The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 40 , Issue 11
Showing 1-25 articles out of 25 articles from the selected issue
  • I. TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION
    HARUMITSU IMAI, KEN-ICHI SUZUKI, MOTO MORIOKA, Yousou NUMASAKI, SHIGEN ...
    1987 Volume 40 Issue 11 Pages 1475-1482
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Okilactomycin, a novel antibiotic, was isolated from the culture filtrate of a strain of actinomycetes. The producing organism, strain YP-02908L, was identified as Streptomyces griseoflavus subsp. zamamiensis subsp. nov. The antibiotic was extracted with ethyl acetate and purified by silica gel column chromatography. It was obtained as colorless prisms from a dichloromethane solution. It exhibited weak antimicrobial activity against Grampositive organisms in vitro. It also exhibited antitumor activity against Ehrlich ascites carcinoma in vivo. The apparent molecular formula of okilactomycin was determined as C24H32O6. It is a new member of the lactone group antibiotics.
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  • II. STRUCTURE DETERMINATION
    HARUMITSU IMAI, HIDETOSHI KAMWA, TATSUHIRO TOKUNAGA, SHIGEO FUJITA, TO ...
    1987 Volume 40 Issue 11 Pages 1483-1489
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Structure of a novel antibiotic, okilactomycin, was determined by a combination of spectroscopic and X-ray crystallographic studies. Okilactomycin has a unique structure containing 13-membered ring cyclized by carbon-carbon bond.
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  • WALTER P. CULLEN, WALTER D. CELMER, LARRY R. CHAPPEL, LIANG H. HUANG, ...
    1987 Volume 40 Issue 11 Pages 1490-1495
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The novel chlorine-containing acidic polycyclic ether antibiotic CP-54, 883 (C41H61O12Cl2) is produced by the fermentation of Actinomadura routienii Huang sp. nov. This report presents the taxonomy and the fermentation conditions for the antibiotic-producing culture. The antibiotic is mainly active against Gram-positive bacteria. It protects chickens against Eimeria challenge in vivo and enhances rumen propionic acid in vitro. The physico-chemical properties are also characterized.
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  • JON BORDNER, PAUL C. WATTS, EARL B. WHIPPLE
    1987 Volume 40 Issue 11 Pages 1496-1505
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The structural formula of the novel antibiotic ionophore CP-54, 883 is deduced by systematic reduction from its 13C and 1H NMR spectra. The molecule consists of a polyether ring network and side chain terminated by an aromatic ring containing a phenoxy and two chlorine substituents. Based partly on an assumed analogy to corresponding regions of the similar structure nigericin-A1, the configurations about the sixteen asymmetric carbons are also derived. A belated crystal structure determination confirms, with the exception of one configuration assumed from nigericin-A1, the conclusions drawn, and shows that the anionic charge is in the phenoxy group, rather than the carboxylic acid function.
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  • I. ISOLATION AND CHARACTERIZATION
    KEIJI KURUSU, KENKICHI OHBA, TADASHI ARAI, KAZUTAKA FUKUSHIMA
    1987 Volume 40 Issue 11 Pages 1506-1514
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A strain of Bacillus polymyxa produced a new peptide antibiotic complex, named LI-F, composed of more than ten components. The components, antibiotics LI-F03, F04, F05, F07, and F08 were isolated from the complex by reversed phase HPLC. They are active against fungi, yeasts, and Gram-positive bacteria. The fast atom bombardment mass spectra revealed that the individual isolated antibiotics are still mixture of two homologous components, being very difficult to separate from each other.
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  • I. TAXONOMY, ISOLATION AND BIOLOGICAL ACTIVITY
    E. MEYERS, G. S. BISACCHI, L. DEAN, W. C. Liu, B. MINASSIAN, D. S. SLU ...
    1987 Volume 40 Issue 11 Pages 1515-1519
    Published: November 25, 1987
    Released: April 19, 2006
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    Xylocandin is a complex of novel peptides with potent antifungal activity that is produced by Pseudomonas cepacia ATCC 39277. The complex was isolated from the fermentation broth by extraction with butanol - methanol, 9:1, followed by collection of the precipitate formed upon concentration of the solvent extract. Purification was effected by chromatography on reversed phase and size exclusion gels followed by TLC on silica gel. These techniques afforded eight components: Al, A2, B1, B2, C1, C2, D1 and D2. A mixture of the two closely related components, xylocandins A1 and A2, displayed potent anticandidal and antidermatophytic activities in vitro. The activity was diminished by the presence of serum or vaginal washings. No antibacterial activity was demonstrable.
