]-N-(1-phenylethyl)formamides (4a, b, ent-4a, b) using the Pummerer-type cyclization reaction as a key step. The cyclization leading to the isoquinoline ring proceeded in a quantitative manner when trifluoromethane sulfonic acid (TFSA) was used as the super acid, although Friedel–Crafts-type alkylation of 4-phenylsulfanyl TIQ derivatives (5) with benzene used as the solvent accompanied cyclization to yield the 4-phenyl-TIQs (7). The byproduct (7) was exclusively formed when a large excess amount of TFSA was used.View full abstractDownload PDF (103K) -
Junichi Kitajima, Akane Kamoshita, Toru Ishikawa, Akihito Takano, Tats ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 673-678
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSFive sesquiterpenoid glycosides (two guaiane-type glycosides and three eudesmane-type glucosides) and a glucoside of an acetylene derivative were newly isolated from the water-soluble portion of the methanolic extract of Atractylodes lancea rhizome together with 26 known compounds. Their structures were characterized as atractyloside A 14-O-β-D-fructofuranoside, (1S,4S,5S,7R,10S)-10,11,14-trihydroxyguai-3-one 11-O-β-D-glucopyranoside, (5R,7R,10S)-isopterocarpolone β-D-glucopyranoside, cis-atractyloside I, (2R,3R,5R,7R,10S)-atractyloside G 2-O-β-D-glucopyranoside, and (2E,8E)-2,8-decadiene-4,6-diyne-1,10-diol 1-O-β-D-glucopyranoside on the basis of chemical and spectroscopic investigation. The presence of six characteristic guaiane-type glucosides in both rhizomes of A. lancea and Atractylodes japonica suggested a close chemotaxonomic relationship between them.View full abstractDownload PDF (100K) -
Quan Le Tran, Myint Myint Than, Yasuhiro Tezuka, Arjun H. Banskota, Ky ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 679-682
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSGinseng, the underground parts of plants of Panax species, has been used in oriental traditional medicine for centuries. Unfortunately, because of extensive exploitation over thousands of years, the natural source of these species has been almost exhausted. Recently, we have found a wild ginseng growing in Myanmar. Here, by a combination of chemical composition study and gene sequence analysis, we unambiguously demonstrate that the wild ginseng is actually P. zingiberensis, commonly known as ginger ginseng. This ginseng was an indigenous to the southwestern China. However, now it is seriously threatened to brink of extinction and is put on the highest level of protection in China. Therefore, an appropriate protection measure is highly recommended to preserve this valuable resource, since this Myanmar ginseng might turn out to be the last P. zingiberensis, which could ever be seen in the planet.View full abstractDownload PDF (95K) -
Makiko Nishida, Hitoshi Yoshimitsu, Masafumi Okawa, Toshihiro NoharaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 683-687
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSFour new cycloartane glycosides, named aquilegiosides C—F, were isolated from the dried aerial parts of Aquilegia vulgaris. Their structures were determined by two dimensional (2D) NMR spectroscopic analysis and chemical evidence. Aquilegiosides C—F suppressed the proliferation of lymphocytes in mouse allogeneic mixed lymphocyte reaction with IC50, ranging from 3.7×10−5 to 2.2×10−4 M.View full abstractDownload PDF (80K) -
Fumikazu Ito, Tetsuya Moriguchi, Yasuyuki Yoshitake, Masashi Eto, Shoj ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 688-696
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSA series of pairs of stable diastereomeric atropisomers caused by restricted rotation around the Csp3–Csp2 bond of [2-(2-hydroxynaphthalen-1-yl)-3,3-dimethyl-2,3-dihydroindol-1-yl]-(3- or 4-substituted phenyl)-methanone or [2-(2-hydroxynaphthalen-1-yl)-3,3-dimethyl-2,3-dihydroindol-1-yl]-1-alkanone were isolated. The conformational analyses of the atropisomers were performed based on the X-ray crystallographic and 1H-NMR spectral data. It became clear that rotation about the C2–naphthyl bond is restricted at room temperature, whereas the >NCO–Ar bond rotates freely.View full abstractDownload PDF (188K) -
Akira Naya, Kensuke Kobayashi, Makoto Ishikawa, Kenji Ohwaki, Toshihik ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 697-701
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSThe structure activity relationships of novel selective CCR3 receptor antagonists, 2-(benzothiazolylthio)acetamimde derivatives were described. A lead structure (1a) was discovered from the screening of the focused library that was based on the structure of our dual antagonists for the human CCR1 and CCR3 receptors. Derivatization of 1a including incorporation of substituent(s) into each benzene ring of the benzothiazole and piperidine side chain resulted in the identification of potent and selective compounds (1b, r, s) exhibiting nano-molar binding affinity (IC50s: 1.5—3.0 nM) and greater than 800-fold selectivity for the CCR3 receptor over the CCR1 receptor.View full abstractDownload PDF (90K) -
Hiroyuki Nogami, Motomu Kanai, Masakatsu ShibasakiArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 702-709
