All issues
Volume 42, Issue 11
Displaying 1-42 of 42 articles from this issue
- |<
- <
- 1
- >
- >|
-
Yoji TACHIBANA1994 Volume 42 Issue 11 Pages 2215-2218
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSyntheses of (20R)- and (20S)-1α, 3β-diacetoxypregna-5, 7-dien-20-ol (1 and 2), important synthetic intermediates for the preparation of 1α, 25-dihydroxy-22-oxa-vitamin D3 derivatives, were achieved starting from pregnenolone. Similar treatment of androst-5-ene-3β, 17β-diol afforded 1α, 3β-diacetoxyandrosta-5, 7-dien-17β-ol.View full abstractDownload PDF (763K) -
Etuo OISHI, Ken-ichi IWAMOTO, Tomomi OKADA, Sumiko SUZUKI, Ken-ichi TA ...1994 Volume 42 Issue 11 Pages 2219-2224
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1-Chlorophthalazine (1) reacts with a 2-fold molar excess of ynamines 2a, b to give penta-substituted pyridine derivatives 3a, b by nitrogen-nitrogen bond cleavage of the pyridazine ring with release of hydrogen chloride. Similarly, other fused pyridazines having a chloro substituent α to nitrogen in the pyridazine ring, i.e., pyrido[3, 4-d]- (10a), pyrido[2, 3-d]- (10b), thiazolo[4, 5-d]- (10c, d), furo[2, 3-d]- (10e) and pyrrolo[2, 3-d]- (10f, g) pyridazine derivatives, gave the corresponding penta-substituted pyridines 11a-11k.View full abstractDownload PDF (809K) -
Masayuki YOSHIKAWA, Emiko HARADA, Yoshikazu NAITOH, Kimiyo INOUE, Hisa ...1994 Volume 42 Issue 11 Pages 2225-2230
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the less polar fraction of Hydrangeae Dulcis Folium, the fermented and dired leaves of Hydrangea macrophylla SERINGE var. thunbergii MAKINO, eight antiallergic and antimicrobial principles were isolated together with several known compounds. Among the newly isolated bioactive constituents, the chemical structures of thunberginols A, B, and F have been determined on the basis of chemical and physicochemical evidence. Thunberginols A, B, and F were found to exhibit more potent antiallergic activity than phyllodulcin, hydrangenol, disodium cromoglycate (DSCG), and tranilast. In addition, these thunberginols showed antimicrobial activity against oral bacteria.View full abstractDownload PDF (916K) -
Akira ONO, Tomoko OKAMOTO, Michiyo INADA, Hiroshi NARA, Akira MATSUDA1994 Volume 42 Issue 11 Pages 2231-2237
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThymidine was converted into 5-formyl-2'-deoxyuridine (1), which was incorporated into oligonucleotides, 5'd(GGAGA1CTCC)3' (I-1) and 5'd(GCTGC1GCGAAAGCTG)3' (II-1). To avoid side-reactions and degradation, protection of the formyl group of 1 using a newly developed protecting group, N, N-di-(3, 5-dichlorophenyl)ethylenediamine, was necessary. Compound 1 was unstable under the conditions employed for enzymatic complete degestion of oligonucleotides, so that a peak corresponding to 1 was notodetected clearly by HPLC analysis of a nucleoside mixture obtained by complete hydrolysis of I-1. Therefore, the oligonucleotide I-1 was treated with cyanomethylenetriphenylphosphorane to give an oligonucleotide containing (E) and (Z)-5-(2-cyanovinyl)-2'-deoxyuridine, which was then hydrolyzed, and the newly generated nucleosides were detected by HPLC analysis. The Tm of the self-complementary oligonucleotide I-1 (40°C) was higher than that of the parent oligonucleotide, 5'd(GGAGATCTCC)3', (31°C) in a buffer containing 0.01M sodium phosphate (pH 7.0) and 0.1M NaCl. DNA replication study on a template-primer system [primer, 5'd(32P-CAGCTTTCGC)3'; template, 3'd(GTCGAAAGCGXCGTCG)5' (X=1 or T)] showed that dATP was incorporated into the DNA strand at a site opposite to 1 by Klenow DNA polymerase, but with a reduced rate. The formyl group of 1 in the oligonucleotides reacted with amines to geve Schiff base derivatives.View full abstractDownload PDF (1097K) -
Leila CHAKER, Felix PAUTET, Houda FILLION1994 Volume 42 Issue 11 Pages 2238-2240
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe nucleophilic addition of dimethylamine to bromojuglones and bromomethyljuglones is followed by elimination of hydrogen bromide or oxidation. With 2-bromojuglone, the oxidative process predominates at low temperature. The regiochemistry of the addition is a function of the temperature and of the position of the bromine atom (C-2 or C-3) on the quinone.View full abstractDownload PDF (550K) -
