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PRODUCTION, ISOLATION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
BRIGITTE KUNZE, WOLFRAM TROWITZSCH-KIENAST, GERHARD HÖFLE, HANS R ...
1992 Volume 45 Issue 2 Pages
147-150
Published: February 25, 1992
Released on J-STAGE: April 19, 2006
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Novel citrate-hydroxamate siderophores, named nannochelins A, B and C, were isolated from the culture broth of the myxobacterium
Nannocystis exedens strain Na e485. The new substances showed weak growth-inhibitory activity against some bacteria and fungi.
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I. TAXONOMY, FERMENTATION, ISOLATION AND STRUCTURAL ELUCIDATION
SHOKO MATSUKUMA, TATSUO OHTSUKA, HIROMICHI KOTAKI, HARUYOSHI SHIRAI, T ...
1992 Volume 45 Issue 2 Pages
151-159
Published: February 25, 1992
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A new series of antifungal antibiotics, Ro 09-1470 and its 6 congeners were isolated from the fermentation broth of
Penicillium sp. NR6564. Their structures were determined as tetrahydropyran derivatives with an alkenyl side chain on the basis of their spectroscopic and physico-chemical properties. Among these compounds, Ro 09-1470 and Ro 09-1545 possessing a glycyl or an
N-substituted glycyl ester residue had high antifungal activity. Ro 09-1469, one of the congeners, was found in the fermentation broth of several strains of
Aspergillus sclerotiorum Huber.
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II. MODE OF ACTION
YUHKO AOKI, TOSHIKAZU YAMAZAKI, MASUMI KONDOH, YURI SUDOH, NOBORU NAKA ...
1992 Volume 45 Issue 2 Pages
160-170
Published: February 25, 1992
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From a
Penicillium sp. we identified a new series of antifungals having a tetrahydropyran skeleton with an alkenyl side chain. We elucidated the mode of action of Ro 09-1470, the most active compound of the series. Treatment of
Candida albicans with the compound caused an accumulation of C-14 methyl intermediates of ergosterol at concentrations of which no significant interference with the biosyntheses of other macromolecules and respiration was observed. P450 lanosterol C-14 demethylase (P450
14DM) activity was inhibited and furthermore, the binding of Ro 09-1470 to the heme of the enzyme was demonstrated by a difference spectrum. We conclude that Ro 09-1470 is the first natural antifungal that inhibits the P450
14DM of fungi.
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PRODUCING ORGANISM, FERMENTATION, ISOLATION, STRUCTURE ELUCIDATION AND BIOLOGICAL PROPERTIES
MASANORI YAMAZAKI, TAKUMI YAMASHITA, TAKASHI HARADA, TAKAAKI NISHIKIOR ...
1992 Volume 45 Issue 2 Pages
171-179
Published: February 25, 1992
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Oligomycin antibiotics, 44-homooligomycin A (NK86-0279 II) and B (NK86-0279 I) are newly discovered antitumor antibiotics with the substitution of ethyl for methyl at carbon 26. They were isolated from the culture broth of
Streptomyces bottropensis NK86-0279. The structure of these two compounds was deduced by spectroscopic and X-ray crystallographic analyses. These antibiotics showed potent antitumor activities against various tumor cells
in vitro, and were active against Colon 26 carcinoma
in vivo. Although they showed no activity at 1, 000 μg/ml against Gram-positive and Gram-negative bacteria and yeast, they have antifungal activity.
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I. PRODUCTION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND ANTIVIRAL ACTIVITY
MITSUAKI TSUNAKAWA, OSAMU TENMYO, KOJI TOMITA, NOBUAKI NARUSE, CHIKAKO ...
1992 Volume 45 Issue 2 Pages
180-188
Published: February 25, 1992
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A strain of
Amycolatopsis orientalis No. Q427-8 (ATCC 53884) was found to produce a complex of new antiviral antibiotics, quartromicin which consisted of at least six components A
1, A
2, A
3, D
1, D
2 and D
3. Structural studies suggested that they are a novel type of molecules unrelated to any known antibiotics. Each component of quartromicin exhibited antiviral activity against herpes simplex virus type 1, influenza virus type A and human immunodeficiency virus.
