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TOSHIAKI HAYASHI, TAKAO NOTO, YOSHIHARU NAWATA, HIROSHI OKAZAKI, MIKIO ...
1982 Volume 35 Issue 7 Pages
771-777
Published: 1982
Released on J-STAGE: April 12, 2006
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A new antibiotic, cyanocycline A, was isolated from the fermentation broth of
Streptomyces flavogriseus strain No. 49, a soil isolate. The molecular formula of cyanocycline A was determined to be C
22H
26N
4O
5. The antibiotic has a cyano group and a
N-heterocyclic quinone moiety in its structure. Cyanocycline A was found to have broad spectrum antimicrobial and antitumor activity.
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I. TAXONOMY, PRODUCTION, AND CHEMICAL AND BIOLOGICAL PROPERTIES
MASAHIRA NAKAGAWA, AKIRA HIROTA, HEIICHI SAKAI, AKIRA ISOGAI
1982 Volume 35 Issue 7 Pages
778-782
Published: 1982
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A new antibiotic, terrecyclic acid A was isolated from the culture filtrate of a new isolate of fungus, identified as
Aspergillus terreus. The fermentation yields reached about one gram per liter of the broth. Chemical and biological characterization of the antibiotic revealed that it was a new sesquiterpene having a wide antimicrobial spectrum and antitumor activity.
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II. STRUCTURE OF TERRECYCLIC ACID A
AKIRA HIROTA, MASAHIRA NAKAGAWA, HEIICHI SAKAI, AKIRA ISOGAI
1982 Volume 35 Issue 7 Pages
783-787
Published: 1982
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The structure of a new antibiotic, terrecyclic acid A, from a strain of
Aspergillus terreus Thom, was established as
I on the basis of spectroscopic and chemical evidences, by comparison of spectroscopic data with quadrone, a known antitumor substance, and further by conversion of terrecyclic acid A to quadrone through pyrolysis.
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EUGENE ROSENBERG, SHLOMO FYTLOVITCH, SHMUEL CARMELI, YOEL KASHMAN
1982 Volume 35 Issue 7 Pages
788-793
Published: 1982
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Antibiotic TA was purified and crystallized from culture fluids of
Myxococcus xanthus TA. The antibiotic (C
34H
57O
9N, M. W. 623.8) contained the following functional groups: ketone, lactone, secondary amide, methoxy-substituted diene (λ
max 239 nm), primary alcohol and three secondary alcohols, two of which were
cis-vicinal. Mild alkaline hydrolysis opened the lactone with concomitant loss of antibiotic activity. Periodate oxidation also destroyed biological activity.
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VI. PREPARATION AND CHARACTERIZATION OF THE SEMISYNTHETIC IPROCINODINE
W. J. MCGAHREN, F. BARBATSCHI, N. A. KUCK, G. O. MORTON, B. HARDY, G. ...
1982 Volume 35 Issue 7 Pages
794-799
Published: 1982
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Conditions for the preparation and purification of iprocinodine are described. This material is the isopropylated derivative of active glycocinnamoylspermidine metabolites of a
Nocardia species. The resolution and characterization of minor components generated during the chemical reaction are also outlined.
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H. BERG, G. HORN, W. IHN
1982 Volume 35 Issue 7 Pages
800-805
Published: 1982
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The preparative electrochemical reduction of a series of anthracycline antibiotics was performed using the technique of large scale electrolysis and d. c. polarography for recording different reaction pathways. The reduction products were identified by mass spectrometric and chromatographic analyses. Only anthracyclines with sugar residues in the C-10 position (iremycin, roseorubicin A) were reduced reversibly by 2e- to the corresponding hydroquinones. All others with sugar residues in the C-7 position (daunomycin, 5-iminodaunomycin, adriamycin, carminomycin, β-rhodomycin II, aclacinomycin A, 1-deoxypyrromycin) showed an irreversible behavior because of the reductive splitting of the glycosidic bond under formation of 7-deoxy compounds or-if the C-11 OH-group was not present-of dimers, respectively.
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NORIYUKI NAOI, TOSHIAKI MIWA, TAKESHI OKAZAKI, KIYOSHI WATANABE, TOMIO ...
