-
TADAAKI MORISHITA, AIYA SATO, TOMOKO ANDO, KIYOSHI OIZUMI, MASAAKI MIY ...
1998 Volume 51 Issue 6 Pages
531-538
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
A novel bone resorption inhibitor, A-75943, was isolated from
Streptomyces sp. SANK 61296. Its structure was determined to be (1″
S, 2′
R, 3″
S, 4
S′, 5″
S)-2-[3″, 5″-dimethyl-2″-oxocyclohexan-1″-yl)-6′-oxotetrahydropyran-4′-yl]acetamide by spectral analyses and chemical conversion of cycloheximide. A-75943 inhibited bone resorption
in vitro in a concentration-dependent manner with an IC
50 of 0.35 μM, and also displayed an inhibitory effect on bone resorption in thyroid and parathyroid-extracted rats.
View full abstract
-
I. Biological Activities
MASAKI GOTO, MASA-AKI MASEGI, TOSHIHIKO YAMAUCHI, KEN-ICHI CHIBA, YOSH ...
1998 Volume 51 Issue 6 Pages
539-544
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
K1115 A, a new anthraquinone derivative, was isolated from the culture broth of
Streptomyces griseorubiginosus (Mer-K1115). K1115A inhibited the direct binding of activator protein-1 (AP-1) to AP-1 oligonucleotide (IC
50 = 100 μM), and the production of collagenase in IL-1α-stimulated rat synovial cells (IC
50 = 60 μM).
In vivo, the application of K1115 A decreased phorbol myristate acetate (PMA)-induced mouse ornithine decarboxylase (ODC) activity. These results indicated that K1115 A is able to attenuate the inflammatory response mediated by AP-1.
View full abstract
-
II. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Structure Determination
NOBUAKI NARUSE, MASAKI GOTO, YOSHIO WATANABE, TADASHI TERASAWA, KAZUYU ...
1998 Volume 51 Issue 6 Pages
545-552
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
A new inhibitor of the action of activator protein-1 (AP-1), designated K1115 A, was isolated from the fermentation broth of an actinomycete strain Mer-K1115. K1115 A was determined to be a new anthraquinone, 3, 8-dihydroxy-1-propylanthraquinone-2-carboxylic acid, based on spectroscopic analysis, derivatization experiments and biosynthetic studies with
13C-enriched acetic acid. Two co-produced compounds, K1115 B
1 and B
2, were also isolated and characterized as new members of the naphthopyranomycin and exfoliamycin group.
View full abstract
-
I. Taxonomy of Producing Strain, Production, Isolation, Physico-chemical Properties and Biological Properties
TETSUO AKIYAMA, SHIGEKO HARADA, FUKIKO KOJIMA, YOSHIKAZU TAKAHASHI, CH ...
1998 Volume 51 Issue 6 Pages
553-559
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
New inhibitors of dipeptidyl peptidaseIII (EC 3.4.14.4) from human placenta, designated as fluostatins A and B, were discovered in the fermentation broth of a strain isolated in our institute. The strain has been identified as
Streptomyces sp. TA-3391 on the basis of taxonomic studies. Fluostatins A and B were purified by Diaion HP-20 chromatography, ethyl acetate extraction, silica gel chromatography and reverse phase preparative HPLC.
With the synthetic substrate, arginyl-arginine-2-naphthylamide, the IC
50 values of fluostatins A and B were 0.44 and 24.0 μg/ml, respectively. Fluostatins A and B were slightly inhibitory against other dipeptidyl peptidases. Fluostatin A showed mixed-type (competitive and noncompeptitive) inhibition with human leucine-enkephalin as a substrate, and the inhibition constant (
Ki) was 14.2 μM.
View full abstract
-
MICHAEL J. RODRIGUEZ, NANCY J. SNYDER, MARK J. ZWEIFEL, STEPHEN C. WIL ...
