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Volume 35, Issue 11
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HIDEO KUBODERA, HIDEAKI UMEYAMA1987 Volume 35 Issue 11 Pages 4377-4394
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAn index which corresponds to charge transfer interaction is presented as a tool to study the correlation of molecular orbital (MO) distributions. The MO distribution correlation (MODIC) index was applied to Diels-Alder reaction systems (1-methoxy-1, 3-butadiene-acrolein system and cyclopentadiene-maleic acid anhydride system), and the dihydrofolate reductase (DHFR) system. In the Diels-Alder reaction systems, the positions of reaction centers and orientations of substitutional groups predicted by the index were consistent with experimental findings. In the DHFR system, the reactivities of different ligands were explained by the index.
Frontier electron theory provides some indexes to predict reactivities, based on the molecular orbital coefficients of the isolated molecule in its ground state. The MODIC index has the advantage that it contains information on the three-dimensional distribution of MO's. It can predict the MO's in the transition state of a reaction.View full abstractDownload PDF (2473K) -
TOKIHIRO NIIYA, MIHO YUKAWA, HIROKI MORISHITA, YOSHINOBU GOTO1987 Volume 35 Issue 11 Pages 4395-4404
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe reactions of acetaldehyde with amide (NH-2), hydroxide (OH-) or fluoride (F-) ions were investigated by ab initio calculations. Acetaldehyde, which has an active methyl group, was taken as the model compound. The hydrogen-abstraction steps were studied in detail in terms of the energies and the structures of all the complexes in the reaction process. It became clear that the order of the deprotonation ability, i.e., NH -2 > OH-> F - can be reasonably explained when deformation energy is taken into account in the calculation of the energies of the complexes in each reaction pathway. The reactions of methane with these three anions are also discussed as reference reactions.View full abstractDownload PDF (1196K) -
MASAMICHI TSUBOI, TERUKI IKEDA, HEIZABURO SHINDO1987 Volume 35 Issue 11 Pages 4405-4409
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA deoxyribonucleic acid (DNA) solution was placed in the gap (1 mm) between two coaxial cylinders; the inside diameter of the outer cylinder was 12 mm, and the outside diameter of the inner cylinder was 10 mm. When the inside cylinder was rotated at 2500 revolutions per minute, a sufficiently large velocity gradient of the liquid flow was produced across the gap so that the DNA molecules were oriented along the flow direction. Anisotropy of the Raman scatterings of the DNA molecule was examined by passing an exciting laser beam into the gap from the bottom of the cylinder in the direction parallel to the cylinder axis. An antitumor drug, aclacinomycin A (HCl salt), was added to the DNA solution, and the anisotropy of its emission and Raman spectra was also examined. It has been established that aclacinomycin binds to DNA with its chromophore oriented parallel to the base plane of the DNA duplex.View full abstractDownload PDF (730K) -
TATSUYA KITADE, KEISUKE KITAMURA, KEI HOZUMI1987 Volume 35 Issue 11 Pages 4410-4417
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAntipyrine powder was coated by deposition of a polymer thin film within a glow discharge of tetrafluoroethylene and propargyl alcohol blend monomer under reduced pressure (plasma polymerization) and drug release from the product was investigated. A dissolution test revealed that the use of the blend monomer was superior to that of the individual plain monomer. The plasma coating of the powder was done with intermittent agitation or with continuous mixing under electromechanical vibration; in the former case the product gave slow drug release, but the reproducibility was poor, while in the latter case, reproducibility was good, but the release rate was faster. It was found that the release rate could be fairly well controlled by changing the film thickness of the plasma polymer, and was not influenced by the pH of the dissolution medium.View full abstractDownload PDF (2902K) -
MAKOTO MIYAHARA, NAOKI MIYATA, MASAAKI HIROBE, SHOZO KAMIYA1987 Volume 35 Issue 11 Pages 4418-4428
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe degradation of 1, 3-di (p, p'-disubstituted) aryl-1-nitrosoureas (I) in aqueous buffer solutions (at 0 °C over pH-0.5 to 5.4) and in several organic solvents (benzene, chloroform, etc.) has been kinetically studied. In aqueous solution, the overall rates of degradation followed pseudo-first-order kinetics at constant pH. The decomposition reaction of 1, 3-diphenyl-1-nitrosourea (Ia) was first-order in hydrogen ion over the pH range of-0.5 to 1.5 and denitrosated 1, 3-diphenylurea (IIa) was formed predominantly. In the range of pH 1.5 to 5.4, the degradation of Ia was catalyzed by hydroxide ion and the main product was IIa, which was formed by the recombination of reactive products. In organic solvents, thermal degradation of Ia obeyed first-order kinetics and gave similar products to those yielded in the base-catalyzed degradation. The acid-and base-catalyzed and thermal degradations of Ia were about 102 to 103 times more rapid than those of related 1, 3-dialkyl-1-nitrosoureas. The reaction mechanisms are discussed.View full abstractDownload PDF (1381K) -
