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Masakazu SONO, Naoko TOYODA, Kahori SHIMIZU, Eiji NODA, Yoshikazu SHIZ ...
1996 Volume 44 Issue 6 Pages
1141-1145
Published: June 15, 1996
Released on J-STAGE: March 31, 2008
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Nitrogen-containing compounds have been subjected to electrochemical oxidation with Et
3N-3HF as an electrolyte. Caffeine afforded 8-fluorocaffeine as a sole product in 40.3% yield. Guanosine tetraacetate and uridine triacetate gave the fluorinated compounds in 17.5 and 4.6% yields, rspectively. Similar electrochemical oxidation of caffeine with methanol, KCl, or KCN afforded 8-methoxycaffeine, 8-chlorocaffeine, or 8-cyanocaffeine, respectively.
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Naoyoshi MAEZAKI, Manabu MURAKAMI, Motohiro SOEJIMA, Tetsuaki TANAKA, ...
1996 Volume 44 Issue 6 Pages
1146-1151
Published: June 15, 1996
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Asymmetric desymmetrization of a prochiral 1, 3-diol was established by diastereoselective C-O bond fission of the chiral α-sulfinyl acetal 6. Treatment of 6 with titanium tetrachloride afforded mainly 7a via an oxonium intermediate, while with lithium diisopropylamide 7b was selectively obtained via diastereoselective β-elimination followed by an olefin isomerization.
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Ryuichiro TANAKA, Kazumoto MIYAHARA, Naoki NODA
1996 Volume 44 Issue 6 Pages
1152-1156
Published: June 15, 1996
Released on J-STAGE: March 31, 2008
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Nine homogehous glycosphingolipids were isolated from the earthworm, Pheretima asiatica (Annelida). All of them are digalactosylceramides carrying a choline phophate group in the outer galactose moiety. Their full structures including the position of a phosphocholine unit were determined based on chemical and spectral evidence.
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Isao KITAGAWA, Partomuan SIMANJUNTAK, Taifo MAHMUD, Motomasa KOBAYASHI ...
1996 Volume 44 Issue 6 Pages
1157-1161
Published: June 15, 1996
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Following the previous studies on caesaldekarins a (1) and b (2), the chemical structures of three additional cassane-type furanoditerpenes named caesaldekarins c (3), d (4), and e (5), isolated from the roots of Caesalpinia major (Fabaceae) collected in Flores Island, Indonesia, have been elucidated on the bases of physicochemical evidence and chemical derivations. Several interesting NBS(N-bromosuccinimide) reaction products of 1 have been elucidated.
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Isao KITAGAWA, Hong WEI, Sanae NAGAO, Taifo MAHMUD, Kazuyuki HORI, Mot ...
1996 Volume 44 Issue 6 Pages
1162-1167
Published: June 15, 1996
Released on J-STAGE: March 31, 2008
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A new secoiridoid glucoside named 3'-O-caffeoylsweroside (1), and two new phenolic apioglucosides, named kelampayoside A (4) and kelampayoside B (6), together with eleven known compounds (five iridoids and six alkaloids), were isolated from the bark of Anthocephalus chinensis (Rubiaceae), an Indonesian medicinal plant from Sumatra Island, Indonesia. The chemical structure of 1, 4 and 6 have been elucidated respectively as 3'-O-caffeoylsweroside (1), antiarol I-O-β-D-apiofuranosyl(1→6)-β-D-glucopyranoside (4), and antiarol 1-O-β-D-5"-O-caffeoylapiofu-ranosyl(1→6)-β-D-glucopyranoside (6) on the bases of their chemical and physicochemical properties. Among fourteen constituents characterized, cadambine (13), one of the major indole alkaloidal constituents of A. chinensis, was shown to exhibit moderate growth-inhibitory activity against the malarial parasite Plasmodium falciparum (a chloroquine-resistant K1 strain) cultured in human erythrocytes.
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Hiroshi SAI, Yasuhiko OZAKI, Kimiaki HAYASHI, Yuichi ONODA, Kenji YAMA ...
