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Producing Organism, Fermentation, Isolation, and Biological Activity
SUZANNE M. MANDALA, ROSEMARY A. THORNTON, BETH R. FROMMER, JAMES E. CU ...
1995 Volume 48 Issue 5 Pages
349-356
Published: May 25, 1995
Released on J-STAGE: April 19, 2006
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Potent antifungal activity was detected in fermentation extracts of
Sporormiella australis and two related components were isolated from solid fermentations using silica gel and high speed countercurrent chromatography. The most active antifungal component, australifungin, contained a unique combination of α-diketone and β-ketoaldehyde functional groups. Australifungin exhibited broad spectrum antifungal activity against human pathogenic fungi with MICs against
Candida spp.,
Cryptococcus neoformans, and
Aspergillus spp. between 0.015 and 1.0 μg/ml. Mode of action studies revealed that australifungin interfered with fungal lipid metabolism by specifically inhibiting sphingolipid synthesis at the step converting Sphinganine to ceramide.
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HIDEYUKI SHIOZAWA, MASAAKI TAKAHASHI, TOSHIO TAKATSU, TAKESHI KINOSHIT ...
1995 Volume 48 Issue 5 Pages
357-362
Published: May 25, 1995
Released on J-STAGE: April 19, 2006
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Trachyspic acid, a new metabolite that inhibited heparanase, was isolated from the culture broth of
Talaromyces trachyspermus SANK 12191. Its structure was deduced from NMR spectral analyses and chemical reactions as a tricarboxylic acid derivative containing a spiroketal. The IC
50 value of trachyspic acid against heparanase was 36 μM.
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Taxonomy, Fermentation, Isolation, Structure Elucidation and Biological Activity
YUKIHIRO AKEDA, KOZO SHIBATA, XU PING, TOSHIO TANAKA, MAKOTO TANIGUCHI
1995 Volume 48 Issue 5 Pages
363-368
Published: May 25, 1995
Released on J-STAGE: April 19, 2006
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An antibiotic complex, AKD-2, was isolated from the mycelial cake of
Streptomyces sp. OCU-42815. The lipophilic substances in this complex were further purified by a recycling HPLC procedure and were designated AKD-2A, C and D. AKD-2B was obtained as a mixture of AKD-2B
1 and AKD-2B
2. These substances were identified as monoglycerides having branched chain fatty acids and exhibited both antibacterial and antifungal activities.
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Taxonomy, Fermentation, Isolation, Physico-chemical and Biological Properties
NARINDER S. MAKKAR, THOMAS E. NICKSON, MINHTIEN TRAN, NANCY BIEST, MAR ...
1995 Volume 48 Issue 5 Pages
369-374
Published: May 25, 1995
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A new derivative of phenylalanine, phenamide, was discovered from the fermentation broth of an actinomycete identified as a member of the
Streptomyces albospinus cluster. Phenamide was purified using successive CIS reverse phase and cation exchange chromatography. Its structure was determined by spectroscopic and chemical methods. Its molecular formula, C
14H
20N
2O
3, was determined by HRFAB-MS. Phenamide showed activity against
Septoria nodorum, the causal agent of wheat glume blotch.
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GERHARD SCHLINGMANN, LISA MILNE, CEDRIC J. PEARCE, DONALD B. BORDERS, ...
1995 Volume 48 Issue 5 Pages
375-379
Published: May 25, 1995
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Antibiotic 07F275 (
1), produced by submerged fermentations of fungal culture LL-07F275, was isolated and characterized despite its inherent instability. Its UV spectrum was identical with that of nemo tin, a member of the allenic polyacetylene family, but a molecular weight of 218 daltons indicated a new compound. Structure
1 was determined on the basis of spectroscopic evidence, particularly NMR. Since
1 is a thirteen carbon-containing allenic diyne, it is closely related to mycornycin.
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NEAL S. BURRES, USHA PREMACHANDRAN, SHARON HOSELTON, DOLORES CWIK, JIL ...
1995 Volume 48 Issue 5 Pages
380-386
Published: May 25, 1995
Released on J-STAGE: April 19, 2006
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Determination of the mechanism of action of FK506 and cyclosporin A has yielded new molecular targets involved in signal transduction during T cell activation. A common target of FK506 and cyclosporin A is inhibition of activation of the NFAT transcription factor, for which a specific binding region is present in the promoter of the IL-2 gene. A reporter gene assay has been used to screen for agents that interfere with this early step in T cell activation. Simple aromatic compounds that block NFAT-dependent transcription and show
in vitro immunosuppressive activity were isolated from the broth and mycelia of two
Streptomyces sp. fermentations. The compounds were active at concentrations that were not directly cytotoxic.
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HIDEAKI UI, MASAYA IMOTO, KAZUO UMEZAWA
1995 Volume 48 Issue 5 Pages
387-390
Published: May 25, 1995
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We isolated fluvirucin B
2 from the culture broth of
Streptomyces as an inhibitor of phosphatidylinositol-specific phospholipase C (PI-PLC). It inhibited PI-PLC of A431 cell cytosol with an IC
50 of 1.6 μg/ml. Fluvirucin B
2 also inhibited PI-PLC in cultured A431 cells, whereas it did not inhibit phosphatidylinositol synthesis and macromolecular synthesis markedly. It also inhibited epidermal growth factor-induced rapid rounding of A431 cells, in which PI turnover is involved.
