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JACK E. BALDWIN, GREGORY P. LYNCH, JANOS PITLIK
1991 Volume 44 Issue 1 Pages
1-24
Published: January 25, 1991
Released on J-STAGE: April 19, 2006
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PRODUCTION, ISOLATION, CHEMICAL PROPERTIES, STRUCTURE AND BIOLOGICAL ACTIVITY
YASUMASA ISHIHARA, MASAHISA OKA, MITSUAKI TSUNAKAWA, KOJI TOMITA, MASA ...
1991 Volume 44 Issue 1 Pages
25-32
Published: January 25, 1991
Released on J-STAGE: April 19, 2006
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Melanostatin, a new antibiotic with melanin synthesis inhibitory activity, was isolated from the fermentation broth of
Streptomyces clavifer No. N924-2. Its structure was determined by spectral analysis and degradation experiments. Melanostatin strongly inhibited melanin formation in
Streptomyces bikiniensis NRRL B-1049 and B16 melanoma cells.
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PRODUCING ORGANISM, FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES
MITSUNOBU KARA, TOSHIMITSU TAKIGUCHI, TADASHI ASHIZAWA, KATSUSHIGE GOM ...
1991 Volume 44 Issue 1 Pages
33-39
Published: January 25, 1991
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In screening actinomycetes for antitumor compounds,
Streptomyces sp. DO-116 was found to produce a new antitumor antibiotic sapurimycin. It is structurally related to, but distinct from, kapurimycins. The antibiotic was produced in a fermentation medium supplemented with high porus polymer resin which adsorbs antibiotic in the culture and results in an increase of titer. Active material was separated from the polymer resin by a solvent extraction procedure and isolated by repeated solvent extraction, adsorption chromatography and HPLC. Sapurimycin was active against bacteria, particularly Gram-positive organisms. It exhibited antitumor activity against leukemia P388 and sarcoma 180 in mice. Sapurimycin caused single strand breaks in supercoiled plasmid DNA
in vitro. These results are discussed in comparison with data for kapurimycins.
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STRUCTURE DETERMINATION
YOUICHI UOSAKI, TOHRU YASUZAWA, MITSUNOBU HARA, YUTAKA SAITOH, HIROSHI ...
1991 Volume 44 Issue 1 Pages
40-44
Published: January 25, 1991
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The structure of a new anthra-γ-pyrone antitumor antibiotic sapurimycin was determined by the spectral studies of its methyl ester. Sapurimycin has the same anthra-γ-pyrone skeleton as pluramycin, but is distinctly different because of the absence of sugars on the D ring and possessing a carboxylmethyl group on C-5.
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I. FERMENTATION, ISOLATION, AND BIOLOGICAL ACTIVITY
FRANK VANMIDDLESWORTH, MARY NALLIN OMSTEAD, DENNIS SCHMATZ, KEN BARTIZ ...
1991 Volume 44 Issue 1 Pages
45-51
Published: January 25, 1991
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A new β-1, 3-D-glucan synthesis inhibitor, L-687, 781 is produced by the cultivation of
Dictyochaeta simplex ATCC 20960. L-687, 781 exhibits potent
in vitro antifungal activity as well as anti-
Pneumocystis activity in a rat model.
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TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES, BIOLOGICAL CHARACTERISTICS AND STRUCTURE DETERMINATION
YOSHIMASA NAKANO, TOMOYUKI KAWAGUCHI, JUNKO SUMITOMO, TAEKO TAKIZAWA, ...
1991 Volume 44 Issue 1 Pages
52-58
Published: January 25, 1991
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A new inhibitor of superoxide anion generation by guinea pig macrophages, OPC-15160, was isolated from the culture broth of fungus
Thielavia minor OFR-1561, and a more potent inhibitor, OPC-15161, was obtained as a major degradation product of OPC-15160. OPC-15161 was five times more active than the natural inhibitor and its IC
50 value was 2.8 × 10
-5 M. The structure of OPC-15161 was elucidated by X-ray analysis to be 6-(1
H-indol-3-ylmethyl)-5-methoxy-3-(2-methylpropyl)-2-(1
H)-pyrazinone, 4-oxide and had a novel and highly functionalized pyrazine skeleton.
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XXXVIII. 2-METHOXY-5-METHYL-1, 4-BENZOQUINONE, A THROMBOXANE A2 RECEPTOR ANTAGONIST FROM LENTINUS ADHAERENS
URSULA LAUER, TIMM ANKE, FRITZ HANSSKE
1991 Volume 44 Issue 1 Pages
59-65
Published: January 25, 1991
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In the course of our screening for antithrombotic compounds using platelet rich plasma from bovine slaughter blood, 2-methoxy-5-methyl-1, 4-benzoquinone (
1) has been isolated from mycelial cultures of
Lentinus adhaerens. The compound inhibits the U46619-induced aggregation of human blood platelets with an IC
50 of 2.5 μg/ml (16.45 μM) and is a new thromboxane A
2 receptor antagonist.
This is the first report on an inhibitor of platelet aggregation derived from secondary metabolism of basidiomycetes.
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XIII. ANTI-TUBULIN ACTIVITY AND CYTOTOXICITY OF RHIZOXIN DERIVATIVES: SYNTHESIS OF A PHOTOAFFINITY DERIVATIVE
Yuzo KATO, YUJI OGAWA, TAKASHI IMADA, SHIGEO IWASAKI, NAOMI SHIMAZAKI, ...