1996 Volume 44 Issue 6 Pages
1168-1173
Published: June 15, 1996
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Trimebutine derivatives were synthesized by utilizing alkylation or acylation of isonitriles and nitrile as a key step. The colonic contractile effects of these compounds were examined, and T-1815 was found to have strong colonic propulsive activity.
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Kenji TSUJIHARA, Mitsuya HONGU, Kunio SAITO, Masanori INAMASU, Kenji A ...
1996 Volume 44 Issue 6 Pages
1174-1180
Published: June 15, 1996
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Based on our new concept that inhibitors of the Na
+-glucose contransporter (SGLT) would be useful as antidiabetics, 4'-dehydroxyphlorizin derivatives 1a-f were designed, synthesized, and examined for various pharmacological properties related to antidiabetic activity. In normal rats, 1a, e and phlorizin showed a strong SGLT-inhibitory effect and significantly increased urinary glucose on intraperitoneal administration at 10 mg/kg, through only 1a resulted in excretion of large quantities of urinary glucose on oral administraiton at 100 mg/kg. Compounds 1a, e, and phlorizin markedly inhibited glucose uptake in the small intestine during enteric perfusion in normal rats. Compound 1a had a significant reducing effect on blood glucose in the glucose tolerance test in mice when administered orally and also lowered blood glucose in steptozotocin-induced diabetic rats. The aglycons 2a, e of 1a, e, and 1a showed weak inhibitory effects on the facilitated glucose transporter-1 (GLUT-1) in human erythrocytes, while phloretin had a strong inhibitory effect on GLUT-1. Compound 1a caused no apparent renal damage in rats when administered orally at 1 g/kg for 4 successive weeks. Thus, 1a was considered to be a promising candidate as a lead compound for antidiabetics of a new type, and was selected for further pharmacological evaluation.
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Jin-Cherng LIEN, Li-Jiau HUANG, Jih-Pyang WANG, Che-Ming TENG, Kuo-Hsi ...
1996 Volume 44 Issue 6 Pages
1181-1187
Published: June 15, 1996
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Modification of 2-acetamido-3-chloro-1, 4-naphthoquinone, which has potent antiplatelet, antiallergic and antiinflammatory activities, led to a series of 2, 3-disubstituted 1, 4-naphthoquinones. Some of these compounds showed significant antiplatelet, antiallergic and antiinflammatory activities. Among them, 2-methoxy-3-chloro-1, 4-naphthoquinone (15) and 2-ethoxy-3-chloro-1, 4-naphthouinone (17) exhibited potent inhibitory effects on neutrophil and mast cell degranulation. 2-Methoxy-1, 4-naphthoquinone (20) and 2-ethoxy-1, 4-naphthoquinone (21) exhibited potent inhibitory effect on neutrophil superoxide formation. These four compounds were thus selected for further evaluation.
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Kiyoshi TANIGUCHI, Yasuhiro MIYAO, Katsuhiro YAMANO, Takao YAMAMOTO, T ...
1996 Volume 44 Issue 6 Pages
1188-1195
Published: June 15, 1996
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We synthesized the racemates of five presumed metabolites (1b-f) of (S)-(-)-N-tert-butyl-4, 4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(-)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate thier inhibitory activity against detrusor contraction. (±)-N-tert-Butyl-4-(4-hydroxyphenyl)- and 4-(4-hydroxy-3-methoxyphenyl)-4-phenyl-2-cyclopenetenyl-amines (1b-e) were synthesized via 5-(4-methoxyphenyl)- and 5-(4-benzyloxy-3-methoxyphenyl)-5-phenyl-2-cyclopenten-1-one (9g, h), respectively. Compounds 1b-f prepared in this study were identical with the metabolites in human urine in gas chromatography-mass specrometry and analytical HPLC. The inhibitory activity of compounds 1b-f against detrusor contraction in vitro induced by electrical field stimulation in guinea-pigs was less potent than that of FK584.
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Naoyuki HARADA, Mitsuya HONGU, Takayuki KAWAGUCHI, Motoaki OHOHASHI, K ...
