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I. TAXONOMY, PRODUCTION, ISOLATION AND BIOLOGICAL ACTIVITIES
YUJI YAMAGISHI, MICHIKO MATSUOKA, ATSUO ODAGAWA, SHINICHIRO KATO, KAZU ...
1993 Volume 46 Issue 11 Pages
1633-1637
Published: November 25, 1993
Released on J-STAGE: April 19, 2006
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Thiazohalostatin has been isolated from the culture broth of
Actinomadura sp. by a screening program designed to find novel cytoprotective substances. It was purified by use of column chromatography on silica gel, reversed phase HPLC and then isolated as colorless powder. Thiazohalostatin prevented cell death caused by calcium overload and exhibited an inhibitory activity against lipid peroxidation.
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II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE DETERMINATION
KAZUTOSHI SHINDO, YUJI YAMAGISHI, HIROYUKI KAWAI
1993 Volume 46 Issue 11 Pages
1638-1642
Published: November 25, 1993
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Thiazohalostatin is a new cytoprotective substance produced by
Actinomadura sp. HQ24. Its structure was elucidated as shown in Fig. 1 by NMR spectral analyses and chemical modifications. Thiazohalostatin was found to possess a novel skeleton containing trichloropyrrole and thiazoline ring moieties.
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TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
MASAAKI TAKAHASHI, TAKESHI KAGASAKI, TSUYOSHI HOSOYA, SHUJI TAKAHASHI
1993 Volume 46 Issue 11 Pages
1643-1647
Published: November 25, 1993
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New inositol-1, 4, 5-trisphosphate (InsP
3) agonists, adenophostins A(
1) and B(
2), were isolated from the culture broth of
Penicillium brevicompactum SANK 11991 and SANK 12177. Its structures were related to adenine nucleotides. The agonistic activity of adenophostins A or B for binding to the InsP
3 receptor was higher than InsP
3 itself.
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TAXONOMY, FERMENTATION, ISOLATION, STRUCTURE DETERMINATION AND BIOLOGICAL PROPERTIES
KIYOSHI HAMANO, MASAKO KINOSHITA-OKAMI, KATSUHIRO MINAGAWA, HIDEYUKI H ...
1993 Volume 46 Issue 11 Pages
1648-1657
Published: November 25, 1993
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A new inhibitor of mammalian adenosine triphosphatases, designated aquastatin A, has been isolated from a fungus identified as
Fusarium aquaeductuum. The structure of this compound has been determined by MS and NMR analyses. It inhibits Na
+/K
+-ATPase with an IC
50 value of 7.1 μM, and H
+/K
+-ATPase with an apparent IC
50 value of 6.2 μM.
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PRODUCTION, ISOLATION, STRUCTURE DETERMINATION AND BIOLOGICAL ACTIVITY
MITSUHIRO UENO, MASAHIDE AMEMIYA, TETSUYA SOMENO, TORU MASUDA, HIRONOB ...
1993 Volume 46 Issue 11 Pages
1658-1665
Published: November 25, 1993
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In our search for inhibitors of cell adhesion to components of extracellular matrix (ECM), fibronectin, laminin and collagen type IV, we succeeded in finding a novel cyclic hexadepsipeptide antibiotic, named IC101, which was isolated from cultured mycelium of
Streptomyces albulus MJ202-72F3. It was purified by centrifugal partition chromatography, preparative reverse phase HPLC and Sephadex LH-20 and was obtained as a white powder. 1C 101 strongly inhibited cell adhesion to ECM components, suppressed immune responses
in vitro and
in vivo, and exhibited antimicrobial activity on Gram-positive bacteria.
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TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL CHARACTERISTICS
KANKI KOMIYAMA, KAZUHIKO OTOGURO, TOSHIAKI SEGAWA, KAZURO SHIOMI, HONG ...
1993 Volume 46 Issue 11 Pages
1666-1671
Published: November 25, 1993
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A new peptide antibiotic, cypemycin, with a molecular weight of 2, 097 (M + H), was isolated from the culture broth of
Streptomyces sp. OH-4156. The antibiotic possesses cytocidal activity against P388 leukemia cells
in vitro at a concentration of 1.3μg/ml (IC
50 values), and the antibiotic showed antimicrobial activities against
Micrococcus luteus (MIC, 0.2μg/ml).
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I. TAXONOMY OF THE PRODUCING ORGANISM, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITIES
NAOKI ABE, YASUKAZU NAKAKITA, TAKEHIKO NAKAMURA, NOBUYASU ENOKI, HIDEA ...
1993 Volume 46 Issue 11 Pages
1672-1677
Published: November 25, 1993
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In the course of our investigation aimed at the discovery of novel antitumor antibiotics from microorganisms,
Streptomyces sp. G324 was found to produce the antitumor antibiotic, lavendamycin, and also, to yield the novel β-carboline compounds, oxopropalines. We isolated five compounds as oxopropalines A, B, D, E and G. Oxopropalines B, D and G showed cytocidal activities against human or murine tumor cell lines
in vitro.