MASANORI KUROYANAGI, MAKOTO SATO, AKIRA UENO, KOUZABURO NISHI1987 Volume 35 Issue 11 Pages 4429-4435
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new flavanone glucoside, named andrographidine A (1), and five new flavone glucosides, named andrographidines B (2), C (3), D (4), E (5) and F (6), were isolated from the root of Andrographis paniculata. Their structures were determined on the basis of spectral data, especially carbon-13 and proton nuclear magnetic resonance spectra, and chemical derivatization. They have uncommon O-substitution patterns involving 5-, 7-, 8-, 2'-, 3'-and 4'-O-substituents.View full abstractDownload PDF (1241K) -
KIYOSHI IKEDA, SHIN-ICHI NAKAMOTO, TOSHIO TAKAHASHI, KAZUO ACHIWA1987 Volume 35 Issue 11 Pages 4436-4441
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAn efficient synthesis of lipid Y by the use of chemoselective debenzylation as a key step is described.View full abstractDownload PDF (1031K) -
YOSHINOBU MUROFUSHI, MISAKO KIMURA, YASUTERU IIJIMA, MITSUO YAMAZAKI, ...1987 Volume 35 Issue 11 Pages 4442-4453
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSubstituted derivatives of the hydroxy group at the 2'-or 7'-position in griseolic acid (1) were synthesized by selective substitution in order to study the relationship between structure and inhibitory activity against adenosine 3', 5'-cyclic monophosphate (cAMP) or guanosine 3', 5 '-cyclic monophosphate (cGMP) phosphodiesterase (PDE). All of the derivatives which had a configurationally inverted substituent at the 2'-position instead of the hydroxy group were almost equal to natural griseolic acid in cAMP PDE inhibitory activity, except when the substituent was an amino group. On the other hand, substitution of 7'-OH with inversion tended to reduce the inhibitory activity a little.View full abstractDownload PDF (2430K) -
ZHUO-FENG XIE, HIROSHI SUEMUNE, IZUMI NAKAMURA, KIYOSHI SAKAI1987 Volume 35 Issue 11 Pages 4454-4459
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSOptically active cyclopentane and bicyclo [3.3.0] octane derivatives were synthesized by utilizing biochemical methods. Pseudomonas fluorescens lipase was found to be an effective enzyme for the enantioselective hydrolysis of monoacetoxy-and diacetoxycyclopentanes such as (±) -4a, (±) -5a, (±) -6a, and 7a. However, hydrolysis of bicyclo [3.3.0] octane trans-acetate ((±) -8a) using this enzyme resulted in low enantioselectivity. Optically pure (+) -8b for the synthesis of carbacyclin was obtained from (+) -8a by using porcine pancreatic lipase. Reduction of 3-acetyl-7-oxobicyclo [3.3.0] -oct-2-ene with baker's yeast afforded a useful intermediate ((+) -11b) for the synthesis of hirsutic acid.View full abstractDownload PDF (662K) -
TAKASHI TSUCHIDA, MASARU KOBAYASHI, Ko KANEKO, HIROSHI MITSUHASHI1987 Volume 35 Issue 11 Pages 4460-4464
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThree new ligustilide derivatives (3-5) were isolated from the crude drug toki, the dried roots of the Umbelliferae plant Angelica acutiloba, together with a known ligustilide dimer, levistolide A (2), and four known oxygenated ligustilide derivatives, senkyunolide E (6), senkyunolide F (7), senkyunolide H (8) and senkyunolide I (9). Compound 3 was shown to be the angeloyl ester of 7. Compounds 4 and 5, designated tokinolide A and tokinolide B, are dimeric ligustilide derivatives with Diels-Alder-type (5) and cyclobutane-type (4) cyclization systems, respectively. The occurrence of compounds 2 to 9 in a fresh A. acutiloba sample was confirmed.View full abstractDownload PDF (746K) -
TOKUNARU HORIE, MASAO TSUKAYAMA, YASUHIKO KAWAMURA, SHIGEO YAMAMOTO1987 Volume 35 Issue 11 Pages 4465-4472
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS2-Hydroxy-3, 4, 6-trimethoxy-ω- (ρ-methoxybenzoyloxy) acetophenone was prepared from 2, 3, 4, 6-tetramethoxyacetophenone via the corresponding ω-bromoacetophenone. Cyclization of the acetophenone with ρ-methoxybenzoic anhydride by application of the Allan-Robinson reaction afforded 3-hydroxy-4', 5, 7, 8-tetramethoxyflavone along with 2- (α-hydroxy-4-methoxybenzylidene) -4, 6, 7-trimethoxycoumaranone. The 5-methoxy group in the tosylate or mesylate of the 3-hydroxyflavone was selectively cleaved with anhydrous aluminum bromide in acetonitrile to give the corresponding 5-hydroxyflavone, which was converted into 3, 5-dihydroxy-4', 7, 8-trimethoxyflavone with anhydrous potassium carbonate in methanol. 3, 3', 4', 5-Tetrahydroxy-7, 8-dimethoxyflavone was also synthesized by a similar method. The demethylation of the 5-methoxy group in flavones with a 3-hydroxy group is applicable to the synthesis of 3, 5-dihydroxyflavones.View full abstractDownload PDF (1207K) -
HIDENOBU OHMORI, HATSUO MAEDA, KOHICHI KONOMOTO, KIYOSHI SAKAI, MASAIC ...1987 Volume 35 Issue 11 Pages 4473-4481