1982 Volume 35 Issue 7 Pages
806-813
Published: 1982
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The chromophores extracted from macromomycin (MCR) and auromomycin (AUR) with methanol had identical ultraviolet absorption spectra, antibacterial spectra and analytical profiles in high pressure liquid chromatography. The chromophore content of AUR was about 8 times higher than that of MCR. MCR reconstituted from the chromophore and protein fraction was identical with native MCR by Sephadex G-50 chromatography, ultraviolet absorption spectrum and antibacterial spectrum. The antibacterial activity of MCR and AUR was due to the chromophore; the protein moiety had no activity. However, the protein moiety enhanced the activity of the chromophore against Gram-positive bacteria, while it suppressed the activity against Gram-negative organisms. It also protected the chromophore from heat-inactivation.
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J. SCOTT WELLS, JENNIE C. HUNTER, GAIL L. ASTLE, JEAN C. SHERWOOD, CAR ...
1982 Volume 35 Issue 7 Pages
814-821
Published: 1982
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Over one million bacteria were isolated from a large variety of soil, plant and water samples collected from different environments and examined in an extremely sensitive and highly specific screen for β-lactam production. A group of seven related monocyclic β-lactams (monobactams) were isolated from strains representing four genera-
Agrobacterium, Chromobacterium, Gluconobacter and
Pseudomonas. Monobactam-producing strains of
Agrobacterium and
Pseudomonas were isolated only rarely. Producing strains of
Chromobacterium were isolated from a relatively limited number of habitats while the Gluconobacter strains appeared to be widespread in nature. In addition, three closely related β-lactone-containing molecules were isolated from strains representing three genera-Arthrobacter, Bacillus and Pseudomonas. The Bacillus and Pseudomonas strains were isolated infrequently but from a variety of samples. The producing strain of Arthrobacter was isolated only once.
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YOSHIHARU WAKISAKA, YOSHIMI KAWAMURA, YUKIO YASUDA, KENZO KOIZUMI, YOJ ...
1982 Volume 35 Issue 7 Pages
822-836
Published: 1982
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A selective medium containing 25 to 50 μg per ml of tunicamycin was devised to isolate micromonosporae from soil samples, making possible simple, preferential isolation of a variety of Micromonospora. When a large amount of Gram-negative bacteria was present in a sample, alkaline treatment (0.01 N NaOH, 5-10 minutes at 15°C) was employed to reduce the numbers. Using the tunicamycin agar medium, 1, 585 strains of presumably different micromonosporae were obtained from 400 soil samples collected from various regions around the world. In average, 4 different
Micromonospora strains could be isolated from one soil sample. This tunicamycin method made possible a concentrated screening method for new antibiotics from
Micromonospora.
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CORNELIS M. VOS, DICK SCHIPPER, JACOBUS D. M. HERSCHEID, GERRIT WESTER ...
1982 Volume 35 Issue 7 Pages
837-842
Published: 1982
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Demethylation of Co-bleomycin A
2 by heating yields three different complexes: form I and form II and "orange" Co-bleomycin-demethyl A
2. These complexes can be separated by HPLC and show different 1H NMR spectra. Preparation of Co-bleomycin-demethyl A
2by chelation of bleomycin-demethyl A
2 with cobalt yields a Co-bleomycin-demethyl A
2, which is auto-oxidized into Co-bleomycin A
1.
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P. SCHNEIDER, W. TOSCH, M. MAURER, O. ZAK
1982 Volume 35 Issue 7 Pages
843-849
Published: 1982
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A pharmacokinetic model has been developed, by means of which all possible time courses of the concentrations of antibiotics in the plasma of treated individuals can be exactly simulated
in vitro without diluting the test organism and affecting the growth curves. Equieffective concentrations in the system corresponded to the plasma concentrations in man produced by cefroxadine in a single oral dose of 250 mg and cephalexin and cephradine in a single oral dose of 500 mg.
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EFFECT OF A CEPHALOSPORIN AND SIX PENICILLINS ON FIVE AMINOGLYCOSI DES
LOUISE J. RIFF, JESSICA L. THOMASON
1982 Volume 35 Issue 7 Pages
850-857
Published: 1982
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Gentamicin, tobramycin, netilmicin, kanamycin and amikacin were evaluated over time for biologic activity in human serum, in combination with 6 β-lactams. Simple addition of aminoglycoside and 250 μg/ml penicillin produced aminoglycoside inactivation at 8-48 hours. However, all β-lactam antibiotics exhibited decay in human serum at 37°C, even when present as a single component. All aminoglycosides could be inactivated by penicillins but differed markedly in their susceptibility. Amikacin, at 20 μg/ml, was the least inactivated by any penicillin; netilmicin, at 10 μg/ml, was the next least inactivated. Tobramycin had pronounced loss of biological activity exceeding that of any aminoglycoside, appearing as early as 8 hours. The ability of the various penicillins to produce aminoglycoside inactivation, in approximate descending order, was; carbenicillin, ticarcillin, penicillin G, oxacillin, methicillin, ampicillin. Cephalothin produced minimal inactivation. Aminoglycoside inactivation also occurred at 25°C, and with many samples stored at 4°C, although at proportionately slower rates. For samples stored at -20°C, only tobramycin had substantial loss of activity. These data indicate that adequate handling and prompt assay of the specimen are important.
