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I. TAXONOMY OF PRODUCING ORGANISM AND FERMENTATION
TAKAYA IKEMOTO, HIDEKO MATSUNAGA, KIYOSHI KONISHI, TAKAO OKAZAKI, RYUZ ...
1983 Volume 36 Issue 9 Pages
1093-1096
Published: 1983
Released on J-STAGE: April 12, 2006
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A soil isolate of actinomycete, strain TI-1, was found to produce a new antibiotic aculeximycin which killed insects as well as inhibited the growth of bacteria, yeasts and molds
in vitro. Yellowish gray colonies on agar media, formation of spherical to oval sporangia at the tip of aerial mycelium and the presence of meso-diaminopimelic acid and madurose in the cell wall ascribed this strain to genus Streptosporangium. From its morphological, cultural and physiological characteristics, the strain was determined to be
S. albidum. Production of aculeximycin was carried out by conventional submerged culture: the highest antibiotic titer obtained was 1, 250 μg/ml.
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II. ISOLATION, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES
TAKAYA IKEMOTO, TOSHIAKI KATAYAMA, AKIO SHIRAISHI, TATSUO HANEISHI
1983 Volume 36 Issue 9 Pages
1097-1100
Published: 1983
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A new larvicidal antibiotic, aculeximycin, was found in the culture broth of an actinomycete identified as
Streptosporangium albidum. Aculeximycin was isolated from the culture filtrate by adsorption on a Diaion HP-20 column and successive elution with acidic aqueous acetone. It was extracted from the concentrated active fraction with 1-butanol and subjected to column chromatography on a Sephadex LH-20 column. Aculeximycin exhibited strong larvicidal activity against mosquito larvae as well as antimicrobial activities against Gram-positive and Gram-negative bacteria, yeasts and molds.
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TAXONOMY, FERMENTATION, ISOLATION, CHARACTERIZATION AND BIOLOGICAL PROPERTIES
JOSEPH A. MARQUEZ, ANN C. HORAN, MANOHAR KALYANPUR, BONG K. LEE, DAVID ...
1983 Volume 36 Issue 9 Pages
1101-1108
Published: 1983
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The hazimicins, a new class of broad spectrum antibiotics with at least 2 active components (5 and 6), were isolated from the fermentation of
icromonospora echinospora var
challisensis SCC 1411. The complex was separated from the broth by a solvent extraction procedure, and the individual components were separated by column chromatography. The two primary active components are isomers, with unique structures shown to be di-tyrosine analogs containing two isonitrile groups. The antibiotic has
in vitro and
in vitro activity against Gram-positive and Gram-negative bacteria, and
in vitro activity against yeasts and dermatophytes.
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KENNETH E. WILSON, AUGUST J. KEMPF, JERROLD M. LIESCH, BYRON H. ARISON
1983 Volume 36 Issue 9 Pages
1109-1117
Published: 1983
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Two new carbapenem antibiotics, northienamycin and 8-epi-thienamycin have been isolated from culture broth of
Streptomyces cattleya grown under conditions for thienamycin production. The isolation, structure elucidation and
in vitro antibacterial spectra of the new carbapenems are reported. In addition, comparison of the
in vitro potency of the correspond ing formamidine derivatives to that of MK787 is presented.
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CHAO-MIN LIU, M. CHIN, B. LA T. PROSSER, N. J. PALLERONI, J. W. WESTLE ...
1983 Volume 36 Issue 9 Pages
1118-1122
Published: 1983
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Antibiotic X-14885A is a novel divalent cation ionophore produced by a Streptomyces culture isolated from soil sample collected in Wyoming. Its cation binding sequence has been found to be: Mg
2+>Ca
2+, Sr
2+>Ba
2+>>>Li
+, Na
+, Rb
+, K
+, Cs
+.
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1. TAXONOMY, ISOLATION AND CHARACTERIZATION
MICHIO YAMASHITA, MORITA IWAMI, KOICHI IKUSHIMA, TADAAKI KOMORI, HATSU ...
1983 Volume 36 Issue 9 Pages
1123-1128
Published: 1983
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FR-900109 is a new antibiotic obtained from fermentation broth of a streptomyces which was identified as
Streptomyces prunicolor. Its elementary analysis and mass spectroscopic measurement suggest that the molecular formula is C
27H
32O
9. It has an ultraviolet absorption maximum at 254 nm. The antibiotic is active against Gram-positive bacteria. Acute toxicity in mice is very low.