Nobutaka FUJII, Kazuo NAKAI, Hiromu HABASHITA, Yuka HOTTA, Hirokazu TA ...1994 Volume 42 Issue 11 Pages 2241-2250
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of three cis-trans pairs of N-sulfonylated-2-aziridinemethanols starting from (S)-threonine, (R)-allothreonine, a chiral 2-amino alcohol, or enantiomerically enriched 2, 3-epoxy alcohols is described. A synthetic route to N-tosyl- and N-mesyl-2-aziridinemethanols from (R)- and (S)-serines is also presented.View full abstractDownload PDF (1750K) -
Tsutomu NAKANISHI, Masatoshi NISHI, Midori SOMEKAWA, Hiroko MURATA, Mi ...1994 Volume 42 Issue 11 Pages 2251-2255
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new cyanoglucoside, purshianin (1), was isolated together with a known cyanoglucoside, menisdaurin (2a), from stems of Purshia tridentata DC. (Rosaceae) collected in Oregon, U.S.A. and the structure was established as (4S, 6S)-(Z)-6-(β-D-glucopyranosyloxy)-4-hydroxy-2-cyclohexene-Δ1, α-acetonitrile (1) based on chemical and spectral evidence. Notably, the absolute structure of 1 and the revised stereostructure (2), (4S, 6R)-(Z)-6-(β-D-glucopyranosyloxy)-4-hydroxy-2-cyclohexene-Δ1, α-acetonitrile for menisdaurin were decided based on combined studies of difference NOE spectra and Dreiding model inspection.View full abstractDownload PDF (711K) -
Takahiro TANASE, Akito NAGATSU, Nobutoshi MURAKAMI, Shin-ichi NAGAI, T ...1994 Volume 42 Issue 11 Pages 2256-2262
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNew bufotoxin homologues (3) with various lengths of alkyl chain including longer ones than a suberoyl group at C-3 of the steroid nucleus were prepared from proscillaridin (1) via its genuine aglycone, scillarenin (2), in excellent yield. In the course of preparation, we established conditions for efficient enzymatic glycolysis of 1 to give 2 quantitatively. The pharmacological activities of the resulting bufotoxin homologues (3) were evaluated by measurement of the effect on smooth muscle using the mesenteric artery from spontaneously hypertensive rats, inhibitory effect on Na+, K+-adenosine triphosphatase (ATPase) prepared from dog kidney, and positive inotropic effect (PIE) on isolated guinea-pig papillary muscle preparations. The bufotoxin homologues (3) showed only slight contraction of vascular muscle followed by a small relaxation, in addition to the high Na+, K+-ATPase inhibitory activity and PIE comparable to those of clinically used ouabain, digoxin, and digitoxin. Those bufotoxin homologues (3) may be useful as cardiac agents with a minimal vascular contractile effect.View full abstractDownload PDF (938K) -
Tohru SAITO, Yayoi ASAHI, Satoshi NAKAJIMA, Tozo FUJII1994 Volume 42 Issue 11 Pages 2263-2268
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDiazotization of 5-amino-N'-methoxy-1-methylimidazole-4-carboxamidine (4a) with NaNO2 in 1N aqueous HCl was found to give the 1-methoxy-2-azaadenine derivative 8a·HI, which produced 5-azido-1-methylimidazole-4-carbonitrile (5a) on treatment with aqueous Na2CO3. The ribosyl analogue 5b, obtained from the riboside 4b by similar diazotization, was utilized for the synthesis of 5-azido-1-β-D-ribofuranosylimidazole-4-carboxamide (9b), a novel AICA riboside analogue. On heating in HCONMe2 at 70°C for 10min, 8a·HI yielded the 1-N-oxide 7a. Several reactions to transform the functional groups in 5a were also investigated.View full abstractDownload PDF (962K) -
Akito NAGATSU, Tadashi TAKAHASHI, Miki ISOMURA, Shin-ichi NAGAI, Taise ...1994 Volume 42 Issue 11 Pages 2269-2275
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS7-O-(4-Substituted benzyl)monensins (3a-g) were synthesized from monensin (1), and their lipophilicity, antibacterial activity, and Na+ ion permeability were examined. 7-O-(4-Ethylbenzyl)monensin (3a) showed the largest Na+ ion permeability, but 3c, f, g showed smaller Na+ ion permeability than 7-O-benzylmonensin (2) in spite of higher lipophilicity. An X-ray study of the sodium salt of 3e revealed that the benzyl group was located over the position between the D and E rings, and that the ethyl substituent on the benzyl group was close to the C(28) methyl group on the E ring.View full abstractDownload PDF (979K) -
