All issues
Volume 42, Issue 10
Displaying 1-50 of 50 articles from this issue
- |<
- <
- 1
- >
- >|
-
Kaoru NAKAJIMA, Yoshiko TAKEUCHI, Heihachiro TAGUCHI, Koji HAYASHI, Mi ...1994 Volume 42 Issue 10 Pages 1977-1983
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo evaluate the profile of the crude drug components transferred into the decoction, decoctions of about 30 kampo prescriptions, comprising 13 quantitatively assayable crude drugs, were prepared; the quantities (mg/daily dose) and ratios (%) of these components transferred from the drug into the decoctions were determined by HPLC. Then, a chromatographic substitute for the hydrophobic parameter was determined in various crude drug components, and its relationship with the quantities and ratios transferred was examined. The transfer of stable crude drug components into the decoctions was found to be regulated by the hydrophobicity of the components, which is related to their transfer ratio, rather than the amount transferred. In addition, the transfer ratio and the value of the hydrophobic parameter did not exhibit a simple linear relationship.View full abstractDownload PDF (1048K) -
Kaoru NAKAJIMA, Yoshiko TAKEUCHI, Heihachiro TAGUCHI, Koji HAYASHI, Mi ...1994 Volume 42 Issue 10 Pages 1984-1990
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAssuming that the general partition of crude drug components between oil and water can be replaced by that between the crude drug residue and the decoction solution, the following equation can be derived linking the transfer ratio (rT) of the components and the capacity factor (k') on reverse-phase HPLC : log (100/rT-1)=alogk'+b In this equation, a and b are constants when the method of preparation of decoctions and the HPLC conditions are kept constant. In order to verify this relationship, some model decoctions were prepared using small size preparations (0.5-1.0mm) of crude drugs, and the correlation between log (100/rT-1) and logk' of the components was examined. Since the correlation coefficient of the equation was calculated to be 0.9 or higher in these model decoctions, the assumption was useful for investigating this relationship between the transfer ratio and the hydrophobic or related parameters. Thus, the transfer ratios of all components in a decoction could be evaluated as a single continuous line rather than an aggregation of single points for the transfer ratios, and most of the highly hydrophobic components could be transferred to the decoctions without dissolution in water.View full abstractDownload PDF (1007K) -
Kaoru NAKAJIMA, Tomoko HORIUCHI, Heihachiro TAGUCHI, Koji HAYASHI, Min ...1994 Volume 42 Issue 10 Pages 1991-1997
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUsing a model decoction of Schisandrae Fructus, the effect of the volume ratio of the crude drug vs. extractant was studied. On changing the alteration ratio of the volume ratio according to a two-fold geometric series, the transfer ratios of each lignan into model decoctions generally decreased with increasing alteration ratio. However, the transfer ratios of the high hydrophobic lignans increased partially with the high alteration ratios. As a result, a comprehensive equation involving to the transfer ratios of all the low molecular weight organic components of Schisandrae Fructus in the model decoctions was derived from the analyses of the variant alteration ratios. This equation might be applicable to other crude drug components in kampo decoctions.View full abstractDownload PDF (946K) -
Md. RAFIQUZZAMAN, Kyoko YOSHINAGA, Keiko KOMAGOE, Keietsu TAMAGAKE1994 Volume 42 Issue 10 Pages 1998-2001
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe rate of peroxidation of methyllinoleate in methanol was measured by monitoring oxygen consumption in the presence and absence of ferric chloride and L-histidine. Histidine enhanced the ferric-inducing peroxidation of methyllinoleate in a non-aqueous system, which was likewise reported in an aqueous solvent. The rate depended on the ratio of the relative concentration of iron to histidine. The ratio of 1 : 6 in a molar concentration gave the maximum rate. Spectroscopic observation for the first time strongly suggested the formation of two ferric-histidine chelates of the composition of 1 : 1 and 1 : 2 in methanol. The apparent formation constants of the 1 : 1 and 1 : 2 complexes, logβ1 and logβ2, were calculated to be 4.6 and 8.3, respectively. Correlation of the peroxidation rates to the spectroscopically observed species led to the conclusion that the 1 : 2 chelate was responsible for the maximum peroxidation rate of methyllinoleate under the conditions of this investigation.View full abstractDownload PDF (635K) -
Xiaolin SUN, Min XIN, Xiaojin WANG, Xueping NIU1994 Volume 42 Issue 10 Pages 2002-2004
