YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Volume 106, Issue 11
Displaying 1-16 of 16 articles from this issue
  • KEIICHIRO FUWA, KIN-ICHI TSUNODA
    1986 Volume 106 Issue 11 Pages 951-963
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The present status of spectrochemical analysis is discussed after a brief review on the role of trace elements in organisms. In particular, inductively coupled plasma emission spectrometry (ICP-ES) and graphite furnace atomic absorption spectrometry (GFAAS), which are ones of the most convenient and sensitive analytical methods for trace elements, are reviewed, and the problems rising to chromium determination in biological samples are discussed in detail. Furthermore, ICP/mass spectrometry (ICP/MS) and colorimetry using long capillary cells are mentioned as possible new methods for the next generation of trace elemental analysis.
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  • TOHRU HINO
    1986 Volume 106 Issue 11 Pages 964-981
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Biomimetic synthesis of tryptophan metabolites and some indole alkaloids from tryptophan are summarized. Dye-sensitized photooxygenation of tryptophan gave 3a-hydroperoxy-pyrroloindole (12) in aqueous solution, formylkynurenine in acetic acid-sodium carbonate buffer (pH 7) and 5-hydroxy-formylkynurenine (16) in phosphate buffer (pH 8). On the other hand, dye-sensitized photooxygenation in formic acid or Tl (III) oxidation of tryptamine (21) and the diketopiperazine (25) gave oxidative dimers which furnished (±) folicanthine on reduction and (-)-ditryptophenaline. The dye-sensitized photooxygenation of the indoloquinolizidine (29) gave 2-acylindole (30). Cyclic tautomers of tryptophans (40, 42, 44) obtained by dissolving tryptophans in phosphoric acid have been shown to be a useful intermediate to prepare 5-halo, 5-nitro, 5-hydroxy, 5-methoxy, and 6-methoxytryptophans (47, 50, 52, 55) by the electrophilic substitution or oxidation with lead tetraacetate in trifluoroacetic acid. Biomimetic synthesis of tryptoquivalines, tremorgic micotoxins, from D- and L-tryptophans using oxidative double cyclization of the indole-3-propionic acids (79, 90) as key steps have been discussed.
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  • TAKAO MURAKAMI, HIROSHI WADA, NOBUTOSHI TANAKA, TSUNEHIRO KIDO, HIDEKI ...
    1986 Volume 106 Issue 11 Pages 982-988
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    From the fronds of the following ferns the flavonoid compounds, including three new glycosides, were isolated and their structures elucidated by chemical and spectroscopic methods. From Brainea insignis J. SM. a new flavonol acylglycoside kaempferol 3-O[2-O-(6-O-caffeoyl)-β-D-glucopyranosyl]-β-D-galactopyranoside (I), from Thelypteris palustris SCHOTT a new flavanone glycoside (2S)-5, 7-dihydroxy-6-methylflavanone 7-O-β-D-glucopyranoside (II), cryptostrobin ((2S)-5, 7-dihydroxy-8-methylflavanone), kaempferol 3-O-β-D-glucopyranoside and kaempferol 3-O-β-rutinoside and from Adiantum malesianum GATAK. a new flavonol glycoside kaempferol 3-O-α-D-galactopyranoside (III), vitexin, isovitexin, hyperin (quercetin 3-O-β-D-galactopyranoside) and kaempferol 3-O-β-D-galactopyranoside were isolated.
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  • HIROSHI WADA, TAKAO MURAKAMI, NOBUTOSHI TANAKA, MASASHI NAKAMURA, YASU ...
    1986 Volume 106 Issue 11 Pages 989-994
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    From the fronds of Pseudocyclosorus subochthodes CHING and P. esquirolii CHING, a new flavanone glycoside (2S)-eriodictyol 7-O-methylether 3'-O-β-D-glucopyranoside (I) and maltol 3-O-β-D-glucopyranoside (V) were isolated. Besides them, from the former a new glycoside 5-hydroxymaltol 5-O-α-L-rhamnopyranoside (II) and (2E, 6E)-(10S)-2, 6, 10-trimethyl-2, 6-11-dodecatriene-1, 10-diol (12-hydroxynerolidol) (III) were isolated and from the latter astragalin and shikimic acid were isolated. Their structures were elucidated by chemical and spectroscopic methods.