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I. TAXONOMY AND BIOLOGICAL ACTIVITY
HIROYUKI OSADA, HIROYUKI KOSHINO, TAKUJI KUDO, RIE ONOSE, KIYOSHI ISON ...
1992 Volume 45 Issue 2 Pages
189-194
Published: February 25, 1992
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A novel inhibitor of protein kinase C was found in the fermentation of a soil actinomycete, strain RK-1409. According to the taxonomic studies, the producing strain was designated as
Streptomyces platensis subsp.
malvinus RK-1409. The protein kinase C inhibitor, RK-1409 (7-oxostaurosporine) inhibited the morphological change of a human chronic erythroleukemia cell, K-562, induced by phorbol 12, 13-dibutyrate (PDBu) at the concentration of 10ng/ml. The concentration of 3ng/ml inhibited the activity of protein kinase C
in vitro. RK-1409 inhibited the cell cycle progression at G
2 phase of K-562 cells.
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II. FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE
HIROYUKI KOSHINO, HIROYUKI OSADA, KIYOSHI ISONO
1992 Volume 45 Issue 2 Pages
195-198
Published: February 25, 1992
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RK-1409, a new inhibitor of protein kinase C, was isolated from the culture broth of
Streptomyces platensis subsp.
malvinus RK-1409. The structure was elucidated as 7-oxostaurosporine on the basis of spectroscopic analyses and oxidation of staurosporine.
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NIKKOMYCINS Sz, Sx, Soz and Sox, NEW INTERMEDIATES ASSOCIATED TO THE NIKKOMYCIN BIOSYNTHESIS OF Streptomyces tendae
TRAUGOTT C. SCHÜZ, HANS-PETER FIEDLER, HANS ZÄHNER, MATTHIAS ...
1992 Volume 45 Issue 2 Pages
199-206
Published: February 25, 1992
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New intermediates associated with nikkomycin biosynthesis, called nikkomycins S
z, S
x, So
z and So
x, were isolated and characterized from the culture broth of
Streptomyces tendae Tü 901/S 2566. They are analogues to octosyl acids, shunt metabolites of polyoxin biosynthesis. The decreasing amounts of nikkomycins S
z and S
x, produced in the culture medium, shows a significant correlation to the increasing amounts of the biologically active nikkomycins Z and X, dependent on the increasing concentration of iron.
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AKIRA KAWASHIMA, YOSHIKUNI NAKAMURA, YOSHIE OHTA, TOMOKO AKAMA, MICHIO ...
1992 Volume 45 Issue 2 Pages
207-212
Published: February 25, 1992
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In the course of our screening for microbial compounds which possessed inhibitory activities against biosynthesis of cholesterol from mevalonate, we isolated four new compounds from the cultural broth of
Streptomyces sp. A7361. They are structurally related to, but distinct from chlorothricin.
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1. STRUCTURE-ACTIVITY RELATIONSHIPS OF 3-ISOPROPYLIDENE AND 3-ISOPROPYL ANALOGS
STEVEN J. BRICKNER, JEFFREY J. GAIKEMA, GARY E. ZURENKO, LAURA J. GREE ...
1992 Volume 45 Issue 2 Pages
213-226
Published: February 25, 1992
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The synthesis and antibacterial activity of a series of
N-acyl 3-isopropylidenyl-and 3-isopropyl 2-azetidinones having potent
in vitro antibacterial activity, particularly against anaerobic organisms, is described. A distinguishing structural feature of these compounds is the lack of any ionizable moiety appendant to the lactam nitrogen.
