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I. TAXONOMY, ISOLATION AND BIOLOGICAL ACTIVITY
HIDEO SUZUKI, MAKOTO TAHARA, MASAKO TAKAHASHI, FUMIKO MATSUMURA, TAKAY ...
1990 Volume 43 Issue 2 Pages
129-134
Published: February 25, 1990
Released on J-STAGE: April 19, 2006
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Resorthiomycin, a novel antitumor antibiotic, was isolated from the fermentation broth of a strain of
Streptomyces collinus by ethyl acetate extraction, silica gel chromatography and HPLC. Resorthiomycin exhibited an
in vitro cytotoxic activity against mouse leukemia L5178Y cells (IC
50, 15.5 μg/ml) and also inhibited the clonogenic activity of a multidrug-resistant mutant of human hepatoma PLC/PRF/5 cells to a greater extent than that of the parental cells. On the other hand, this antibiotic does not possess any antibacterial or antifungal activity.
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II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE ELUCIDATION
MAKOTO TAHARA, TAKAYOSHI OKABE, KAZUO FURIHATA, NOBUO TANAKA, HIDEYO Y ...
1990 Volume 43 Issue 2 Pages
135-137
Published: February 25, 1990
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Resorthiomycin was revealed to be a new antibiotic with a molecular weight of 284 and a chemical formula of C
14H
20O
4S as determined by MS and elemental analysis. The structure of resorthiomycin was determined to be 6-acetyl-4-(3-hydroxybutyl)-2-methyl-5-methylthioresorcinol by IR spectrum and
1H and
13C NMR.
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III. POTENTIATION OF ANTITUMOR DRUGS AND ITS MECHANISM OF ACTION
MAKOTO TAHARA, AKIHIRO TOMIDA, TOSHIO NISHIMURA, HIDEYO YAMAGUCHI, HID ...
1990 Volume 43 Issue 2 Pages
138-142
Published: February 25, 1990
Released on J-STAGE: April 19, 2006
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Resorthiomycin suppressed the clonogenic activity of a multidrug-resistant mutant cell line of Chinese hamster V79 cells more potently than its parental cells. Moreover, resorthiomycin at 40μg/ml potentiated the cytotoxic activity of vincristine and actinomycin D on V79 cells over 3-fold. Uptake of [
3H]actinomycin D into V79 cells was stimulated 2-fold by 40μg/ml of resorthiomycin during 2 hours incubation. On the other hand, incorporation of [
3H]thymidine and [
3H]uridine into mouse leukemia L5178Y cells was inhibited in a dose-dependent manner at resorthiomycin concentrations ranging from 5 to 40μg/ml. In ATP-depleted L5178Y cells, membrane transport of [
3H]thymidine and 2-[
3H]deoxyglucose was strongly suppressed by resorthiomycin. These results suggest that resorthiomycin acts on the plasma membrane and perturbes some membrane function.
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I. TAXONOMY, PRODUCTION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
TAKAAKI AOYAGI, SHIGEMI YOSHIDA, YASUSHI NAKAMURA, YASUHIRO SHIGIHARA, ...
1990 Volume 43 Issue 2 Pages
143-148
Published: February 25, 1990
Released on J-STAGE: April 19, 2006
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Probestin has been isolated as part of a program designed to find microorganism-produced inhibitors of aminopeptidase M from
Streptomyces azureus MH663-2F6. It was purified by use of column chromatography of Amberlite XAD-4, silica gel, YMC-gel, Toyopearl HW-40, YMC D-ODS-5 (HPLC) and then isolated as colorless powders. Probestin is competitive with the substrate, and the inhibition constant (
Ki) of it was 1.9×10
-8 M.
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II. STRUCTURE DETERMINATION OF PROBESTIN
SHIGEMI YOSHIDA, YASUSHI NAKAMURA, HIROSHI NAGANAWA, TAKAAKI AOYAGI, T ...