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  • YASUO FUJIMURA, YUGO IKEDA, ISAO MATSUNAGA
    1986 Volume 106 Issue 11 Pages 995-1001
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    3-Phenylindazoles with substituents at 1 and 5-positions were synthesized and their pharmacological activities (reversal of reserpine-induced hypotherimia and barbiturate potentiation) were studied. 5-Methyl-1-[3-(dimethylamino)propyl]-3-phenyl-1H-indazole (FS-32) and 5-methyl-1-[3-(methylamino)propyl]-3-phenyl-1H-indazole (FS-97) were found to be effective in preventing hypothermia induced by reserpine in analogy with Imipramine.
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  • YASUO FUJIMURA, YASUYUKI SHIRAKI, YOSHIHARU NAWATA, ISAO MATSUNAGA
    1986 Volume 106 Issue 11 Pages 1002-1007
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    2, 3-Dihydro-1H-pyrazolo[1, 2-a]indazolium halides were synthesized and their bronchodilating activities were studied. 2, 3-Dihydro-7-methyl-9-phenyl-1H-pyrazolo[1, 2-a]indazolium bromide (7m, FKK) was found to be effective in reducing the tracheal intraluminal pressure (bronchodilation).
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  • KUNIRO SAITO, KAZUYOSHI OKUTANI
    1986 Volume 106 Issue 11 Pages 1008-1016
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    A series of 3-carboxamides of pyrido[4, 3-e]-1, 2-thiazine was synthesized and evaluated for antiinflammatory activity in carrageenin rat paw edema. These compounds were prepared by cyclization of N-(substituted carbamoylmethyl)-4-methoxycarbonyl-N-methylpyridine-3-sulfonamides in the presence of sodium methoxide. Some of them were prepared alternatively by aminolysis of pyrido[4, 3-e]-1, 2-thiazine-3-carboxylic ester with aryl- and heteroarylamines. Among the compounds tested, N-phenyl- and N-(2-pyridyl)-carboxamides showed a potent antiinflammatory activity and a weaker action in causing gastrointestinal lesions than that of the reference drug, piroxicam.
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  • TADASHI SUGIYAMA, KIMIO YASUDA, TAMAHIKO FURUZAWA, SHIRO YOSHIOKA, KIK ...
    1986 Volume 106 Issue 11 Pages 1017-1020
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    A sensitive and accurate gas chromatographic method was developed for the determination of isosorbide dinitrate (ISDN) in the human plasma. ISDN was extracted from the plasma with n-hexane in alkaline conditions and analysed by gas chromatography with an electron capture detector. As ISDN has high adsorptive activity on glass, fused silica capillary column with low surface-activity was used for the separation of ISDN. Isomannide dinitrate was used as an internal standard. This procedure provided a linear calibration curve ranging 0.25 to 16.0 ng of ISDN/ml of the plasma. The lower limit of detection for ISDN was 0.1 ng/ml of plasma. This method may be used more widely for the clinical pharmacokinetic study and bioavailability study of ISDN.
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  • YASUYO OKADA, KYOKO KOIZUMI
    1986 Volume 106 Issue 11 Pages 1021-1027
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Cyclosophoraoses (CySs) are unbranched cyclic (1→2)-β-D-glucans, produced by many strains of Agrobacterium and Rhizobium, and their degree of polymerizations (DPs) vary from 17 to at least 40. Among them CyS-A(DP 17), B(DP 18), C(DP 19), D(DP 20), E(DP 21), F(DP 22), G(DP 23), and H(DP 24) predominate. Acid hydrolyses of CyS-A-H were studied in the range of 65 to 95°C. Cyclic and linear (1→2)-β-D-glucans having the same DP in partial hydrolysates were separated by taking advantage of differences in their chromatographic behavior on C18-bonded silica and determined by high performance liquid chromatography on an NH2-bonded silica column. The hydrolyses of CySs were apparent first-order reactions, and an activation energy for each reaction was approximately 30 kcal/mol. The values of rate constants for hydrolyses of CySs decreased in order of CyS-G(DP 23)>E(DP 21)〓B(DP 18)〓H(DP 24)〓F(DP 22)〓D(DP 20)>C(DP 19)>A(DP 17).