1996 Volume 44 Issue 6 Pages
1196-1201
Published: June 15, 1996
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In an attempt to improve the effectiveness of action of 5-fluoro-2'-deoxyuridine (FUdR), various kinds of O-alkylated water-soluble analogues were synthesized. Antitumor activities against sarcoma 180 (solid) were also evaluated. Some compounds exhibited potent activities. In particular, 3'-O-p-chlorobenzyl-3-N-aminoacyloxy-methylester derivatives were effective over a very wide range of dose and gave extremely large therapeutic ratios compared with known 5-fluorouracil (5-FU) derivatives.
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Toshihiro AKIHISA, Yumiko KIMURA, Wilhelmus C. M. C. KOKKE, Takashi IT ...
1996 Volume 44 Issue 6 Pages
1202-1207
Published: June 15, 1996
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Eight novel sterols, 4, 4-dimethyl-5α-poriferasta-7, 25-dien-3β-ol, (24E)-24-ethyl-29-nor-5α-lanosta-7, 24(24
1)-dien-3β-ol, (24E)-24-ethyl-29-nor-5α-lanosta-9(11), 24(24
1)-dien-3β-ol, (24E)-24-ethyl-29-nor-5α-lanosta-7, 9(11), 24(24
1)-trien-3β-ol, (22E, 24Z)-5α-stigmasta-7, 22, 24(24
1)-trien-3β-ol, 5α-stigmasta-7, 9(11)-dien-3β-ol, (24E)-5α-stigmasta-7, 9(11), 24(24
1)-trien-3β-ol, and (24E)-14α-methyl-5α-stigmasta-7, 24(24
1)-dien-3β-ol, were isolated (as acetates) from the saponified neutral fraction of Bryonia dioica root extract. The structures were determined by spectroscopic methods. The compounds are new because the 4, 4-dimethy-Δ
7-cholestene-, 4α, 14α-dimethyl-Δ
7-cholestene (or 29-nor-Δ
7-lanostene)-, and 14α-methyl-Δ
7-cholestene-skeletons and the (22E, 24Z)-Δ
22, 24(241)-stigmastadiene side chain have not been found before in nature. Abundances are given of fifty three identified triterpene alcohols and sterols.
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Takeshi KINOSHITA, Jin-Bin WU, Feng-Chi HO
1996 Volume 44 Issue 6 Pages
1208-1211
Published: June 15, 1996
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Three new prenylcoumarins, murpaniculol senecioate, 5-methoxymurrayatin and omphamurin isovalerate were isolated from the leaves of Murraya paniculata var. omphalocarpa (Rutaceae), together with six known coumarins, paniculatin, (-)-sibiricin, 5, 7-dimethyoxy-8-(3'-methyl-2'-oxobutyl)coumarin, (-)-mexoticin, omphamurin and omphalocarpin. Their structures were characterizied on the basis of spectroscopic evidence. The absolute configulation of omphamurin at the C-2' position has been determined to be S by Horeau's method. THe absolute stereochemistry of (-)-mexoticin and (-)-sibiricin has also been established by their chemical correlation with omphamurin.
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Masayuki YOSHIKAWA, Toshiyuki MURAKAMI, Masashi KADOYA, Hisashi MATSUD ...
1996 Volume 44 Issue 6 Pages
1212-1217
Published: June 15, 1996
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Betavulgarosides I, II, III, and IV, oleanolic acid oligoglycosides having an unique acidic substituent, were isolated from the root of Beta vulgaris L. (sugar beet) together with betavulgarosides VI, VII, and VIII. The chemical structures of betavulgarosides I, II, III, and IV were identified from chemical and physicochemical evidence. Betavulgarosides II, III and IV were found to exhibit hypoglycemic activity in an oral glucose tolerance test in rats.
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Takeshi KINOSHITA, Kiichiro KAJIYAMA, Yukio HIRAGA, Kunio TAKAHASHI, Y ...