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2. COMBINED EFFECTS OF A MACROLIDE WITH A FOSFOMYCIN AND AN AMINOGLYCOSIDE ANTIBIOTIC
TAKAO KASAI, J. YUZURU HOMMA
1982 Volume 35 Issue 7 Pages
858-865
Published: 1982
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Synergistic effects of the cell wall-affecting antibiotics, dibekacin (DKB) and fosfomycin (FOM) and a macrolide antibiotic, midecamycin (MDM) or its derivative 9, 3"-di-O-acetylmidecamycin (MOM) against
Pseudonionas aeruginosa were investigated
in vitro and
in vivo.
Synergistic effects were evaluated by estimating the number of viable bacteria at varying intervals after the two kinds of antibiotics were added to the logarithmic phase of the bacterial solution. Six hours after addition of antibiotic, the viable bacterial count of the culture treated with FOM and MOM underwent 2 log reduction compared to that which treated with FOM alone. Thus synergistic effect was significant. The number of viable bacteria treated with DKB and MDM showed slight reduction at 3 hours after addition of the two antibiotics and a marked reduction was noted after 20 hours compared with the control. Synergistic action was also demonstrated in
in vivo experiments using mice. Three experimental mouse infection models, intraperitoneal infection, subcutaneous infection with carrageenan solution and burn infection were used. FOM was administered subcutaneously. DKB was administered intramuscularly. MDM or MOM was administered by the oral route. In all three experiments the survival rate of infected mice treated with FOM and MOM increased significantly compared to control mice. Similar synergistic effect was also obtained with DKB and MDM.
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CHARACTERISTICS OF DIHYDROROSARAMICIN BINDING TO ESCHERICHIA COLI RIBOSOME AND THE EFFECTS OF SOME COMPETITORS
SYLVIE SIEGRIST, SYLVIE VELITCHKOVITCH, FRANCOIS LE GOFFIC, NICOLE MOR ...
1982 Volume 35 Issue 7 Pages
866-874
Published: 1982
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The macrolide [
13H]dihydrorosaramicin binds specifically to 50S and 70S bacterial ribosomal particles. We have studied the influence of salts, pH and additives on the interaction and found that the optimum requirement for salts was 10 mM tris-HCl (pH 7.6), 6 mM MgCl
2, 60 mM NH
4Cl, and the β-mercaptoethanol which reacts on rosaramicin and its dihydro derivative cannot be used. The parameters of the binding were not dependent on the technique used,
i.e. equilibrium dialysis, ethanol precipitation or two-phase partitioning. In our search for effectors of this binding, we have found that it is inhibited by other macrolides, little effected by tobramycin and chloramphenicol and enhanced by puromycin.
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REVERSIBILITY OF THE EFFECTS
FRANCISCO HERNÁNDEZ, MICHAEL CANNON
1982 Volume 35 Issue 7 Pages
875-881
Published: 1982
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Inhibition of protein synthesis by trichodermol, diacetoxyscirpenol and verrucarin A in cells and spheroplasts of
Saccharomyces cerevisiae was investigated. Inhibition was reversible for trichodermol and diacetoxyscirpenol, both drugs being removed from their target site(s) by washing, but was irreversible for verrucarin A. These results are interpreted in relation to variations in chemical structure between these trichothecenes.
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AKIRA YOSHIDA, MASAHIKO HIRAMATSU, KEIKO HATAKEYAMA, NAOMI MINAMI
1982 Volume 35 Issue 7 Pages
882-885
Published: 1982
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The single intratracheal instillation of bleomycin sulfate (0.5mg (potency) per 100g body weight) in hamsters rapidly increased the activity of glucosamine 6-phosphate synthetase (EC 2.6.1.16) of the lung, a major regulatory enzyme for the synthesis of acidic glycosaminoglycan (AGAG). The activity increased as early as day 2, reached maximum level at day 10, then decreased and returned to the control level at day 45. The content of AGAG was also in creased by bleomycin treatment, but the increase of AGAG followed the elevation of the enzyme activity. These results suggest that the early elevation of glucosamine 6-phosphate synthetase activity is closely related to the accumulation of AGAG in the fibrosing lung caused by bleomycin.