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SATOSHI OMURA, AKIRA NAKAGAWA, HIROSHI AOYAMA, YUZURU IWAI, MASAO KUWA ...
1983 Volume 36 Issue 9 Pages
1129-1135
Published: 1983
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Karabemycin, a new peptide antibiotic, was isolated from the culture filtrate of
Streptomyces sp. AM-6424, a soil isolate. The molecular formula of the antibiotic was determined as C
15H
24N
4O
6 on the basis of elemental analysis, FD-mass spectrum and
1H and
13C NMR. Acid hydrolysate of karabemycin contains one mol each of valine, alanine and an unknown amino acid. The antibiotic is active against Gram-positive and -negative bacteria on a synthetic medium. The inhibitory activity is reversed by L-glutamine and L-glutamic acid.
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SHIGEYOSHI MIYASHIRO, TAKAO KIDA, HIROSHIRO SHIBAI, TSUYOSHI SHIIO, SH ...
1983 Volume 36 Issue 9 Pages
1136-1143
Published: 1983
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A new macromolecular peptide antibiotic, named AN-3, was isolated from the culture broth of
Streptomyces albulus. From 19 liters of culture broth containing AN-3 with 90 units/ml activity, a 400 mg sample with a specific activity of 109 units/mg was obtained. Purified AN-3 gave a single band on polyacrylamide gel electrophoresis. AN-3 was a basic polypeptide with a molecular weight of 12, 000-12, 500 and an isoelectric point of pH 7.6. It showed a peak of absorption at 280 nm and seemed to have no nonprotein chromophoric component. It was soluble in water but insoluble in ethanol, butanol and acetone, and was stable at pH 4-9 but unstable at pH 2. AN-3 had no antibacterial activity against Gram-positive and Gram-negative bacteria so far as tested. But, it showed a strong inhibitory effect on a macromolecule permeable mutant of
Escherichia coli. It was not mutagenic. It appeared to inhibit synthesis of DNA and RNA without affecting DNA itself. It also inhibited the
in vitro cell growth of L1210 and its ED50 was 5 μg/m1. AN-3 had antitumor activity against Lewis lung carcinoma in mouse
in vivo.
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IWAO UMEZAWA, HIROFUMI OKA, KANKI KOMIYAMA, KEIKO HAGIWARA, SHIGERU TO ...
1983 Volume 36 Issue 9 Pages
1144-1149
Published: 1983
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A new antibiotic, awamycin, was isolated from the culture broth of
Streptomyces sp. No. 80-217. It appeared to belong to the quinone indicator group from results of physicochemical studies and has the empirical formula C
38H
49NO
12S. This antibiotic possessed antibacterial and antitumor activities against Gram-positive bacteria and experimental murine tumors. The antibiotic also showed direct cytotoxic activity against HeLa cells
in vitro.
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I. PRODUCTION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES, AND MECHANISM OF ACTION
K. GERTH, R. JANSEN, G. REIFENSTAHL, G. HÖFLE, H. IRSCHIK, B. KUN ...
1983 Volume 36 Issue 9 Pages
1150-1156
Published: 1983
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From the cell mass and culture supernatant of
Myxococcus xanthus strain Mx X12 an antibiotic activity against yeasts, molds and some Gram-positive bacteria could be extracted. It consisted of 4 biologically active compounds which were named myxalamid A, B, C and D. The main component, myxalamid B, was shown to block in beef heart submitochondrial particles the respiratory chain at the site of complex I,
i.e. NADH: ubiquinone oxidoreductase. The myxalamids are new antibiotics.
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I. ISOLATION, CHARACTERIZATION AND BIOLOGICAL ACTIVITIES OF TRESTATINS A, B AND C
KAZUTERU YOKOSE, KIYOSHI OGAWA, TAKASHI SANO, KIMIHIRO WATANABE, HIROM ...
1983 Volume 36 Issue 9 Pages
1157-1165
Published: 1983
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Trestatin complex which exhibited a potent inhibitory activity on various α-amylases has been isolated from the culture filtrate of
Streptomyces dimorphogenes nov. sp. NR-320-OM7HB. Three major components, trestatins A, B and C, have been purified by adsorption and ion-exchange chromatography. Their spectral and chemical properties suggested that trestatins were novel basic oligosaccharide homologues each characterized by the possession of a trehalose moiety at the non-reducing end of the molecule.