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSChiral building block syntheses of promising drugs were achieved using two types of catalytic stereoselective cyanosilylations of aldehydes promoted by Lewis acid–Lewis base bifunctional catalysts 1 and 2 as the key steps (diastereoselective cyanosilylation of amino aldehyde and enantioselective cyanosilylation). In the first part of this article, syntheses of chiral building blocks (6) of Atazanavir (3: human immunodeficiency virus (HIV) protease inhibitor) using the bifunctional catalyst 2 are discussed. The reaction of Boc-protected phenylalaninal 21 in the presence of 1 mol% catalyst 2 selectively afforded the anti isomer 22 as the major product (diastereomeric ratio=97 : 3), which was successively converted to the corresponding epoxide 6 in six steps. In the second part, we describe a chiral building block synthesis of β3-adrenergic receptor agonists. The enantioselective cyanosilylation of 3-chlorobenzaldehyde (38) with 9 mol% catalyst 1 gave the chiral cyanohydrin 39, which was converted to β-hydroxyethylamine 40 by reduction. Moreover, the chiral ligand of catalyst 1 could be recovered without column chromatography and reused without decreasing its activity.View full abstractDownload PDF (138K) -
Takuro Maruyama, Kazumasa Yokoyama, Yukiko Makino, Yukihiro GodaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 710-714
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESS“Magic mushrooms” (MMs) are psychoactive fungi containing the and Psychotropics Control Law in Japan. Because there are many kinds of MMs and they are often sold even as dry powders in local markets, it is very difficult to identify the original species of the MMs by morphological observation. Therefore, we investigated the rRNA gene for a large subunit (LSU) of several MMs to classify them by a genetic approach. In this paper, we described the phylogeny of species of MMs based on the partial sequence (about 970 bp) of the LSU and the rapid identification of MMs using the TaqMan PCR assay.View full abstractDownload PDF (99K)
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Yoshiko Usami, Tsuyoshi Oki, Masahiko Nakai, Masafumi Sagisaka, Tsuguh ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 715-718
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSWe developed a simple HPLC method for the simultaneous determination of lopinavir (LPV), ritonavir (RTV) and efavirenz (EFV) to evaluate the efficiency of co-administration of LPV/RTV and EFV in Japanese patients enrolled in a clinical study. The monitoring of LPV plasma concentration is important because co-administration of LPV/RTV with EFV sometimes decreases plasma concentrations of LPV caused by EFV activation of cytochrome P-450 3A. A solution of acetonitrile, methanol and tetramethylammonium perchlorate (TMAP) in dilute aqueous trifluoroacetic acid (TFA) has been used as the mobile phase in a HPLC method to elute LPV and RTV. We found that a solvent ratio of 45 : 5 : 50 (v/v/v) of acetonitrile/methanol/0.02 M TMAP in 0.2% TFA optimized separation of LPV, RTV and EFV. A column temperature of 30 °C was necessary for the reproducibility of the analyses. Standard curves were linear in the range 0.060 to 24.06 μg/ml for LPV, 0.010 to 4.16 μg/ml for RTV, and 0.047 to 37.44 μg/ml for EFV. Coefficients of variation (CVs) of LPV, RTV and EFV in intraday and interday assays ranged from 1.5 to 4.0%, 2.5 to 16.8% and 1.0 to 7.7%, respectively. Accuracies ranged from 100 to 110%, 101 to 116% and 99 to 106% for LPV, RTV and EFV, respectively. The extraction recoveries were 77—87, 77—83 and 81—91% for LPV, RTV and EFV, respectively.View full abstractDownload PDF (71K) -
Viqar Uddin Ahmad, Javid Hussain, Hidayat Hussain, Amir Reza Jassbi, F ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 719-723
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSThree new diterpene esters with a myrsinol-type skeleton have been isolated from Euphorbia decipiens BOISS. & BUHSE. The structure elucidation of the isolated compounds was based primarily on two-dimensional (2D)-NMR techniques including correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple bond correlation (HMBC) and nuclear Overhauser effect spectroscopy (NOESY) experiments. Compounds 1 and 3 are active against prolyl endopeptidase and compound 2 showed inhibitory activity against urease enzyme.View full abstractDownload PDF (72K) -
Motoya Suzuki, Kinzo Watanabe, Shoko Fujiwara, Toshie Kurasawa, Takako ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 724-727
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSTwo norcarotenoids, 1 and 2, related to peridinin (3) were isolated from the cultured dinoflagellate of the genus Symbiodinium, a symbiont of the Okinawan soft coral Clavularia viridis, which contains in abundance antitumor marine prostanoids such as clavulones. The structures of 1 and 2 were elucidated on the basis of spectroscopic analysis. These compounds showed significant growth-inhibitory activity in vitro toward cancer cells. Analysis of fatty acids of the dinoflagellate was also carried out, suggesting that the marine prostanoids are produced by the host soft coral itself.View full abstractDownload PDF (72K) -
Chatchanok Loetchutinat, François Chau, Samlee MankhetkornArticle type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 728-730