Nobuhiko IWASAKI, Jun SAKAGUCHI, Tetsuo OHASHI, Eiji TAKAHARA, Nobuo O ...1994 Volume 42 Issue 11 Pages 2276-2284
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple method of transforming classical antihistaminics into nonsedative antiallergic agents with strong effects in rat models is described. Various [4-(diphenylmethoxy)piperidino]- (series A), [4-(diphenylmethyl)piperazinyl]- (series B) and [4-(diphenylmethylene)piperidino]alkanoic acid derivatives (series C) were synthesized and examined for antiallergic activities and effects on the central nervous system (CNS), in comparison with the corresponding N-methyl derivatives (1a-c). N-Alkylcarboxylic acids (5a-c) showed stronger ingibitory effects on compound 48/80-induced lethality in rats than the corresponding N-methyl derivatives (1a-c). In particular, N-alkylcarboxylic acids (5a) in series A exhibited approximately 100-fold stronger inhibitory effects than 1a, and were the least effective in prolonging the sleeping time on hexobarbital-induced anesthesia in mice in all series. As a result of chemical modification in series A, it was found that introduction of a methyl group at the para-position on one benzene ring in the (diphenylmethoxy)piperidine system effectively reduced CNS side-effects without reducing antiallergic activityl. (+)-3-[4-[(4-Methylphenyl)phenylmethoxy]piperidino]propionic acid ((+)-5l), an optically active isomer of 5l, exhibited a stronger antiallergic effect (ED50=0.17mg/kg, p.o.) than ketotifen and terfenadine in the 48h homologous passive cutaneous anaphylaxis (PCA) test, and moreover exhibited no CNS side-effects, such as prolongation of the sleeping time on hexobarbital-induced anesthesia, at an oral dose of 30mg/kg. Compound (+)-5l was thus proved to be a promising candidate as a nonsedative antiallergic agent.View full abstractDownload PDF (1013K) -
Nobuhiko IWASAKI, Jun SAKAGUCHI, Tetsuo OHASHI, Masahiro YAMAZAKI, Nob ...1994 Volume 42 Issue 11 Pages 2285-2290
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple method of transforming clalssical tricyclic antihistaminics into nonsedative antiallergic agents with equal potency in rats and guinea-pigs is described. A series of [4-(5H-dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]alkanoic acid derivatives (6a) and related compounds (6b-f) were synthesized and examined for antiallergic and antihistaminic activities and effects on the central nervous system (CNS) in comparison with the corresponding N-methyl derivatives (2a-f). N-Alkylcarboxylic acids (6a-f) showed stronger inhibitory effects on 48h homologous passive cutaneous anaphylaxis (PCA) in rats than 2a-f, and also were less effective in prolongation of the sleeping time on hexobarbital-induced anesthesia in mice in comparison with 2a-f. As a result of further modification, it was found that introduction of an oxygen atom into the central ring of the tricyclic system in amphoteric compounds enhanced their antiallergic and antihistaminic activities. 3-[4-(6H-Dibenz[b, e]oxepin-11-ylidene)piperidino]propionic acid (6c) exhibited strong inhibitory effects on 48h homologous PCA in rats (ED50=0.067mg/kg, p.o.) and on histamine-induced bronchoconstriction in anesthetized guinea-pigs (ED50=0.0085mg/kg, p.o.), and thus is a promising candidate as an antiallergic agent.View full abstractDownload PDF (883K) -
Tetsuo NAGANO, Kumi ARAKANE, Akemi RYU, Takuji MASUNAGA, Kouichi SHINM ...1994 Volume 42 Issue 11 Pages 2291-2294
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSinglet oxygen generation from laser-excited C60 was measured directly by using a sensitive near-infrared emission spectrometer to monitor the O2(1Δg)→O2(3Σg-) transition at 1268nm. The emission intensity was proportional to both the laser power and the concentration of C60. When nitrogen gas was bubbled into the C60 solution, the spectrum disappeared. Dose-dependent quenching of singlet oxygen by β-carotene was observed by monitoring the 1268nm emission. Based on the quenching, the rate constant of the reaction of singlet oxygen with β-carotene was determined to be 1.5-2.3×1010M-1s-1, which is consistent with the reported value (1.5-2.5×1010M-1s-1). A comparison of the singlet oxygen-producing ability of C60 as a photosensitizer with those of rose bengal. eosin and methylene blue, revealed C60 to have considerably higher efficiency.View full abstractDownload PDF (632K) -