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe molecular and electronic structures of some fasciolicidal o-hydroxybenzenesulfonanilides (HBSA) have been studied using X-ray diffraction and semiempirical MO calculation. In these compounds, the phenolic hydroxyl forms a strong intramolecular hydrogen bond with an adjacent sulfonyl oxygen atom and the strength of the d-p dative S←N bond, which may control the electron delocalization throughout the entire molecule, is affected by substituents on the phenyl rings on both sides. Owing to the poor delocalization, the contribution of the keto-form of the resonance structure is larger for some phenolate anions of HBSA in solution, and this may be a key factor determining the potency of fasciolicidal activity of HBSA.View full abstractDownload PDF (530K) -
Takashi YOSHIDA, Osamu NAMBA, Kenji KUROKAWA, Yoshiaki AMAKURA, Yan-Ze ...1994 Volume 42 Issue 10 Pages 2005-2010
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new ellagitannin dimers, euphorbins G (20) and H (21), together with 12 known polyphenols, were isolated from the leaves of Euphorbia prostrata (E. chamaesyce). Their structures, having 1C4 and 4C1 glucopyranose cores in each molecule, were established by spectroscopic and chemical methods. These new dimers, and 13 known hydrolyzable tannins, among which six are the same as those from E.prostrata, were also isolated from E.makinoi.View full abstractDownload PDF (782K) -
Naoki NODA, Kyoko TSUJI, Kazumoto MIYAHARA, Chon-Ren YANG1994 Volume 42 Issue 10 Pages 2011-2016
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTen resin glycosides (jalapins) named tuguajalapins I-X were isolated from the root of Merremia hungaiensis. Their structures have been determined on the bases of chemical and spectral data. Unlike the jalapins so far reported, all of their acyl groups consist of two or three long-chain fatty acids, that is, palmitic, stearic and/or arachidic acids.View full abstractDownload PDF (783K) -
Akira MIYASHITA, Hideaki MATSUDA, Yumiko SUZUKI, Ken-ichi IWAMOTO, Tak ...1994 Volume 42 Issue 10 Pages 2017-2022
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe ability of 1, 3-dimethylimidazolium iodide (1) to catalyze the aroylation of the chloroheteroarenes 4-8 with arenecarbaldehydes 3 as sources of the aroyl groups was examined in order to develop a preparative method of aroylheteroarenes. In the presence of 1, the treatment of the 4-chloroquinazolines (4 : 2-H, 5 : 2-Me, 6 : 2-Ph) with arenecarbaldehyde 3 in refluxing THF (tetrahydrofuran) or dioxane led to the 4-aroylquinazolines (9 : 2-H, 10 : 2-Me, 11 : 2-Ph) in excellent yields, as had been found with 1, 3-dimethylbenzimidazolium iodide (2). Similar reaction of the 4-chloro-1H-pyrazolo[3, 4-d]pyrimidines (7 : 1-Ph, 8 : 1-Me) with arenecarbaldehyde 3 yielded the corresponding 4-aroyl-1H-pyrazolo[3, 4-d]pyrimidines (12 : 1-Ph, 13 : 1-Me). Compound 1 seems to catalyze the aroylation of a wider range of arenecarbaldehydes 3 as compared with 2.View full abstractDownload PDF (788K) -
Kazuko YOSHIKAWA, Hitomi TANINAKA, Yukiko KAN, Shigenobu ARIHARA1994 Volume 42 Issue 10 Pages 2023-2027
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the fresh stem of Stephanotis lutchuensis var.japonica, we have isolated five new oleane glycosides named sitakisosides I-V (1-5). Their structures were determined on the basis of spectroscopic data and chemical evidence. Sitakisoside V showed the strongest antisweet activity among sitakisosides I-V.View full abstractDownload PDF (764K) -
Fumiko ABE, Tatsuo YAMAUCHI1994 Volume 42 Issue 10 Pages 2028-2031
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSteroidal constituents from the roots of Apocynum cannabinum L. were investigated. (20S)-, (20R)-18, 20-Epoxycymarin and (20S)-18, 20-epoxyapocannoside were isolated along with cannogenin, strophanthidin and cannogenol glycosides, including D-cymaroside, D-oleandroside, D-digitoxoside and D-digitaloside, and their glucosyl, cellobiosyl or gentiobiosyl glycosides. Two pregnanes, neridienone A and 6, 7-didehydrocortexone, were obtained, accompanied with cardenolides.View full abstractDownload PDF (546K) -
Takao SAKAMOTO, Akito YASUHARA, Yoshinori KONDO, Hiroshi YAMANAKA1994 Volume 42 Issue 10 Pages 2032-2035
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPalladium-catalyzed reaction of aryl and heteroaryl iodides with ethoxy(trialkylstannyl)acetylenes gave the ethoxyethynylarenes and -heteroarenes, which were easily transformed by hydration reaction into ethyl areneacetates and heteroareneacetates.View full abstractDownload PDF (707K) -
Li-Jiau HUANG, Sheng-Chu KUO, Jih-Pyang WANG, Katsumi ISHII, Hideo NAK ...1994 Volume 42 Issue 10 Pages 2036-2041