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  • II. STRUCTURAL STUDIES AND CHEMICAL MODIFICATIONS
    GREGORY S. BISACCHI, DEBORAH R. HOCKSTEIN, WILLIAM H. KOSTER, WILLIAM ...
    1987 Volume 40 Issue 11 Pages 1520-1529
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Xylocandins A1, A2, B1, B2, C1, C2, D1 and D2 are new antifungal peptides isolated from Pseudomonas cepacia ATCC 39277. The molecular weights of the xylocandins were determined by fast atom bombardment mass spectrometry (A1 m/z 1, 215; A2 1, 199; B1 1, 229; B2 1, 213; C1 1, 097; C2 1, 081; D1 1, 083; D2 1, 067). Each xylocandin is a cyclic peptide containing glycine (1), serine (2), asparagine (1 - 3 residues), β-hydroxytyrosine (1), and an unusual amino acid with the formula C18H37NO5 (1). Additionally A1, A2, D1 and D2 contain 2, 4-diaminobutyric acid (1); A1, B1, C1 and D1 contain erythro-β-hydroxyasparagine (1); and A1, A2, B1 and B2 contain xylose (1). For each xylocandin pair, an erythro-β-hydroxyasparagine residue in the first component of the pair is thus replaced by an asparagine in the second component, accounting for the 16 dalton mass difference for each pair. Chemical modification of A1 and A2 at the diaminobutyric acid and β-hydroxytyrosine residues was used to probe structural requirements for activity.
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  • I. CHARACTERIZATION, STRUCTURE ELUCIDATION AND BIOLOGICAL ACTIVITY
    AXEL ZEECK, KARSTEN SCHRÖDER, KLAUS FROBEL, RALPH GROTE, RALF THI ...
    1987 Volume 40 Issue 11 Pages 1530-1540
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Manumycin (1), produced by Streptomyces parvulus (strain Tü 64), was isolated from the mycelium by extraction with acetone and could easily be purified chromatographically. Chemical degradation of 1 (C81H38N2O7) gave 2-acetamino-3-hydroxycyclopent-2-enone (2) by acetolysis, 2, 4, 6-trimethyl-2, 4-decadienoic acid (3) by alkaline hydrolysis, and 2-(2, 4, 6-trimethyl-2, 4-decadienoylamino)-5, 6-epoxy-l, 4-benzoquinone (5) by mild chromic acid oxidation. In connection with a detailed spectroscopic analysis, the structure of 1 could be elucidated and the (E)-configuration of the double bonds in the triene and diene chain was established. Manumycin exhibits biological activity against Gram-positive bacteria and fungi and furthermore, an inhibition of the developmental processes of some insects.
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  • II. DERIVATIVES
    AXEL ZEECK, KLAUS FROBEL, CHRISTA HEUSEL, KARSTEN SCHRÖDER, RALF ...
    1987 Volume 40 Issue 11 Pages 1541-1548
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Derivatives of manumycin (1) were obtained by acetylation and reduction, respectively, and characterized by their spectroscopic data. Structure-activity relationships of the antibiotic were discussed.
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  • III. ABSOLUTE CONFIGURATION AND CONFORMATIONAL STUDIES
    RALF THIERICKE, MICHAEL STELLWAAG, AXEL ZEECK, GÜNTHER SNATZKE
    1987 Volume 40 Issue 11 Pages 1549-1554
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Chromic acid oxidation of manumycin (1), an antibiotic produced by Streptomyces parvulus (strain Tü 64), led to the isolation of 2-(2-methyl-4-oxo-2-pentenoylamino)-5, 6-epoxy-l, 4-benzoquinone (3) and (-)-(R)-2-methylhexanoic acid (4). From the absolute configuration of 4, determined by comparing its optical rotation with published data, follows the absolute configuration at the center of chirality in the diene side chain of manumycin (1) to be (6'R). Based on the direct comparison of the CD spectra of the two chromic acid oxidation products 2 and 3 with those of the antibiotic G7063-2 (5) and (-)-terreic acid (6) the stereochemistry at C-5 and C-6 of 1 was determined as (5R, 6S). From the negative CD-couplet of manumycin (1) its stereochemistry at C-4 was assigned as (4R).
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  • ALBERTO SALA, DARIO CHIARINO, MAURO NAPOLETANO, ENRICO ALBINI, ANGELO ...