1996 Volume 44 Issue 6 Pages
1218-1221
Published: June 15, 1996
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Two new pyrano-2-arylbenzofuran derivatives named glabrocoumarones A and B were isolated from commercially available licorice of Glycyrrhiza glabra origin, and thier structures were elucidated as 4'-6-dihydroxy-[6", 6"-dimethylpyrano(2", 3" : 2', 3')]-2-arylbenzofuran and 2', 6-dihydroxy-[6", 6"-dimethylpyrano(2", 3" : 4', 3')]-2-aryl-benzofuran, respectively, on the basis of spectroscopic evidence. Six known compounds were also obtained and identified spectroscopically as glabrol, 3-hydroxygrabrol, shinflavanone, [6", 6"-dimethylpyrano(2", 3" : 7, 8)]-[6''', 6'''-dimethylpyrano(2''', 3''' : 4', 3')]-flavanone (xambioona), 3, 3'-di-γ, γ-dimethylallyl-2'-4, 4'-trihydroxychalcone and [6", 6"-dimethylpyrano(2", 3" : 4, 5)]-3'-γ, γ-dimethylallyl-2', 3, 4'-trihydroxychalcone.
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Hideo MIYAO, Yusuke SAKAI, Takashi TAKESHITA, Junei KINJO, Toshihiro N ...
1996 Volume 44 Issue 6 Pages
1222-1227
Published: June 15, 1996
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From Abri Herba, the whole plant of Abrus cantoniensis (Leguminosae), ten new oleanene saponins together with thirteen known onew were isolated. Among them, four saponins called abrisaponins L, A, D
1 and Ca have been elucidated to be 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-galactopyranosyl-(1→2)-β-D-glucuronopyranosyl (designated as β-fabatriosyl) abrisapogenol L (1), 3-O-β-fabatriosyl abrisapogenol A (2), 3-O-β-fabatriosyl abrisapogenol D (3), and 3-O-β-fabatriosyl cantoniensistriol (4), respectively.
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Hideo MIYANO, Yusuke SAKAI, Takashi TAKESHITA, Yasuyuki ITO, Junei KIN ...
1996 Volume 44 Issue 6 Pages
1228-1231
Published: June 15, 1996
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The chemical structures of abrisapoinins So
1 (1), So
2 (2), D
2 (3), D
3 (4), F (5) and SB (6), six of twenty-three saponins from Abri Herba, the whole plants of Abrus cantoniensis (Leguminosae), were investigated. They were elucidated to be 3-O-α-L-rhamnopyranosyl-(1→2)-[O-β-D-glucopyranosyl-(1→3)]-β-D-galactopyranosyl-(1→2)-β-D-glucuronopyranosyl (designated as β-abrietraosyl) sophoradiol (1), 3-O-β-abritetraosyl sophoradiol 22-O-β-D-xylopyranoside (2), 3-O-β-abritetraosyl abrisapogenol D (3), 3-O-β-abritetraosyl abrisapogenol D 22-O-β-D-glucopyranoside (4), 3-O-β-abritetraosyl abrisapogenol F (5) and 3-O-β-abritetraosyl soyasapogenol B (6), respectively.
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Masanao ISHIKAWA, Kotaro HATTORI, Shin-ichi KONDO, Masayuki KUZUYA
1996 Volume 44 Issue 6 Pages
1232-1237
Published: June 15, 1996
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With a view to expanding the application of a drug delivery sysetm (DDS) preparation using plasma-irradiated pharmaceutical aids for various dosage forms, we studied the theophylline release property from plasma-irradiated polymer-coated granules, the polymers of which differ in the plasma irradiation effect. We used a new type of rotational plasma-irradiation reactor to perform plasma-irradition uniformly on the surface of polymer-coated granules based on scanning electron microscope (SEM) observation. It was shown that an increase in theophylline release rate with an increase in plasma duration was observed in all polymer-coated granules, although the factors of such release propertis vary with the polymers, as evidenced by the SEM observations. Such results provided the criteria for selecting polymer structures for granule coating. Thus, the present method for the control of drug release is considered principally applicable not only to polymer-coated granules but also to various drug forms under consideration of the above criteria.
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Masashi NAKAMURA, Yasuki KATO, Eiji HAYAKAWA, Kunio ITO, Tokuyuki KURO ...