Eiji HIMENO, Tsuneatsu NAGAO, Junko NONDA, Hikaru OKABE, Nobuto IRINO, ...1994 Volume 42 Issue 11 Pages 2295-2300
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe bitter constituents in the root of Cayaponia tayuya (VELL.) COGN. were investigated, and 24 29-norcucurbitacin glucosides, named cayaponosides were isolated. Among them, the structures of cayaponosides A, A3, A4, A6, B, B2, B3, B4, C, C2, C5a, D and D1 were determined based mainly on spectral analyses. They are all glucosides of 29-nor-1, 2, 3, 4, 5, 10-hexadehydrocucurbitacins, different only in side chain structure.View full abstractDownload PDF (828K) -
Eiji HIMENO, Tsuneatsu NAGAO, Junko HONDA, Hikaru OKABE, Nobuto IRINO, ...1994 Volume 42 Issue 11 Pages 2301-2304
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe bitter constituents in the root of Cayaponia tayuya (VELL.) COGN. were investigated, and 24 29-norcucurbitacin glucosides, named cayaponosides, were isolated. Among the 24 29-norcucurbitacin glucosides, named cayaponosides, isolated from the root of Cayaponia tayuya (VELL.) COGN., structures of cayaponosides A1, B6a, B6b, C3 D3a and C3b were determined based mainly on spectral analyses. They are all 3-O-glucosides of 29-nor-2, 11-dioxocucurbita-3, 5-diene, only different in side chain structure.View full abstractDownload PDF (510K) -
Yukinobu IKEYA, Ko SUGAMA, Masao MARUNO1994 Volume 42 Issue 11 Pages 2305-2308
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new xanthone C-glycoside, polygalaxanthone III (1), and a new acylated sugar, tenuifoliside E (2) were isolated from the roots of Polygala tenuifolia. Their structures were characterized as 4-C-[β-D-apiofuranosyl-(1→6)-β-D-glycopyranosyl]-1, 3, 6-trihydroxy-7-methoxyxanthone (1) β-D-(1-O-acetyl-3-O-feruloyl-6-O-sinapoly)-fructofuranosyl-α-D-(2, 4, 6-O-triacetyl)glucopyranoside (2), respectively, on the basis of chemical and spectral evidence including two dimensional nuclear magnetic resonance (2D-NMR) studies.View full abstractDownload PDF (623K) -
Zhonghua JIA, Kazuo KOIKE, Tamotsu NIKAIDO, Taichi OHMOTO, Muyun NI1994 Volume 42 Issue 11 Pages 2309-2314
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo novel triterpenoid saponins, ardisicrenoside C(1)[3β-O-{α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-[β-D-glucopyranosyl-(1→2)]-α-L-arabinopyranosyl}-16α, 28-dihidroxy-olean-12-en-30-oic acid 30-O-β-D-glucopyranosyl ester] and ardisicrenoside D (2) [3β-O-{β-D-xylopyranosyl-(1→2)-β-D-glucopyranoxyl-(1→4)-[β-D-glucopyranosyl-(1→2)]-α-L-arabinopyranosyl}-16α, 28-dihydroxy-olean-12-en-30-oic acid 30-O-β-D-glucopyranosyl ester] were isolated from the roots of Ardisia crenata. Structure assignments are based on spectroscopic data including 2D-NMR (correlation spectroscopy (COSY), homonuclear Hartmann-Hahn spectroscopy (HOHAHA), heteronuclear correlated spectroscopy (HETCOR), heteronuclear multiple bond correlation (HMBC) and rotating frame NOE spectroscopy (ROESY)) experiments and some chemical reactions. In addition, the isolated saponins along with their prosapogenins and sapogenins have been evaluated for their inhibitory activity on cAMP phosphodiesterase as a primary screening test for new medicinal compounds.View full abstractDownload PDF (849K) -
Tatsuya SUZUKI, Kazuichi WATANABE, Suehiro KIKKAWA, Hiroaki NAKAGAMI1994 Volume 42 Issue 11 Pages 2315-2319
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSGranulation was carried out using binary mixtures of microcrystalline cellulose (MCC) and cornstarch (CS); water was used as granulating liquid. The effect of crystallinity of MCC on granulation was examined using MCC pulverized by a jet mill (J-MCC) and a vibrational rod mill (R-MCC). Crystallinity of J-MCC was nearly equal to that of intact MCC (I-MCC), but that of R-MCC was remarkably low due to the mechanochemical effect. The growth rate of granules with R-MCC was greater than those with I-MCC and J-MCC; the latter two had a grnule having a core (MCC and CS) around which CS was layered. R-MCC provided granules in which CS and abraded MCC were homogeneously mixed. In addition, R-MCC remarkably decreased the difference in drug content among the size fractions of granules compared with I-MCC. These results suggest that the decrease in crystallinity of MCC may increase the tendency of its abrasion by shear force of impeller, because of an increase of the fragile amorphous region swollen by added water; this, in turn, results in a difference in the growth mechanism and in a greater growth rate.View full abstractDownload PDF (1250K) -
