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SALLY J. TREW, STEPHEN K. WRIGLEY, LYDIE PAIRET, JESS SOHAL, PATRICK S ...
2000 Volume 53 Issue 1 Pages
1-11
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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A series of halogenated pyrrolo [2, 1-b] [1, 3] benzoxazines (
1-
9) was isolated from fermentations of an actinomycete strain X10/78/978 (NCIMB40808), identified as
Streptomyces rimosus, during a microbial extract screening programme to identify inhibitors of bacterial histidine kinase. The structures of these compounds were elucidated by spectroscopic methods including the HMQC, HMBC and INADEQUATE NMR experiments. The structure of
1 was confirmed by X-ray crystallographic studies. Compounds
5 and
6 were produced in fermentations in the presence of NaBr and Nal respectively. The most abundant member of the series, streptopyrrole,
1, inhibited the nitrogen regulator II (NRII) histidine kinase from
Escherichia coli with an IC
50 of 20μM and exhibited antimicrobial activity against a range of bacteria and fungi.
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I. Taxonomy, Production, Isolation and Biological Activities
TAKAYUKI NAKANO, TSUKASA KOIWA, SENJI TAKAHASHI, AKIRA NAKAGAWA
2000 Volume 53 Issue 1 Pages
12-18
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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Two new inhibitors of ICAM-1/LFA-1 mediated cell adhesion molecule, adxanthromycins A and B were isolated from the cultured broth of a streptomycete strain. The strain was identified as
Streptomyces sp. NA-148 from its morphological and physiological characteristics. Adxanthromycins A and B inhibited the formation of the JY cell aggregates from 1.5μg/ml, respectively, in a dose dependent manner. Components A and B also inhibited a human T cell leukemia cell line SKW-3 adhesion to soluble ICAM-1 in a dose-dependent manner with an IC
50 of 18.8μg/ml and 25.0μg/ml, respectively.
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ICHIJI NAMATAME, HIROSHI TOMODA, MASAYOSHI ARAI, SATOSHI OMURA
2000 Volume 53 Issue 1 Pages
19-25
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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Effects of seven cytochalasans including cytochalasins B, D and E and novel phenochalasins A and B were tested on cytosolic lipid droplet formation and neutral lipid synthesis in mouse peritoneal macrophages. Phenochalasin A inhibited lipid droplet formation in a dose-dependent manner at least up to 20μM without any morphological changes in macrophages. Cytochalasins D and E also inhibited lipid droplet formation only in a narrow range of concentrations, around 1 and 0.1μM, respectively. At higher concentrations they gave morphological changes in macrophages. The other four cytochalasans only showed severe morphological changes in macrophages. Phenochalasin A and cytochalasins D and E inhibited cholesteryl ester (CE) synthesis specifically with IC
50 values of 0.61, 2.4 and 0.20μM, respectively, while the other cytochalasans inhibited both CE and triacylglycerol syntheses. Thus, among the cytochalasans tested, phenochalasin A showed very specific inhibition of CE synthesis and gave the lowest morphological changes in macrophages, resulting in the best inhibitor of lipid droplet formation in macrophages.
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MASAO TSUKAMOTO, SHIGERU NAKAJIMA, KUMIKO MUROOKA, MIOKO HIRAYAMA, KAO ...
2000 Volume 53 Issue 1 Pages
26-32
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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New cytotoxic substances, designated BE-54238A and B, were isolated from the culture broth of
Streptomyces sp. A54238. The active principles were extracted from the mycelium by methanol and purified by Diaion HP-20 and Sephadex LH-20 column chromatographies. BE-54238A and B exhibited cytotoxic activity against murine and human tumor cell lines.
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I. Taxonomy of Producing Strain, Fermentation, Isolation and Biological Activities
HIROSHI NOSE, ASAKO SEKI, TAKASHI YAGUCHI, AYAKO HOSOYA, TORU SASAKI, ...
2000 Volume 53 Issue 1 Pages
33-37
Published: January 25, 2000
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Two novel antifungal antibiotics, PF1163A and B, were isolated from the fermentation broth of
Penicillium sp. They were purified from the solid cultures of rice media using ethyl acetate extraction, silica gel and Sephadex LH-20 column chromatographies. PF1163A and B showed potent growth inhibitory activity against pathogenic fungal strain
Candida albicans but did not show cytotoxic activity against mammalian cells. These compounds inhibited the ergosterol biosynthesis in
Candida albicans.
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II. Physico-chemical Properties and Structure Elucidation
TORU SASAKI, HIROSHI NOSE, AYAKO HOSOYA, SHIGEMI YOSHIDA, MAMI KAWAGUC ...