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II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE ELUCIDATIONS
NAOKI ABE, NOBUYASU ENOKI, YASUKAZU NAKAKITA, HIDEAKI UCHIDA, TAKEHIKO ...
1993 Volume 46 Issue 11 Pages
1678-1686
Published: November 25, 1993
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Novel cytocidal compounds designated oxopropalines A, B, D, E and G were isolated from the fermentation of an actinomycete named
Streptomyces sp. G324, a strain that also produced an antitumor antibiotic, lavendamycin. All these compounds possessed a β-carboline chromophore. The structures of the oxopropalines were elucidated by several NMR spectral analyses and other spectroscopic experiments.
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MASAJI KAWATSU, TAKASHI YAMASHITA, MICHIYO OSONO, MASAAKI ISHIZUKA, TO ...
1993 Volume 46 Issue 11 Pages
1687-1691
Published: November 25, 1993
Released on J-STAGE: April 19, 2006
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Conagenin (CNG), a low molecular immunomodulator, enhanced incorporation of [
3H]thymidine into T cells activated by concanavalin A but did not to non-activated T cells. The culture supernatants of activated T cells treated with CNG enhanced incorporation of [
3H]thymidine into cytokine dependent cell lines, CTLL-2 and IC-2 cells. This indicates that CNG exclusively acts on activated T cells and stimulates them to promote DNA synthesis and to produce lymphokines, which may include T cell growth factors and hematopoietic growth factors. These activities were also observed with T cells taken from mice given CNG.
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ANTITUMOR ACTIVITY, GENERATION OF EFFECTOR CELLS AND CYTOKINE PRODUCTION
MASAJI KAWATSU, TAKASHI YAMASHITA, MICHIYO OSONO, TOHRU MASUDA, MASAAK ...
1993 Volume 46 Issue 11 Pages
1692-1698
Published: November 25, 1993
Released on J-STAGE: April 19, 2006
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Antitumor effects and function of T cells in tumor bearing mice given conagenin (CNG), a low molecular immunomodulator, were investigated. The administration of CNG, once a week for 4 weeks, was the most effective schedule in inhibiting growth of IMC carcinoma, a syngeneic tumor. In this regimen, cytotoxic T lymphocytes and natural killer activities in spleens of CNG treated mice were maintained at higher levels than those of non-treated mice. Lymphokine production by splenic T cells was also enhanced in cultures, whereas monokine production by macrophages, which was increased in accordance with tumor growth, was reduced by CNG administration.
The autitumor effect of CNG was not observed in mice given anti-asialo GM1 serum and in athymic mice.
Results shown in this report suggest that CNG exerts its antitumor effects through activation of T cells and enhancement of generation of antitumor effector cells.
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BIOLOGICAL ACTIVITIES
MIHO TANAKA, YASUHIRO HORI, FUMIHIKO SAKAI, HIROTSUGU UEDA, TOSHIO GOT ...
1993 Volume 46 Issue 11 Pages
1699-1706
Published: November 25, 1993
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WS1279, a new lipopeptide isolated from the fermentation broth of
Streptomyces willmorei No. 1279, stimulated the proliferation of mouse bone marrow cells
in vitro and accelerated the recovery of granulocyte counts in bone marrow from leukopenia induced by mitomycin C (MMC) in mice. The glycerylcysteine moiety of WS1279 is necessary and the lipid peptide structure is required for manifestation of full stimulating activity
in vitro. WS1279 was the most effective on the proliferation of bone marrow cells among the tested immunostimulants
in vitro. However, the effect of WS1279 on restoration of reduced granulocyte counts in MMC-induced leukopenia in mice was less than that of FK-565, lipopolysaccharide, picibanil or forphenicinol. WS1279 augmented host resistance to infection with
Staphylococcus aureus 47 in normal and immunosuppressed mice.
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NAO-AKI WATANABE, KANEMASA KATSU
1993 Volume 46 Issue 11 Pages
1707-1715
Published: November 25, 1993
Released on J-STAGE: April 19, 2006
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Potent antistaphylococcal activity was conferred on E1077 by the introduction of the propenylammonium group at the 3-position in the cephem nucleus and of the fluoromethoxyimino group in the 7β-side chain. Antistaphylococcal activity was more markedly increased by the former group than by the latter. This effect seemed likely to be due to the increased high affinity for penicillin-binding protein (PBP) 3, which may be one of the essential PBPs of
Staphylococcus aureus, and secondly for PBP 4. E1077 also showed more potent bactericidal activity than did cefpirome at concentrations above the MICs, although the MICs of E1077 for
S. aureus were only half those of cefpirome. While cefpirome showed little killing activity within 4 hours at its MIC, the addition of cefoxitin (0.05 μ/ml), a specific inhibitor for PBP 4, enhanced the killing activity of cefpirome to match that of E1077. In addition, peptidoglycan (PG) obtained from cells grown with the subinhibitory E1077 concentration was more susceptible to lytic enzymes than that from untreated cells or cefpirome-treated cells. These results indicated that the increased inhibition of PBPs 3 and 4 by E1077, which was brought about by the introduction of two distinctive functional groups, led to the enhanced antistaphylococcal activity and to the production of poorly cross-linked PG, and thereby to rapid bactericidal activity.