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II. STRUCTURE DETERMINATION OF TRESTATINS A, B AND C
KAZUTERU YOKOSE, KIYOSHI OGAWA, YUKIKO SUZUKI, ISAO UMEDA, YASUJI SUHA ...
1983 Volume 36 Issue 9 Pages
1166-1175
Published: 1983
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The structures of trestatins A (C
56H
94N
2O
40)B, (C
37H
63NO
28)a nd C (C
75H
125N
3O
52), new basic oligosaccharides with potent inhibitory activity against various α-amylases, have been shown by spectroscopic and chemical methods to be 1, 2 and 3, respectively.
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TAKAO OKAZAKI, NOBUFUSA SERIZAWA, RYUZOU ENOKITA, AKIO TORIKATA, AKIRA ...
1983 Volume 36 Issue 9 Pages
1176-1183
Published: 1983
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Three actinomycetes having capability of 3β-hydroxylation of ML-236B were isolated from soil samples collected in Australia. Strain SANK 62781 was identified as
Nocardia autotrophica. Strain SANK 62881 and strain SANK 62981 were identified as new subspecies of
N. autotrophica for which the name
N. autotrophica subsp.
canberrica and
N. autotrophica subsp.
amethystina are proposed, respectively. The type strains of
N. autotrophica subsp.
canberrica and
N. autotrophica subsp.
amethystina are ATCC 35203 and ATCC 35204.
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J. WILLIAM LOWN, CHRISTOPHER C. HANSTOCK, ALUMMOOTTIL V. JOSHUA, TADAS ...
1983 Volume 36 Issue 9 Pages
1184-1194
Published: 1983
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The chemical structure and conformation of the new antitumor antibiotic saframycin R have been determined by high field
1H and
13C NMR as well as FAB mass spectrometry. Unlike other members of the saframycin family, saframycin R contains a reduced quinone ring bearing a glycolic ester moiety. Saframycin R exhibits acid promoted equilibrium and reversible covalent binding to DNA templates and, in the presence of a reducing agent, oxygen dependent single strand scission of supercoiled DNA. The extent of DNA scission is enhanced by
in situ porcine carboxyl esterase or base catalyzed cleavage of the glycolic ester function plausibly by the release of the more reactive reduced saframycin A. This suggests that saframycin R may be regarded as a less toxic pro-drug for the active forms of saframycins A or S.
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JOHN W. WESTLEY, CHAO-MIN LIU, RALPH H. EVANS, Jr., LILIAN H. SELLO, N ...
1983 Volume 36 Issue 9 Pages
1195-1200
Published: 1983
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Conversion of the monovalent polyether antibiotic monensin into a series of urethane derivatives substituted at C-26 causes a ten-fold increase in the cation transporting properties of the antibiotic as well as making the resulting semisynthetic urethanes divalent ionophores. These changes must in part account for the enhanced antimicrobial activities of the urethanes. The most active derivatives are the phenylurethanes which are ten times more active
in vitro against Gram-positive bacteria and unlike monensin are active against
Candida albicans and
Penicillium digitatum. Another novel activity exhibited by four of the urethanes was against
Plasmodium berghei, the causative agent for malaria.
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JERAULD S. SKOTNICKI, THOMAS J. COMMONS, RICHARD W. REES, JOHN L. SPET ...
1983 Volume 36 Issue 9 Pages
1201-1204
Published: 1983
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The synthesis and
in vitro antibacterial activity of (±)(
cis)-3-[2-(2-aminothiazol-4-yl)-(
Z)-2-methoxyiminoacetamido]-4-fluoromethyl-2-oxo-1-azetidinesulfonic acid, potassium salt are presented.
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THE SYNTHESIS AND ANTIBACTERIAL ACTIVITIES OF 7-[2-(2-(AMINO-1, 3, 4-THIADIAZOL-5-YL)ACETAMIDO]-CEPHALOSPORINS
KENJI SAKAGAMI, TADASHI MISHINA, TSUYOSHI KURODA, MINORU HATANAKA, TOS ...
1983 Volume 36 Issue 9 Pages
1205-1210
Published: 1983
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Synthesis and antibacterial activities of 7-[2-(2-amino-1, 3, 4-thiadiazol-5-yl)acetamido]-cephalosporins and their derivatives having the methoxyimino group at the 2-position of the 7-acyl moiety are described. These compounds are of interest as structural analogues of potent antibiotics, 7-[2-(2-aminothiazol-4-yl)acetamido]cephalosporins. 7-[2-(2-Amino-1, 3, 4-thiadi-azol-5-yl)acetamido]cephalosporins showed comparable activity with cefazolin. Introduction of methoxyimino group to the 7-side chain resulted in a lowering of activity.