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M. G. ANDERSON, T. B. JARMAN, R. W. RICKARDS
1995 Volume 48 Issue 5 Pages
391-398
Published: May 25, 1995
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Spectroscopic data define the structures of three new antibiotics, 4', 5'-dihydro-oligosporon (
4), hydroxyoligosporon (
5) and 10', H'-epoxy oligosporon (
6) from the nematode-trapping fungus
Arthrobotrys oligospora, and confirm the structures of the recently reported antibiotics oligosporon (
1) and oligosporol B (
3). The absolute configuration of the substituted 7-oxabicyclo[4.1.0]hept-3-ene nucleus of these metabolites is determined by circular dichroic spectroscopy. Oligosporon (
1) and its dihydro-derivative (
4) represent the second and most complex structural type of nematocidal metabolite to be characterised from cultures of nematophagous fungi.
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G. PENTASSUGLIA, G. TARZIA, D. ANDREOTTI, C. BISMARA, R. CARLESSO, D. ...
1995 Volume 48 Issue 5 Pages
399-407
Published: May 25, 1995
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6-α and 6-β Alkylcarbonylmethyl penems were synthesized from 6-α-bromo and 6-oxo penicillanates respectively and their
in vitro antibacterial activity was studied. The compounds were generally active against Gram-positive but not against Gram-negative strains, the compounds of the 6-β series being more active. Relatively to imipenem, taken as reference compound, the penems resulted more stable towards chemical hydrolysis in Tris-HCl buffered medium (pH 7.4) but more sensitive towards dehydropeptidase-I (DHP-I).
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MAKOTO SUNAGAWA, HARUKI MATSUMURA, YOSHIHIRO SUMITA, HIROSHI NOUDA
1995 Volume 48 Issue 5 Pages
408-416
Published: May 25, 1995
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The neurotoxicity of meropenem was much lower than that of both imipenem and panipenem after intraventricular administration to mice. To clarify the major structural features responsible for the induction of convulsions by carbapenem antibiotics, the structure-activity relationship on convulsant activity was investigated in
N-acetyl-2-pyrroline and cyclopentene derivatives which correspond to the 5-membered ring containing the C-2 side chain of carbapenem antibiotics. Among these derivatives, compounds with strong basicity in the side chain showed convulsant activity similar to that of the parent carbapenem compounds. In addition to the strength of the basicity of the amino group, the distance from the carboxyl to the amino group and steric crowding around the amino group also appeared to play an important role in the induction of convulsions. The results of gamma aminobutyric acid (GABA
A) receptor binding assays indicated that the induction of convulsions was caused predominantly by the inhibition of GABA
A-mediated inhibitory transmission. However, the
in vivo convulsant activity of some of these compounds did not correlate with their
in vitro inhibitory effect on GABA
A receptor binding.
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Synthesis and Biological Properties of BRL 57342 and Some Close Analogues
RICHARD G. ADAMS, EDWARD G. BRAIN, CLIVE L. BRANCH, ANGELA W. GUEST, F ...
1995 Volume 48 Issue 5 Pages
417-424
Published: May 25, 1995
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(6
R, 7
R)-7-[2-(2-Amino-4-thiazolyl)-2-[(
Z)-[(
S)-carboxy(3, 4-dihydroxyphenyl)methyl]oxyimino]acetamido]-3-(l-methylaminopyridinium-4-thiomethyl)ceph-3-em-4-carboxylate sodium salt (BRL 57342,
1f) combines excellent
in vitro antibacterial potency against Gram-positive and Gram-negative bacteria, including
P. aeruginosa and
Acinetobacter spp., with excellent stability to extended spectrum β-lactamases. This potency is reflected in
in vivo efficacy studies.
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JON S. MYNDERSE, DAVID S. FUKUDA, ANN H. HUNT
1995 Volume 48 Issue 5 Pages
425-427
Published: May 25, 1995
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K. GOEKE, P. HOEHN, O. GHISALBA
1995 Volume 48 Issue 5 Pages
428-430
Published: May 25, 1995
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The Structures of the Exfoliamycins
CORINNA VOLKMANN, AXEL ZEECK, OLIVIER POTTERAT, HANS ZÄHNER, FRAN ...
1995 Volume 48 Issue 5 Pages
431-432
Published: May 25, 1995
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MITSUAKI TSUNAKAWA, SHU-LOK HU, YUTAKA HOSHINO, DAVID J. DETLEFSON, SU ...
1995 Volume 48 Issue 5 Pages
433-434
Published: May 25, 1995
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NAOTO KAWAMURA, RYUICHI SAWA, YOSHIKAZU TAKAHASHI, KUNIO ISSIKI, TSUTO ...
1995 Volume 48 Issue 5 Pages
435-437
Published: May 25, 1995
Released on J-STAGE: April 19, 2006
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