    1987 Volume 40 Issue 11 Pages 1555-1562
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The synthesis of new 2-(3-substituted-5-isoxazolyl)-2-methoxyiminoacetic acids and their condensation derivatives with a suitable cephalosporanic nucleus, is reported. Their antibacterial properties were tested in vivo and in vitro also against β-lactamase producer microorganisms; particularly the oral bioavailability of some of these new derivatives was studied.
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  • RICHARD E. MEWSHAW, THOMAS J. COMMONS
    1987 Volume 40 Issue 11 Pages 1563-1571
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The synthesis and in vitro antibacterial profile of several novel C-4 substituted monobactam analogs are reported.
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  • A. MALABARBA, A. TRANI, P. FERRARI, R. PALLANZA, B. CAVALLERI
    1987 Volume 40 Issue 11 Pages 1572-1587
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A series of ester derivatives of teicoplanin-N-acetylglucosaminyl aglycone (T-A3-2) and deglucoteicoplanin was prepared starting from teicoplanin and from the corresponding deglycosylation compounds.
    The modification of the ionic and lipophilic character of the parent antibiotic strongly influences the spectrum of antibacterial activity in vitro.
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  • CHANTAL LATOUD, FRANCHISE PEYPOUX, GEORGES MICHEL
    1987 Volume 40 Issue 11 Pages 1588-1595
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The action of iturin A on non-growing cells of Saccharomyces cerevisiae was tested. This antibiotic gave important modifications in the membrane permeability which permitted nucleotides, proteins, polysaccharides and lipids to escape from cells. The lipid content of cells was strongly disturbed; the level of phospholipids, essentially phosphatidylcholine, decreased while the level of fatty acids increased. A part of these fatty acids were extruded from yeast cells. The role of iturin A in these modifications was discussed.
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  • ELSAKU YOSHIDA, KANKI KOMIYAMA, KYOZO NAITO, YOSHINORI WATANABE, KEIKO ...
    1987 Volume 40 Issue 11 Pages 1596-1604
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Kazusamycin B, a novel antibiotic (MW 542) isolated from fermentation broth of Streptomyces sp. No. 81-484 showed a broad antitumor spectrum both in vitro and in vivo. IC50 against the growth of tumor cells was around 1 ng/ml at 72 hours-exposure in vitro. Intraperitoneal injection of the antibiotic was effective in inhibiting the growth of murine tumors, S180, P388, EL-4, and B16. It was also active against doxorubicin-resistant P388, hepatic metastases of L5178Y-ML, pulmonary metastases of 3LL, and human mammary cancer MX-1 xenografted to nude mice. However, the activity of kazusamycin B toward L1210 or human lung cancer LX-1 was weaker.
    According to the results of comparative studies on the effect of kazusamycins B and A, an analog of B, there seemed to be no significant difference in their effectiveness. The effective dose range and toxicity were markedly dependent on tumor lines tested and the regimen used. Maximum tolerated dose in mice with subcutaneous tumors was much higher than that in mice bearing ascitic leukemia as P388. Although intermittent administration could greatly reduce the cumulative toxicity of the drug, therapeutic effect was similar with both successive and intermittent administration schedules.
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  • HLROSHI KURAMOCHI, AKIKO MOTEGI, MLNORU IWABUCHI, KATSUTOSHI TAKAHASHI ...
    1987 Volume 40 Issue 11 Pages 1605-1611
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The action of ubenimex on aminopeptidase (APase) activity was studied in intact spleen cells and peritoneal macrophages from mice. Ubenimex strongly inhibited hydrolyzing activities against arginine-β-naphtylamide (Arg-NA), Lys-NA and Pro-NA in both cells. Inhibition of hydrolysis of Leu-NA, Met-NA and Ala-NA was relatively small or not observed. When both cells were incubated in HANKS' solution, hydrolyzing activities against Arg-NA, Lys-NA and Pro-NA were released to the medium, while Leu-NA and Met-NAhydrolyzing activities were mostly bound. In addition, the Leu-NA-hydrolyzing activity in the spleen cells was kinetically studied. The Arg-NA and Leu-NA-hydrolyzing activities in four fractions prepared from the homogenate of spleen cells were also studied kinetically. From these studies it was suggested that ubenimex inhibits aminopeptidase B and a Pro-NAhydrolyzing enzyme more effectively than Leu-APase in intact spleen cells and peritoneal macrophages from mice.