Kaori IKEDA, Izumi SAITOH, Takayoshi OGUMA, Yasushi TAKAGISHI1994 Volume 42 Issue 11 Pages 2320-2326
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHydrophobically-modified hydroxypropyl methylcellulose (HM-HPMC), possessing long-chain alkyl groups, is a new thickening agent for gel preparations. The solubility of indomethacin (IM) in supersaturated solutions increased with HM-HPMC concentration, but HM-HPMC did not solubilize IM crystals. This is not due to the suppression of the transformation of IM crystals from α to γ. HM-HPMC would thus appear to suppress the crystallization of IM from supersaturated solutions. Nucleation and crystal growth rates in a supersaturated solution of IM in the absence and presence of HM-HPMC were determined by measuring light transmittance under cooling. It became clear that HM-HPMC caused a slight stimulation of nucleation and a strong suppression of crystal growth. This activity of HM-HPMC was derived from the original polymer, HPMC, but was greater than that of HPMC itself. The suppression of crystal growth by HM-HPMC may thus be due to the hydrophobic interaction between hydrophobic regions, particularly long-chain alkyl groups, and IM molecules.View full abstractDownload PDF (1376K) -
Hiroshi YUASA, Daisuke ASAHI, Yuki TAKASHIMA, Yoshio KANAYA, Kazuya SH ...1994 Volume 42 Issue 11 Pages 2327-2331
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCalcium silicate (Florite[○!R] RE, FLR), a fine porous powder, was recently approved as a medicinal additive. In this study we sought to make a solid preparation by adsorbing an oily medicine to FLR; tocopheryl nicotinate (TN) was used as the oily medicine.TN adsorbed to FLR powder (TN-PO) was prepared by adsorbing TN ethanol solution to FLR and granulating with hydroxypropylcellulose (HPC) in order to improve the flowability. The results were as follows.FLR showed an excellent liquid holding ability compared with other excipients, and this was attributed to the high capillarity of the pores. In the absorbing process, FLR particles were granulated with TN overflowing from the pores or adhering to the particle surface. The angle of repose was decreased with increasing TN content, which was attributed to the process of granulation, and the angle of repose of the granules with a binder (TN-GR) was below 40°at any TN content.These results show that FLR is an useful additive for the solid preparation of an oily medicine.View full abstractDownload PDF (1032K) -
Kazufumi SHIOTANI, Keiko UEHATA, Tetsumi IRIE, Fumitoshi HIRAYAMA, Kan ...1994 Volume 42 Issue 11 Pages 2332-2337
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe inclusion mode of β-cyclodextrin sulfate (β-CyD-sul) with a cationic drug, chlorpromazine, was investigated, and the effect of β-CyD-sul on the hemolytic activity of chlorpromazine was compared with that of parent β-CyD. The interaction of β-CyD-sul with chlorpromazine was weaker than that of parent β-CyD, probably because of the steric or electrostatic repulsion between anionic sulfate groups and hydrophobic phenothiazine moiety. Spectroscopic studies, including pH- and salt-effects, as well as thermodynamic parameters, suggested that both electrostatic and hydrophobic interactions are operative in the inclusion complexation of β-CyD-sul with chlorpromazine. The inhibiting effect of parent β-CyD on the chlorpromazine-induced hemolysis of rabbit erythrocytes was accounted for by the decreased fraction of free drug through the complexation. In the case of β-CyD-sul, the hemolysis and binding of the drug to the erythrocyte membrane was higher than those estimated from the fraction of free drug, probably due to the increased hydrophobicity of the drug through the complexation. However, the chlorpromazine-induced shape change of the erythrocytes was significantly suppressed by β-CyD-sul, and its inhibiting effect was greater than that of β-CyD, because of the counterbalance of the opposite effects, i.e., internalization and externalization induced by chlorpromazine and β-CyD-sul, respectively.View full abstractDownload PDF (1410K) -