1996 Volume 44 Issue 6 Pages
1238-1241
Published: June 15, 1996
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The electrochemical stability of desmopressin acetate (DDAVP) was investigated. After a direct current of 1 mA was passed through two electrodes chosen from platinum, silver and silver chloride, the decomposition of DDAVP was observed. The degradation products of DDAVP yielded with a Pt(anode) and AgCl(cathode) pair were similar to those observed in an anodic donor after in vivo iontophoresis. Although the Ag(anode)/Pt(cathode) degradation pattern of DDAVP was similar to that of an in vivo cathodic donor HPLC chromatogram, it was different from that of the anodic donor. In the anodic system, the stability of DDAVP was independent of the pH, and decreased with increasing concentration of NaCl.
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Yueh-Hsiung KUO, Ming-Tsang YU
1996 Volume 44 Issue 6 Pages
1242-1244
Published: June 15, 1996
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Three new labdane-type diterpenes, (13S)-15-hydroxylabd-8(17)-en-19-oic acid, (13S)-15-acetoxylabd-8(17)-en-19-oic acid, and (13S)-15-octadecanoyloxylabd-8(17)-en-19-oic acid, together with one known compound, enantio-oliveric acid, were found from the bark of Juniperus formosana HAY. var. concolor HAY. Their structures were elucidated on the basis of spectral data and chemical transformation.
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Tadamasa TERAI, Mamoru SATO, Isao NARAMA, Tetsuro MATUURA, Jun'ichi KA ...
1996 Volume 44 Issue 6 Pages
1245-1247
Published: June 15, 1996
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Grayanotoxin(GTX) III, a tetracyclic diterpenoid, is the main toxic component obtained from the leaves of Leucothoe grayama MAX. In this paper, we report the correlation between toxicity and C
10 stereostructure of GTX-III. 10-epi-GTX-III was derived from GTX-III in four steps. Oxidation of the GTX-II-3, 6, 14, 16-tetraacetate with formic acid/hydrogen peroxide in chloroform gave 10, 20-epoxy derivative in high yield. Reduction of the 10, 20-epoxyacetate with LiAlH
4 in tetrahydrofuran gave the two products, 10-epi-GTX-III and 10, 20-epoxy-GTX-II. The absolute structure of the 10-epi-GTX-III was deduced from the results of X-ray crystallographic analysis. Dosage level of acute toxicity of 10-epi-GTX, III in mice was estimated at about half of natural GTX-III.
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Noriyuki HORI, Norihiko SEKO, Goro TSUKAMOTO, Kohichiro YOSHINO
1996 Volume 44 Issue 6 Pages
1248-1249
Published: June 15, 1996
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To study the pharmacokinetics and metabolism of 4-acetoxy-2-(4-methylphenyl)benzothiazole (KB-2683), which has potential immunomodulating activity, a practical preparation of labeled KB-2683 was needed. This paper describes an efficient method for the synthesis of
14C-labeled KB-2683 by means of procedures which include a metal-catalyzed cross-coupling reaction.
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Yoshihiro ABE, WANG Qing, Tomoko SHOJI, Shikie FUKUI, Mayumi SUZUKI, T ...
1996 Volume 44 Issue 6 Pages
1250-1251
Published: June 15, 1996
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Enantioselective distribution of (±)-pindolol was observed in a chloroform-boric acid two-phase system in the presence of (1R, 2R)-(+)-hydrobenzion, 1, 4-di-O-dodecyl L-threitol, (R)-(+)- or (S)-(-)-1, 1'-2-binaphthol in the organic phase.