1991 Volume 44 Issue 1 Pages
66-75
Published: January 25, 1991
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Chemical modification of the side chain in rhizoxin, a potent antimitotic agent, was attempted in order to study structure-activity relationships and also to devise a probe for photoaffinity labeling of tubulin. An OsO
4/NaIO
4 oxidation gave a nor-rhizoxin 20-al (
5) which was converted to 20-ol (
6) by a NaBH
3CN reduction. Starting from these two compounds as key intermediates, a series of Wittig reaction products
7-
12, and of 20-
O-acylates
13-
21 were prepared and their anti-tubulin activity and cytotoxicity were determined. An aryl azide derivative
23 was synthesized as a photoaffinity analogue.
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KIYOTO IMAE, HAJIME KAMACHI, HARUHIRO YAMASHITA, TAKAAKI OKITA, SATSUK ...
1991 Volume 44 Issue 1 Pages
76-85
Published: January 25, 1991
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Syntheses of melanostatin and feldamycin have been completed from L-serine and L-threonine, respectively, and the configuration of unknown asymmetric carbons determined. Feldamycin analogs have also been prepared and the L-tryptophyl analog was the most potent in the depigmentation of
Streptomyces bikiniensis and B16 melanoma cells.
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YUKIO NARITA, SHINJI MASUYOSHI, TETSURO YAMASAKI, TAKAYUKI NAITO, HIRO ...
1991 Volume 44 Issue 1 Pages
86-92
Published: January 25, 1991
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The preparation and antibacterial activity of the 5"-guanidino (
6) and 5"-amidino (
7) derivatives of 4'-deoxybutirosin A (
1) as well as the 5"-guanidino derivative (
8) of butirosin A are described. The key intermediates, tetra-
N-benzyloxycarbonyl-5"-azido derivatives were selectively reduced with NiCl
2-NaBH
4 to give the corresponding 5"-amino derivatives. Subsequent guanidination or amidination followed by deblocking afforded the final compounds
6,
7 and
8. The 5"-guanidino derivatives (
6 and
8) were more active against Gram-positive and Gram-negative bacteria than the corresponding 5"-hydroxy derivatives (
1 and butirosin A). Compound
6 was also active against a variety of methicillin-resistant
Staphylococcus aureus (MRSA).
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Ross E. LONGLEY, DEDRA HARMODY
1991 Volume 44 Issue 1 Pages
93-102
Published: January 25, 1991
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A rapid, colorimetric, microassay for detection of agents which are known agonists/antagonists of protein kinase C (PKC) was developed, utilizing their effects on adherence of EL-4.IL-2 cells. Cells that were incubated with agents which are known inducers of PKC activation, phorbol 12-myristate 13-acetate (PMA), phorbol 12, 13-dibutyrate (PDBu), mezerein and indolactam V, readily adhered to wells of 96 well microtiter plates within 1 - 2 hours, whereas cells incubated with the negative PKC activator, 4α-phorbol 12-myristate 13-acetate (4α-PMA), which is structurally related to PMA (4β-PMA), did not adhere. The adherent cells withstood repeated vigorous washings with tissue culture medium. Adherence of EL-4.IL-2 cells in the presence of PMA could be blocked by the addition of two known inhibitors of PKC, 1-(5-isoquinoline-sulfonyl)-2-methylpiperazine dihydrochloride and staurosporine. Detection of the presence of adherent cells was accomplished by the addition of a tetrazolium salt to culture wells and determination of the remaining viable cells by scanning using a multiwell spectrophotometer (ELISA reader). The EL-4.IL-2 adherence assay meets several important criteria for use as a primary screen in the detection of potential PKC agonists/antagonists,
i.e. its selectivity, simplicity, rapid performance through automation and reproducibility.
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DENISE PARISOT, MICHEL DEVYS, MICHEL BARBIER
1991 Volume 44 Issue 1 Pages
103-107
Published: January 25, 1991
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6-
O-Demethyl-5-deoxyfusarubin and 6-
O-demethyl-5-deoxyanhydrofusarubin have been isolated from the mutant redD169.yelY9 of the fungus
Nectria haematococca blocked in fusarubin biosynthesis. These products were identified on the basis of physico-chemical data by comparison with known substances.
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JAVIER MARTÍN-VILLACORTA, ANGEL REGLERO, JOSE M. LUENGO
1991 Volume 44 Issue 1 Pages
108-110
Published: January 25, 1991
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Acyl-CoA: 6-APA acyltransferase (AT) from
Penicillium chrysogenum Wis 54-1255 catalyzes the hydrolysis of different acyl-CoA derivatives generating, in the absence of 6-APA, free acid and CoA. The hydrolytic efficiency of AT is highest for acyl-CoA variants in which the acyl-moiety is higher than six carbon atoms. The maximal rate of catalysis was achieved in 50 mM Tris-HCl buffer, pH 8.5 at 35°C. Unlike the AT activity, the acylase activity has a different optimum temperature and substrate specificity and dithiothreitol is not required for the reaction.
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SHIGEMI YOSHIDA, TAKAAKI AOYAGI, SHIGEKO HARADA, NAOKO MATSUDA, TAKAKO ...
1991 Volume 44 Issue 1 Pages
111-112
Published: January 25, 1991
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SATOSHI OMURA, TOMOKO FUJIMOTO, KAZUHIKO OTOGURO, KEIICHI MATSUZAKI, R ...
1991 Volume 44 Issue 1 Pages
113-116
Published: January 25, 1991
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SATOSHI OMURA, KEIICHI MATSUZAKI, TOMOKO FUJIMOTO, KAZUHITO KOSUGE, TO ...
1991 Volume 44 Issue 1 Pages
117-118
Published: January 25, 1991
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YOSUKE SAWADA, TSUTOMU MURAKAMI, TOMOKAZU UEKI, YASUO FUKAGAWA, TOSHIK ...
1991 Volume 44 Issue 1 Pages
119-121
Published: January 25, 1991
Released on J-STAGE: April 19, 2006
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