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M. N. PREOBRAZHENSKAYA, N. V. HOLPNE-KOZLOVA, E. I. LAZHKO
1992 Volume 45 Issue 2 Pages
227-234
Published: February 25, 1992
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A method of synthesis of antibiotic streptonigrin 8'-
O-alkyl ethers by alkylation of streptonigrin diphenylmethyl ester and consequent deprotection of carboxylic group with CF
3COOH is developed. An attempt to deblock carboxylic group of 8'-
O-methylstreptonigrin diphenylmethyl ester by hydrogenation over Pd produced 8'-
O-methylstreptonigrone. Similarly streptonigrin was transformed into streptonigrone over Pd-black in H
2 stream. Methylation of streptonigrone afforded 5', 5'-
N-dimethyl-2'8'-
O-dimethylstreptonigrone and 1', 5', 5'-tri-
N-trimethyl-8'-
O-methylstreptonigrone. Alkyl streptonigrin ethers demonstrated lower antibacterial activity
in vitro than the parent antibiotic.
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TOSHIHISA UEDA, KUMIKO KIYOHARA, SANNAMU LEE, HARUHIKO AOYAGI, NOBUO I ...
1992 Volume 45 Issue 2 Pages
235-239
Published: February 25, 1992
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The four diastereoisomers of cyclo(-Asp-Val-) were synthesized to compare with a proposed structure of cairomycin A. Their antimicrobial activities were determined against both Gram-positive and Gram-negative bacteria. The physico-chemical properties of the isomers were characterized by mp,
1H NMR, IR, FAB-MS, and solubility in solvents, which were different from those reported for cairomycin A.
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GILLES BOUTHILLIER, HAROLD MASTALERZ, MARCEL MENARD, JOAN FUNG-TOMC, E ...
1992 Volume 45 Issue 2 Pages
240-245
Published: February 25, 1992
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An analog, 6-(2'-hydroxyethylidene)-4β-methyl-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate (
11), of the carbapenem β-lactamase inhibitor, asparenomycin A, was synthesized. It possessed a spectrum of antibacterial activity that was comparable to that of asparenomycin A but was less effective as a β-lactamase inhibitor. With ampicillin, it only exhibited a moderate level of synergy against a variety of β-actamase-producing organisms. Although the presence of a 4β-methyl group in the analog brought about a significant increase in chemical stability relative to that of asparenomycin A, it did not result in an increase in stability to kidney dehydropeptidase enzyme.
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JUNJI MAGAE, AYAKO HINO, KIYOSHI ISONO, KAZUO NAGAI
1992 Volume 45 Issue 2 Pages
246-251
Published: February 25, 1992
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Phorbol dibutyrate induced a nitroblue tetrazolium-reducing reaction in differentiated HL-60 cells, which was inhibited by protein kinase inhibitors such as staurosporine and H-7. ID
50 of staurosporine and H-7 were 1.4ng/ml and 0.19 mM, respectively. When tautomycin, an inhibitor of protein phosphatases, was added with the kinase inhibitors, the nitroblue tetrazolium-reducing reaction again appeared. ID
50 of staurosporine was 510ng/ml in the presence of tautomycin. Tautomycin itself weakly induced the reaction, which was inhibited by kinase inhibitors. Such a competitive effect between tautomycin and staurosporine was not observed in a cell-free system of protein kinase C. Okadaic acid had the same effect as tautomycin. The similar results were obtained when respiratory burst was quantitated by measuring H
2O
2 produced by canine peripheral neutrophils. The mechanism of competitive effect of tautomycin and staurosporine on respiratory burst is discussed.
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TOMOHIRO KURISAKI, JUNJI MAGAE, KIYOSHI ISONO, KAZUO NAGAI, MAKARI YAM ...
1992 Volume 45 Issue 2 Pages
252-257
Published: February 25, 1992
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The effects of tautomycin, a protein phosphatase inhibitor, on recycling of cell surface molecules were studied with transferrin receptor (TFR) of human myeloid leukemia K562 cells and with CD4 of murine thymocytes. Tautomycin increased expression of TFR of K562 cells whereas phorbol dibutylate (PDBu) decreased it. Tautomycin inhibited PDBu-induced down-regulation of CD4 although it did not induce up-regulation. Okadaic acid also inhibited down-regulation of CD4 which was induced by PDBu. The results suggest that certain inhibitors of protein phosphatases preferentially inhibit endocytosis of cell surface molecules.