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Toshihisa OHYAMA, Chiyo MATSUBARA, Kiyoko TAKAMURA
1996 Volume 44 Issue 6 Pages
1252-1254
Published: June 15, 1996
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Sensitive TLC for the determination of sugarphosphoesters and nucleotides was established. The individual separation of four sugarphosphoesters and three nucleotides on a silica gel plate was carried out in 1-butanol-acetic acid-water (1 : 1 : 1, v/v). Following the development of phophate esters, alkaline phophatase solution was sprayed on the plate at 45°C to librate phosphate from each phophate ester. After spraying a mixture of molybdic acid and Melachite Green on the plate, the liberated phophate appeared as blue-green spots of molybdophosphate-Malachite Green aggregates on a yellow-brown back ground. The absorbance of each spot on the plate was measured at 620 nm with a densitometer to obtain a chromatogram. Fructose 1-phophate, fructose 1, 6-phophate, glucose 6-phosphate, mannose 6-phophate, adenosine 5'-triphosphate, adenosine 5'-diphosphate and adenosne 5'-monophosphate could be detected separately at a sensitivy of as little as 0.5 pmol/spot. The values of relative standard deviation for the esters was less than 3.9% (n=7) at 20 pmo/spot.
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Toshihiro AKIHISA, Hirotoshi OINUMA, Ken YASUKAWA, Yoshimasa KASAHARA, ...
1996 Volume 44 Issue 6 Pages
1255-1257
Published: June 15, 1996
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A novel 3, 4-seco-triterpene alcohol with a migrated euphane-type skeleton, called helianol, was isolated together with seven known triterpene alcohols from the nonsaponifiable lipid of the tabular flower extract of Helianthus annus L. The structure was determined by extensive spectroscopic analyses.
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Masahiro KAJIWARA, Takeo OKAZAKI, Katsumi IIDA, Shoko NARUMI, Miyako H ...
1996 Volume 44 Issue 6 Pages
1258-1260
Published: June 15, 1996
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We determined the optimum
13C-labeling position in phenacetin for use in a breath test to diagnose liver disease based on infrared spectroscopy detection of
13CO
2 in exhaled air. ([1-
13C]Ethoxy)phenacetin gave the best result. This compound was also employed in a urine test using
13C-NMR spectroscopy. In the urine test, healthy subjects gave a higher signal of phenacetin than of its metabolite, phenetidine, whereas in patients with liver disease the situation was the reverse. The combination of the breath and urine tests may be a valuable new tool for the diagnosis of liver disease.
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Takeshi KINOSHITA, Kurnia FIRMAN
1996 Volume 44 Issue 6 Pages
1261-1262
Published: June 15, 1996
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A new prenylcoumarin was isolated from the leaves of Murraya paniculata (Rutaceae), and its structure was elucidated as 5, 7-dimethoxy-8-[(Z)-3'-methylbutan-1', 3'-dienyl]coumarin on the basis of spectroscopic evidence.Five other coumarins were also obtained and identified with the known compounds coumurrayin, 5, 7-dimethoxy-8-(3'-methyl-2'-oxobutyl)coumarin, toddalenone, toddasin and aurapten.
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Stefan HUTH, Reinhard NEUBERT, Lothar BOLTZE, Axel BUGE
1996 Volume 44 Issue 6 Pages
1263-1266
Published: June 15, 1996
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The penetration of the cosolvent and penetration enhancer propylene glycol (PG) into a multilayer membrane system was examined. Consisting of dodecanol (DD) this acceptor system was used to simulate the intercellular lipid pathway across the stratum corneum. Vehicles with 10%, 40% and 60% PG were investigated. Using a pharmacokinetic description based on Fick's first law of diffusion, the transport rate of PG was simulated. A parameter estimation was carried out to obtain a kinetic velocity parameter k
PG for the transport. k<PG> depends on the diffusion coefficient, the area of application, and the pathlength. The data were validated by determining confidence intervals. The extent of the penetration of PG into the lipophilic acceptor system was shown to be quantitative. The data presented are useful for further investigations to assess the solvent drag effect caused by PG penetration. The multiplayer membrane model was found to provide reasonable results with respect to accuracy and reproducibility.
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Satoru WATANO, Hideo TAKASHIMA, Yoshinobu SATO, Teruhito YASUTOMO, Kei ...