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESS5-Aryl-3-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 3 were prepared by cyclocondensation of 1-(4-hydroxyphenyl)-2-aroylhydrazines with thiophosgene. All compounds exhibited antiproliferation activity in K562, IC50 ranging from 24 to 94 μM comparable efficacy with apigenin and genistein and showed more potent antiproliferation of K562/adr cells, highly expressing P-glycoprotein. Compounds 3g, 3e and 3a inhibited the function of P-glycoprotein with the α0.5 equal to 10±3 μM, 21±5 μM and 34±7 μM, respectively.View full abstractDownload PDF (56K) -
Sei-Joon Jeong, Masanori Inagaki, Ryuichi Higuchi, Tomofumi Miyamoto, ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 731-733
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSAn antiangiogenic purine analog, 1,3-dimethylisoguaninium (1), was isolated from the ethanol (EtOH) extract of the Okinawan sponge Amphimedon paraviridis. The structure was elucidated on the basis of its spectral properties and X-ray crystallographic analysis. Compound 1 exhibited specific inhibition of the basic fibroblast growth factor (bFGF)-induced proliferation of bovine aorta endothelial cells (BAECs). Moreover, compound 1 reduced the tube formation of BAECs in a time-dependent manner.View full abstractDownload PDF (105K) -
Toshinobu Seki, Junko Mochida, Maiko Okamoto, Osamu Hosoya, Kazuhiko J ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 734-736
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSDiffusion coefficients (D) of parabens and steroids in water and 1-octanol were determined by using the chromatographic broadening method at 37 °C, and the relationships between the D values and the physicochemical properties of the drugs were discussed. The D values in 1-octanol were lower than those in water because of the higher viscosity of 1-octanol. The D values depend on not only the molecular weight (MW), but also the lipophilicity of the drugs in water and on the ability for hydrogen-bonding in 1-octanol. When the lipophilic index (LI), calculated from the retention time using in a reverse-phase column, was used as a parameter of drug lipophilicity, the following equation was obtained for D in water (Dw); log Dw=−0.215·log MW−0.077·log LI−4.367. When the hydrogen bond index (HI), the logarithm of the ratio of the partition coefficient of the drugs in 1-octanol and cyclohexane, was used as an index of hydrogen-bonding, the following equation was obtained for D in 1-octanol (Do); log Do=−0.690·log MW−0.074·log HI−4.085.View full abstractDownload PDF (55K) -
Souichi Kawamoto, Takashi Koyano, Thaworn Kowithayakorn, Haruhiro Fuji ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 737-739
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSTwo new pregnane alkaloids, wrightiamines A (1) and B (2), were isolated from the extract of the tropical Apocynaceous plant Wrightia javanica collected in Thailand, and their structures were elucidated by spectral data. Wrightiamine B (2) was preparaed from 3β-hydroxy-5α-pregnan-20-one to establish the configuration of the C-20 position as S. Wrightiamine A (1) exhibited cytotoxic activity against vincristine-resistant murine leukemia P388 cells.View full abstractDownload PDF (62K) -
Shigenori Kumazawa, Masahiro Yoneda, Ikoi Shibata, Jun Kanaeda, Tomoko ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 740-742
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSTo identify the plant origin of Brazilian propolis directly, we observed the behavior of honeybees in Minas Gerais State of Brazil. Honeybee workers bit and chewed leaves of the plant, Baccharis dracunculifolia, packed the material into their pollen basket, brought it back to their nest, and used it as propolis. We collected the leaves of B. dracunculifolia and propolis, and compared their constituents by liquid chromatography-mass spectrometry (LC/MS) analysis. There was no difference between the chemical constituents of the ethanol extracts of B. dracunculifolia and those of propolis. This indicates directly that the plant origin of Brazilian propolis is B. dracunculifolia.View full abstractDownload PDF (193K) -
Fukuji Ebihara, Satoru WatanoArticle type: Note
Subject area: [not specified]
2003 Volume 51 Issue 6 Pages 743-745
Published: 2003
Released on J-STAGE: June 01, 2003
JOURNAL FREE ACCESSThis paper discusses a process for making a novel granular detergent with an interspersion particle comprising an anionic surfactant and a polymeric polycarboxalate. This process contains three steps to develop the interspersion particles with anionic surfactant and polymeric ploycarboxalate. The first step was to form a detergent particle by spray drying of an aqueous detergent slurry comprising anionic surfactant (liner alkyl benzene sulfonate) with the different levels of polymeric polycarboxalate. In the second step, the spray-dried granules were densified and ground by a roll compacter and a grinder. The ground particles were coated by nonionic and zeolite in a vertical batch type high shear mixer (third step). In this study, the feasibility to make better performance of granular detergent was discussed.View full abstractDownload PDF (70K)
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