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 2-substituted 3, 4-dimethylfuro[2, 3-c]pyrazole-5-carboxamides and related compounds have been synthesized and their antiallergic activities were evaluated. Most derivatives with a lower alkyl group at position 2 were orally active. Among them, N-ethyl-2, 3, 4-trimethylfuro[2, 3-c]pyrazole-5-carboxamide (III3), 2-ethyl-N-methyl-3, 4-dimethylfuro[2, 3-c]pyrazole-5-carboxamide (III14), 2-isopropyl-N-methyl-3, 4-dimethylfuro[2, 3-c]pyrazole-5-carboxamide (III27), 5-(4, 5-dihydro-5-oxo-1, 3, 4-oxadiazol-2-yl)-2, 3, 4-trimethylfuro[2, 3-c]pyrazole (IV1) and 5-(4, 5-dihydro-5-oxo-1, 3, 4-oxadiazol-2-yl)-2-isopropyl-3, 4-dimethylfuro[2, 3-c]pyrazole (IV3) showed promising antial-lergic effects. The structure-activity relation of these 3, 4-dimethylfuro[2, 3-c]pyrazole derivatives was examined. An amide or 5-oxo-1, 3, 4-oxadiazole substituent at position 5 was favorable, while introduction of a carboxylic acid or acrylic acid moiety was unfavorable. However, none of these compounds exerted a significant inhibitory effect on mast cell degranulation. Compound III27 and IV3 showed potent anti-allergic activity. We found that they also suppressed histamine-, serotonin-, bradykinin- and substance P-induced ear edema in mice. In compound 48/80-pretreated mice, the preformed mediators in mast cells in the ear were greatly reduced. Under this condition, the bradykinin- and substance P-induced ear edema was suppressed by compound III27 and IV3 to a significantly greater extent than by diphenhydramine combined with methylsergide. These results indicated that the antiallergic effect of 3, 4-dimethylfuro[2, 3-c]pyrazole derivatives probably involves protection of the vasculature against the effects of challenge by several mediators.View full abstractDownload PDF (972K) -
Sachio OHNO, Masayuki KOUMORI, Yuko ADACHI(nee EBIHARA), Kiyoshi MIZUK ...1994 Volume 42 Issue 10 Pages 2042-2048
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of new (5R, 8S, 10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were evaluated in conscious spontaneously hypertensive rats and in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra, respectively. (5R, 8S, 10R)-6-Methyl-8-ergolinemethanols, prepared from the corresponding ergolinecarboxylates, were converted to the tosylates, which were treated with various five-membered heterocycles containing nitrogen atoms to afford the new ergolines. (5R, 8S, 10R)-8-(1-Imidazolylmethyl)-6-methylergoline (5a, BAM-2101) and (5R, 8S, 10R)-2-bromo-6-methyl-8-(1, 2, 4-triazol-1-ylmethyl)ergoline (7c, BAM-2202) exhibited potent antihypertensive activities. The maximum falls of systolic blood pressure after oral administration of 5a and 7c at 3mg/kg were 95 and 132 mmHg, respectively, while those of cianergoline, bromocriptine mesylate, hydralazine, and nifedipine at the same dose were 40, 37, 47, and 49 mmHg, respectively. The durations of significant antihypertensive effects of these compounds except nifedipine were more than 7h. None of the ergolines exhibited potent dopaminergic activity. Structure-activity relationships are discussed.View full abstractDownload PDF (954K) -
Yozo TODO, Hiroyasu TAKAG, Fumihiko IINO, Yoshikazu FUKUOKA, Yasushi I ...1994 Volume 42 Issue 10 Pages 2049-2054
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe title compounds (1a-i) have been synthesized starting with ethyl 1-cyclopropyl-6, 7-difluoro-4-quinolone-3-carboxylate (2). The 7-cyclopropyl and 7-vinyl derivatives (1e and 1i) exhibited potent in vitro antibacterial activities against both gram-positive and gram-negative bacteria, being equipotent with ciprofloxacin (CPFX) except for the activity against Pseudomonas aeruginosa. The two compounds were significantly less toxic than CPFX in terms of convulsion-induction as determined by intracerebral administration to mice, but showed lower urinary recoveries on intravenous administration.View full abstractDownload PDF (870K) -
Yozo TODO, Jun NITTA, Mikako MIYAJIMA, Yoshikazu FUKUOKA, Yasushi IKED ...1994 Volume 42 Issue 10 Pages 2055-2062
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNovel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, comparable to that of ciprofloxacin, against gram-negative bacteria including P. aeruginosa. A good pharmacokinetic profile (serum and brain concentrations and urinary recovery) was obtained for the two cyclic compounds (3e and 3g), but that of the vinylic compounds (3m and 3o) was less favorable. Compound 3g was less toxic than 3e, ciprofloxacin, or ofloxacin in terms of acute toxicity and convulsion-induction.View full abstractDownload PDF (1142K) -
Yozo TODO, Jun NITTA, Mikako MIYAJIMA, Yoshikazu FUKUOKA, Yoshiko YAMA ...1994 Volume 42 Issue 10 Pages 2063-2070
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Oxo-1, 8-naphthyridine- and 4-oxoquinoline-3-carboxylic acids (2a, b and 3a-l) possessing a 1-amino-cyclopropyl group at the 7-position have been synthesized and evaluated for in vitro antibacterial activities. The three quinolones (3d, h, i) exhibited potent antibacterial activities against both gram-positive and gram-negative bacteria, which are comparable to those of ciprofloxacin (CPFX) and ofloxacin (OFLX). Among the three compounds, the best pharmacological and pharmacokinetic profile was obtained with 3i, an OFLX analogue, which was considerably less toxic than three reference quinolones (1, CPFX, and OFLX).View full abstractDownload PDF (1193K) -
Yoshinari SATOH, Teruaki MATSUO, Hajime SOGABE, Harunobu ITOH, Toshiji ...1994 Volume 42 Issue 10 Pages 2071-2083
