YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Volume 110, Issue 9
Displaying 1-11 of 11 articles from this issue
  • Toshihiko OZAWA
    1990 Volume 110 Issue 9 Pages 617-638
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    One of the active oxygen species, superoxide (O2-), was generated by the electrolytic reduction of molecular oxygen in acetonitrile. O2- was determined by the ultraviolet (UV) (λmax/nm=255, ε=1.48×103 M-1cm-3) and the electron spin resonance (ESR) (g⫽=2.083, g=2.008) spectrum. O2- could easily react with tocopherols (vitamin E and its derivatives) to give the corresponding chromanoxyl radicals of which structures were determined by ESR. ESR studies of the reactions of O2- with tocopherols or their model compounds indicate that the radical concentrations from tocopherol models correlate with the physiological activities of the tocopherols. O2- could also react with some biologically active quinones such as vitamin K8 and vitamin E quinone to give the corresponding semiquinone radicals. The fact that vitamin E quinone, an irreversible metabolite of vitamin E, was reduced by O2- to the semiquinone radical suggests that, like vitamin E, vitamin E quinone may also scavenge O2- and protect living cells from the effects of O2- in a hydrophobic environment. Further, O2- could react with some metalloporphyrins. In this case, non-redox metalloporphyrins such as Zn (II) TPP (TPP : tetraphenylporphine), Cd (II) TPP, Mg (II) TPP generated the superoxide adduct by the reaction with O2-. On the other hand, redoxactive metalloporphyrins such as Cr (III) TPP·Cl, Mn (III) TPP·Cl, Co (II) TTP (TTP : tetra-p-tolylporphine) and Co (III) TTP·Cl underwent the addition and/or redox reactions with O2-. Another active oxygen species, hydroxyl radical (OH·), was first detected from some copper (II) coplexes such as Cu (en)2 (en : ethylenediamine) with hydrogen peroxide (H2O2) by ESR spin trapping and thiobarbituric acid (TBA) methods. Further, by using Cu (en)2-H2O2 system the most active OH·scavenger was determined. This Cu (en)2-H2O2 system will be useful for determing the antioxidant ability against OH·.
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  • Ei MOCHIDA, Nobuhisa OGAWA, Hiroyuki SHINKAI, Takashi KUDO
    1990 Volume 110 Issue 9 Pages 639-651
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Determination of estrogen concentrations in the urine is widely utilized for a variety of purposes, such as the assessing of fetoplacental unit function and ovarian function, and the monitoring of follicle in inducing ovulation in the treatment of infertility. Since hapten antigens such as estrogen have low molecular weight, unlike high molecular substances, they do not form visible agglutination of antigen-antibody reaction, so there has been no other choice but to depend on radioimmunoassay for the determination of estrogen concentrations. However, radioimmunoassay requires special facilities and apparatus and is complicated in procedure, and these drawbacks have prevented the estrogen assay from routine tests in spite of clinical usefulness. As a result of various researches, a new immunochemical principle called competitive agglutination inhibition reaction has been developed for the determination of hapten concentrations, and succeeded in putting this principle to practical use with a fetoplacental unit function test kit (Estrotec slide test) and highly sensitive semi-quantitative analysis kits for urinary estrogen (Hi-estrotec and Hi-estrotec slide).
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  • Toshio MIYASE, Akira UENO, Tetsuya KITANI, Hiromi KOBAYASHI, Yuzo KAWA ...
    1990 Volume 110 Issue 9 Pages 652-657
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    A new iridoid glycoside, stachysoside A (2) and two new phenylethanoid glycosides, stachysosides B (3) and C (5) have been isolated from the tuber of Stachys sieboldii MIQ. (Labiatae), together with six known glycosides. The structures of new compounds were established on the basis of chemical evidence and spectral data.