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HIROSHI YAMAKI, HIDEO SUZUKI, EUNG CHIL CHOI, NOBUO TANAKA
1982 Volume 35 Issue 7 Pages
886-892
Published: 1982
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The mechanism of action of geldanamycin, a benzoquinoid ansamycin, was investigated with murine lymphoblastoma L5178Y cells. The agent inhibited the cell growth at concentrations over 0.01μg/ml. The antibiotic blocked DNA synthesis more markedly than RNA and protein syntheses. Mitosis was not significantly affected by the drug in the cells synchronized with demecolcine (Colcemid). The antibiotic did not interfere with
in vitro assembly of tubulin. In the synchronized cells, strong inhibition of DNA synthesis was observed when geldanamycin was introduced into the culture prior to S phase of the cell cycle. The degree of inhibition was stronger with prolongation of incubation period and with increase of DNA synthesis rate. The results suggested that initiation of DNA synthesis or S phase is affected by the drug. DNA degradation was not significantly induced
in vivo by the antibiotic. Geldanamycin blocked DNA polymerase α more markedly than β and γ. The degree of inhibition depended upon concentrations of enzyme but not upon those of template, suggesting a drug-enzyme interaction. IC
50 for DNA polymerase α was 10μg/ml and for DNA polymerase β 100μg/ml at low concentrations of enzyme. The inhibition of DNA polymerase α by the antibiotic was non-competitive and
Ki was 20μM.
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YUZURU MATSUDA, MIKIO KITAHARA, KENJI MAEDA, HAMAO UMEZAWA
1982 Volume 35 Issue 7 Pages
893-899
Published: 1982
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D-Cycloserine showed a decreased lethality against paraquat-treated
E. coli than against non-treated cells.
E. coli K12 mutants which were deficient in DNA repair were more sensitive than the wild type strain to D-cycloserine. Furthermore, D-cycloserine caused PM2 DNA cleavage in the presence of Fe
2+, and the cleavage was strongly inhibited by singlet oxygen scavengers. These results indicate that D-cycloserine interacts with DNA and an active oxygen species is involved in the interaction.
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WILLIAM L. PARKER, MARLENE L. RATHNUM, WEN-CHIH LIU
1982 Volume 35 Issue 7 Pages
900-902
Published: 1982
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NORIMASA ONISHI, TOSHIHIKO WATANABE, KAZUO IZAKI, HAJIME TAKAHASHI
1982 Volume 35 Issue 7 Pages
903-904
Published: 1982
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MAHENDRA N. SHARMA, VIRENDRA KUMAR, WILLIAM A. REMERS
1982 Volume 35 Issue 7 Pages
905-912
Published: 1982
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J. J. KIM WRIGHT, JAMES A. ALBARELLA, DAVID LOEBENBERG
1982 Volume 35 Issue 7 Pages
911-914
Published: 1982
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KATSUKIYO YAZAWA, TAKEMITSU ASAOKA, KATSUHIRO TAKAHASHI, YUZURU MIKAMI ...
1982 Volume 35 Issue 7 Pages
915-917
Published: 1982
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PETER S. F. MEZES, ANTHONY J. CLARKE, GARY I. DMITRIENKO, THAMMAIAH VI ...
1982 Volume 35 Issue 7 Pages
918-920
Published: 1982
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ROKURO OKAMOTO, KOHKI KIYOSHIMA, MASAO YAMAMOTO, KAZUAKI TAKADA, TETSU ...
1982 Volume 35 Issue 7 Pages
921-924
Published: 1982
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SHOICHI KUSUMOTO, YOSHIKAZU KAMBAYASHI, SUSUMU IMAOKA, KEIYU SHIMA, TE ...
1982 Volume 35 Issue 7 Pages
925-927
Published: 1982
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YUZURU MATSUDA, MIKIO KITAHARA, KENJI MAEDA, HAMAO UMEZAWA
1982 Volume 35 Issue 7 Pages
928-930
Published: 1982
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YUZURU MATSUDA, MIKIO KITAHARA, KENJI MAEDA, HAMAO UMEZAWA
1982 Volume 35 Issue 7 Pages
931-933
Published: 1982
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NORIYUKI NAOI, YOSHIKI KUMADA, TOSHIAKI YAMASHITA, TOMIO TAKEUCHI, HAM ...
1982 Volume 35 Issue 7 Pages
934-936
Published: 1982
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HAMAO UMEZAWA
1982 Volume 35 Issue 7 Pages
937-938
Published: 1982
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