Satoru WATANO, Hiroko TAKAYA, Ikuko WADA, Kei MIYANAMI1994 Volume 42 Issue 11 Pages 2338-2341
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple model, which can be used to analyze data of the controlled release of a water-soluble drug from spherical particles coated with an aqueous-based system of acrylate methacrylate by a tumbling fluidized bed process, is presented. This model predicts that the fractional release of a drug is related to the exponential of release time. Drug release data of several samples prepared by various levels of operational moisture content were studied by the analytical equations, and the effect of operational moisture content on fil thickness and permeability of a drug were investigated. It was found that the experimental results were very well represented by the analytical equations, and the mechanism of an aqueous coating was elucidated.View full abstractDownload PDF (614K) -
Setsuo SAITO, Satoshi NAGASE, Koki ICHINOSE1994 Volume 42 Issue 11 Pages 2342-2345
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the rhizome of Anemarrhena asphodeloides BUNGE (Liliaceae), four new steroidal saponins named anemarrhenasaponins I-IV (1-4) were isolated, together with known saponins, timosaponin A-III (5), marcogenin diglycoside (6) and timosaponin B-II (7) and a xanthone C-glycoside, mangiferin. These saponins are coprostane type steroidal glycosides. Their structures were established on the basis of spectroscopic and chemical evidence.View full abstractDownload PDF (673K) -
Masaji INOUE, Hideo UTSUMI, Yutaka KIRINO1994 Volume 42 Issue 11 Pages 2346-2348
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe ESR properties of three types of paramagnetic material, active charcoal, fusinite and a stable nitroxide radical 4-oxo-2, 2, 6, 6-tetramethylpiperidine-1-oxyl (TEMPONE), were examined in order to evaluate their suitability as probes to measure dissolved intra- and extra-cellular oxygen. Although, with changes in oxygen concentration, a greater change in the linewidth of ESR signals was observed with fusinite or active charcoal, it took a long time (15min for active charcoal and more than 6h for fusinite) for equilibrium to be achieved. On the other hand, equilibrium was reached very rapidly in the case of the TEMPONE spectra although the sensitivity to changes in oxygen concentration was only moderate. Furthermore, since lipid bilayers are permeable to TEMPONE, this compound can be used to measure intracellular oxygen concentration when employed in combination with membrane-impermeable spin-broadening reagents which act on ESR signals arising from extracellular probes. A perdeuterated derivative of TEMPONE is useful in that it gives a greater signal-to-noise ratio and greater sensitivity to changes in oxygen concentration. In conclusion, active charcoal is suitable as a probe for extracellular oxygen in a system where changes are slow, while nitroxide is a versatile probe for measuring rapidly changing intra- and extra-cellular oxygen concentrations.View full abstractDownload PDF (543K) -
Yoji TACHIBANA1994 Volume 42 Issue 11 Pages 2349-2351
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn alternative synthesis of 24, 24-dihomo-1α, 25-dihydroxyvitamin D3 was achieved starting from stigmasterol or cholenic acid.View full abstractDownload PDF (546K) -
Xue-Long SUN, Naoki HAGA, Haruo OGURA, Hiroaki TAKAYANAGI1994 Volume 42 Issue 11 Pages 2352-2356
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSα-N-Glycosides of 3-deoxy-D-glycero-D-galacto-2-nonulosonic acid (KDN) having a nucleobase, such as uracil, thymine, 5-fluorouracil or cytosine, were synthesized. Their acetone-sensitized photocycloaddition to 2, 3-dimethyl-2-butene under near-UV irradiation gave a pair of diastereomers having a cyclobutane ring. The absolute configuration of the bridgehead carbon atoms in the products was identified by measurement of specific rotation as well as 1H-NMR spectral analysis.View full abstractDownload PDF (803K) -
