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HIROYUKI NAGATA, KEIKO OCHIAI, YUMIKO AOTANI, KATSUHIKO ANDO, MAYUMI Y ...
1997 Volume 50 Issue 7 Pages
537-542
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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In the course of screening for inhibitors of the lymphocyte kinase, Lck (p56
lck), aiming at novel immunosuppressants, we isolated a novel alkaloid, lymphostin (LK6-A), from the culture broth of
Streptomyces sp. KYI 1783. Lymphostin was produced in a fermentation medium supplemented with a highly porous polymer resin, which prevented the degradation of this compound in the culture broth. Lymphostin inhibited the kinase activity of Lck with an IC
50 value of 0.05μM, and exhibited potent inhibitory activity against the mixed lymphocyte reaction (MLR) with an IC
50 value of 0.009μM.
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YUMIKO AOTANI, HIROYUKI NAGATA, MAYXJMI YOSHIDA
1997 Volume 50 Issue 7 Pages
543-545
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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Lymphostin (LK6-A), a novel immunosuppressant, was isolated from the culture broth of
Streptomyces sp. KYI 1783. Lymphostin showed potent inhibitory activity against the lymphocyte kinase, Lck (p56
lck). The structure of lymphostin was determined by spectroscopic methods to be a novel tricyclic aromatic alkaloid. A key feature of the structure is the pyrrolo[4, 3, 2-
de]quinoline moiety which is rare among natural products.
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WOQN-HYUNG YEO, BQNG-SIK YUN, NAM-IN BACK, YOUNG-HO KIM, SANG-SEOCK KI ...
1997 Volume 50 Issue 7 Pages
546-550
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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9-Hydroxycrisamicin A, a new cytotoxic isochromanquinone antibiotic, was isolated from a soil microorganism SA246 which was identified as
Micromonospora sp. The molecular formula of 9-hydroxycrisamicin A was determined as C
32H
22O
13 based on the HRFAB-MS analysis, and the structure was determined by various NMR experiments. 9-Hydroxycrisamicin A showed weak antimicrobial activity against Gram-positive bacteria and strong cytotoxic activity against some human cancer cell lines such as SK-OV-3 (ovarian), HCT15 (colon), SK-MEL-2 (melanoma), A549 (lung), XF498 (central nervous system) with ED
50 of 0.47-0.65 μg/ml.
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MASASHI UEKI, ATSUSHI KUSUMOTO, MUHAMMAD HANAFI, KOZO SHIBATA, TOSHIO ...
1997 Volume 50 Issue 7 Pages
551-555
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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A novel antifungal antibiotic, UK-3A, was obtained from the mycelial cake of
Streptomyces sp. 517-02. UK-3A was very similar in structure to UK-2A, a structural relative of antimycin A. The antifungal spectrum of UK-3A was relatively broad (MICs for yeasts and filamentous fungi: 1.56 - 6.25 and 0.39 - 1.56 μg/ml, respectively). The cytotoxic activity of UK-3A was weak (IC
50: 18-100μg/ml).
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KAZUMA KAMIGIRI, TATSUHIRO TOKUNAGA, TAKEO SUGAWARA, KOJI NAGAI, MITSU ...
1997 Volume 50 Issue 7 Pages
556-561
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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Two new types of macrolide antibiotics, YM-32890 A and B, have been isolated from the fermentation broth of
Cytophaga sp. YL-02905S. In this paper, the taxonomy of the producing strain, fermentation, isolation, structure elucidation, and biological activity of the antibiotics are reported. YM-32890 A inhibits the growth of staphylococci including a macrolide-resistant strain, but shows no antimicrobial activity against other Gram-positive, Gram-negative bacteria and yeast.
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JAMES A. JAMISON, DOUGLAS J. ZECKNER, MICHAEL J. RODRIGUEZ
1997 Volume 50 Issue 7 Pages
562-566
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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The synthesis and biological activity of a series of
N-alkylated derivatives of echinocandin B are described and compared with the
N-acylated analogs. The linear, rigid geometry of the side chain that was essential to improve the antifungal potency of the N-acylated series gave similar
in vitro results with the
N-alkylated derivatives. However the slight structural variation forfeited all
in vivo activity.
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NORIKAZU OHTAKE, KOJI YAMADA, EIICHI MANO, OSAMU OKAMOTO, RYOSUKE USHI ...
1997 Volume 50 Issue 7 Pages
567-585
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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The synthesis and biological activity of (l
R, 5
S, 6
S)-2-[(3
S, 5
S)-5-substituted pyrrolidin-3-ylthio]6-[(
R)-1-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylic acid, in which lactams and cyclic amines are introduced as substituents, are described. They showed potent antibacterial activity against Gram-positive and Gram-negative bacteria including
P. aeruginosa. Among them, BO-2502A (
4h-1) was selected for further evaluation.
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NORIKAZU OHTAKE, OSAMU OKAMOTO, SHINJI KATO, RYOSUKE USHIJIMA, HIROSHI ...
1997 Volume 50 Issue 7 Pages
586-597
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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The synthesis and biological activity of (1
R, 5
S, 6
S)-2-[(3
S, 5
S)-5-substituted pyrrolidin-3-ylthio]6-[(
R)-1-hydroxyethyl]-1-methyl- l-carbapen-2-em-3-carboxylic acid, in which aminopropyl, aminopropenyl, and aminopropynyl groups were introduced as substituents, are described. Aminopropyl and aminopropenyl derivatives showed potent
in vitro and
in vivo antibacterial activity against Gram-positive and Gram-negative bacteria including
P. aeruginosa.
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NORIKAZU OHTAKE, OSAMU OKAMOTO, RYUJI MITOMO, YOSHIAKI KATO, KATSUMI Y ...
1997 Volume 50 Issue 7 Pages
598-613
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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The synthesis and biological activity of (1
R, 5
S, 6
S)-2-[(3
S, 5
S)-5-substituted pyrrolidin-3-ylthio]6-[(
R)-1-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylic acid in which hydroxy-substituted aminoethyl, aminopropyl, and aminobutyl groups were introduced as substituents, are described. These derivatives showed potent antibacterial activity against Gram-positive and Gram-negative bacteria including
P. aeruginosa. Among them, lenapenem (BO-2727, 7b), carrying an (
R)-1-hydroxy-3-(
N-methylamino)propyl group, was selected as a development candidate.
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SEIICHI SATO, RYUSUKE NAKAGAWA, RYOSUKE FUDO, YUMIKO FUKUDA, TOSHIHIKO ...
1997 Volume 50 Issue 7 Pages
614-616
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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DI ZHANG, MURALEEDHARAN G. NAIR, MARCIA MURRY, ZHONGZE ZHANG
1997 Volume 50 Issue 7 Pages
617-620
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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MAKOTO SUNAGAWA, HARUKI MATSUMURA, AKIRA SASAKI, HIROSHI YAMAGA, YUTAK ...
1997 Volume 50 Issue 7 Pages
621-627
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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JIN WOO KIM, HISASI ADACHI, KAZUO SHIN-YA, YOICHI HAYAKAWA, HARUO SETO
1997 Volume 50 Issue 7 Pages
628-630
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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MIDORI HOSHI, KUMIKO W. SHIMOTOHNO, TOYOSHIGE ENDO, KAZUO FURIHATA, HA ...
1997 Volume 50 Issue 7 Pages
631-634
Published: July 25, 1997
Released on J-STAGE: November 25, 2006
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