The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 38 , Issue 7
Showing 1-22 articles out of 22 articles from the selected issue
  • FUMIO NAKAGAWA, TAKAO OKAZAKI, ATSUSHI NAITO, YASUTERU IIJIMA, MITSUO ...
    1985 Volume 38 Issue 7 Pages 823-829
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Griseolic acid, a potent inhibitor of cyclic adenosine 3', 5'-mono phosphate (cyclic AMP) phosphodiesterase (EC 3.1.4.17) was isolated from the cultured broth of Streptomyces griseoaurantiacus SANK 63479. Griseolic acid has an adenine moiety and two carboxyl groups and possesses the molecular formula C14H13N5O8. Griseolic acid inhibited cyclic AMP phosphodiesterase competitively with regard to cyclic AMP, the substrate and the resulting Ki value was 0.26μM. Griseolic acid showed the most potent inhibitory effect on rat aorta cyclic AMP phosphodiesterase among the enzymes of several rat organs tested. The plasma level of cyclic AMP was increased when griseolic acid was subcutaneously injected rats.
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  • SHUJI TAKAHASHI, FUMIO NAKAGAWA, KAYOKO KAWAZOE, YOJI FURUKAWA, SADAO ...
    1985 Volume 38 Issue 7 Pages 830-834
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Griseolic acid, a potent inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase, was isolated from the fermentation broth of Streptomyces griseoaurantiacus SANK 63479. Treatment of griseolic acid with HCl-MeOH gave adenine and pseudo-sugar. The structure of griseolic acid, adenine nucleoside type structure, was elucidated by chemical degradation and X-ray analysis, and was shown to be structure 1.
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  • MORITA IWAMI, SUMIO KIYOTO, MOTOAKI NISHIKAWA, HIROSHI TERANO, MASANOB ...
    1985 Volume 38 Issue 7 Pages 835-839
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    An actinomycete which was isolated from a soil sample produces new antitumor substances. The morphological and cultural characteristics of the strain resemble those of the genera Streptomyces Waksman and Henrici 1943 and Actinomadura Lechevalier and Lechevalier 1970. Cell wall composition analysis showed that strain No. 6049 contained meso-2, 6-diaminopimelic acid in its cell wall, and madurose in whole-cell sugars. No sporangia, zoospores or fragmentations of vegetative mycelium are observed. From these results, strain No. 6049 is designated as Actinomadura pulveracea sp. nov.
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  • SUMIO KIYOTO, MOTOAKI NISHIKAWA, HIROSHI TERANO, MASANOBU KOHSAKA, HAT ...
    1985 Volume 38 Issue 7 Pages 840-848
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The new antitumor antibiotics, FR-900405 and FR-900406, were isolated from the culture broth of Actinomadura pulveracea sp. nov. No. 6049. These compounds which contain sulfur in the molecule, represent a novel class of antitumor agents. R-900405 and FR-900406 are highly active in mice against experimental tumors and exhibit antimicrobial activity against Gram-positive and Gram-negative bacteria and fungi.
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  • T. F. BRODASKY, S. MIZSAK, J. R. HOFFSTETTER
    1985 Volume 38 Issue 7 Pages 849-855
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Mother liquors from steffimycin B crystallizations have been processed to yield steffimycin C, a new member of the steffimycin family of anthracyclines. It has been identified, using spectroscopic methods, as 10-deoxysteffimycin B. Steffimycin C has antibacterial activity only against Streptococcus pneumoniae. Whether steffimycin C is a precursor of steffimycin B or a metabolic reduction product is unknown at this time.
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  • GIUSEPPE CASSINELLI, MARZIA BALLABIO, FEDERICO ARCAMONE, ANNA MARIA CA ...
    1985 Volume 38 Issue 7 Pages 856-867
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The new anthracyclines 7-O-(2, 3, 5-trideoxy-3-C-formyl-α-L-threo-pentofuranosyl) daunomycinone (8) and -adriamycinone (10) have been obtained upon nitrous acid deamination of daunorubicin and doxorubicin respectively. Deamination of the L-ribo analogue of daunorubicin (6) gave a mixture of 2, 3, 6-trideoxy-L-glycero-hexopyranosid-4-ulose (α-L-cinerulosyl) (11) and 2, 6-dideoxy-α-L-arabino-hexopyranosyl (12) glycosides. The corresponding adriamycinone glycosides 13 and 14, obtained by deamination of the doxorubicin L-ribo analogue 7, were found to display an outstanding antileukemic activity in mice.
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  • KEN-ICHI HARADA, NAOHITO TAKEDA, MAKOTO SUZUKI, MITSUO HAYASHI, MASARU ...