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe prepared various novel tricyclic 1, 4-benzodiazepine derivatives as cholecystokinin (CCK) A antagonists, which were evaluated preliminarily for inhibition of <125>I-CCK-8 binding to rat pancreatic membranes in vitro and inhibiting effect on CCK-8-induced inhibition of charcoal meal gastric emptying in mice. On the basis of structure-activity relationship (SAR) studies, as well as the stability and availability of the starting materials of those compounds, (S)-N-[1-(2-fluorophenyl)-3, 4, 6, 7-tetrahydro-4-oxo-pyrrolo[3, 2, 1-jk][1, 4]benzodiazepin-3-yl]-1H-indole-2-carboxamide (9f, FK-480) was selected as a candidate compound for further evaluation. The absolute configuration of the precursor of FK-480, (3S)-amino-1, 4-benzodiazepine derivative ((S)-8a, R1=F) was determined by an X-ray crystallographic study of its ureido derivative with (S)-α-methylbenzyl isocyanate.FK-480 is now undergoing clinical studies for the treatment of chronic pancreatitis.View full abstractDownload PDF (1574K) -
Hidetsugu TSUBOUCHI, Koichi TSUJI, Koichi YASUMURA, Hiroshi ISHIKAWA1994 Volume 42 Issue 10 Pages 2084-2089
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 2-oxaisocephems with a thio-substituted methyl group at the 3-position and a 2-aminothiazol-4-yl moiety at the 7-position was synthesized via benzyl 3-acetyloxymethyl-7-azido-8-oxo-1-aza-4-oxabicyclo[4.2.0]oct-2-ene-2-carboxylate (2), derived from benzyl acetoacetate (1). The new 2-oxaisocephems were tested for antibacterial activities. Among them, the derivatives having a [2-(2-aminothiazol-4-yl)-2-(Z)-cyclopentyloxyimino]acetamido group at the 7-position characteristically showed potent activities against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus faecalis as compared with cefuzonam and cefmenoxime, which are third-generation cephalosporins.View full abstractDownload PDF (763K) -
Hiroshi SUSAKI, Kokichi SUZUKI, Masahiro IKEDA, Harutami YAMADA, Hiros ...1994 Volume 42 Issue 10 Pages 2090-2096
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSArgiine-vasopressin (AVP) derivatives modified at the glutamine side chain amide with carbohydrate via an alkylene spacer (1a-d) were synthesized from new glycosylated glutamine derivatives (3a-d) by solid-phase synthesis. Glycoconjugates of AVP modified at the C-terminal amide (2a-d) were also synthesized from vasopressionic acid. All of them exhibited antidiuretic activity.View full abstractDownload PDF (1205K) -
Hirokazu HASHIZUME, Hajime ITO, Tadanori MORIKAWA, Naoaki KANAYA, Haji ...1994 Volume 42 Issue 10 Pages 2097-2107
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSStructural analogs of 1233A, a microbial metabolite inhibiting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase, were designed and synthesized. The 2-oxetanone moiety was left intact. All analogs prepared were tested for inhibition of HMG-CoA synthase activity and sterol synthesis in mouse liver and for effect on serum triglyceride levels. Of these analogs, trans-4-[2-[3-(7-carboxy-2-naphthyl)phenyl]ethyl]-3-hydroxymethyl-2-oxetanone (4a) showed the highest inhibitory activity in vitro, and also had in vivo inhibitory activity without causing any increase in triglyceride level.View full abstractDownload PDF (1479K) -
Maria L. LOPEZ RODRIGUEZ, M. Jose MORCILLO, Fernando BENITO, Bellinda ...1994 Volume 42 Issue 10 Pages 2108-2112
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of (-)-(3S)-6-hydroxy-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid (3a) with isocyanates and isothiocyanates gave the (±)-β-carboline-hydantoin (4a-d) and -thiohydantoin systems (5a-d). The treatment of (-)-(1S, 3S)-6-hydroxy-1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid (3b) with isocyanates yielded the (±)-cis disatereomer of the β-carboline-hydantoin rings (4e-h). However, the reaction of 3b with isothiocyanates provided the corresponding trans isomer (5e-h). These results have been confirmed by 13C-NMR data and nuclear Overhauser effect (NOE) experiments. The new compounds were tested for in vitro binding affinity to the central-type benzodiazepine receptors.View full abstractDownload PDF (716K) -
Midori TAKASAKI, Takao KONOSHIMA, Mutsuo KOZUKA, Mitsumasa HARUNA, Kaz ...1994 Volume 42 Issue 10 Pages 2113-2116
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the juvenile leaves of Eucalyptus incrassata, a new euglobal having an acylphloroglucinol-sesquiterpene structure, euglobal-In-1 (1), has been isolated along with the known euglobal-III (2) and -V (3). The structure and stereochemistry of 1 were established by spectroscopic methods.View full abstractDownload PDF (526K) -
Masayoshi OHYAMA, Toshiyuki TANAKA, Munekazu IINUMA, Kiyoto GOTO1994 Volume 42 Issue 10 Pages 2117-2120