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThioalkoxyphosphonium salts, Ph3P+ SR ClO-4 (3) and Bu3P+ SR X- (X = ClO4 and BF4) (5), have been prepared from the corresponding tertiary phosphines and disulfides by simple procedures, which involve (i) constant current electrolysis in acetonitrile in the presence of either HClO4 (for 3) or PhCOOH and LiX (for 5), and (ii) stirring an equimolar mixture of a phosphine, a disulfide, PhCOOH, and LiX in acetonitrile at ambient temperature. For the preparation of 3, which have been reported as useful reagents for the synthesis of unsymmetrical disulfides, the electrochemical method is recommended, while for 5 the latter non-electrochemical procedure gave better results. Reactions of the phosphonium salts 5 with carboxylic acids and primary alcohols in benzene at ambient temperature gave thiolesters and unsymmetrical sulfides, respectively, in fair to excellent yields.View full abstractDownload PDF (1329K) -
TOZO FUJII, TOHRU SAITO, TAISUKE ITAYA, KYOKO KIZU, YUKINARI KUMAZAWA, ...1987 Volume 35 Issue 11 Pages 4482-4493
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSCyclizations of the alkoxyamidines 7a, i with formic acid gave N6-methoxy-9-methyladenine (8a) and 9-benzyl-N6-methoxyadenine (8i). Replacement of formic acid by formic-d acid-d in these cyclizations afforded the 2-deuterated species 13a and 13i. A similar cyclization of 22, obtained from 21 by alkaline hydrolysis, with formic-d acid-d yielded 2-deuterio-N6-methoxy-1, 9-dimethyladenine (24). The N6-methyl isomer 19 was prepared from 13a by treatment with NaH and MeI. Comparison of the proton nuclear magnetic resonance (1H-NMR) spectrum of 8a in Me2SO-d6 with that of 13a revealed that 8a exists as an equilibrated 1 : 3.5 mixture of the amino (type 14 or 15) and the imino (type 16 or 17) forms. The deuterated species 19 and 24 were utilized for interpretation of the 1H-NMR spectra of the amino-form model 18 and the imino-form model 23. The existence of amino-imino tautomerism in 8a was also supported by ultraviolet and infrared spectroscopic evidence. Such tautomerism, with a preference for the imino form, in Me2SO-d6 was found to be common to 13 other 9-substituted N6-alkoxyadenines (type 8) including adenosine analogues. On the other hand, comparison of the 1H-NMR spectra of 11, N6, 9-dimethyladenine (12), and N6, N6, 9-trimethyladenine (36) indicated that 12 exists solely in the amino form in CDCl3 or Me2SO-d6.View full abstractDownload PDF (1448K) -
KRZYSZTOF W. PANKIEWICZ, KYOICHI A. WATANABE1987 Volume 35 Issue 11 Pages 4494-4497
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTreatment of 2, 5'-anhydro-3'-O-acetyl-2'-Ο-triflyluridine with a nucleophile such as NaOAc, NaN3, LiCl or LiBr, did not afford the 2'-substituted 2, 5'-anhydro-arabinosyluracil, but gave 2, 2'-anhydro-1- (5-substituted-β-D-arabinofuranosyl) uracil instead.View full abstractDownload PDF (697K) -
KRZYSZTOF W. PANKIEWICZ, KYOICHI A. WATANABE1987 Volume 35 Issue 11 Pages 4498-4502
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTreatment of 2, 3 '-anhydro-1- (5-Ο-acetyl-2-Ο-triflyl-β-D-xylofuranosyl) uracil with LiCl in hexamethylphosphoric triamide afforded the 2 '- “up” chloride of the anhydronucleoside, i.e., the 2'-triflate group was directly displaced by the chloride nucleophile. All attempts to hydrolyze the 2, 3'-anhydro linkage resulted in the formation of 2'-chloro-2', 3'-didehydro-dideoxynucleoside.View full abstractDownload PDF (781K) -
HIROMASA MORI1987 Volume 35 Issue 11 Pages 4503-4509
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSBleomycin decreases the melting temperature (Tm) of deoxyribonucleic acid (DNA) determined by the optical density and viscosity methods and breaks the DNA strand in the presence of 1, 2-benzenediol (catechol). The effect of bleomycin in the presence of catechol is markedly in acidic solution. However, in contrast with the case of sulfhydryl compounds such as 2-hydroxy-1-ethanethiol (2-mercaptoethanol), catechol inhibits the interaction of ultraviolet (UV) -irradiated bleomycin with DNA. These results show that catechol has two functions, i.e., increasing the activity of non-irradiated bleomycin and inhibiting that of UV-irradiated bleomycin. Moreover, it was demonstrated that irradiation is not effective for enhancing the antibacterial activity of bleomycin.View full abstractDownload PDF (969K) -
SHUICHI MIYAMOTO, MASAFUMI YOSHIMOTO1987 Volume 35 Issue 11 Pages 4510-4516
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSome analogs of isocarbacyclin were found to be potent inhibitors of platelet aggregation.Molecular mechanics and molecular orbital calculations on model compounds of prostacyclin and isocarbacyclin analogs were undertaken in an attempt to elucidate structure-activity relationships.It was found that the net atomic charges of the π-electron systems could be correlated with the platelet aggregation-inhibitory potency. The π-electron systems are considered to play an essentialrole directly in binding with the receptor by electronic interaction and a significant role indirectly inregulating the orientation of the α-chain.View full abstractDownload PDF (6205K) -