    1985 Volume 38 Issue 7 Pages 868-876
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Chemical ionization (CI) mass spectra of new macrolide ntibiotics, mycinamicins are reported. Protonated molecules (MH+) are observed as base peaks in the CI mass spectra of all components. Fragmentations are mainly restricted to the glycosidic linkages and the resulting aglycone and sugar-derived ions appear regularly in their mass spectra. Moreover, characteristic fragment ions involving carbon-carbon bond fission are found in the CI mass spectra of the epoxyenone-containing components, mycinamicins I (1) and II (2). The mechanism for the formation of the ion species is also discussed.
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  • SETSUO HARADA, JUNYA OKADA, MASUO TAKEDA, TOSHIYUKI YAMAZAKI
    1985 Volume 38 Issue 7 Pages 877-885
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Lankacidin-group antibiotics formed inclusion compounds with β-cyclodextrin in molar ratios of about 1:1. These compounds showed remarkably improved water-solubility and stability in aqueous solutions. The structure of the inclusion compounds of lankacidin A is proposed based on the facility of their inclusion with β-cyclodextrin and the results of 1H NMR spectral studies.
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  • YOSHIHISA UMEDA, MAKOTO MORIGUCHI, HIROYUKI KURODA, TERUYA NAKAMURA, H ...
    1985 Volume 38 Issue 7 Pages 886-898
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Many analogues and derivatives of an antitumor antibiotic, spergualin, were synthesized. and the relationships between the structure and the activity against mouse L-1210 tumor were studied. Both modification of the 15-hydroxyl group and alteration of chain-length of the ω-guanidinoacyl moiety affected the activity. 15-Deoxyspergualin (18, 1-amino-19-guanidino-11-hydroxy-4, 9, 12-triazanonadecane-10, 13-dione) and its analogue 25 (1-amino-21-guanidino-11-hydroxy-4, 9, 12-triazauneicosane-10, 13-dione) had strong activity, superior to that of spergualin.
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  • SETSUKO KUNIMOTO, KEIKO MIURA, HIRONOBU IINUMA, TOMIO TAKEUCHI, HAMAO ...
    1985 Volume 38 Issue 7 Pages 899-903
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The cytotoxicity of spergualin on cultured L5178Y cells is dependent on the kind of serum contained in culture media. Spergualin has stronger cytotoxicity to L5178Y cells in calf serum (IC50=2μg/ml) than in horse serum (IC5060μg/ml). This was thought to be caused by amine oxidase in sera. Because calf serum was rich in amine oxidase and horse serum was very poor. Spergualin was found to be oxidized by either calf serum or amine oxidase purified from beef plasma. Aminoguanidine, an amine oxidase inhibitor suppressed the spergualin effect to inhibit the growth of L5178Y cells in calf serum to the level in horse serum. On the other hand, in horse serum the spergualin cytotoxicity was enhanced by addition of amine oxidase. These results suggested to us that spergualin might be inactive in itself and that the amine oxidase-oxidized product might play an essential role in inhibiting the growth of cells.
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  • KATSURO KUBO, TOMOYUKI ISHIKURA, YASUO FUKAGAWA
    1985 Volume 38 Issue 7 Pages 904-911
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Radioactive β-alanine was specifically incorporated into the β-alanine moiety of the C-3 pantetheinyl side chain of the OA-6129 group of carbapenems by Streptomyces sp. OA-6129, while no added radioactive pantothenate was taken up into the mycelia. The extracellular concentrations of β-alanine and pantothenate in the broth of Streptomyces sp. OA-6129 increased with the production of the carbapenems. The production levels of β-alanine and pantothenate markedly differed between carbapenem-producing streptomycetes and nonproducers, with the exception of Streptomyces cattleya, a thienamycin producer, suggesting a possible relation of carbapenem biosynthesis with the levels of β-alanine and pantothenate.
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  • WOLFGANG CULLMANN, WOLFGANG DICK
    1985 Volume 38 Issue 7 Pages 912-919
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    With respect to the selection of β-lactam-resistant variants marked discrepancies between the recently developed cephalosporin HR 810 and other recently developed cephalosporins could be observed: β-lactam resistant subpopulations did not emerge during a 16-hour culture in the presence of the 20-fold minimal inhibitory concentration in a clinical Enterobacter cloacae isolate (2240/81) in contrast to cefoperazone, cefotaxime, ceftriaxone and ceftazidime. Breakdown of the antibacterial agents during the 16-hour period as evaluated by monitoring their levels in the medium was not responsible for selection of β-lactam-resistant subpopulations. The study of affinity of various cephalosporins to the chromosomally mediated β-lactamase of E. cloacae strain 2240/81 revealed low affinity of HR 810 to the enzyme (Ki amounted 4.4×10-3 M). It is suggested that the low affinity of this new agent to the E. cloacae enzyme plays a major role in the lack of selection of resistant subpopulations.