Yuji KURIHARA, Mikiko SODEOKA, Masakatsu SHIBASAKI1994 Volume 42 Issue 11 Pages 2357-2359
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAsymmetric Heck-type reaction of 1-cyclohexenylphenyliodonium salt with 2, 3-dihydrofuran was investigated for the first time. The optically active (up to 78% ee) coupling product was obtained in low to moderate yield. The potential and associated problems of this asymmetric reaction are discussed.View full abstractDownload PDF (539K) -
Shunsaku OHTA, Yasunari HINATA, Ikuo KAWASAKI, Masayuki YAMASHITA1994 Volume 42 Issue 11 Pages 2360-2362
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Methylamino-3-(1-piperidinylmethyl)-1, 4-naphthoquinone (7) was prepared via several steps from 2-methyl-1, 4-naphthoquinone (vitamin K3, 3). The quinone (7) was photochemically oxidized to 2-methylamino-3-(1-piperidinylcarbonyl)-1, 4-naphthoquinone (8) and/or 2-alkoxycarbonyl-3-methylamino-1, 4-naphthoquinone (9), depending on the solvent used.View full abstractDownload PDF (458K) -
Mazaahir KIDWAI, Neena NEGI, S.D. GUPTA1994 Volume 42 Issue 11 Pages 2363-2364
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis and antifertility activity of 1, 5-diaryl-3-(3'-indolyl)formazans with a substituted aryl group (2-8) are described.View full abstractDownload PDF (380K) -
Ichiro YAMAWAKI, Scott W. BUKOVAC, Akihiko SUNAMI1994 Volume 42 Issue 11 Pages 2365-2369
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive metabolites of syn-3-ethyl-7-methyl-3, 7-diazabicyclo[3.3.1]non-9-yl 4-chlorobenzoate hydrochloride (YUTAC)(1) were prepared and examined for Na+ current blocking activity in guinea pig ventricular myocytes. These metabolites showed lower inhibitory activities than the parent compound or were inactive.View full abstractDownload PDF (741K) -
Eiji HIMENO, Tsuneatsu NAGAO, Junko HONDA, Hikaru OKABE, Nobuto IRINO, ...1994 Volume 42 Issue 11 Pages 2370-2372
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe bitter constituents in the root of Cayaponia tayuya (VELL.) COGN. were investigated. Among 24 29-norcucurbitacin glucosides, named cayaponosides, the structures of cayaponosides A5, B5, C4, C5b and D2 were determined based mainly on spectral analyses. They are all glucosides of 29-nor-1, 2, 3, 4, 5, 10-hexadehydrocucurbit-6-enes different only in side chain structure.View full abstractDownload PDF (475K) -
Zenei TAIRA, Yoko SAKIYA, Hiroshi TERADA1994 Volume 42 Issue 11 Pages 2373-2375
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe introduced a new binding equation to express drug-protein interaction and applied it to a spectrophotometric titration method. We also discussed its relation to other equations for spectrophotometric titration.View full abstractDownload PDF (484K) -
Saeid RAZEE, Atsushi TAMURA, Tsutomu MASUJIMA1994 Volume 42 Issue 11 Pages 2376-2378
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA powerful permanent magnet which can perform a uniform 10 KG magnetic field was directed perpendicular to the applied electric field in a Capillary Electrophoresis (CE) system. It was found that the current passing through the capillary was decreased due to application of a magnetic field. The electroosmotic flow and electrophoretic mobility of ionic solutes were also observed to be affected and slowed down by this new external field.View full abstractDownload PDF (435K) -
Atsushi TAMURA, Keiko TAMURA, Chitoshi ENOKI, Tsutomu MASUJIMA1994 Volume 42 Issue 11 Pages 2379-2381
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDynamic aspects of the solvent exchange process in stepwise elution liquid chromatography were investigated using a chromato-videoscope system. The migration velocity of a solute's band changed rapidly at the same flow rate when a second eluent overtook the band. The changing time of the migration velocity is termed an inflective time. Since a plot of the relationship between inflective time and the migration distance up to the overtaking point of each solute band showed a straight line, the solvent front of the second eluent seemed to be sharp during passage through the column. In the case where the content of organic solvent in the mobile phase was changed from higher to lower, there was a delay of the inflective time even though the solvent front of the second eluent seemed to be kept sharp.View full abstractDownload PDF (924K) -