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo novel resveratrol trimers, named leachianols A (1) and B (2), were isolated from the roots of Sophora leachiana. Their structures were determined by spectroscopy using correlation spectroscopy involving long range coupling and unclear Overhauser effect experiments. The resveratrol trimers 1 and 2, which are formed by characteristics oligomerization via a pallidol (3), are the first naturally occurring oligostilbenes to be reported.View full abstractDownload PDF (617K) -
Kazumi DANJO, Koji KOZAKI, Hisakazu SUNADA, Akinobu OTSUKA1994 Volume 42 Issue 10 Pages 2121-2125
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTo improve the adhesiveness and cohesiveness of powders for granule formation, binding agents are generally used. In the wet granulation process, the binder solution plays an important role in controlling the mechanical properties of granules. In this study, the effects of the type and molecular weight of the binding agent and the effects of the concentration and viscosity of the binder solution on granule characteristics, i.e., average granule size (D50), granule strength (St) and granule compressibility, were investigated.Polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) of various molecular weights were used for the preparation of granules by the agitating-fluidized granulation method. In each polymer system, the average granule size (D50) and strength (St) increased with increasing concentration and viscosity of the binder solution and as the molecular weight of the binding agent was increased.The compressibility of granules was evaluated by means of the compressibility constant (K) of a modified version of Kawakita's equation and K decreased with increasing molecular weight. An approximately linear relationship was observed between the reciprocal of the compressibility constant (1/K) and granule strength (St). At the same granule strength, K values in the HPMC system were greater than those in the PVP system. The radial tensile strength (σ) of the tablet, obtained by the diametral compression test, increased with increasing concentrations and viscosity of binder solutions and was also affected by the molecular weight of the binding agent. These results indicate that σ is related to granule strength (St).View full abstractDownload PDF (686K) -
Kazumi DANJO, Yukio KITAMURA, Yasuhiko MIYAGAWA, Akinobu OTSUKA1994 Volume 42 Issue 10 Pages 2126-2130
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn vitro release tests and in vivo absorption measurements of oral cavity dosage forms of isosorbide dinitrate (ISDN) prepared from mixed polymer film systems were conducted. Hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose phthalate (HPMCP) were used to make the films, and the tests were conducted with films made from various ratios of these two polymers. The effects of the addition of the accelerator glycyrrhizic acid (GL), on dissolution and absorption were also examined. The mean dissolution time (MDT) in the in vitro dissolution tests varied with the nature of the polymers and drug, as well as with the pH of the testing solution. The MDT for the polymer film system with GL was smaller than that without GL.In the in vivo absorption tests using rats, the absorption of ISDN through the oral mucosa was observed in all the systems. In the mixed polymer film systems, the mean residence time (MRT) increased with increasing the ratio of HPMCP/HPC. The values of the area under the curve (AUC) for the systems with GL was larger than for those without GL. A good correlation was demonstrated between the absorption rate constant, ka and the dissolution rate constant, kd.View full abstractDownload PDF (635K) -
Shinji NARISAWA, Eiji FUKUI, Hiroyuki YOSHINO, Yoshiyuki HIRAKAWA, Kaz ...1994 Volume 42 Issue 10 Pages 2131-2134
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe porous ethylcellulose (EC) film-coating technique was applied to prepare the film-coated (so-called capsule-type) controlled release dosage form of phenylpropanolamine hydrochloride (PPA), which was used as a highly water-soluble model drug. To prepare EC film-coated beads with various film-porosities, the PPA-loaded uncoated beads were spray-coated with an aqueous ethanolic or ethanolic solution of EC, and their drug release behaviors or drug release mechanisms were investigated. Although the amount of coating of the beads was equal, the PPA release rate differed according to the ethanolic concentration in the coating solution, that is, the lower the ethanolic concentration, the faster the release rate. The release profiles were normalized using a reduced time method to compare the profiles of different release rates. It was found that the profiles were well superimposed on the same curve, suggesting that the drug release obeyed the same mechanism. To examine the mechanism of drug release from the EC film-coated beads of PPA, drug release behaviors were investigated under the condition of various osmotic pressure differences. The drug release rate was decreased by decreasing the osmotic pressure difference. The contribution of an osmotic pumping to the drug release was estimated for the EC film-coated beads with different coating porosities. The driving force for drug release from the porous EC film-coated beads was found to be mainly an osmotic pumping mechanism, irrespective of film porosity.View full abstractDownload PDF (721K) -