SHIN-ICHI NAKAMOTO, TOSHIO TAKAHASHI, KIYOSHI IKEDA, KAZUO ACHIWA1987 Volume 35 Issue 11 Pages 4517-4523
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAn efficient method for the synthesis of monosaccharide analogs of the nonreducing sugar moiety of lipid A is described. A brief analysis of their biological activities is also presented.View full abstractDownload PDF (1130K) -
HIDEJI ITOKAWA, JUNPING XU, KOICHI TAKEYA1987 Volume 35 Issue 11 Pages 4524-4529
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSWhen the CHCl3 extract obtained by partitioning the methanolic extract of Periploca sepium between H2O and CHCl3 was subjected to column chromatography on silica gel, the antitumor activity against Sarcoma 180 ascites in mice was concentrated in the fraction eluted with CHCl3-MeOH (10 : 1). From the antitumor fraction, eight products, S-1-S-8, were isolated. S-1 was identified as 12β-hydroxypregna-4, 6, 16-triene-3, 20-dione (neridienone-A), obtained for the first time from Asclepiadaceous plants, by direct comparison with an authentic sample and the others were found to be steroidal glycosides. A new compound S-2A (named periplocogenin), and two known aglycones S-3A and S-5A, obtained by hydrolyzing the above glycosides with diluted acid, were respectively identified as 3β-O- (4', 6'-dideoxy-3'-O-methyl-Δ3'-D-2'-hexosulosyl) -Δ5-pregnene-17α, 20 (S) -diol, periplogenin, and Δ5-pregnene-3β, 20 (S) -diol from the proton and carbon-13 nuclear magnetic resonance spectral data. The structure of S-6A was identical with that of S-5A, and S-7A and S-8A were identical with S-2A.View full abstractDownload PDF (918K) -
TADATO TANI, TADAHISA KATSUKI, MICHINORI KUBO, YUKO OKAZAKI, SHIGERU A ...1987 Volume 35 Issue 11 Pages 4530-4536
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe morphological, histological and chemical characteristics of non-bolting and bolting roots of cultivated Bupleurum falcatum L. were statistically compared. In external characteristics, non-bolting (rosette) roots were found to be lighter, thinner, and more flexible than bolting roots taken from plants with flower-stalks. Histologically, non-bolting roots had a smaller xylem ratio, wider phloem tissue and a tendency to contain greater concentrations of tissue-specifically stored bioactive saikosaponins than did bolting roots, which had well-developed xylem mechanical tissue. Of these two types of growing plants, higher concentrations of magnesium and phosphorus were observed in roots of non-bolting plants.View full abstractDownload PDF (2204K) -
SHIN-ICHI NAKAMOTO, KAZUO ACHIWA1987 Volume 35 Issue 11 Pages 4537-4543
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSynthesis of biologically active tetraacetyl-3-deoxy-D-manno-2-octulosonic acid- (α2→6) -D-glucosamine-4-phosphate analogs of lipid A is described.View full abstractDownload PDF (1031K) -
RIKIO IKENISHI, TAKAYASU KITAGAWA1987 Volume 35 Issue 11 Pages 4544-4551
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAn ion-pair reversed-phase high-performance liquid chromatographic (HPLC) assay method was developed for the sleep inducer 1- (2-ο-chlorobenzoyl-4-chlorophenyl) -3-dimethylcarbamoyl-5-glycylaminomethyl-1H-1, 2, 4-triazole hydrochloride dihydrate (rilmazafone, 1) in animal feed. This method is an ion-pair reversed-phase HPLC using an octadecylsilane chemically bonded silica gel column and dodecanesulfonic acid as an ion-pairing reagent. It can simultaneously assay drug 1 and its six degradation products. Dodecanesulfonic acid caused retention of three compounds (1, 6 and 7) on the column through the ion-pair effect, with good separation from other neutral and acidic compounds.
The drug was extracted from the feed. After clean-up, the extract was subjected to HPLC, with 1 being assayed with a coefficient of variation of less than 4%. The degradation products can be simultaneously assayed with the same precision even when present at only 2-3 mg/kg. This method was used to confirm the stability of 1 in feed. An HPLC method to assay 1 alone was also established;it is more efficient than our previous fluorometric procedure.View full abstractDownload PDF (1017K) -
NORIAKI KOBAYASHI1987 Volume 35 Issue 11 Pages 4552-4556
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA solid-phase enzyme immunoassay for the measurement of anti-ribonucleic acid (RNA) antibodies in the sera from hyperthyroid patients was developed. Three antigens, calf liver RNA, poly (I)·(C) and poly (A)·(U), were fixed to 96-well enzyme immunoassay microtiter plates precoated with poly-L-lysine hydrobromide. Antibodies detected in the present assay cross-reacted with neither double strand-deoxyribonucleic acid (ds-DNA) nor single strand (ss) -DNA, and were RNA-specific.
In twenty (66.6%) out of 30 sera from hyperthyroid patients, anti-RNA antibodies were detected. Interestingly, in seven positive cases out of 8 patients with malignant thyrocele, the levels of antibodies against poly (I)·(C) and poly (A)·(U) were much higher than those against calf liver RNA, while antibodies against calf liver RNA were commonly high in hyperthyroid patients.
