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SATOSHI NAKANISHI, KATSUNORI KITA, YOUICHI UOSAKI, MAYUMI YOSHIDA, YUT ...
1994 Volume 47 Issue 8 Pages
855-861
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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MS-282a and MS-282b were isolated from the culture broth of
Streptomyces tauricus ATCC 27470 as inhibitors of smooth muscle myosin light chain kinase (MLCK). MS-282a and MS-282b inhibited the activity of chicken gizzard MLCK with IC
50 values of 3.8μM and 5.2μm, respectively. Cyclic AMP-dependent protein kinase, cyclic GMP-dependent protein kinase and protein kinase C were not inhibited by 150μM MS-282a at all. It is likely that MS-282a blocks MLCK activity by antagonizing calmodulin since 1) the compound inhibited calmodulin-dependent but not calmodulin-independent activity of MLCK; 2) the inhibition of MLCK was antagonized by increasing concentrations of calmodulin, and 3) the compound inhibited calmodulin-dependent cyclic nucleotide phosphodiesterase.
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I. TAXONOMY OF THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY
JAMES P. KARWOWSKI, MARIANNA JACKSON, GABRIELA SUNGA, PAUL SHELDON, JE ...
1994 Volume 47 Issue 8 Pages
862-869
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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The dorrigocins are new secondary metabolites produced by submerged fermentation of a streptomycete which was isolated from a soil sample collected in Australia. The dorrigocins show moderate antifungal activity and reverse the morphology of
ras-transformed NIH/3T3 cells from a transformed phenotype to a normal one. The producing culture was identified as
Streptomyces platensis subsp.
rosaceus strain AB1981F-75.
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II. ISOLATION AND ELUCIDATION OF STRUCTURES
JILL E. HOCHLOWSKI, DAVID N. WHTTERN, PRESTON HILL, JAMES B. MCALPINE
1994 Volume 47 Issue 8 Pages
870-874
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Two novel antifungal antibiotics, named dorrigocin A and B have been isolated from the fermentation broth and mycelium of
Streptomyces platensis subsp.
rosaceus. These closely related compounds were separated from one another by countercurrent chromatography on an Ito coil planet centrifuge. The structures of the dorrigocins were determined by NMR and IR spectroscopy and mass spectrometry. Each is a putative propionate - acetate derived straight chain fatty acid terminating in cycloheximide. The dorrigocins differ from one another only in their oxidation pattern.
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III. BIOLOGICAL PROPERTIES AND MECHANISM OF ACTION
SUNIL KADAM, JAMES B. MCALPINE
1994 Volume 47 Issue 8 Pages
875-880
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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The dorrigocins are unique glutarimide antibiotics which were found to reverse the morphology of
ras-transformed NIH/3T3 cells from a transformed phenotype to a normal one. The compounds also inhibited the release of yeast mating pheromone, a-factor. The activity of these compounds was not dependent on inhibition of prenylation or protein synthesis. Dorrigocin A was instead found to inhibit the carboxyl methylation in
K-
ras transformed cells.
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PRODUCTION, ISOLATION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
BRIGITTE KUNZE, ROLF JANSEN, GERHARD HÖFLE, HANS REICHENBACH
1994 Volume 47 Issue 8 Pages
881-886
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Crocacin was isolated from the biomass of the myxobacterium
Chondromyces crocatus, strain Cm c3. It inhibited the growth of a few Gram-positive bacteria and a wide spectrum of yeasts and molds. In beef heart submitochondrial particles, crocacin blocked the electron transport within the
bc1 -segment (complex III) and caused a red shift in the reduced spectrum of cytochrome
b with a maximum at 569 nm.
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I. TAXONOMY, FERMENTATION AND BIOLOGICAL EVALUATION
D. A. STEINBERG, V. S. BERNAN, D. A. MONTENEGRO, D. R. ABBANAT, C. J. ...
1994 Volume 47 Issue 8 Pages
887-893
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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The new glycothiohexide antibiotics, which are related to nosiheptide, were identified in fermentations of an actinomycete belonging to the genus "
Sebekia". Strain LL-14E605 was classified as a "
Sebekia" based on the presence of both mesodiaminopimelic acid and madurose in the cell wall and the presence of pseudosporangia encasing the spores. Culture LL-14E605 was successfully fermented in 10 to 3, 000 liters of a complex medium. Antibiotic activity closely followed cell mass accumulation and usually peaked after 4 to 5 days of incubation. Glycothiohexide α demonstrated excellent
in vitro activity against Gram-positive bacteria with MICs of 0.03 to 0.06μ/ml against methicillin-resistant
Staphylococcus aureus and vancomycin-resistant
Enterococcus faecalis. However, glycothiohexide α failed to protect mice against a lethal challenge with
Staphylococcus aureus Smith unless it was administered prior to challenge.
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II. ISOLATION AND PHYSICAL-CHEMICAL CHARACTERIZATION
P. T. NORTHCOTE, D. WILLIAMS, J. K. MANNING, D. B. BORDERS, W. M. MAIE ...
1994 Volume 47 Issue 8 Pages
894-900
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Glycothiohexide α was recovered from the fermentation broth of a "
Sebekia" sp. by mixed solvent extraction, selective precipitation and adsorption chromatography on Diaion HP-20. The amount of glycothiohexide α present in the crude preparation was enriched by photolysis. Purification of glycothiohexide α was accomplished by repetitive countercurrent Chromatography.
