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I. Taxonomy of Producing Strain, Fermentation and Isolation
TAKEO TANAKA, Eui TSUKUDA, KEIKO OCHIAI, HIDEMASA KONDO, SADAO TESHIBA ...
1996 Volume 49 Issue 11 Pages
1073-1078
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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EI-1511-3, -5 and EI-1625-2, novel interleukin-1β converting enzyme (ICE) inhibitors, were isolated from the culture broths of
Streptomyces sp. E-1511 and E-1625. EI-1511-3, -5 and EI-1625-2 selectively inhibited the recombinant human ICE activity with IC
50 values of 0.09, 0.38 and 0.2μM, respectively. Taxonomy, fermentation of the producing strain and isolation of EI-1511-3, -5 and EI-1625-2 are described.
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II. Structure Determination
YOUICHI UOSAKI, TSUTOMU AGATSUMA, TAKEO TANAKA, YUTAKA SAITOH
1996 Volume 49 Issue 11 Pages
1079-1084
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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The structures of three novel interleukin-1β converting enzyme inhibitors, EI-1511-3, -5 and EI-1625-2 were determined by spectroscopic methods. Their absolute configurations were also determined by analyses of the CD spectra of the inhibitors and their oxidation products with chromium trioxide.
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III. Biochemical Properties of EI-1511-3, -5 and EI-1625-2
TAKEO TANAKA, EUI TSUKUDA, YOUICHI UOSAKI, YUZURU MATSUDA
1996 Volume 49 Issue 11 Pages
1085-1090
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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EI-1511-3, -5 and EI-1625-2, novel interleukin-1β converting enzyme (ICE) inhibitors from the culture broths of
Streptomyces sp. selectively inhibited the recombinant human ICE activity with IC
50 values of 0.09, 0.38 and 0.2μM, respectively, without inhibiting elastase and cathepsin B. Manumycin G,
ent-alisamycin, U-56, 407, and manumycin A and B isolated simultaneously from the same strains also inhibited ICE. EI-1511-3, -5 and EI-1625-2 also inhibited mature interleukin-1β secretion from THP-1 cells with IC
50 values of 5.4, 3.6 and 2.2μM, respectively. In this article, biological properties of EI-1511-3, -5 and EI-1625-2 and, in addition, properties of manumycinrelated compound are described.
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I. Taxonomy, Fermentation, Isolation and Biological Activities
MASAHIKO HAYASHI, YONG-PIL KIM, SATOSHI TAKAMATSU, AKIKO ENOMOTO, MAYU ...
1996 Volume 49 Issue 11 Pages
1091-1095
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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Selective growth inhibition against IL-6-dependent cells was detected in fermentation extracts of a microbial strain, K93-0711, which was characterized as
Streptomyces species. Active metabolite, termed madindoline A and B, were isolated, and the structure was determined to be 3a-hydroxyindoline with diketocyclopentene at the
N position. Madindoline A and B displayed dose-dependent inhibition of MH60 cells, an IL-6-dependent cell line, in presence of 0.1 U/ml IL-6. The IC
50 for madindoline A and B against this cell line was 8μM and 30 μM, respectively. These compounds did not inhibit the growth of cell lines which are not IL-6 dependent and the growth inhibition of the MH60 cell line was reversed by addition of excess, 0.4 U/ml, of IL-6 to the culture media. These compounds did not show any antimicrobial activity at a concentration of l, 000μg/ml.
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I. Taxonomy of the Producing Organism, Fermentation and Biological Activity
MAKOTO UBUKATA, TETSU-ICHIRO MORITA, HIDEAKI KAKEYA, KIMIE KOBINATA, T ...
1996 Volume 49 Issue 11 Pages
1096-1100
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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Streptomyces sparsogenes SN-2325 isolated from a soil sample collected in Hokkaido, was found to produce Sparoxomycins Al and A2, new modulators of proliferation of mammalian cells. Sparoxomycins Al and A2 reverse the morphology of temperature-sensitive mutant Rous sarcoma virus-infected NRK cells (
srcts-NRK cells) from the transformed phenotype to the normal phenotype at the permissive temperature.
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MONIKA JAKOBI, GÜNTHER WINKELMANN, DIETMAR KAISER, CHRISTOPH KEMP ...
1996 Volume 49 Issue 11 Pages
1101-1104
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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Strains of
Stenotrophomonas maltophilia R3089, isolated from the rhizosphere of rape plants (
Brassica napus L.), produced a novel antifungal compound, named maltophilin, which inhibited the growth of various saprophytic, human-pathogenic and phytopathogenic fungi but was inactive against Gram-positive and Gram-negative bacteria. Maltophilin is a novel macrocyclic lactam antibiotic with a molecular mass of 510mu. The compound was isolated from the culture filtrate by ethyl acetate extraction and gel filtration on Sephadex LH20 and purified by preparative HPLC on reversed phase. The structure of maltophilin was elucidated by electrospray mass spectrometry and
1H and
13C NMR spectroscopy.