The present assay requires no radioactive materials, and is sensitive and specific. It is expected to be practically useful to measure anti-RNA antibodies. Furthermore, this assay may provide an aid to diagnose the disease type, e.g., autoimmune or nonautoimmune, and the degree of the hyperthyroidosis.View full abstractDownload PDF (543K) -
WILLY J.M. UNDERBERG, Jos H. BEIJNEN1987 Volume 35 Issue 11 Pages 4557-4561
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe stereoselectivity in the acid hydrolysis mechanism of mitomycins was studied. The predominance of the 1, 2-cis-mitosene degradation products occurring at low pH was ascribed to the directing force exterted on the incoming nucleophile by the protonated 2-amino function of an intermediate in the process as well as to steric hindrance due to the orientation of the C9 urethane substituent in one of the degradation steps preceding the formation of the intermediate. The differences in electron density in the intermediate chromophore and the resulting differences in pKa value of the amino function involved are discussed.View full abstractDownload PDF (591K) -
JUNICHI GOTO, YOSHIHISA SANO, TOSHIYUKI CHIKAI, TOSHIO NAMBARA1987 Volume 35 Issue 11 Pages 4562-4567
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe disulfates of unconjugated, and glycine- and taurine-conjugated bile acids have been synthesized. Cholic acid derivatives appropriately protected were sulfated with sulfur trioxide-triethylamine complex in pyridine in the usual manner. Subsequent hydrolysis and/or sodium borohydride reduction provided the desired disulfates of cholates in satisfactory yields. Dihydroxylated bile acid disulfates were also prepared. The nuclear magnetic resonance spectral data for bile acid disulfates and related compounds are tabulated.View full abstractDownload PDF (959K) -
JUN-ICHI ANZAI, MASAHIKO SHIMADA, HONGDA Fu, TETSUO OSA1987 Volume 35 Issue 11 Pages 4568-4573
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA silver wire electrode coated with a poly (vinyl chloride) /tri-n-dodecylamine composite membrane was used to fabricate potentiometric enzyme sensors. The coated Ag electrode was further covered with a penicillinase or urease membrane to make a penicillin or urea sensor, respectively. The penicillin sensor was useful for determining penicillin at concentrations of millimolar level. Some operating variables such as pH and ionic concentration of the working buffer of the sensor were examined. The urea sensor could be used to determine urea in human blood.View full abstractDownload PDF (631K) -
YOHJI HAYASHI, KIYOSHI ZAITSU, YOSUKE OHKURA1987 Volume 35 Issue 11 Pages 4574-4578
Published: November 25, 1987
Released on J-STAGE: February 12, 2010
JOURNAL FREE ACCESSA sensitive assay for purine nucleoside phosphorylase (PNP) in human erythrocytes is described. Erythrocyte lysate is incubated with the substrate inosine in the presence of phosphate for the enzyme reaction, and the resulting mixture is deproteinized with perchloric acid and neutralized. The supernatant containing the reaction product, hypoxanthine, is applied to a flow-injection system in which immobilized enzyme columns of xanthine oxidase, urate oxidase and horseradish peroxidase are connected in series in that order in the flow line. Hydrogen peroxide formed in the enzymatic conversion of hypoxanthine is measured fluorimetrically by reaction with 3- (p-hydroxyphenyl) propionic acid in the system. The lower limit of determination (signal-to-noise ratio=5) for hypoxanthine is 0.3 pmol in a 20-μl injection volume, which corresponds to a PNP activity of 0.117 μmol/min/ml erythrocytes. This method permits the assay of PNP in only 10 nl of human erythrocytes in 50 μl of erythrocyte lysate.View full abstractDownload PDF (599K) -
TSUTOMU MIMURA, HIROSHI NAKAJIMA, YASUHIRO KOHAMA, KAZUTAKE TSUJIKAWA, ...1987 Volume 35 Issue 11 Pages 4579-4584
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTwo series of bis [2- (E-2-alkenoylamino) ethyl] disulfides (compds. I) and 2- (E-alkenoyl-amino) ethyl carbamoylmethyl sulfides (compds. II) were synthesized from 2-trans unsaturated fatty acids (C6 : 1-C14 : 1) and cystamine, and their effects on carrageenin-induced paw edema were studied. Several of compds. I and II showed significant anti-edema activity at a dose of 25 mg/kg, i. p. These derivatives were much more potent than the starting materials. The alkene chain length influenced the activity. The compounds (compds. I-3, I-8, II-3 and II-8) with C8 : 1 and C13 : 1 fatty acids showed the highest activity in both series. Compounds I-3 and II-3 with the C8 : 1 fatty acid were also effective when administered orally at a dose of 10 mg/kg.View full abstractDownload PDF (770K) -
TSUTOMU MIMURA, HIROSHI NAKAJIMA, YASUHIRO KOHAMA, MASARU OKABE, KAZUT ...1987 Volume 35 Issue 11 Pages 4585-4591
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe anti-inflammatory action of bis [2- (E-2-octenoylamino) ethyl] disulfide (compd. I-3) and 2- (E-octenoylamino) ethyl carbamoylmethyl sulfide (compd. II-3) was evaluated in various experimental inflammation models. By using the xylene ear method in mice, the bradykinin-induced capillary permeability test in rat skin and the ultraviolet erythema method in guinea pigs, it was demonstrated that compd. I-3 had a significant inhibitory effect on the first phase of inflammation, but compd. II-3 did not. It was also shown that leucocyte emigration into the pouch fluid (the second phase), which accumulated after carboxymethyl cellulose injection in rats, was suppressed by the administration of both compounds. Moreover, granuloma formation (the third phase) generated by the felt pellet or croton oil method in rats was reduced by both compds. I-3 and II-3. Successive administrations of compd. II-3 caused hypertrophy of the spleen and thymus and atrophy of the kidney, but similar administrations of compd. I-3 did not.View full abstractDownload PDF (869K) -