Katsuya AKIMOTO, Akiko KAWAI, Kazumi OHYA1994 Volume 42 Issue 10 Pages 2135-2138
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of pH and temperature on the reaction rate of the hydrolysis and lactonization of camptothecin and its derivatives, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11) and 7-ethyl-10-hydroxycamptothecin (SN-38), in aqueous solution was studied by high-performance liquid chromatography or two-wavelength spectrophotometry. Hydrolysis and lactonization of each compound progressed according to pH-and temperature-dependent pseudo-first-order kinetics. The ratio of the lactone form of each compound to its hydroxy-acid form was determined mainly by the pH of the solution and was not influenced by temperature. Half-lives of the lactone and hydroxy-acid forms of CPT-11 at 37°C and pH 7.4 were 13.7 min and 4.25 h, respectively.View full abstractDownload PDF (590K) -
Eihei FUKUOKA, Midori MAKITA, Shigeo YAMAMURA, Yasuo YOSHIHASHI1994 Volume 42 Issue 10 Pages 2139-2142
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA microcalorimetric method for measurement of the dissolution rate of sodium chloride was presented. The method applied the deconvolution theory to heat conduction microcalorimetry. When a calorimetric curve for the heat of dilution was regarded as the response for a unit impulse input (heat conduction profile), a calorimetric curve for the heat of solution was considered to be the convolution of dissolution profile and heat conduction profile. Thus, the dissolution profile was calculated from the calorimetric curves for the heat of dilution and for the heat of solution by a numerical deconvolution. Dissolution rate determined by the calorimetric method coincided well with that obtained by a titration method.View full abstractDownload PDF (567K) -
Nobuo OKABE, Yoh SASAKI1994 Volume 42 Issue 10 Pages 2143-2145
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal structure of d-desthiobiotin was determined by the X-ray diffraction method. The crystals are orthorhombic, space group P212121, with cell dimensions, a=7.516(5), b=29.100(8), c=5.148(6)Å, and Z=4. The structure was refined to R=0.065. The molecular conformation is characterized by the extended trans planar zig-zag conformation of the caproic acid chain. The ureido carbonyl oxygen forms a strong hydrogen-bond with the carboxyl group of a neighboring molecule (O…O distance, 2.649(7)Å). These structural features resemble those of d, l-desthiobiotin, indicating that the structure observed in d-desthiobiotin is characteristic of desthiobiotin.View full abstractDownload PDF (528K) -
Seiki TANADA, Takeo NAKAMURA, Naohito KAWASAKI, Jun IZAWA, Toshimitsu ...1994 Volume 42 Issue 10 Pages 2146-2149
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe adsorption characteristics of trichloroethylene (TCE), a major volatile chlorinated hydrocarbon, onto 16 kinds of granular activated carbons (GACs) in gaseous phase were investigated.The amount of TCE adsorbed on GACs was proportional to the pore volume, and the adsorption was recognized to be a physical one.Applying the Dubinin-Radushkevich (D-R) eqation to the adsorption isotherms of TCE, GACs could be classified into two types : the D-R plot was either a straight line or not depending on pore size distribution. TCE was believed to be adsorbed not only into micropores but also into transitionalpores.View full abstractDownload PDF (457K) -
Hiroyuki ISHIBASHI, Susumu AKAMATSU, Hiroko IRIYAMA, Masazumi IKEDA1994 Volume 42 Issue 10 Pages 2150-2153
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe indolone 1 reacted with organomagnesium or lithium reagents to give the carbinols 6 and 10, which, upon treatment under appropriate acidic conditions or neutral thermal conditions, gave the 1-phenylsulfonylindoles 8 and 11 bearing various kinds of alkyl, alkenyl, and alkynyl substituents at the 4-position. The indolone 1 was also converted to the 4-cyanoindole 14 via the cyanohydrin O-trimethylsilyl ether 13.View full abstractDownload PDF (693K) -
Mayumi KOYAMA, Mihoko TAMURA, Akira ANDO, Itsumaro KUMADAKI1994 Volume 42 Issue 10 Pages 2154-2156
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-[4, 8-Dimethyl-12-(trifluoromethyl)tridecyl]-2, 5, 7, 8-tetramethyl-6-chromanol and 2-[4, 12-dimethyl-8-(trifluoromethyl)tridecyl]-2, 5, 7, 8-tetramethyl-6-chromanol, were synthesized by means of the Wittig reaction using the phosphonium salt of 2-(3-chloropropyl)-2, 5, 7, 8-tetramethyl-6-chromanol.View full abstractDownload PDF (557K) -
Seiji MORITA, Kenji OHTSUBO, Jun MATSUBARA, Tadaaki OHTANI, Minoru UCH ...1994 Volume 42 Issue 10 Pages 2157-2160