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  • MASATO HORIUCHI, HIDEO TAKASHINA, KEN-ICHI FUJIMURA, TADASHI ISO
    1986 Volume 106 Issue 11 Pages 1028-1033
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The reactivity of iodoplatinate with 36 compounds was surveyed. Most of organosulfur compounds such as thiols, disulfides, thioethers, thioketones and compounds having thiazolidine ring reacted with colored iodoplatinate to result in decoloration. However, compounds which contain organosulfur in the molecule as sulfoxide or sulfone group gave weak or no decoloration. Iodoplatinate also reacted with such reductants as nicotinamide adenine dinucleotide phosphate, nicotinamide adenine dinuclaotide and L-ascorbic acid. For the simultaneous determination of (2R, 4R)-2-(o-hydroxyphenyl)-3-(3-mercaptopropionyl)-4-thiazolidinecarboxylic acid (SA446), a thiol group containing angiotensin converting enzyme inhibitor, and its urinary metabolites, the reaction was applied to the postcolumn detection after high performance liquid chromatography (HPLC). Iodoplatinate may be expected as a useful reagent for the postcolumn reaction in HPLC determination of organosulfur compounds and some reductants in biological samples.
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  • KOICHI SAKURAI, TOSHIAKI MIURA, TAKETO OGISO
    1986 Volume 106 Issue 11 Pages 1034-1039
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Protective effects of several hydroxyl radical (HO·) scavengers and superoxide dismutase on alloxan-induced diabetes were studied in vivo. Thiourea, methylthiourea, dimethylthiourea and ethanol, HO· scavengers (type 1), which easily cross cellular membranes, protected initial- and permanent-hyperglycemia. In contrast, mannitol and sorbitol (type 2), which can not cross cellular membranes, protected initial-hyperglycemia, but did not protect permanent-hyperglycemia. Furthermore, superoxide dismutase which is not expected to be incorporated into pancreatic β-cell, strongly protected initial-hyperglycemia but partially protected permanent-hyperglycemia. These results suggest that HO·primarily damages the β-cell membranes by acting at or neat a site involved in insulin release, and subsequently damages the intracellular components. From these results, the possible protective mechanism of these scavengers was discussed.
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  • MUNETSUGU KURATA, MITSURU OHSAWA, TOYOYASU KUWAE, ICHIRO YAMAZAKI, NAO ...
    1986 Volume 106 Issue 11 Pages 1040-1044
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Eicosapentaenoic acid (EPA) was injected into the peritoneal cavity of mice, ICR-male mice 6-8 weeks old, and larger numbers of polymorph nuclear leucocytes (PMN, 2-3×107 cells/mouse) were obtained compared with other irritants (thioglycolate and zymosan). From a normal mouse peritoneal cavity, about 2-3×106 cells were collected; populations were : 1.3-1.9×106 macrophages, 0.6-0.9×106 lymphocytes and 1.4-2.1×105 PMNs. Into the peritoneal cavity of mice one of three irritants in the following amounts was injected : 1 ml 3% thioglycolate, 200 mg of zymosan or 0.05 ml of EPA. Then after intervals of 15, 40 or 60 h collected peritoneal exudate cells were counted and stained by using the Wright-Giemsa methods. In EPA groups, after 40 h the percentage of PMNs to total cells were 80-85%, cell numbers changed 1.4-2.1×105 PMNs in normal to 2-3×107 PMNs. Very similar results were obtained when arachidonic acid was injected into mouse peritoneal cavities. EPA- or arachidonic acid-treated PMNs were analyzed for lipid composition. At 24 h after EPA injection, PMNs contained about 20-30% of EPA in lipid fractions. The amount of EPA in phospholipids' fraction changed similarly to that in total lipids. O2- release from EPA-rich PMNs decreased more than that from thioglycolate treated cells. Phagocytotic activity decreased about 50% compared with thioglycolate-treated PMNs.