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YOSHIKO YOKOTA, YUJI WATANABE, YOSHIMI WAKAI, YASUHIRO MINE
1992 Volume 45 Issue 2 Pages
258-264
Published: February 25, 1992
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The protective effects of FK565 against systemic infections with herpes simplex virus (HSV) and murine cytomegalovirus (MCMV), respiratory tract infection with influenza virus and zosteriform rash with HSV investigated in mice. FK565 showed excellent protective activities against systemic infections with both acyclovir (ACV)-sensitive and-resistant HSV at intravenous and subcutaneous doses of 0.1 and 1 mg/kg and oral dose of 1 mg/kg. FK565 showed superior protective activities at subcutaneous doses of 0.01 and 0.1 mg/kg compared to ACV at subcutaneous dose of 15 mg/kg against MCMV infection. In respiratory tract infection with influenza virus, FK565 showed potent protective effects at intravenous, subcutaneous and oral doses of 0.001 to 1 mg/kg. FK565 markedly inhibited zosteriform spread of HSV on the flank skin at an intravenous dose of 0.1 mg/kg and the mice given FK565 survived longer than the control mice. The peritoneal exudate cells from FK565-treated mice suppressed the growth of HSV in mouse embryo fibroblast more strongly than those from the control mice, although FK565 had no direct antiviral activity against HSV. These findings suggest that FK565 enhanced the host defense ability against viral infections by nonspecific activiation of macrophages.
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RAINER ZOCHER, ULLRICH KELLER, CHAN LEE, KAI HOFFMANN
1992 Volume 45 Issue 2 Pages
265-268
Published: February 25, 1992
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A peptidyl-prolyl
cis-trans isomerase (PPIase) was purified to homogeneity about 24-fold from the cyclosporin-producing fungus
Tolypocladium inflatum. The molecular mass of the enzyme was in the range of 17 kdaltons. Remarkably, the enzyme could be inhibited by cyclosporin A in the nanomolar range as has been shown for numerous other cyclophilins from eukaryotic organisms. This indicates, that
Tolypocladium inflatum must possess a self protection system in order to survive in the presence of cyclosporin.
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BALTASAR MIÑAMBRES, ANGEL REGLERO, JOSÉ M. LUENGO
1992 Volume 45 Issue 2 Pages
269-277
Published: February 25, 1992
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Streptomyces clavuligerus NRRL 3585 grown in a chemically defined medium containing glycerol as the sole carbon source transported this molecule by two different systems. One of these was constitutive with a very low uptake efficiency and insufficient to attend to the metabolic requirements of this bacterium (constitutive glycerol transport system) and the other (glycerol transport system (GTS)) active and specifically induced by o-glycerol which is responsible for the transport of more than 90% of the glycerol taken up the cells. GTS was seen to have an optimal pH and temperature of 7.0 and 30°C, respectively, and its
Km was 14μM. It was repressed by L-serine and addition of this amino acid to the culture broth (10mM) inhibited the growth of
S. clavuligerus but not that of other species of
Streptomyces.
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HIROYUKI OSADA, MASAYUKI SATAKE, HIROYUKI KOSHINO, RIE ONOSE, KIYOSHI ...
1992 Volume 45 Issue 2 Pages
278-279
Published: February 25, 1992
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TAKASHI HORI, TETSURO KONDO, TOMOKO TSUJI, MASAYA IMOTO, KAZUO UMEZAWA
1992 Volume 45 Issue 2 Pages
280-282
Published: February 25, 1992
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KAYOKO S. TSUCHIYA, YUKARI MORIYA, MAKOTO HORI, OSAMU ITOH, TOMIO TAKE ...
1992 Volume 45 Issue 2 Pages
283-285
Published: February 25, 1992
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BRIAN J. TERRY, WEN-CHIH LIU, CHRISTOPHER W. CIANCI, ELIZABETH PROSZYN ...
1992 Volume 45 Issue 2 Pages
286-288
Published: February 25, 1992
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TOSHIO OHTA, ERI HASHIMOTO, MAMORU HASEGAWA
1992 Volume 45 Issue 2 Pages
289-291
Published: February 25, 1992
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KAZUTOSHI SHINDO, HIROYUKI KAWAI
1992 Volume 45 Issue 2 Pages
292-295
Published: February 05, 1992
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