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe enantiomers of 7-fluoro-1-methyl-3-(methylsulfinyl)-4(1H)-quinolinone [(±)-1, flosequinan], a new drug for the treatment of heart failure, were synthesized from the optically active (R)-α-methylbenzylamine derivatives of quinoline. The key intermediates, (R)-α-methylbenzylamine derivatives, were prepared by diastereomeric separation. The configuration of (+)-1 was assigned on the basis of an X-ray crystallographic analysis of the synthetic precursor (4a). The absolute configuration was found to be (R)-(+)-1 and (S)-(-)-1.View full abstractDownload PDF (576K) -
Yuji MORI, Hiroshi FURUKAWA1994 Volume 42 Issue 10 Pages 2161-2163
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCryptocaryalactone, a 1, 3-polyol-derived α, β-unsaturated δ-lactone, has been synthesized in a stereocontrolled manner via the coupling reaction of a chiral dithiane with an epoxide and anti-stereoselective 1, 3-asymmetric reduction of the derived hydroxy ketone.View full abstractDownload PDF (554K) -
Shugo ATSUUMI, Chinatsu IKEURA, Teruki HONMA, Hajime MORISHIMA1994 Volume 42 Issue 10 Pages 2164-2166
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA dihydroxyethylene isostere, (2S, 3R, 4S)-4-amino-5-cyclohexyl-1-morpholino-2, 3-pentanediol (ACMP, 1), which is a component of non-peptidic, orally active, low-molecular-weight renin inhibitors, was synthesized stereospecifically starting from 3-cyclohexyl-L-alanine via iodo-cyclocarbamation as the key reaction.View full abstractDownload PDF (584K) -
Masahiro TADA, Kazuhisa OHTSU, Kazuhiro CHIBA1994 Volume 42 Issue 10 Pages 2167-2169
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPatulin, a mycotoxin from fungi of Penicillium and Aspergillis species, and its cyclohexane analogue were synthesized concisely via oxidation of furan derivatives, followed by cyclization to give a ylidenebutenolide ring.View full abstractDownload PDF (509K) -
Takashi HARAYAMA, Kazumitsu NAKATSUKA, Hiromi NISHIOKA, Kyoko MURAKAMI ...1994 Volume 42 Issue 10 Pages 2170-2173
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of salicylaldehydes (1) with carbethoxymethylenetriphenylphosphorane in diethylaniline under reflux gave coumarins (3) in moderate to high yield except 3-methoxycarbonylsalicyladehyde (1e) as summarized in Table I. The substituent effects are discussed. A substituent at C6 on 1 usually facilitated the formation of the coumarin ring regardless of its electronic character.View full abstractDownload PDF (608K) -
Takeshi OHSHIMA, Mitsuteru HIRATA, Toshiaki ODA, Ai SASAKI, Masami SHI ...1994 Volume 42 Issue 10 Pages 2174-2176
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMany crude drugs were screened for their capacity to inhibit the binding of endothelin-1 (ET-1) to ET receptors ; several crude drugs showed significant binding inhibitory activity. Pheophorbide a (1), a potent non-peptide ET receptor antagonist, was isolated from Altemisiae capillaris Flos ("Inchinko" in Japanese), which has been utilized as a remedy for hepatitis in Oriental medicine. In receptor binding experiments, compound 1 inhibited ET-1 binding specifically to both the ETA receptor (ETAR) and ETB receptor (ETBR), with IC50 values of 8.0×10-8 and 2.1×10-7M, respectively. Thus, compound 1 is an ET-1 binding inhibitor; howver, it exhibited no affinity for the other receptors of angiotensin II and atrial natriuretic peptide. We also evaluated the inhibitory activity of porphyrin compounds, and found that some exhibited moderate activity.View full abstractDownload PDF (547K) -
Midori TAKASAKI, Takao KONOSHIMA, Mutsuo KOZUKA, Mitsumasa HARUNA, Kaz ...1994 Volume 42 Issue 10 Pages 2177-2179
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the juvenile leaves of Eucalyptus blakelyi, a new euglobal, euglobal-Bl-1 (1), having a phloroglucinol-monoterpene structure, has been isolated along with the known euglobals-Ib (2), -Ic (3) and -IIa (4). The structure and stereochemistry of euglobal-Bl-1 (1) and the stereochemistry of euglobal-Ib (2) were established by spectroscopic evidence.View full abstractDownload PDF (507K) -
Junpeng PENG, Xinsheng YAO, Yoshihito OKADA, Toru OKUYAMA1994 Volume 42 Issue 10 Pages 2180-2182
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFurther studies by means of preparative HPLC led to the isolation of two new furostanol saponins, macrostemonoside J (1) and L (3), along with an artifact, macrostemonoside K (2) from the bulbs of Allium macrostemon. On the basis of chemical evidence and spectral analysis (1H, 13C-NMR and FAB-MS), the structure of 1 was elucidated to be 26-O-β-D-glucopyranosyl 2β, 3β, 22, 26-tetrahydroxy-25(R)-5β-furostan 3-O-β-D-glucopyranosyl (1→2)-β-D-galactopyranoside. 3 was deduced to be 26-O-β-D-glucopyranosyl 2β, 3β, 26-trihydroxy-25(R)-5β-furostan-20(22)-ene 3-O-β-D-glucopyranosyl (1→2)-β-D-galactopyranoside.View full abstractDownload PDF (469K) -
Emi OKUYAMA, Kazuhiro UMEYAMA, Shigeru OHMORI, Mikio YAMAZAKI, Motoyos ...1994 Volume 42 Issue 10 Pages 2183-2186