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JUNKO DOSHIDA, HIROSHI HASEGAWA, HIROYUKI ONUKI, NOBUYOSHI SHIMIDZU
1996 Volume 49 Issue 11 Pages
1105-1109
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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Exophilin A, a new antibacterial compound, was discovered in the culture of the marine microorganism
Exophiala pisciphila NI10102, which was isolated from a marine sponge
Mycale adhaerens. The absolute chemical structure of exophilin A was elucidated as a trimer of (3
R, 5
R)-3, 5-dihydroxydecanoic acid by spectroscopic methods and analyses of a degradative product. Exophilin A showed antimicrobial activity against Gram-positive bacteria.
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Jon SASAKI, KAZUTOSHI MIZOUE, SHIGEO MORIMOTO, SADAFUMI OMURA
1996 Volume 49 Issue 11 Pages
1110-1118
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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In the course of our microbial transformation study on erythromycin derivatives,
Streptomyces hygroscopicus ATCC 31080, which produces a poly ether antibiotic carriomycin, was found to transform erythromycin derivatives to their inactivated derivatives. The structures of inactivated derivatives prepared by enzyme reaction using the cell extract, UDP-glucose (or UDP-galactose) and Mg
2+ (or Mn
2+) were elucidated on the basis of analysis of their spectral data to be the compounds glycosylated at C-2' of a desosamine moiety, indicating that the enzyme is a macrolide glycosyl transferase (MGT). The MGT activity of cell extract from
S. antibiotieus ATCC 11891, a producing organism of oleandomycin, could be distinguished from that of ATCC 31080, based on the ability to glycosylate tylosin. We examined 32 actinomycete strains producing such polyketides as macrolide and polyether antibiotics, and found that 15 strains of
Streptomyces have macrolide glycosyl transferase activity. It suggests that the MGTs have been distributed among at least polyketide producing
Streptomyces strains.
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MAKOTO MUROI, KATSUMI SUEHARA, HIROSHI WAKUSAWA, KENICHI SUZUKI, TSUTO ...
1996 Volume 49 Issue 11 Pages
1119-1126
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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The nonapeptide leucinostatin A (LSA) inhibited syncytium formation without profoundly affecting HN glycoprotein synthesis in Newcastle disease virus (NDV)-infected BHK cells. At similar doses of LSA, cytopathic effect and infectious virus production were suppressed in vesicular stomatitis virus (VSV)-infected BHK cells. Blockade by LSA of cell surface expression of NDV-HN and VSV-G glycoproteins was demonstrated, accompanied by intracellular accumulation of these virus glycoproteins. LSA acts as an inhibitor of mitochondrial F-type H
+-translocating ATPase, a key enzyme in the generation of ATP, but its action against cell surface expression of virus glycoproteins was independent of the depletion of intracellular ATP. LSA also acts as an ionophore, but its action on intoxication by ricin and diphtheria toxin was different from that of monensin. This novel action of LSA is expected to be useful in investigation of the mechanism of intracellular trafficking of proteins.
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USMAN CHATIB WARSA, MASATO NONOYAMA, TAKASHI IDA, RYOICHI OKAMOTO, TOY ...
1996 Volume 49 Issue 11 Pages
1127-1132
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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This study describes the use of the polymerase chain reaction (PCR) to detect the
tet(K) and
tet(M) tetracycline resistance genes in
Staphylococcus aureus. Primers based on the DNA sequence of the
tet(K) and
tet(M) genes from
S. aureus were used as primers in the PCR assay to detect the presence of genes for resistance to tetracycline and minocycline. Two-hundred and fifteen isolates of
S. aureus from Asian countries as Japan, Indonesia, China, Korea and Thailand were examined, and the results confirm that
tet(K) specifies resistance to tetracycline but not to minocycline and
tet(M) specifies resistance to both tetracycline and minocycline. We observed two different types of clinical isolates of
S. aureus strains resistant to minocycline and tetracycline: the first carried only the
tet(M) gene, while the second carried both the
tet(M) and the
tet(K) genes. Almost all of the clinical isolates of
S. aureus resistant to minocycline and tetracycline from Indonesia, China and Thailand carried both
tet(M) and
tet(K) genes, while most of clinical isolates of
S. aureuss from Japan and Korea carried only
tet(M) gene.