1996 Volume 44 Issue 6 Pages
1267-1269
Published: June 15, 1996
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In this study, the validity of moisture measurement by an IR sensor was investigated in fluidized bed granulation. The effects of operating variables on the relationship between granule moisture content and the absorbance of IR spectra were examined experimentally. It was found that the air flow rate of purge air used for preventing powder adhesion, fluidizing air velocity, agitator rotational speed and spray mist size had no effect on the relationship. However, if the dampening speed was extremely low, the effects of fluidization air temperature and liquid flow rate on the relationship could be recognized. This was because the surface drying due to the extremely low dampening speed caused water to transfer from the inside to the surface. As a result, it can be concluded that the measurement of moisture content by an IR moisture sensor can be conducted with high accuracy, free of operating conditions, unless the granulation is conducted under an extremely low dampening speed.
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Masahiko KUROKAWA, Haruo OHYAMA, Toyoharu HOZUMI, Tsuneo NAMBA, Michio ...
1996 Volume 44 Issue 6 Pages
1270-1272
Published: June 15, 1996
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We evaluated an antiviral assay procedure using serum obtained from guinea pigs administered 32 herbal extracts. In this assay, 21 of the 32 showed anti-herpes simplex virus type 1 (HSV-1) activity in serum. Ten of the 21 exhibited therapeutic anti-HSV-1 activity, and this was consistent with our previous that 12 of the 32 were effective in murine infection models. Therefore, the serum pharmacological assay procedure was suitable for the selection of possible herbal extracts with biological activity in vivo as a pre-screening method before animal experiments.
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Kazuyuki SAGI, Hiroyuki KAGECHIKA, Hiroshi FUKASAWA, Yuichi HASHIMOTO, ...
1996 Volume 44 Issue 6 Pages
1273-1275
Published: June 15, 1996
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A strategy for development of thyroid hormone analogs was examined based on the combinatorial concept. The reaction of ethyl 3, 3'5-triiodothyroacetate (3b) with Cd/Br
2CF
2/CuBr followed by ester hydrolysis gave a mixture of more than ten products as detected by HPLC. The structures of the products in the bioactive fractions showed that the replacemnt of iodides with trifluoromethyl groups is an effective approach for obtaining thyromimetics.
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Hajime KATAYAMA, Yusuke KAWADA, Takamitu OSHIYAMA, Akio EJIMA
1996 Volume 44 Issue 6 Pages
1276-1278
Published: June 15, 1996
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A new type of synthetic dual inhibitor of DNA topoisomerase I and II was explored. This series of compounds shows high antineoplastic activities against cancer cells, but in vivo activity against P388 was not as high as in vitro activities.
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Nobutoshi MURAKAMI, Masami SAKA, Hiromi SHIMADA, Hisashi MATSUDA, Johj ...
1996 Volume 44 Issue 6 Pages
1279-1281
Published: June 15, 1996
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Bioassay-guided separation of MeOH extract of Japanese Paeoniae Radix inhibiting contractile responses of guinea pig ileum stimulated with electric field disclosed a new monoterpene glycoside, 6-O-β-D-glucopyranosyl-lactinolide (1), as an active constituent together with two new monoterpene glycosides (3 and 4) and two new monoterpenes (2 and 5). Furthermore, 1-O-β-D-glucopyranosyl-paeonisuffrone (2) was fond to inhibit histamine release from rat peritoneal exudate cells induced by antigen-antibody reaction.
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Toshiko KIGUCHI, Mitsuko SHIRAKAWA, Ichiya NINOMIYA, Takeaki NAITO
1996 Volume 44 Issue 6 Pages
1282-1284
Published: June 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL
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A combination of 1, 3-dipolar cycloaddition of Z-nitrone (2) to the chiral dipolarophile (3) and subsequent ring transformation of the resulting adducts (4 and 6) to piperidinol (17) has provided a new practical synthesis of 2, 3, 6-trisubstituted piperidine alkaloid, (+)-azimic acid (1).
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Okiko MIYATA, Atsuko NISHIGUCHI, Ichiya NINOMIYA, Takeaki NAITO
1996 Volume 44 Issue 6 Pages
1285-1287
Published: June 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL
FREE ACCESS
A stereoselective route to (±)-oxo-parabenzlactone has been developed by the combination of thiyl radical addition-cyclization of dienylhydroximate and subsequent conversion of the resulting cyclic hydroximate to lactone.
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