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  • Yoshiko INAMOTO, Kazuo SAKANE, Toshiaki KAMIMURA, Takao TAKAYA
    1990 Volume 110 Issue 9 Pages 658-664
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The synthesis, antibacterial activity and oral absorption of the 7β-[(Z)-2-aryl-2-hydroxyiminoacetamido]-3-vinylcephalosporins (Ia-e) are described. All of these compounds exhibited excellent activity against Staphylococcus aureus. Against Gram-negative bacteria FK482 exhibited more excellent activity than the other compounds (Ia-e). These compounds except Ie showed good oral absorption. The relationship between the oral absorption rates and the lipophilicity of these cephalosporins is discussed.
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  • Youji OKADA, Haruo OKAMJIMA, Misaka TERAUCHI, Hirokazu KONISHI, IMin L ...
    1990 Volume 110 Issue 9 Pages 665-672
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    As a continuation of the study on the biological roles of furan fatty acids (F acids) which are still vague, their inhibitory effects on the hemolysis of erythrocytes induced by singlet oxygen were examined. Hemolysis proceeded smoothly in the absence of F acids, but was suppressed significantly and dose dependently in their presence. No significant differences in inhibitory effects on the hemolysis induced by singlet oxygen between tetra-alkylsubstituted F acid (F3) and di-alkylsubstituted F acid (NMF) could be detected. The acids underwent oxidation to give the corresponding diketo-enes, indicating a reaction with singlet oxygen to suppress hemolysis. The inhibitory effects of F acids on hemolysis were compared with those of known singlet oxygen quenchers such as dimethylfuran, α-tocopherol, ascorbic acid and uric acid and F acids were found to be the most effective quenchers.
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  • Kazuya OOI, Toshiki OHKUBO, Hajime KAWASAKI, Minoru SAKURAI
    1990 Volume 110 Issue 9 Pages 673-677
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The effect of etoposide-induced deoxyribonucleic acid (DNA) damage and its effect on nucleotide pools were examined in murine leukemia L1210 cells. Etoposide (15 mg/kg) was administered intraperitoneally on the third day after peritoneal inoculation of 1×106 L1210 cells. The dosage of etoposide procduced 175% of the increase of lifespan as described previously. Strand breaks in DNA occurred within 10 min after i.p. injection, but as the time interval between injection and removal of the cells from the mice was elongated to 1 and 3 h, the continuous repairing of DNA was observed. At 6 h after the injection, the maximum concentration of DNA was located in the vicinity of that of control. In our previous study, ara-C was most effective when given at 3 to 6 h after the administration of etoposide. The sensitivity to ara-C might increase during the repairing period from the etoposide-induced DNA damage. All four dNTPs increased progressively within 6 h up to 3-fold of control. The changes in rNTPs were similar, but the degree of the changes was smaller than that of dNTPs. These changes in dNTPs and rNTPs would be an important factor for the combination to determine the antitumor effect of etoposide and nucleoside analogues.
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  • Hironobu SHIBATA, Fumiaki SANO, Shinobu FURUSAWA, Hiroaki KAWAUCHI, Ke ...
    1990 Volume 110 Issue 9 Pages 678-681
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The intracellular uptake, retention and cytotoxicity of pirarubicin, an anthracycline derivative, combined with chlorpromazine were investigated in doxorubicin-resistant mouse P388 leukemia (P388/DXR) cells. The number of viable cells was determined by the dye exclusion method. Chlorpromazine increased the cytotoxicity of pirarubicin in a dose-related manner in P388/DXR cells. A similar dose-response relationship was observed for chlorpromazine in increasing net intracellular pirarubicin accumulation. The accumulation was based on block of enhanced pirarubicin efflux from resistant cells by chlorpromazine. However, chlorpromazine did not affect cytotoxicity or transport of pirarubicin in the drug-sensitive cell line. The possible mechanisms of the restoration of pirarubicin sensitivity in P388/DXR cells by chlorpromazine are discussed.