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  • YUKITOSHI HAYASE, MIHO MURAKAMI, YOSHINARI TAKAGI
    1986 Volume 106 Issue 11 Pages 1045-1049
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    O-Phosphoethanolamine (PEA) was previously shown to have potent colony inhibitory activity for mouse bone marrow cells in a medium composed of calf serum (CS). However, colony inhibitory activity of PEA decreased drastically in a medium composed of fetal calf serum (FCS) or heat treated CS. On the other hand, CS and FCS exhibited phosphatase activity which was heat labile and amine oxidase activity which was heat resistant, though amine oxidase activity of FCS was one-sixth of that of CS. And glycolaldehyde (GA) was detected in the incubation mixture of PEA and CS medium, but not in that of PEA and FCS medium. Ethanolamine (EA), a product of hydrolysis of PEA by phosphatase, inhibited colony formation in a medium composed of CS or heat treated CS, but not a medium composed FCS or heat treated FCS. GA, a product of oxidation of EA by amine oxidase, inhibited colony formation in any medium mentioned above. From these results, it is concluded that PEA is enzymatically converted into GA via EA, and GA thus formed inhibits colony formation.
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  • IKUO JOHNO, MASAYA HASEGAWA, TOSHI-AKI NAKAMURA, TAEYUKI OHSHIMA, SHIK ...
    1986 Volume 106 Issue 11 Pages 1050-1056
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Patients hardly take drug(s) at equal doses and dosing intervals because medicines are usually taken in accordance with each meal. Pharmacokinetic analysis and plasma level simulations of drugs under conditions such as unequal doses and dosing intervals are important to examine clinically the effect and/or adverse effect during drug therapy. We developed a personal computer program, which was written in BASIC language, to calculate pharmacokinetic parameters with unequal doses and dosing intervals. Moreover, we propose new pharmacokinetic parameters which are the sum of periods lower than minimum effective concentration and higher than minimum toxic concentration within a definite period of plasma drug level simulation. These new parameters may be useful to evaluate the individual minimum effective (or toxic) concentration, therapeutic effect, and adverse effect of drugs, if we can get a correlation between these parameters and therapeutic drug effect or adverse effect.
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  • TAKAYUKI MATSUNAGA, KENICHI MIYAMOTO, SHINYA WAKUSAWA, RYOZO KOSHIURA
    1986 Volume 106 Issue 11 Pages 1057-1063
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The influence of isoproterenol (IPN) on the metabolism of mitomycin C (MMC) was studied in rat ascites hepatoma AH130 cells. Exposure of the cells to IPN caused an elevation in the metabolic activity of MMC in the cell sonicates in the absence of the regenerating system of the reduced form of nicotinamide adenine dinucleotide phosphate (NADPH), though did not change the metabolism of MMC in the presence of the NADPH-regenerating system. Intracellular concentrations of NADPH decreased in proportion to the treatment time and the concentration of MMC, but the decrease of NADPH was inhibited by the combined treatment with IPN and MMC. IPN did not influence the activities of the metabolic enzymes of MMC and the NADPH-producing enzymes. IPN did not also change the intracellular amount of vinblastine which was taken up into the cells by passive transport similarly to MMC. From these results, our previous observations that IPN elevated the uptake of MMC into the cells were suggested to result from the enhancement of the metabolic activity but not that of the membrane transport of MMC. The enhancement of the metabolic activity seemed to be due to the increased potency of the cells to regenerate the intracellular NADPH consumed by the metabolism of MMC.
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  • TAKASHI HARAYAMA, REIKO YANADA, KUMIKO IIO, FUMIO YONEDA
    1986 Volume 106 Issue 11 Pages 1064-1067
    Published: November 25, 1986
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The solvent effect in reaction of 1, 3-dimethylthymine epoxide with amines was investigated. The results are summarized in Table I, indicating that the ratio of formation of cis product (2) increases as a solvent becomes more polar. This suggests that a polar solvent stabilizes an ionic intermediate (1B), which reacts with amine to afford the cis product selectively.
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