Makoto OTSUKA, Yoshihisa MATSUDA1994 Volume 42 Issue 11 Pages 2382-2384
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe physicochemical properties of phenytoin (PHT)-bile salt complexed comprised of sodium dehydrocholate (DHCNa), sodium deoxycholate (DCNa) or sodium cholate (CNa) prepared by co-grinding were investigated by X-ray diffraction analysis, DSC and dissolution kinetics. All X-ray diffraction peak intensities of the co-ground PHT-bile salt [1 mol : 1 mol] mixtures were decreased by grinding for 3 h, and showed a halo pattern of a noncrystalline solid. The solubility of ground products with DCNa, DHCNa and CNa were 212, 56, 68 times higher, respectively, than those of physical mixtures.View full abstractDownload PDF (451K) -
Yuriko YAMAGATA, Masato KATO, Satoshi FUJII1994 Volume 42 Issue 11 Pages 2385-2387
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSX-Ray crystallographic study shows that 3-methyladenine, the product of methylation of DNA by carcinogenic and/or mutagenic methylating agents, stacks strongly with the indole ring, the aromatic side group of tryptopha.View full abstractDownload PDF (472K) -
Shoko YOKOYAMA, Shin-ya KASUGA, Etsuko ISHIHARA, Tadao FUJIE1994 Volume 42 Issue 11 Pages 2388-2390
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe release of nicotinamide (NAA) from the thermo-sensitive octadecanoic acid complex (C18-NAA) coated with cellulose acetate phthalate was investigated in pH 1.2 and 6.8 aqueous media. No release of NAA from the enteric-coated C18-NAA was found at pH 1.2, while NAA was released at pH 6.8 in response to the temperature. It was confirmed that the thermo-sensitivity of C18-NAA is not affected by the enteric-coating treatment.View full abstractDownload PDF (444K) -
Jun-ichi ANZAI, Bei GUO, Tetsuo OSA1994 Volume 42 Issue 11 Pages 2391-2393
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdsorption of serum albumin on the surface of platinum and gold electrodes was highly accelerated by the application of a constant potential to the electrodes. The accelerated adsorption was significant at the electrode potential of 0.5-1.0 V vs. Ag/AgCl, even in the diluted sokution of albumin (0.01%).View full abstractDownload PDF (464K) -
Motomasa KOBAYASHI, Michio KUROSU, Weiqi WANG, Isao KITAGAWA1994 Volume 42 Issue 11 Pages 2394-2396
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn asymmetric synthesis of a cyclic depsipeptide arenastatin A (1), which was isolated from the marine sponge Dysidea arenaria and exhibited extremely potent cytotoxicity with IC50 5 pg/ml for KB cells, has been accomplished.View full abstractDownload PDF (465K) -
Toshihiro HASHIMOTO, Shigenobu TAHARA, Shigeru TAKAOKA, Motoo TORI, Yo ...1994 Volume 42 Issue 11 Pages 2397-2399
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree novel azaphilone derivatives, daldinins A∼C, have been isolated from the fungus (Ascomycetes) Daldinia concentrica. Their structures including the absolute configuration have been established by a combination of high resolution NMR and CD spectra, X-ray crystallographic analysis, and chemical degradation.View full abstractDownload PDF (439K) -
Mugio NISHIZAWA, Dulce M. GARCIA, Yohko NOGUCHI, Kumiko KOMATSU, Susum ...1994 Volume 42 Issue 11 Pages 2400-2402
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA variety of 1, 1'-disaccharides have been prepared by TMS triflate induced coupling of 1-hydroxy sugars in reasonable yield.View full abstractDownload PDF (378K) -
Tadashi NAKATA, Toshiya KOMATSU, Kazuo NAGASAWA1994 Volume 42 Issue 11 Pages 2403-2405
Published: November 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe C24-C32 segment 4 of swinholide A (1) was stereoselectively synthesized starting from (S)-methyl 3-hydroxybutyrate, and the convergent synthesis of the C11-C32 segment 5 was accomplished via stereoselective aldol condensation of 3 and 4View full abstractDownload PDF (450K)
- |<
- <
- 1
- >
- >|