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TADAAKI MORISHITA, AIYA SATO, MARIE HISAMOTO, TOMIICHIRO ODA, KEIIGHI ...
1997 Volume 50 Issue 6 Pages
457-468
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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N-(3-Acyloxyacyl)glycines were isolated as N-type calcium channel blockers from a marine bacterium
Cytophaga sp. SANK 71996. The identification and fermentation of the producing strain and structure characterization of
N-(3-acyloxyacyl)glycines by spectral analyses and chemical syntheses are described together with their antagonistic activities.
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I. Taxonomy, Fermentation, Isolation and Biological Activities
CHOONG HWAN LEE, MYUNG CHUL CHUNG, HO JAE LEE, KYUNG SOOK BAE, YUNG HE ...
1997 Volume 50 Issue 6 Pages
469-473
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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New melanin synthesis inhibitors (MR566A and B) and six related known isocyanocyclopentenes were isolated from the fermentation broth of
Trichoderma harzianum. The IC
50 values of MR566A and B against mushroom tyrosinase were 1.72 and 47μM, respectively. They inhibited melanin biosynthesis in B16 melanoma cells with MIC values of 0.1 and 2.2μM, respectively. Also isolated from the same culture extract of
T. harzianum was a new oxazole (MR93B), which showed no inhibitory activity against mushroom tyrosinase at a concentration of 1.000μg/ml.
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II. Physico-chemical Properties and Structural Elucidation
CHOONG HWAN LEE, HIROYUKI KOSHINO, MYUNG CHUL CHUNG, HO JAE LEE, JONG ...
1997 Volume 50 Issue 6 Pages
474-478
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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New melanin synthesis inhibitors (MR566A and B) and six related known isocyanocyclopentenes were isolated from the fermentation broth of
Trichoderma harzianum, and their structures were elucidated by spectroscopic methods. The structures of novel isocyanides, MR566A (
1) and B (
2), were elucidated as 1-(3-chloro-1, 2-dihydroxy-4-isocyano-4-cyclopenten-1-yl)ethanol, 1-(1, 2, 3-trihydroxy-3-isocyano-4-cyclopenten-1-yl)ethanol, respectively. The structure of novel oxazole, MR93B (
9), was elucidated as 4-[(1
Z)-3-hydroxy-2-hydroxymethyl-1-propen-1-yl]oxazole.
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KLAUS PUSECKER, HARTMUT LAATSCH, ELISABETH HELMKE, HORST WEYLAND
1997 Volume 50 Issue 6 Pages
479-483
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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The novel 5, 10-dihydrophencomycin methyl ester (
4) and the known microbial metabolites (2-hydroxyphenyl)-acetamide (
1), menaquinone MK9 (II, III, VIII, IX-H8) (
2), and phencomycin (
3a) were isolated from an unidentified marine
Streptomyces sp. and the structures were elucidated by NMR methods. Compound
4 shows weak antibiotic activity against
Escherichia coll and
Bacillus subtilis.
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STEFANIA STEFANELLI, EMILIANA CORTI, NICOLETTA MONTANINI, MAURIZIO DEN ...
1997 Volume 50 Issue 6 Pages
484-489
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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We describe here the results of a screening program conducted to discover inhibitors of the type-I interleukin-1 receptor (IL-1RI) from samples of microbial origin. An innovative approach, based on automated, nonradioactive receptor binding assays has been employed. Specially prepared cell-free systems have allowed the use of high concentrations of microbial metabolites in the reaction mixtures with a low percentage of false positives. More than 30, 000 microbial samples from different species of soil isolates have been tested and two interesting activities have been purified and characterized. One of these, isolated from
Streptomyces sp. GE48009, was identified as niphimycin, an antifungal agent also known as scopafungin. Preliminary evidence suggests that this molecule and azalomycin F, a structural analogue, inhibit IL-1RI by virtue of their long-chain guanidinium moiety. The other activity, isolated from
Aspergillus sp. GE49752, was identified as flavipin, a substituted
o-phthalaldehyde.
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NOBORU FUJII, FUTOSHI TANAKA, YOSHINORI YAMASHITA, TADASHI ASHIZAWA, S ...
1997 Volume 50 Issue 6 Pages
490-495
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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A novel antitumor antibiotic, UCE6 (1, 3, 8, 10, ll-pentahydroxy-2-methyl-10-(2-oxo-4-hydroxypentyl)naphthacene-5, 12-dione) with topoisomerase I-mediated DNA cleavage activity, was isolated from the culture broth of actinomycetes strain UOE6. Addition of silicone oil antifoam agent, KS69 (2%), to the fermentation enhanced the production of UCE6 by -3 fold. A total of 1.15 g of UCE6 was recovered as reddish orange crystals from a 100 liter fermentation supplemented with 2% KS69. UCE6 exhibited growth inhibitory activity against HeLa S3, HCT116 and Lu-65 cells comparable to that of camptothecin.