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III. STRUCTURAL ELUCIDATION
P. T. NORTHCOTE, M. SIEGEL, D. B. BORDERS, M. D. LEE
1994 Volume 47 Issue 8 Pages
901-908
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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The chemical structure of a novel thiopeptide antibiotic, glycothiohexide α (
1), isolated from the fermentation broth of a "
Sebekia" species was determined based on extensive 2D NMR studies, as well as, IR, UV, and mass spectral data. The chemical structure of glycothiohexide α is closely related to nosiheptide (
3) and antibiotic S-54832A.
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YUHKO AOKI, MASUMI KONDOH, MUTSUMI NAKAMURA, TOSHIHIKO FUJII, TOSHIKAZ ...
1994 Volume 47 Issue 8 Pages
909-916
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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A new antifungal, azoxybacilin (an unusual amino acid with an azoxy moiety) was identified from
Bacillus cereusd, and its
in vitro antifungal activity and mode of action were investigated. Azoxybacilin was active against a broad spectrum of fungi. It was especially active against mycelial fungi, such as
Aspergillus, and did not show antibacterial activity. No cross-resistance with antifungals currently on the market was observed.
The IC
50 values of azoxybacilin antifungal activity against
Saccharomyces cerevisiae were significantly greater when amino acids containing sulfur were added to the growth medium, whereas other amino acids were not effective at all. We, therefore, tested the effect of the intermediates involved in the synthetic pathway of these amino acids. The activity markedly diminished when one of the following four intermediates was present in the medium: homocysteine, cysteine, cystathionine or methionine. These four intermediates were the same as those required for the growth of the
O-acetylhomoserine sulfhydrylase mutant,
S. cerevisiae ONO726, indicating that azoxybacilin would inhibit a step or steps in the sulfur-fixation pathway.
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TSUNEAKI HIDA, MASAYUKI MUROI, SEIICHI TANIDA, SETSUO HARADA
1994 Volume 47 Issue 8 Pages
917-921
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Dnacin A
1 and B
1 were revealed to be new naphthyridinomycin-type antitumor antibiotics with formulae of C
20H
23N
5O
4 and C
19H
24N
4O
5, respectively. The gross structure of dnacin A
1 was elucidated by the spectroscopic analyses. Conversion of dnacin B
1 into A
1 by treatment with potassium cyanide indicated the presence of an α-carbinolamine moiety in dnacin B
1. The relative stereochemistry of dnacins was clarified by analysis of the NOESY spectra.
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JENN-JONG YOUNG, LIARNG-JYUR JUNG, WEN-TSSANN LIU, SU-NENG HO, LI-REN ...
1994 Volume 47 Issue 8 Pages
922-931
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Studies on the solution conformation of the cyclic depsipeptide antibiotic enopeptin A have been carried out using 2D NMR and molecular modelling techniques. The proton resonances of the antibiotic in DMSO-
d6 have been assigned by the use of TOCSY and ROESY experiments. The interproton distance information obtained from the ROESY experiments have been used as the basis for elucidating the probable structures in solution. The restrained molecular dynamics technique was applied to calculate the structures in solution, and six resultant structures with fewer distance constraint violations were obtained that satisfy the experimental restraints very well. The conformation of the cyclic moiety of the molecule is well defined whereas the aliphatic chain segment is disordered.
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YOSHIYUKI KOBAYASHI, HIDEKI MIYAZAKI, MASAO SHIOZAKI, HIDEYUKI HARUYAM ...
1994 Volume 47 Issue 8 Pages
932-938
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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Synthesis of 5-
epi-trehazolin (trehalostatin) (
2) was accomplished
via the crucial intermediate, epoxide (
6α), from D-glucose. The stereochemistry of epoxide (
6α) and its isomer (
6β) which were obtained from Sharpless epoxidation, was determined by comparison between the NMR relaxation times of relevant protons.
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HIDEHARU ODAI, KAZUTOSHI SHINDO, ATSUO ODAGAWA, JUNICHIRO MOCHIZUKI, M ...
1994 Volume 47 Issue 8 Pages
939-941
Published: August 25, 1994
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ROBERT D. STIPANOVIC, CHARLES R. HOWELL, PAUL A. HEDIN
1994 Volume 47 Issue 8 Pages
942-944
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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RIE TANAKA, KOSHI NAMIKAWA, TAKASHI NAKATSUKA, HIDEKI ADACHI, TAKURO Y ...
1994 Volume 47 Issue 8 Pages
945-948
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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NOBORU FUJII, YOSHINORI YAMASHITA, KATSUHIKO ANDO, TSUTOMU AGATSUMA, Y ...
1994 Volume 47 Issue 8 Pages
949-951
Published: August 25, 1994
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MASATO MARUYAMA, CHIGUSA NISHIDA, YOSHIKAZU TAKAHASHI, HIROSHI NAGANAW ...
1994 Volume 47 Issue 8 Pages
952-954
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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SHUNJI KAGEYAMA, TSUTOMU TSUCHIYA
1994 Volume 47 Issue 8 Pages
955-956
Published: August 25, 1994
Released on J-STAGE: April 19, 2006
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