1990 Volume 43 Issue 2 Pages
149-153
Published: February 25, 1990
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Probestin, a new inhibitor of aminopeptidase M, has been isolated from the culture broth of
Streptomyces azureus MH663-2F6. The
1H and
13C NMR studies and amino acid analysis confirmed the presence of one 3-amino-2-hydroxy-phenylbutanoic acid, leucine and two proline residues in the molecule. Stereochemistries of these amino acids were determined by HPLC analysis. The fragmentation pattern shown in the mass spectrum and the chemical analysis on probestin clarified the amino acid sequence. Thus the structure of probestin was defined as (2
S, 3
R)-3-amino-2-hydroxy4-phenylbutanoyl-L-leucyl-L-prolyl-L-proline.
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I. TAXONOMY, AND FERMENTATION OF PRODUCING STRAIN
KENICHI SUZUKI, HIROSHI YAMAGUCHI, SIGERU MIYAZAKI, KOUJI NAGAI, SHUN- ...
1990 Volume 43 Issue 2 Pages
154-157
Published: February 25, 1990
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We found a new inhibitor of mammalian DNA topoisomerase I, named topostin, from a bacterial culture. The bacteria was identified as
Flexibacter topostinus sp. nov., B-572. Morphological and physiological characteristics, and utilization of sugars were examined. Comparison of the strain with known species of the genus
Flexibacter was made and indicates that the strain is a new species of the genus
Flexibacter. The bacteria produced the inhibitor in parallel with their growth up to 72 hours.
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II. PURIFICATION AND SOME PROPERTIES OF TOPOSTIN
YOJI IKEGAMI, NORIAKI TAKEUCHI, MINORU HANADA, YOKO HASEGAWA, KAZUYUKI ...
1990 Volume 43 Issue 2 Pages
158-162
Published: February 25, 1990
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We describe the isolation of inhibitors of mammalian DNA topoisomerase I, named topostins, from a culture broth of
Flexibacter topostinus sp. nov. and some properties of the inhibitors. Topostins Al, A2 and B were isolated by differential solubility in solvents, adsorption chromatography on silica gel and gel nitration on a Sephadex LH-20 column. Topostins Al, A2 and B had specific activities of 4, 700, 16, 000 and 22, 000 U/mg, respectively. The most active metabolite topostin B comprised two components with MW of 567 and 553 in an equimolar ratio.
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I. SCREENING, TAXONOMY, FERMENTATION AND BIOLOGICAL ACTIVITY
HIROYUKI OSADA, HIDETOSHI TAKAHASHI, KYOKO TSUNODA, HIROO KUSAKABE, KI ...
1990 Volume 43 Issue 2 Pages
163-167
Published: February 25, 1990
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In the course of our screening program using a bleb-forming assay, a new inhibitor of protein kinase C (PKC) was found in the fermentation of a streptomycete. The inhibitor, RK-286C (4'-demethylamino-4'-hydroxystaurosporine), inhibited the morphological change of K562 cells, a human chronic erythroleukemia cell, induced by phorbol 12, 13-dibutylate at the concentration of 3 μM. The same concentration of the compound inhibited the activity of PKC
in vitro and the aggregation of rabbit platelets induced by collagen and arachidonic acid.
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II. ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE
HIDETOSHI TAKAHASHI, HIROYUKI OSADA, MASAKAZU URAMOTO, KIYOSHI ISONO
1990 Volume 43 Issue 2 Pages
168-173
Published: February 25, 1990
Released on J-STAGE: April 19, 2006
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RK-286C, a new inhibitor of protein kinase C, has been found by the bleb-forming assay using K562 cells. It was produced by
Streptomyces sp. RK-286 and purified by solvent extraction, silica gel chromatography and preparative HPLC. Spectrometric analysis revealed that the structure is 4'-demethylamino-4'-hydroxystaurosporine.
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I. SYNTHESIS AND BIOLOGICAL ACTIVITY OF CEPHALOSPORIN DERIVATIVES LEADING TO MT0703
HIROKO OGINO, KATSUYOSHI IWAMATSU, KIYOAKI KATANO, SATORU NAKABAYASHI, ...
1990 Volume 43 Issue 2 Pages
174-188
Published: February 25, 1990
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A series of new aminothiazolylglycylcephalosporins with a mono- or dihydroxypyridonecarbonyl group at the α-amino group of the C-7 substituent have been prepared and antibacterial activity of these compounds was investigated. Among them, the compounds having a l, 5-dihydroxy-4-pyridone-2-carbonyl group showed excellent anti-pseudomonal activity. In particular, (6
R, 7
R)-7-[(
RS)-2-(2-aminothiazol-4-yl)-2-(1, 5-dihydroxy-4-pyridone-2-carboxamido)-acetamido]-3-[[l-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3-em-4-carboxylate(MT0703,
7g) was found to be a well balanced compound with respect to antibacterial activity.