TADAKAZU TOKUMURA, YOSHIHARU MACHIDA, YUKI TSUSHIMA, MASANORI KAYANO, ...1987 Volume 35 Issue 11 Pages 4592-4596
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIntestinal absorption of d-α-tocopherol from four model preparations was investigated after oral administration to beagle dogs. The bioavailability of d-α-tocopherol from the model preparations was evaluated by determination of the plasma level after oral administration. It was found that the absorption of d-α-tocopherol was not affected by food, and that the difference in dosage forms caused a difference in bioavailability. The tablet showed lower availability than capsules filled with oily solution.View full abstractDownload PDF (771K) -
KIYOSHI SAKAI, TOSHIKO YAMANE, YUKIKO SAITOH, CHIE IKAWA, TOSHIAKI NIS ...1987 Volume 35 Issue 11 Pages 4597-4604
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSOral administration of ethanol to rats at a dose of 3 g/kg decreased the alcohol dehydrogenase (ADH) activity in liver cytosol. The effects of water extracts of eight crude drugs, which are believed to have protective activities against alcohol toxicity, on the blood ethanol concentration and on the ADH activity in liver cytosol were examined. Water extracts of these crude drugs caused a rapid elimination of ethanol from the blood of normal rats when they were administered orally at 30 min before oral ethanol administration or simultaneously with ethanol. The rapid elimination of ethanol seems to be due to the effect of the water extracts in inhibiting the decrease of ADH activity in rat liver cytosol, and in supplementing nicotinamide adenine dinucleotide (a coenzyme in ethanol metabolism). Among the eight crude drugs, water extracts of only three crude drugs (Mori Albae Fructus, Alpiniae Katsumadai semen and Dolichoris semen) decreased the blood ethanol concentration and inhibited the decrease of ADH activity in liver cytosol when they were administered at 30 min after ethanol. Water extracts of the other crude drugs did not accelerate the ethanol elimination or inhibit the decrease of the ADH activity when administered 30 min after ethanol.View full abstractDownload PDF (1009K) -
HIROKAZU OKAMOTO, HIROKO TSUKAHARA, MITSURU HASHIDA, HITOSHI SEZAKI1987 Volume 35 Issue 11 Pages 4605-4608
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effects of five new compounds containing an azacyclo ring and a terpene or an alkyl chain, i. e., 1-geranylazacyclohexan-2-one (6GU), 1- (3, 7-dimethyloctyl) azacycloheptan-2-one (7GS), 1- (3, 7, 11-trimethyldodecyl) azacycloheptan-2-one (7FS), 1-geranylgeranylazacycloheptan-2-one (7GGU), and 1-geranylgeranylazacyclohexan-2-one (6GGU), on percutaneous penetration of mitomycin C (MMC) through rat skin in vitro were investigated in comparison with those of 1-farnesylazacycloheptan-2-one (7FU) and 1-dodecylazacycloheptan-2-one (Azone). In an in vitro diffusion experiment, 6GU, 7GS, 7FU, 7FS, 7GGU, 6GGU, and Azone significantly enhanced MMC penetration through rat skin compared with the control. The size of the azacyclo ring had little effect on the potency of these penetration enhancers. On the other hand, the changes in the length of the hydrophobic chain resulted in some variation in the activity of these compounds. Azone and 7FU, which have a hydrophobic chain of length of twelve carbons, were the most effective among enhancers with an azacycloheptanone ring, and 7GGU, with the longest hydrophobic chain, showed the weakest MMC penetration-enhancing activity. Among the compounds with an azacyclohexanone ring, 6GGU (with a longer hydrophobic chain) was more effective than 6GU (with a shorter hydrophobic chain). Saturation of the double bonds of the farnesyl group of 7FU decreased the enhancing ability.View full abstractDownload PDF (585K) -
YOSHINOBU NAKAI, KEIJI YAMAMOTO, KATSUHIDE TERADA, DAIICHI WATANABE1987 Volume 35 Issue 11 Pages 4609-4615
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new method for preparing a solid inclusion compound was developed. A physical mixture of benzoic acid and α-or β-cyclodextrin (CD) or the ground mixture was sealed in a container after adsorbing a definite amount of water vapor, then heated to a temperature ranging from 43 to 142 °C. The results of powder X-ray diffraction and infrared spectroscopy showed that the crystalline inclusion compound was produced when the container was heated at over 70°C. The combining molar ratio of benzoic acid to α-CD in the inclusion compound prepared by this method was higher than that obtained by the coprecipitation method. Physical mixtures of benzoic acid and α-or β-CD were also sealed in a stainless steel vessel under nitrogen gas pressure, then heated to 127 °C. The pressurized samples had a higher combination ratio than the non-pressurized samples.View full abstractDownload PDF (832K) -
MASAKAZU IWAI, ISAO KOHDA, CHIKARA FUKAYA, YOICHIRO NAITO, KAZUMASA YO ...1987 Volume 35 Issue 11 Pages 4616-4625
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSBis [2- (E-2-alkenoylaminoethyl)] disulfides (I) and 2- (E-2-alkenoylamino) ethyl carbamoylmethyl sulfides (II) with various alkenyl chain lengths were synthesized and their inhibitory effects on gastric secretion in rats were compared. There was a relationship between the alkenyl chain length of a series of sulfide derivatives (II) and their biological activities (C10 and C11 alkenyl derivatives were the most effective compounds). On the other hand, variation of the alkenyl chain length did not affect the anti-ulcerogenic activity of the disulfide derivatives (I). The derivatives (II) showed stronger biological activity than (I) when the same alkenyl group was present in both.