1998 Volume 51 Issue 6 Pages
560-569
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
LY264826 (A82846B) is a naturally-occurring glycopeptide antibiotic, differing from vancomycin in the stereochemistry of the amino-sugar of the disaccharide function, and the presence of a third sugar attached at the benzylic position of amino acid residue 6. Despite these seemingly subtle differences, LY264826 is approximately 10 times more active than vancomycin against the enterococci. In the pursuit of new antibiotics active against multiresistant Gram-positive organisms, an extensive side chain SAR was developed focusing on the reductive alkylation of LY264826 at the amino function of the disaccharide moiety. A new series of derivatives having varying degrees of structural diversity in the side chain (
e.g. varying lengths and degrees of rigidity) was found to have potent activity against vancomycin-resistant enterococci (MIC's < 1.0 μg/ml) as well as activity against staphylococci and streptococci as good or better than vancomycin.
View full abstract
-
MARTHA C. CONE, ASTRID K. PETRICH, STEVEN J. GOULD, T.MARK ZABRISKIE
1998 Volume 51 Issue 6 Pages
570-578
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
Two small chromosomal DNA fragments (2.6 and 4.8 kb) from the blasticidin S producer
Streptomyces griseochromogenes were cloned in the high copy number vector pIJ702 and shown to confer increased resistance to blasticidin S upon
S. lividans TK24. These fragments were used to screen a library of
S. griseochromogenes DNA prepared in the cosmid shuttle vector pOJ446. Cosmids containing DNA inserts of at least 23 kb were identified which hybridized to one or the other resistance fragment, but not to both. Transformation of
S. lividans TK24 with several cosmids hybridizing with the 4.8 kb resistance fragment resulted in clones that produced cytosylglucuronic acid, the first intermediate of the blasticidin S biosynthetic pathway, and other blasticidin-related metabolites. A strain of
S. lividans TK24 harboring both the 4.8 kb-hybridizing cosmid and the 2.6 kb resistance fragment cloned in pIJ702 produced 12.5 times as much demethylblasticidin S as the transformant harboring the cosmid alone.
View full abstract
-
I. Fermentation, Isolation, Physico-chemical Properties and Biological Activities
S.R. NADKARNI, TRIPTIKUMAR MUKHOPADHYAY, R.G. BHAT, S.V. GUPTE, B. SAC ...
1998 Volume 51 Issue 6 Pages
579-581
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
II. Structure Elucidation
TRIPTIKUMAR MUKHOPADHYAY, E.K.S. VIJAYAKUMAR, S.R. NADKARNI, H.-W. FEH ...
1998 Volume 51 Issue 6 Pages
582-585
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
II. Structure Determination
TETSUO AKIYAMA, KAZUO T. NAKAMURA, YOSHIKAZU TAKAHASHI, HIROSHI NAGANA ...
1998 Volume 51 Issue 6 Pages
586-588
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
YASUSHI TANAKA, UDO GRÄEFE, KATSUKIYO YAZAWA, YUZURU MIKAMI
1998 Volume 51 Issue 6 Pages
589-591
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
KOZO OCHI, YOSHIKO HOSOYA
1998 Volume 51 Issue 6 Pages
592-595
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
SENJI TAKAHASHI, NORIHIRO KAKINUMA, KENICHI UCHIDA, RYUJU HASHIMOTO, T ...
1998 Volume 51 Issue 6 Pages
596-598
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
GEORGE BURTON, STEVEN COULTON, FRANK P. HARRINGTON, JEREMY D. HINKS, R ...
1998 Volume 51 Issue 6 Pages
599-601
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
KUNIAKI TATSUTA, NAOYUKI MASUDA
1998 Volume 51 Issue 6 Pages
602-606
Published: June 25, 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
1998 Volume 51 Issue 6 Pages
C2a
Published: 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS
-
1998 Volume 51 Issue 6 Pages
C2b
Published: 1998
Released on J-STAGE: January 27, 2009
JOURNAL
FREE ACCESS