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  • Satoru IKEDA, Masahiro KANEKO, Yoshio KUMAZAWA, Chiaki NISHIMURA
    1990 Volume 110 Issue 9 Pages 682-687
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Effect of Hochu-ekki-to (HET) on the number of peripheral leukocytes (PL) and their functions in cyclophosphamide (CY)-treated or γ ray-irradiated mice was investigated. By treatment of mice with anticancer agent CY or γ ray irradiation, unfavorable side effects usually occured to impair hematopoietic organs, causing bone marrow disorder. However, it was significantly protected by oral administration of HET (1 g/kg/d) to CY-treated or γ ray-irradiated mice. The numbers of neutrophils and monocytes in PL were restored to the normal level, and colony-stimulating factor (CSF) was induced in the sera of mice by HET in a dose-dependent manner. The induction of serum CSF reached a peak at 3h after HET administration. Colony-forming unit of bone marrow cells in the spleen adoptively transfered into syngeneic mice, that is defined as CFU-S, was extremely reduced by CY-treatment. However, when HET was orally administered, CFU-S of CY-treated mice was markedly stimulated, suggesting that bone marrow cells were reactivated for further proliferation and mobilization. HET enhanced other leukocyte functions in CY-treated mice; i.e., superoxide production of neutrophils and phagocytic activity of macrophages. Thus, oral administration of HET to CY-treated mice enforced protection against Pseudomonas aeruginosa infection.
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  • Toshiaki TANAKA, Koichi METORI, Satoshi MINEO, Hitoshi MATSUMOTO, Tosh ...
    1990 Volume 110 Issue 9 Pages 688-692
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The inihibitory activities of 44 anthraquinones against bacterial collagenase were assayed in vitro. Emodin (1, 6, 8-trihydroxy-3-methylanthraquinone, 41) was the most potent active inhibitor among them (IC50; 4.0×10-5M). The type of inhibition by 41 was found to be a mixture type by use of Lineweaver-Burk plots. Since the inhibitory activities of anthraquinones were not affected by the concentration of Ca2+ in the assay medium, it is considered that the inhibitory mechanism is not a chelate effect on Ca2+. In mono-substituted anthraquinones, the compounds which have a substituent (OH or SO3Na) at 2-position show more potent inhibitory activity than the corresponding 1-substituted compound.
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  • Hiroyuki FUJINO, Shujiro GOYA
    1990 Volume 110 Issue 9 Pages 693-696
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    This paper describes the preparation of the acid fluoride, 7-dimethylaminocoumarin-3-carbonyl fluoride (MACF), and a preliminary investigation as a precolumn fluorescence derivatization reagent for primary and secondary amines in high performance liquid chromatography (HPLC). Amines were derivatized quantitatively into the corresponding fluorescent amides by treating with MACF at 20°C for 30 s in aqueous 70% acetonitrile solution in the presence of 4-dimethylaminopyridine. The derivatives were subjected to HPLC on a TSK gel ODS-80TM column (4.6 mm i.d.×250mm, 5μm) with methanol-water (10 : 3) as the mobile phase and monitored with an excitation wavelength of 415 nm and an emission wavelength of 470 nm. The detection limits of amines were 0.6-4.6 pmol for an injection volume of 10μl.
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  • Makoto SUZUKI, Noriko KUMAZAWA, Setsuko OHTA, Asahi KAMOGAWA, Masato S ...
    1990 Volume 110 Issue 9 Pages 697-701
    Published: September 25, 1990
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Protective effects of 14 kinds of antioxidant on liver injury induced by carbon tetrachloride (CCl4) were investigated in terms of serum enzyme activities and bilirubin concentration. Consequently, the significant protective effects were found in sesamol, ellagic acid, cysteamine and cysteine. These antioxidants clearly decreased the lipid peroxide in the liver tissue. The protective effects on CCl4-induced liver injury in vivo were independent of the inhibitory activities on lipid peroxidation in hepatic mitochondria fraction in vitro.
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