The administration of 2- (E-2-decenoylamino) ethyl carbamoylmethyl sulfide (II-5) or 2- (E-2-undecenoylamino) ethyl carbamoylmethyl sulfide (II-6) at a dose of 20 mg/kg (i.p.) caused significant inhibition of various experimental ulcerations caused by stress, aspirin and HCl-ethanol. Oral administration of both acetamides (II-5, II-6) also caused 50-60% inhibition of ulceration in the water-immersion stress model at a dose of 20 mg/kg, although the activity was not as strong as that after i.p. injection. An improvement in anti-ulcerogenic activity was observed when acetamides were administered as a suspension in 10% HCO-60. Both acetamides (II-5, II-6) caused a dose-dependent decrease of the ulcer index of restrained and water-immersion stress-loaded rats in the dosage range from 0.5 mg/kg p.o. to 5 mg/kg p.o. The lethal dose 50% values (LD50) for both acetamides were over 8 g/kg (p.o. or i.p.).View full abstractDownload PDF (1502K) -
KYOKO TAKAHASHI, TADANORI MAYUMI, TAKEO KISHI1987 Volume 35 Issue 11 Pages 4626-4631
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIn order to elucidate the biochemical mechanism by which doxorubicin (DX) induces cumulative dose-dependent cardiomyopathy, the effect of DX on beating and on lipid peroxide level in myocardial cells was investigated by using a mouse myocardial cell culture system. Inhibition by DX of the beating of cultured myocardial cells was dose-and exposure time-dependent. When incubated with DX for 0.5 h, the number of beating cells decreased to 74% at 172 μM, 52% at 345 μM and 37% at 517 μM, and the lipid peroxide level in the cells increased significantly at 345 μM DX or more. At the low dose of 3.5 μM DX, though the number of beating cells decreased to 72% at 24 h, the lipid peroxide level in the cells was about the same as that without DX at 24 h, and increased to about 1.5 times that of the control at 48 h. Under the same conditions as above, 120μM α-tocopherol (Toc) added in advance of the treatment reduced by 86% the lipid peroxidation by DX, but did not protect the beating from DX toxicity. In contrast, 120 μM coenzyme Q10 (CoQ10) reduced the lipid peroxidation by only 33%, but increased the number of beating cells at 48 h from 42% to 68%. We conclude that the lipid peroxidation by DX does not initiate the beat inhibition of cultured myocardial cells, and that the protective effect of CoQ10 on beating is also based on biochemical actions other than reduction of the lipid peroxidation.View full abstractDownload PDF (947K) -
TSUYOSHI SATOH, ATSUSHI SUGIMOTO, KOJI YAMAKAWA1987 Volume 35 Issue 11 Pages 4632-4636
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSMagnesium chloride in alcohols was found to be effective to promote the opening of α, β-epoxy sulfoxides, giving a variety of compounds such as α-chloro ketones, α-alkoxy ketones, or α, β-unsaturated ketones. The products of the reaction were dependent upon the combination of the substituents on the epoxy group of α, β-epoxy sulfoxides, magnesium salt, solvent, and reaction conditions.View full abstractDownload PDF (593K) -
HIROSHI OHTAKA, TOSHIRO KANAZAWA, KEIZO ITO, GORO TSUKAMOTO1987 Volume 35 Issue 11 Pages 4637-4641
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS1-Benzyl-4-diphenylmethylpiperidine derivatives were prepared to investigate the role of the nitrogen atom in their cerebral vasodilating activity. The pharmacological test results revealed that the piperidine derivatives are roughly equipotent to the piperazine derivatives in our test system. Structure-activity analyses are presented.View full abstractDownload PDF (699K) -
YASUKO ISHII, HISAYUKI TANIZAWA, YOSHIO TAKINO1987 Volume 35 Issue 11 Pages 4642-4644
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA procedure for assay of barbaloin by thin layer chromatography (TLC) -densitometry was developed. The method is based on measuring the yellow-green fluorescence, which is produced by the reaction of barbaloin and borax (Schoutelen's reaction), on the TLC plate with a fluorophotometer. The limit of detection was about 0.01 μg of barbaloin, corresponding to about 0.033 μg/ml of barbaloin in rat serum. This method was applied for the determination of barbaloin in serum after oral administration of barbaloin (100 mg/kg) to rats. The serum concentration of barbaloin was extremely low; the peak concentration was only 0.34 μg/ml.View full abstractDownload PDF (351K) -
REIKO IWAOKU, MASAHIRO NAKANO1987 Volume 35 Issue 11 Pages 4645-4649
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSDissolution and permeation patterns of phenobarbital (PB) from basic amino acid and choline salts of PB indicated that drug dissolution from the salts was faster than that of PB itself. Release of the drug from Vosco H15 suppositories containing the salts was faster than that from the suppository containing PB itself. After rectal administration of suppositories containing the salts to rabbits, the blood levels were significantly (p < 0.05) higher than those following administration of the suppository containing PB itself during a period from 30 min to 2 h.View full abstractDownload PDF (565K) -
KAZUMOTO CHIBA, SATOSHI KIKUCHI, Kouzou MINO, SEIKUN NISHIMURA, SHOZO ...1987 Volume 35 Issue 11 Pages 4650-4655