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe methanol extract of Huira-Huira (Culcitium canescens) showed analgesic effects in acetic acid-induced writhing and tail pressure tests, and it also produced potent prolongation of hypnosis induced by pentobarbital. The latter activity was used as an isolation-guide to determine the active components which were identified as dehydrocacalohastine, cacalohastine and cacalonol.View full abstractDownload PDF (596K) -
Yueh-Hsiung KUO, Wen-Ching CHEN1994 Volume 42 Issue 10 Pages 2187-2189
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new dimeric sesquiterpene, chinensiol, was isolated from the roots of Juniperus chinensis Linn. Its structure was deduced to be a dimeric cis -himachalane-type sesquiterpene by spectroscopic analysis and chemical evidence. The structure of the oxidative product (eleven-member ring) obtained from chinensiol was elucidated by X-ray analysis.View full abstractDownload PDF (408K) -
Munetaka KUNISHIMA, Kazuhito HIOKI, Kazuhiro KONO, Takayuki SAKUMA, Sh ...1994 Volume 42 Issue 10 Pages 2190-2192
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBarbier-type reaction of aryl halides with ketones took place on treatment with samarium diiodide in benzene containing 10 % hexamethylphosphoric triamide (HMPA). The reaction involves an aryl samarium as an intermediate.View full abstractDownload PDF (457K) -
Kenji SHIOJIMA, Hideki SUZUKI, Nobuyuki KODERA, Ken-ichi KUBOTA, Sakik ...1994 Volume 42 Issue 10 Pages 2193-2195
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel triterpenoid, 17-epilupenyl acetate (1), has been isolated together with twelve known triterpenoid acetates, and the structure was determined by extensive spectroscopic analyses.View full abstractDownload PDF (424K) -
Motomasa KOBAYASHI, Michio KUROSU, Naoki OHYABU, Weiqi WANG, Satoshi F ...1994 Volume 42 Issue 10 Pages 2196-2198
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe absolute stereostructure of arenastatin A (1), which was isolated from the Okinawan marine sponge Dysidea arenaria, has been determined on the bases of NMR and synthetic studies. Arenastatin A (1) is a cyclic depsipeptide exhibiting extremely potent cytotoxicity against KB cells with IC50 5pg/ml.View full abstractDownload PDF (470K) -
Yoshiyasu FUKUYAMA, Kazumi OKAMOTO, Youko KUBO, Naomi SHIDA, Mitsuaki ...1994 Volume 42 Issue 10 Pages 2199-2201
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures of two new chlorine-containing C6-C3 compounds isolated from the woods of Illicium tashiroi have been established as 2(R)-12-chloro-2, 3-dihydroillicinone E (1) and 12-chloroillicinone E (2) by X-ray crystallographic analysis and spectroscopic data, respectively. Compound 1 has been found to significantly increase ChAT activity in culture of P10 rat sepatl neurons.View full abstractDownload PDF (437K) -
Jin-Bin WU, Yih-Dih CHENG, Shen-Chu KUO, Tian-Shung WU, Yoichi IITAKA, ...1994 Volume 42 Issue 10 Pages 2202-2204
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new alkaloid of hydro-oxadiazine with a four-ring fused structure has been isolated from Fissistigma oldhamii (Memsl.) Merr. (Annonaceae) and named fissoldhimine (1), the structure of which was solved by X-ray analysis. NMR spectra were assigned based on the established structure, and its possible biogenesis is also discussed.View full abstractDownload PDF (440K) -
Mamoru KOEDA, Yoshinobu AOKI, Nobuko SAKURAI, Ken-ichi KAWAI, Masahiro ...1994 Volume 42 Issue 10 Pages 2205-2207
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree novel xylosides, cimicifugosides H-1(1), -3(2) and -4(3), were isolated from a commercial Cimicifuga Rhizome. Their structures were determined on the basis of chemical and spectrometric evidence including an X-ray crystallographic analysis. The xyloside 1 is 3-O-xyloside of (20R, 24R)-24, 25-epoxy-3β, 11β-dihydroxy-9, 19-cyclolanost-7-ene-16, 23-dione, while 2 and 3 are 3-O-xylosides of 25, 26, 27-trinor-derivatives from the genin of 1.View full abstractDownload PDF (408K) -
Atsuko ITOH, Takao TANAHASHI, Naotaka NAGAKURA1994 Volume 42 Issue 10 Pages 2208-2210
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the fruits of Alangium lamarckii, three new tetrahydroisoquinoline-monoterpene glucosides, isoalangiside, 3-O-demethyl-2-O-methylisoalangiside and methylisoalangiside, were isolated. Their structures were determined by spectroscopic and chemical methods. This is the first instance of the isolation of glucosides with the same absolute configurations as deacetylisoipecoside, and strongly supports the intermediacy of the latter compound in ipecac alkaloid biosynthesis.View full abstractDownload PDF (477K) -
Yoshiyasu FUKUYAMA, Yuuko KIRIYAMA, Mitsuaki KODAMA, Hideyuki IWAKI, S ...1994 Volume 42 Issue 10 Pages 2211-2213
Published: October 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSArdisiaquinone A (1), isolated as a potent 5-lipoxygenase inhibitor from the woods of Ardisia sieboldii, has been synthesized efficiently via a cross-coupling reaction between the yne 5 and the iodide 6 derived from the common intermediate 4. Inhibitory activity for 1 and its derivatives is also reported.View full abstractDownload PDF (417K)
- |<
- <
- 1
- >
- >|