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1. Modification at the Four Hydroxyl Groups
RIKA OBATA, TOSHIAKI SUNAZUKA, ZHUORONG LI, ZHIMING TIAN, YOSHIHIRO HA ...
1996 Volume 49 Issue 11 Pages
1133-1148
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
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Four hydroxyl groups of pyripyropenes have been modified and evaluated for their ability to inhibit microsomal acyl-CoA: cholesterol acyltransferase (ACAT) activity
in vitro and to lower cholesterol absorption
in vivo in a cholesterol-fed hamster. 7-
O-n-Valeryl derivative (
8c) improved the
in vitro ACAT inhibitory activity (IC
50=13nM) about 7 times better than pyripyropene A. Introduction of methanesulfonyl group at 11-hydroxyl group (
17a) increased both
in vitro activity (IC
50=19nM) and
in vivo efficacy (ED
50=10mg/kg).
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2. 1, 11-Cyclic Analogs
RIKA OBATA, TOSHIAKI SUNAZUKA, YUMIKO KATO, HIROSHI TOMODA, YOSHIHIRO ...
1996 Volume 49 Issue 11 Pages
1149-1156
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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A series of 1, 11-cyclic analogs of pyripyropene A were prepared. Replacement of the 1, 11-acyl groups of pyripyropenes with 1, 11-cyclic acetals effectively improved
in vitro acyl Co A: cholesterol acyltransferase (ACAT) inhibitory activity. Especially noteworthy is benzylidene acetal analog
35, the most potent inhibitor (IC
50=5.6nM) among the derivatives prepared so far, which showed 16 times more potent inhibitory activity than pyripyropene A.
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O. V. MIROSHNIKOVA, T. F. BERDNIKOVA, E. N. OLSUFYEVA, A. Y. PAVLOV, M ...
1996 Volume 49 Issue 11 Pages
1157-1161
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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An Edman degradation of the antibiotic eremomycin aglycone produced the corresponding hexapeptide, which was aminoacylated with D-lysine, D-histidine or D-tryptophan derivatives to give new hep tapep tide analogs of the eremomycin aglycone. The aminoacylation of the eremomycin aglycone produced an octapeptide analog. The substitution of D-lysine for the
N-terminal
N-methyl-D-leucine does not seriously affect the
in vitro antibacterial properties of the eremomycin aglycone whereas the heptapeptides with the
N-terminal D-tryptophan or D-histidine moieties and the octapeptide with the
N-terminal D-lysine are practically devoid of the antibacterial properties.
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RYUICHIRO HARAI, KENICHIRO SAKAMOTO, HIROYUKI HISAMICHI, NORIAKI NAGAN ...
1996 Volume 49 Issue 11 Pages
1162-1171
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
JOURNAL
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A series of cephalosporins having a (dimethylisoxazolidinio)vinyl group at their 3-position were synthesized to investigate their structure-activity relationships. With regard to the olefin geometry, the (
E)-vinyl compound exhibited higher
in vitro activity than the (
Z)-compound. Regarding the C-7 substituents, the replacement of 2-aminothiazole with 5-amino-l, 2, 4-thiadiazole increased the anti-pseudomonal activity. Determination of the absolute configuration of the C-3 substituent is also presented. Among the compounds synthesized, we selected 7β-[(
Z)-2-(5-amino-l, 2, 4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(
E)-2-((
S)-2, 2-dimethyl-5-isoxazolidinio)vinyl]-3-cephem-4-carboxylate (YM-40220), which showed well-balanced
in vitro activity and an excellent
in vivo efficacy against
Staphylococcus aureus Smith, as a candidate for further development.
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JUNG-SIK KIM, KAZUO SHIN-YA, JUN EISHIMA, KAZUO FURIHATA, HARUO SETO
1996 Volume 49 Issue 11 Pages
1172-1174
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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MAKOTO SUNAGAWA, HARUKI MATSUMURA, AKIRA SASAKI, HIROSHI YAMAGA, YOSHI ...
1996 Volume 49 Issue 11 Pages
1175-1178
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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RYUICHIRO HARA, HIROTSUNE ITAHANA, HIROYUKI HISAMICHI, SUMIE FUKUOKA, ...
1996 Volume 49 Issue 11 Pages
1179-1181
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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RYUICHIRO HARA, HIROTSUNE ITAHANA, KENICHIRO SAKAMOTO, HIROYUKI HISAMI ...
1996 Volume 49 Issue 11 Pages
1182-1185
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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KIRITY ROY, SUGATA CHATTERJEE, S. K. DESHMUKH, E. K. S. VIJAYAKUMAR, B ...
1996 Volume 49 Issue 11 Pages
1186-1187
Published: November 25, 1996
Released on J-STAGE: November 21, 2006
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