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  • TORU MASUDA, SHIGETOSHI MIZUTANI, MASATOMI IIJIMA, HIDEHARU ODAI, HIRO ...
    1987 Volume 40 Issue 11 Pages 1612-1618
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The immunosuppressive activity of spergualin analogues, 15-deoxyspergualin and N-30, is presented. These compounds suppressed antibody formation and establishment of delayedtype hypersensitivity to sheep red blood cells (SRBC) in mice. Among spergualin, 15-deoxyspergualin, and N-30, 15-deoxyspergualin was most effective in suppressing immune responses. It suppressed antibody formation against SRBC by spleen cell cultures in a dose-dependent fashion without reducing cell viability. The spergualins also suppressed the mixed lymphocyte culture reaction. Peritoneal exudate cells taken from mice given immunosuppressive doses of 15-deoxyspergualin were not reduced in their functions measured: Release of lysosomal enzymes and production of superoxide anions. 15-Deoxyspergualin and N-30 were markedly effective in prolonging skin graft in rats.
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  • I. SCREENING METHOD AND THERAPEUTIC EFFECT FOR TREPONEMA HYODYSENTERIAE-CAUSED INFECTION IN CF-1 MICE
    SATOSHI OMURA, AKIRA NAKAGAWA, TOMOKO FUJIMOTO, KAZUNORI SAITO, KAZUHI ...
    1987 Volume 40 Issue 11 Pages 1619-1626
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    In vitro and in vivo screening methods were established for the discovery of new active substances against Treponema hyodysenteriae. During the screening methods, hygromycin A produced by Streptomyces hygroscopicus KA-355 was found to be active against T. hyodysenteriae. Hygromycin A did not show high antitreponemal activity in in vitro test using the paper disc method on the agar plate inoculated with T. hyodysenteriae. However, the antibiotic exhibited highly therapeutic effect in CF-1 mice, compared with of lincomycin, tiamulin, lankacidin C or olaquindox drinking water. The effective dose (ED50) of hygromycin A was 1.1μg/ml
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  • II. THERAPEUTIC EFFECT FOR SWINE DYSENTERY
    AKIRA NAKAGAWA, TOMOKO FUJIMOTO, SATOSHI OMURA, JAMES C. WALSH, RONALD ...
    1987 Volume 40 Issue 11 Pages 1627-1635
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    This study was conducted to evaluate hygromycin A fed to growing swine at 1, 5, 10 or 20 g/ton feed for the control of Treponema hyodysenteriae-causGd dysentery. Pigs provided carbadox at 50 g/ton feed served as an infected treatment control group. All pigs were orally, via stomach intubation, administered 100ml of a T. hyodysenteriae broth culture. During the in vivo test, rectal swabs were taken for T. hyodysenteriae isolation, body weights of all pigs and the feed consumption was determined. All pigs were euthanized and necropsied at study end; the large intestine was cultured for T. hyodysenteriae and gross intestinal lesions were noted. T. hyodysenteriae-causQd swine dysentery was successfully controlled by feeding hygromycin A at 5 g/ton. Hygromycin A medicated pigs performed as well as or better than carbadox-medicated pigs.
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  • ETTORE PERRONE, MARCO ALPEGIANI, ANGELO BEDESCHI, FRANCO GIUDICI, FRAN ...
    1987 Volume 40 Issue 11 Pages 1636-1639
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • SATORU KANEDA, CHEN HOUR-YOUNG, KATSUKIYO YAZAWA, KATSUHIRO TAKAHASHI, ...
    1987 Volume 40 Issue 11 Pages 1640-1642
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • MITSUNOBU HARA, MAYUMI YOSHIDA, MAKOTO MORIMOTO, HIROFUMI NAKANO
    1987 Volume 40 Issue 11 Pages 1643-1646
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • MIKIO KITAHARA, MASAAKI ASANO, HIROSHI NAGANAWA, KENJI MAEDA, MASA HAM ...
    1987 Volume 40 Issue 11 Pages 1647-1650
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • SETSUKO KUNIMOTO, CHIN-ZHI Xu, HIROSHI NAGANAWA, MASA HAMADA, TORU MAS ...
    1987 Volume 40 Issue 11 Pages 1651-1652
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • JOSEPH E. BISKUPIAK, JANICE H. JOHNSON, MICHAEL FORTE, SUZANNE MORELAN ...
    1987 Volume 40 Issue 11 Pages 1653-1656
    Published: November 25, 1987
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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