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II. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF MT0703 AND ITS DIASTEREOMERS
HIROKO OGINO, KATSUYOSHI IWAMATSU, KIYOAKI KATANO, SATORU NAKABAYASHI, ...
1990 Volume 43 Issue 2 Pages
189-198
Published: February 25, 1990
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A practical synthetic method for large scale production of MT0703, (6
R, 1
R)-l-[(
RS)-2-(2-aminothiazol-4-yl)-2-(l, 5-dihydroxy-4-pyridone-2-carboxamido)acetamido]-3-[[l-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3-em-4-carboxylate, was established. Its two diastereomers on configuration of the aminothiazolylglycyl moiety were synthesized using chemico-enzymatic method. The S-isomer of MT0703 was found to be more active against Gram-positive and Gram-negative bacteria including β-lactamase-producing strains than the
R-isomer.
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GILLES ETIENNE, ELISE ARMAU, GÉRARD TIRABY
1990 Volume 43 Issue 2 Pages
199-206
Published: February 25, 1990
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Strains of
Saccharomyces cerevisiae FL200 capable of growing on a solid medium containing a mixture of polyene macrolide antibiotics (nystatin, 40 μg/ml, amphotericin B, 40 μg/ml, pimaricin, 150 μg/ml and RP9971 antibiotic, 10 μg/ml) have been isolated after successive selection steps. The mutant strains, PR13 and PRC24, are 10 to 100 times more resistant than the wild-type strain to 8 polyene macrolide antibiotics. When 4% Tween 80 is added to the medium, resistance to these antifungal drugs is further increased. In addition, strain PRC24, derived from strain PR13, is resistant to a non-polyene macrolide antifungal antibiotic, cycloheximide. In contrast, PR13 and PRC24 are both highly susceptible to a large range of compounds, including non-polyenic antifungal, antitumor and antibacterial agents. These particular characteristics make these strains useful for the rapid detection of antifungal compounds of the polyene macrolide and cycloheximide types, as well as for the recognition of antimitotic substances.
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XXXII. STROBILURIN E: A NEW CYTOSTATIC AND ANTIFUNGAL (E)-β-METHOXYACRYLATE ANTIBIOTIC FROM CREPIDOTUS FULVOTOMENTOSUS PECK
WOLFGANG WEBER, TIMM ANKE, BERT STEFFAN, WOLFGANG STEGLICH
1990 Volume 43 Issue 2 Pages
207-212
Published: February 25, 1990
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Strobilurin E is a novel antibiotic of the (
E)-β-methoxyacrylate (MOA) class produced by mycelial cultures of the agaric
Crepidotus fulvotomentosus. In addition to an inhibition of fungal respiration, a feature of all MOA-antibiotics, the compound exhibits very high cytostatic activities which are accompanied by reversible morphological alterations of the cells.
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HIDEJI FUJII, TERUYO TAKADA, KYUICHI NEMOTO, TAKUMI YAMASHITA, FUMINOR ...
1990 Volume 43 Issue 2 Pages
213-219
Published: February 25, 1990
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The effect of deoxyspergualin (DSG, NKT-01) on humoral immunity was investigated both
in vitro and
in vivo. DSG inhibited the primary and secondary responses to T cell-dependent antigens and the response to T cell-independent antigens in thymic and athymic mice. However, natural antibodies in non-sensitized mice were affected less by the administration of DSG. The agent produced a dose-dependent inhibition of B cell proliferation and antibody production to lipopolysaccharide
in vitro. Suppression of secondary antibody response was also shown, whenever antigen stimulation was not given, antibody production was not affected. These results suggest that DSG affects the proliferative stage of B lymphocytes in such a way as to inhibit their growth and antibody production.
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A. B. MAUGER, O. A. STUART
1990 Volume 43 Issue 2 Pages
220-221
Published: February 25, 1990
Released on J-STAGE: April 19, 2006
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