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II. STRUCTURE DETERMINATION
HIDEAKI KAKEYA, MASAYA IMOTO, YOSHIKAZU TAKAHASHI, HIROSHI NAGANAWA, T ...
1993 Volume 46 Issue 11 Pages
1716-1719
Published: November 25, 1993
Released on J-STAGE: April 19, 2006
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Dephostatin, a novel tyrosine phosphatase inhibitor, was isolated from the culture broth of
Streptomyces sp. MJ742-NF5. The structure was elucidated to be 2-(
N-methyl-
N-nitroso)hydroquinone by spectral and chemical analyses of dephostatin and its derivatives.
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DEREK HORTON, WALDEMAR PRIEBE, MARCOS L. SZNAIDMAN, OSCAR VARELA
1993 Volume 46 Issue 11 Pages
1720-1730
Published: November 25, 1993
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Daunosamine, as its 4-
O-acetyl-3-
N-trifluoroacetyl glycosyl chloride derivative (
1b), has been coupled α-L-glycosidically to the 3- and 4-mono-
O-acetyl derivatives of L-rhamnal to afford disaccharide glycal derivatives, whose conversion into the corresponding 2-deoxyglycosides by sequential alkoxyiodination-tributylstannane reduction has been evaluated. The sequence successfully demonstrated with the methyl glycosides was successfully extended with daunomycinone as the aglycon, providing a preparative route to 7-
O-[3-
O-(3-amino-2, 3, 6-trideoxy-α-L-
lyxo-hexopyranosyl)-2, 6-dideoxy-α-L-
arabino-hexopyranosyl]daunomycinone hydrochloride (
15), an analogue of natural anthracycline antibiotics containing daunosamine and a 2, 6-dideoxy-L-hexose.
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A. Y. PAVLOV, T. F. BERDNIKOVA, E. N. OLSUFYEVA, E. I. LAZHKO, I. V. M ...
1993 Volume 46 Issue 11 Pages
1731-1739
Published: November 25, 1993
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Nitrosation, carbamoylation or acylation of the glycopeptide antibiotics eremomycin or vancomycin produced series of derivatives substituted at the
N-terminus of the peptides. Though the modified amino group in these derivatives is not capable of protonation,
N-nitroso derivatives retain antibacterial activity
in vitro and
in vivo.
N-Carbamoyleremomycin has low activity, and
N-Cbz-eremomycin and
N-Boc-eremomycin are devoid of antibacterial activity, both
in vitro and
in vivo.
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TOSHIYUKI NISHI, KUNIO HIGASHI, MAKOTO TAKEMURA, MAKOTO SATO
1993 Volume 46 Issue 11 Pages
1740-1751
Published: November 25, 1993
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A new type of penem derivative (
3-
6) having a cyclic amidine moiety or a quaternary heterocycle moiety at the C-2 position was prepared. The susceptibility to renal dehydropeptidase-1 (DHP-1) and the antimicrobial activity of these compounds were determined. Some of these compounds (
5,
6) showed a broad spectrum of antibacterial activity, including activity against
Pseudomonas aeruginosa,
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BRIGITTE KUNZE, ROLF JANSEN, LUTZ PRIDZUN, ELKE JURKIEWICZ, GERHARD HU ...
1993 Volume 46 Issue 11 Pages
1752-1755
Published: November 25, 1993
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GERARD HELYNCK, CATHERINE DUBERTRET, JEAN-FRANCOIS MAYAUX, JEAN LEBOUL
1993 Volume 46 Issue 11 Pages
1756-1757
Published: November 25, 1993
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III. NEW ANTHRACYCLINE METABOLITES PRODUCED BY BLOCKED MUTANTS 4L-660 AND YDK-18
AKIHIRO YOSHIMOTO, OSAMU JOHDO, HIROSHI NISHIDA, ROKURO OKAMOTO, TOMIO ...
1993 Volume 46 Issue 11 Pages
1758-1761
Published: November 25, 1993
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MURALEEDHARAN G. NAIR, AMITABH CHANDRA, DEBORAH L. THOROGOOD
1993 Volume 46 Issue 11 Pages
1762-1763
Published: November 25, 1993
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MARCIA S. OSBURNE, WILLIAM M. MAIESE, MICHAEL GREENSTEIN
1993 Volume 46 Issue 11 Pages
1764-1766
Published: November 25, 1993
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SHIRO AKINAGA, KAYO NOMURA, KATSUSHIGE GOMI, MASAMI OKABE
1993 Volume 46 Issue 11 Pages
1767-1771
Published: November 25, 1993
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TOSHIO TSUCHIDA, HIRONOBU IINUMA, NAOKO KINOSHITA, TAKAKO IKEDA, RYUIC ...
1993 Volume 46 Issue 11 Pages
1772-1774
Published: November 25, 1993
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