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DEREK HORTON, WALDEMAR PRIEBE
1983 Volume 36 Issue 9 Pages
1211-1215
Published: 1983
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A range of 14-esters (
8-13) of the title compound, 3'-deamino-3'-hydroxydoxorubicin 3', 4'-diacetate (
5), has been synthesized by nucleophilic substitution of the corresponding 14-bromide (
6) by the appropriate sodium carboxylate salts. Antitumor activities were determined
in vivo in the murine P388 lymphocytic leukemia assay and compared with those of the 14-hydroxy and 14-acetoxy analogs.
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KAZUHISA FUJIMOTO, MAKOTO MORIMOTO
1983 Volume 36 Issue 9 Pages
1216-1221
Published: 1983
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The novel antitumor antibiotic, trioxacarcin C, was studied for antitumor activities against murine tumor systems. When mice with i.p.-inoculated B16 melanoma were given intraperitoneal injections of trioxacarcin C, the maximal T/C% was 164 by successive administration of 0.125 mg/kg/day (day 1-10). It also gave the prolongation of life span of mice bearing i.p. P388 leukemia (T/C 141%) by i.p. injection for 10 days, and inhibited the growth of sarcoma 180 (T/C 42%) and Lewis lung carcinoma implanted s.c. (T/C 23%) by i.v. administration for 6 or 7 days. It inhibited the growth of P388 leukemia cells
in vitro and showed significant inhibition on the colony formation of HeLa S
3 cells. DNA and RNA synthesis were more strongly inhibited than protein synthesis by trioxacarcin C. Also, it induced strand scission of PM-2 DNA without reducing agents or metals. It did not effect the number of white blood cells and blood urea nitrogen value of the peripheral blood.
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VIII. BINDING PARAMETERS OF ACLACINOMYCIN A TO DNA
ULRICH KATENKAMP, EBERHARD STUTTER, INGEBORG PETRI, FRIEDRICH A. GOLLM ...
1983 Volume 36 Issue 9 Pages
1222-1227
Published: 1983
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The binding of aclacinomycin A to DNA was investigated spectrophotometrically under equilibrium conditions. The self-association behaviour of aclacinomycin A was identified as dimerization. Based on a model of overlapping potential binding sites the subsequent results were obtained: equilibrium constant of cooperative binding
K=(7.58±2.15)×10
6 M
-1, size of a binding site α=3.98± 0.14 base pairs, cooperativity parameter σ=0.12±0.10. These parameters were compared with those of adriamycin, daunomycin, and iremycin to draw some conclusions regarding the structural specialities of aclacinomycin A.
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TOSHIAKI HAYASHI, TSUNEO OKUTOMI, SEIKICHI SUZUKI, HIROSHI OKAZAKI
1983 Volume 36 Issue 9 Pages
1228-1235
Published: 1983
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Cyanocycline A was cytotoxic against Meth A cells
in vitro, and also showed marked activity against the same cell line grown as an experimental ascites tumor. This antibiotic inhibited nucleic acid synthesis in
Escherichia coli and Meth A cells. The antimicrobial activity of the antibiotic was reversed by addition of exogenous herring sperm DNA. Cytofluorometric analysis of cyanocycline A-treated Meth A cells showed an unusual pattern of the relative content of DNA and RNA per cell. These results suggested that cyanocycline A binds to DNA, and that it inhibits nucleic acid synthesis.
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TSUYOSHI KIHARA, KIYOSHI SONO
1983 Volume 36 Issue 9 Pages
1236
Published: 1983
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2. X-RAY STRUCTURE DETERMINATION OF FR-900109 p-BROMOPHENYL ESTER
SHIGETAKA KODA, YUKIYOSHI MORIMOTO, MICHIO YAMASHITA, TADAAKI KOMORI, ...
1983 Volume 36 Issue 9 Pages
1237-1238
Published: 1983
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J. GUMIENIAK, R. ANDRUSZKIEWICZ, A. CZERWINSKI, J. GRZYBOWSKA, E. BORO ...
1983 Volume 36 Issue 9 Pages
1239-1241
Published: 1983
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AKIRA TANAKA, KIKUO SEN, JUNJI MORITA, TOHRU KOMANO
1983 Volume 36 Issue 9 Pages
1242-1244
Published: 1983
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