2000 Volume 53 Issue 1 Pages
38-44
Published: January 25, 2000
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The structures of new antifungal antibiotics, PF1163A and B, were elucidated by spectroscopic analyses of the degradation products and by X-ray crystallography of the de-2-hydroxyethyl derivative of PF1163B. Both antibiotics consist of a 13-membered macrocyclic structure containing a derivative of
N-methyl tyrosine and a hydroxy fatty acid. PF 1163A differs from PF1163B by having an additional hydroxyl group on the side chain.
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YOSHIKATSU SUZUKI, HIROSHI TAKAHASHI, YASUAKI ESUMI, TSUTOMU ARIE, TET ...
2000 Volume 53 Issue 1 Pages
45-49
Published: January 25, 2000
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A new antifungal diketopiperazine named haematocin was isolated from the culture broth of
Nectria haematococca Berk, et Br. (880701 a-1) causing blight disease on ornamental plants,
Phalaenopsis spp. and
Doritanopsis spp. Its structure was established by spectroscopic methods. Haematocin inhibited the germ-tube elongation and spore-germination of
Pyricularia oryzae at the ED
50 values of 30μg/ml and 160μg/ml, respectively.
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KAZUHIKO OTOGURO, KAZURO SHIOMI, YUUICHI YAMAGUCHI, NORIKO ARAI, TOSHI ...
2000 Volume 53 Issue 1 Pages
50-57
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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The mutant of
Penicillium sp. FO-4259, an arisugacins A and B producing strain, was found to produce a series of metabolites, designated arisugacins C, D, E, F, G and H, which were structurally related to arisugacins A and B. These compounds were isolated from the culture broth and the physico-chemical and biological properties were examined. The IC
50 values of arisugacins C and D against acetylcholinesterase (AChE) were 2.5μM and 3.5μM, respectively. However arisugacins E, F, G and H did not inhibit AChE at 100μM. Though they showed only weak or no activity against AChE compared with arisugacins A and B, they may be useful for the study of the structure-activity relationship.
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II. Biosynthetic and Bioconversion Studies
HIROSHI KANZAKI, DAISUKE IMURA, TERUHIKO NITODA, KAZUYOSHI KAWAZU
2000 Volume 53 Issue 1 Pages
58-62
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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Albonoursin production was greatly enhanced when cyclo (L-Leu-L-Phe) (CFL), a tetrahydro derivative of albonoursin, was added to the 2-day culture of an albonoursinproducing actinomycete,
Streptomyces albulus KO-23. The increase in albonoursin production paralleled the amount of CFL added. Furthermore, the resting cells of the strain catalyzed the bioconversion of CFL to albonoursin. The optimum pH and temperature for the conversion were found to be pH 10.0 and 50°C. The feeding experiments and the resting-cell reactions revealed that albonoursin is biosynthesized by dehydrogenation of CFL in the actinomycete. This is the first report for a dehydrogenation of amino acid residues at the α, β-positions in cyclic dipeptides.
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II. Physico-chemical Properties and Structure Determination
YUTAKA KOGUCHI, JUN KOHNO, SFFLN-ICHI SUZUKI, MAKI NISHIO, KOHEI TAKAH ...
2000 Volume 53 Issue 1 Pages
63-65
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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AKIRA ASAI, YASUSHI SAKAI, HARUMI OGAWA, YOSHINORI YAMASHITA, SHINGO K ...
2000 Volume 53 Issue 1 Pages
66-69
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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YUZURU MIKAMI, HISAYUKI KOMAKI, TAMAE IMAI, KATSUKIYO YAZAWA, AKIRA NE ...
2000 Volume 53 Issue 1 Pages
70-74
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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HISAYUKI KOMAKI, YASUSHI TANAKA, KATSUKIYO YAZAWA, HIROAKI TAKAGI, AKI ...
2000 Volume 53 Issue 1 Pages
75-77
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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HO-JAE LEE, HYO-KON CHUN, MYUNG-CHUL CHUNG, CHOONG-HWAN LEE, JOON-SHIC ...
2000 Volume 53 Issue 1 Pages
78-80
Published: January 25, 2000
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AKIRA ASAI, ATSUHIRO HASEGAWA, KEIKO OCHIAI, YOSHINORI YAMASHITA, TAMI ...
2000 Volume 53 Issue 1 Pages
81-83
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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H. LACKNER, HEIKE HÜLSMANN, STEPHAN HEINZE, HANNELORE SIMON, HORS ...
2000 Volume 53 Issue 1 Pages
84-87
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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KUNIAKI TATSUTA, MASAAKI TAKAHASHI, NOBORU TANAKA
2000 Volume 53 Issue 1 Pages
88-91
Published: January 25, 2000
Released on J-STAGE: September 19, 2008
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