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TERO KUNNARI, JAANA TUIKKANEN, ANNE HAUTALA, JUHA HAKALA, KRISTIINA YL ...
1997 Volume 50 Issue 6 Pages
496-501
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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Streptomyces steffisburgensis (NRRL 3193, ATCC 27466) is described as a steffimycin producer. Steffimycin belongs to the anthracycline group of aromatic polyketide antibiotics. The structural analysis of the products accumulated by the wild type ATCC 27466 strain revealed three different forms of 8-demethoxy steffimycin suggesting the loss of C-8 hydroxylation/methylation activity. In our approach to generate new anthracycline molecules, we used this strain as a host in gene cloning. The genes encoding the polyketide ketoreductase and aromatase enzymes of nogalamycin biosynthesis caused the production of 2-demethoxy Steffimycins in
S. steffisburgensis.
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ELENA ORTEGA, MANUEL A. DE PABLO, AURELIA Ma GALLEGO, CARME ...
1997 Volume 50 Issue 6 Pages
502-508
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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The imipenem/cilastatin constitutes a broad spectrum β-lactam antibiotic formulation, especially used in pre and post-operatory treatments for transplanted or drug-immunosuppresed patients. The effect of the dose and the duration of the treatment with imipenem/cilastatin on some parameters of natural immunity in BALB/c mice were examined. The treatment by intraperitoneal route with 1 or 2 g/70 kg/day during 7 days did not alter significantly the parameters tested, whereas the greater dose used (4 g/70 kg/day) had an inhibitory effect on peritoneal cell counts and phagocytic activity, as well as it caused an increase on IL-1 production and natural killer activity. The greater stimulating effect of innate immunity was obtained with the lowest imipenem/cilastatin dose used (0.5 g/70 kg/day). Since this antibiotic apparently does not impair the studied innate immune responses at 1 or 2 g/70 kg/day, it seems to be especially suited for the therapy of systemic bacterial infections in immunocompromised patients.
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ANDREI Y. PAVLOV, EDUARD I. LAZHKO, MARIA N. PREOBRAZHENSKAYA
1997 Volume 50 Issue 6 Pages
509-513
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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A series of derivatives of eremomycin aminomethylated at the 7d position of the resorcinol ring of the amino acid No. 7 was prepared by interaction of eremomycin with formaldehyde and various primary and secondary amines and ammonia. The most active compound obtained was 7d-decylaminomethyl derivative, whose minimal inhibitory concentrations for clinical isolates of staphylococci are 2-8 times lower than those of the parent antibiotic. 7d-Decylaminomethyl derivative was also active against vancomycin-resistant VanA enterococci (8 μg/ml) and
Neisseria gonorrhoeae (16 μg/ml).
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SHIGERU F. HAYASHI, LAURA J. L. NORCIA, SCOTT B. SEIBEL, ANNETTE M. SI ...
1997 Volume 50 Issue 6 Pages
514-521
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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Several analogs of hygromycin A were tested in an
Escherichia coli cell free protein synthesis inhibition assay and in a
Serpulina hyodysenteriae whole cell assay. The aminocyclitol moiety is essential for antibacterial activity in both cell free and whole cell assays. However a 4'-
O-allyl ether of hygromycin A aglycone showed an equivalent MIC to hygromycin A, while having a less potent IC
50 in the cell free assay. Hence 6-deoxy-5-keto-D-arabino-hexofuranose can be replaced by a hydrophobic allyl group and still retain antibacterial activity. However, this replacement reduces the intrinsic protein synthesis inhibition activity. The loss of intrinsic activity with replacement by the allyl group may be compensated for by better transport into the bacterial cell. In addition to the SAR analysis, we demonstrated that the ineffectiveness of hygromycin A against Gram-negative enteric bacteria such as
Escherichia coli is mainly due to the efflux mechanism (Acr A/B pump) existing widely among the enteric bacteria rather than the impermeable barrier of the outer membrane.
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OSAMU JOHDO, TAKEO YOSHIOKA, TOMIO TAKEUCHI, AKIHIRO YOSHIMOTO
1997 Volume 50 Issue 6 Pages
522-525
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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ANTONIETA TADDEI, AXEL ZEECK
1997 Volume 50 Issue 6 Pages
526-528
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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KEN-ICHI KIMURA, SHOJI NAKAYAMA, JUNJI NAKAMURA, TAKEKO TAKADA, MAKOTO ...
1997 Volume 50 Issue 6 Pages
529-531
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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ANDREW HESKETH, KOZO OCHI
1997 Volume 50 Issue 6 Pages
532-535
Published: June 25, 1997
Released on J-STAGE: November 25, 2006
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