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  • AKIRA ENDO, KENJI HASUM, KENJI HASUMI, KAORU SAKAI, TOMOMI KANBE
    1985 Volume 38 Issue 7 Pages 920-925
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A sesquiterpene named koningic acid has been isolated from a strain of Trichoderma koningii as a potent inhibitor of ATP generation in the glycolytic pathway. From experiments with both cultured mouse carcinoma FM3A cells and isolated enzymes, it was shown that koningic acid is a specific inhibitor of glyceraldehyde 3-phosphate dehydrogenase that catalyzes the conversion of glyceraldehyde 3-phosphate to 3-phosphoglycerate.
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  • MOTOHIRO HINO, OSAMU NAKAYAMA, YASUHISA TSURUMI, KIMIKO ADACHI, TOSHIH ...
    1985 Volume 38 Issue 7 Pages 926-935
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Swainsonine isolated from Metarhizium sp., was found to enhance the activities of the mouse immune system in vitro. Concanavalin A stimulated lymphocyte proliferation and proliferative response in mixed lymphocytes culture, which were suppressed by immunosuppressive factor obtained from serum of sarcoma 180 tumor bearing mouse, were restored to normal levels by the addition of swainsonine. Furthermore, the concanavalin A induced incorporation of [3H] thymidine into mouse spleen cells was remarkably increased by treatment with swainsonine over a wide dose range. From studies using fluorescence activated cell sorting, swainsonine was shown to enhance the expression of concanavalin A receptors of spleen cells.
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  • TOHRU KINO, NORIAKI INAMURA, KUNIO NAKAHARA, SUMIO KIYOTO, TOSHIO GOTO ...
    1985 Volume 38 Issue 7 Pages 936-940
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    We examined the effect of swainsonine on antibody response to sheep red blood cells (SRBC) in immunodeficient mice which were treated with immunosuppressive factor or antitumor drugs, or inoculated with sarcoma 180 ascites tumor. The administration of swainsonine restored the capacities of the immunodeficient mice to produce antibody against SRBC. Furthermore, swainsonine inhibited completely the growth of sarcoma 180 ascites tumor in mice. Swainsonine also reduced lung metastases of B16 melanoma in mice. These results suggest that swainsonine has potential as an immunomodulator for the treatment of immunocompromised hosts.
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  • YOSHIKI OBANA, TAKESHI NISHINO, TERUO TANINO
    1985 Volume 38 Issue 7 Pages 941-947
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The therapeutic efficacy of six β-lactam and aminoglycoside antibiotics were compared in diabetic mice with experimentally induced Klebsiella pneumoniae pneumonia. β-Lactams caused a reduction in the numbers of bacteria, with clearance of bacteria from the lungs of diabetic and normal mice. The effect in diabetic mice, however, was very poor. In contrast thereto, no remarkable difference was seen between diabetic and normal mice when treated with aminoglycosides. The concentration of the test antibiotics to the lungs in diabetic mice was lower than in normal mice. The aminoglycosides were more effective than the β-lactams. These data suggest that in treating acute and more chronic forms of pulmonary infection caused by. K. pneumoniae in diabetic mice aminoglycoside antibiotics are particularly valuable, whereas β-lactams must be given in large quantities using multiple administrations.
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  • T. MUKHOPADHYAY, C. M. M. FRANCO, G. C. S. REDDY, B. N. GANGULI, H. W. ...
    1985 Volume 38 Issue 7 Pages 948-951
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • M. S. PUAR, H. MUNAYYER, J. DESAI, J. J. WRIGHT
    1985 Volume 38 Issue 7 Pages 952-954
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • SUMIO KIYOTO, TOSHIHIRO SHIBATA, YOSHIO KAWAI, YASUHIRO HORI, OSAMU NA ...
    1985 Volume 38 Issue 7 Pages 955-956
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • YOICHI HAYAKAWA, TAKAFUMI IWAKIRI, KANJI IMAMURA, HARUO SETO, NOBORU O ...
    1985 Volume 38 Issue 7 Pages 957-959
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • YOICHI HAYAKAWA, TAKAFUMI IWAKIRI, KANJI IMAMURA, HARUO SETO, NOBORU O ...
    1985 Volume 38 Issue 7 Pages 960-963
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • TAKAYOSHI OKABE, FUJIO ISONO, MASAMI KASHIWAGI, MASAKO TAKAHASHI, TOSH ...
    1985 Volume 38 Issue 7 Pages 964-965
    Published: 1985
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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