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effects of three non-steroidal anti-inflammatory drugs, ibufenac, sulindac and mepirizole, on the renal excretion of sulfamethizole in rats were investigated, in order to clarify the mechanisms involved. The clearance ratio of sulfamethizole was markedly decreased after infusion of ibufenac, while sulindac or mepirizole had no effect on the clearance ratio of sulfamethizole. From this result, it is speculated that the decrease of renal excretion of sulfamethizole caused by ibufenac is mainly due to competitive interaction between sulfamethizole and ibufenac at the renal secretory level. The correlation between the chemical structures of some anionic non-steroidal anti-inflammatory drugs and the characteristics of renal tubular transport is discussed.View full abstractDownload PDF (730K) -
KIYOMI KIKUGAWA, TAKAMI NAKAHARA, KEIZO SAKURAI1987 Volume 35 Issue 11 Pages 4656-4660
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS1, 4-Disubstituted-1, 4-dihydropyridine-3, 5-dicarbaldehydes, models of fluorogens in age pigments, show a high intensity of fluorescence comparable to that of quinine sulfate. Relationships between the structures and fluorescence emission of the 1, 4-dihydropyridine derivatives were studied. Loss of substituents at the 1- or 4-positions had little effect on the fluorescence. Reduction of one of the aldehyde groups to an alcoholic group greatly decreased the fluorescence intensity. When the aldehyde groups were replaced by acetyl groups, the fluorescence was greatly decreased. A derivative without aldehyde or carbonyl groups at the 3- and 5-positions was virtually nonfluorescent. Thus, the aldehyde groups at the 3- and 5-positions are requisite for the high intensity of fluorescence of the 1, 4 dihydropyridines.View full abstractDownload PDF (663K) -
FUMIKO ABE, TATSUO YAMAUCHI1987 Volume 35 Issue 11 Pages 4661-4663
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA pyrrolizidine alkaloid was isolated from the stems of Parsonsia laevigata ALSTON, a plant upon which the larvae of Idea leuconoe ERICHSON feed, and its structure was determined to be 1- (2 'S, 3 'S) -2 ', 3 '-dihydroxy-2 '-isopropylbutanoyloxymethyl-5, 6-dihydropyrrolizin-7-one.View full abstractDownload PDF (473K) -
Junya Okada, Sadao Kondo1987 Volume 35 Issue 11 Pages 4664-4667
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe major radioactive components found in pig adipose tissue after successive administration of the macrolide antibiotic 14 C-sedecamycin were isolated and chemically identified. Eighty-nine percent of the whole radioactivity in the adipose tissue was extracted into the lipid fraction, and 82% of the lipid radioactivity was recovered in the fatty acid fraction, 92% of which was found in palmitate, oleate, and stearate. No significant radioactivity was found in linoleic acid. These results indicate that some metyl carbons of sedecamycin are incorporated into fatty acids, presumably via the usual pathway of de novo biosynthesis in mammals.View full abstractDownload PDF (380K) -
Shin-ichiro Sakai, Sumphan Wongseripipatana, Dhavadee Ponglux, Masaki ...1987 Volume 35 Issue 11 Pages 4668-4671
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSStructures of the new indole alkaloids, 19- (Z) -akuammidine, 16-epi-voacarpine, 19-hydroxydihydrogelsevirine isolated from the root of Gelsemium elegans have been determined by the spectral method, X-ray analysis and chemical correlation. Koumidine was revised to show the 19- (Z) ethylidene configuration in the structure.View full abstractDownload PDF (420K) -
Takuo Chiba, Takenori Ishizawa, Jun-ichi Sakaki, Chikara Kaneko1987 Volume 35 Issue 11 Pages 4672-4675
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSerythro-3-Hydroxyamino-2-alkylbutanoate and its derivatives were prepared stereoselectively by reduction of the oximes of the corresponding β-ketoesters with sodium cyanoborohydride in acidic media. Cyclization of the β-amino acids obtained by reduction and successive hydrolysis gave 3, 4-cis-substituted azetidin-2-ones.View full abstractDownload PDF (496K) -
Haruki Sashida, Mamoru Kaname, Takashi Tsuchiya1987 Volume 35 Issue 11 Pages 4676-4679
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe photolysis in the presence of sodium methoxide of the 4-azidoquinolines (5a-g) having a carbonyl group or its analogue in the 2- or 8-position resulted in ring expansion to give the stable N-unsubstituted 1H-1, 4-benzodiazepines (6a-g). These were assumed to be stabilized by intramolecular hydrogen bonding between the NH and the 2- or 9-acyl groups. It is known that the N-unsubstituted 1H-1, 4-benzodiazepines having no acyl group are too unstable to be isolated.View full abstractDownload PDF (389K) -
Kiyoshi Iwagoe, Sanetaka Kodama, Tenji Konishi, Shiu Kiyosawa, Yasuhir ...1987 Volume 35 Issue 11 Pages 4680-4682
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSNew bi- and tri-2- (2-phenylethyl) chromones, tentatively named AH15 and AH18 were isolated from Agalwood “Jinko” and their structures were determined.View full abstractDownload PDF (351K) -
Hitoshi Hori, Guo-Mao Pang, Kenzo Harimaya, Yoichi Iitaka, Seiichi Ina ...1987 Volume 35 Issue 11 Pages 4683-4686
Published: November 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSRegelidine (1), a new nicotinoyl sesquiterpene alkaloid, was isolated from the roots of Tripterygium regelii. The structure of 1 was determined on the basis of 1H-, 13C-NMR spectrometry and X-ray crystallography. The absolute configuration of 1 was deduced unambiguously by the anomalous dispersion method.View full abstractDownload PDF (458K)
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