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I. Taxonomy, Fermentation, Isolation and Biological Properties
TAMOTSU FURUMAI, KEIICHI TAKAGI, YASUHIRO IGARASHI, NORIKO SAITO, TOSH ...
2000 Volume 53 Issue 3 Pages
227-232
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Arisostatins A and B, new members of tetrocarcin class of antibiotics were isolated from the culture broth of an actinomycete strain. The producing strain, TP-A0316, was identified as
Micromonospora sp. Arisostatins were obtained from the culture fluid by solvent extraction and chromatographic purification. They showed antibiotic activity against Gram-positive bacteria and antitumor activity.
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II. Structure Determination
YASUHIRO IGARASHI, KEIICHI TAKAGI, YUKIKO KAN, KIYONAGA FUJII, KEN-ICH ...
2000 Volume 53 Issue 3 Pages
233-240
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Structures of arisostatins A and B were determined by spectroscopic analyses. Arisostatins were found to be new analogs of tetrocarcin A and possess an
iso-butanoyldigitoxose unit instead of the acetyldigitoxose one. NMR analyses of arisostatins and tetrocarcin A led to the revision of the anomeric configurations in the tetrasaccharide moiety of tetrocarcin A.
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WEIMIN HU, SHIGEKI OHYAMA, KEIJI HASUMI
2000 Volume 53 Issue 3 Pages
241-247
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Two novel staplabin analogs, SMTP-7 and -8, have been isolated from cultures of
Stachybotrys microspora IFO 30018. Spectroscopic analyses showed that the SMTP-7 molecule consisted of two identical staplabin core structures and ornithine which bridges the two partial structures. In the SMTP-8 molecule, the bridging unit was lysine. At concentrations of 80-150μM, the two compounds caused 2- to 12-fold increase in urokinase-catalyzed plasminogen activation, fibrin binding of plasminogen, and urokinase- and plasminogen-mediated fibrinolysis. These activities of SMTP-7 and -8 were two to ten times higher than those of staplabin and previously isolated SMTPs, which exerted such effects at concentrations ranging from 150 to 800 μM.
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EUI-IL HWANG, BONG-SIK YUN, YOUNG-KOOK KIM, BYOUNG-MOG KWON, HONG-GI K ...
2000 Volume 53 Issue 3 Pages
248-255
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Chaetoatrosin A, a novel chitin synthase II inhibitor, was isolated from the culture broth of fungus F449, which was identified as
Chaetomium atrobrunneum F449. Chaetoatrosin A was purified by solvent partition, silica gel, ODS, preparative TLC, and Sephadex LH-20 column chromatographies, consecutively. The structure of Chaetoatrosin A was assigned as 1, 8-dihydroxy-3(2-hydroxypropionyl)-6-methoxynaphthalene on the basis of various spectroscopic analyses including Uy IR, mass spectral, and NMR. Its molecular weight and formula were found to be 262 and C
14H
14O
5, respectively. Chaetoatrosin A inhibited chitin synthase II by 50% at the concentration of 104 μg/ml in an enzyme assay system. This compound showed antifungal activities against
Rhizoctonia solani,
Pyricularia oryzae,
Botrytis cinerea,
Cryptococcus neoformans and
Trichophyton mentagrophytes.
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M. P. SINGH, J. E. JANSO, S. W. LUCKMAN, S. F. BRADY, J. CLARDY, M. GR ...
2000 Volume 53 Issue 3 Pages
256-261
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Fermentation extracts of culture CR115, an unknown plant endophyte originally isolated from Costa Rica, were found to be active against antibiotic-resistant bacteria. The metabolite responsible for activity was identified as a novel diterpenoid antibiotic guanacastepene (mol. wt. 374.47 and mol. formula C
22H
30O
5). Mechanistic studies done in an
E. coli imp strain suggested membrane damage as the primary mode of bactericidal action. This compound also lysed human RBCs and caused leakage of intracellular potassium from
E. coli imp.
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CHIKARA SHINOHARA, TOSHIHIRO CHIKANISHI, SHIGEMITSU NAKASHIMA, AKIKO H ...
2000 Volume 53 Issue 3 Pages
262-268
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Four fungal metabolites, chaetoglobosin A (CGA), crinipellin B (CPB), geodin (GE) and triticone B (TTB), were found to enhance fibrinolytic activity of bovine aortic endothelial cells. Plasmin generation on the cells was elevated 2- to 4-fold when treated with these agents at a concentration of 3-100 μM. These effects were dependent on plasminogen and inhibited by anti-urokinase antibody. The effect of CGA, but not of CPB, GE and TTB, was abolished by cycloheximide. In a cell-free system, plasmin and urokinase activities as well as urokinase-catalyzed plasminogen activation were not enhanced by these agents. CGA, but not others, induced the production of urokinase in endothelial cells. CPB and GE accelerated plasminogen activator inhibitor-1 (PAI-1) inactivation, and TTB caused direct, reversible inhibition of PAI-1. Thus, induction of urokinase by CGA and inhibition of PAI-1 by CPB, GE and TTB may, at least partly, account for the elevation of fibrinolytic activity of endothelial cells.
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NAOKO MORISAKI, YUICHI HASHIMOTO, KAZUO FURIHATA, TAMAE IMAI, KAYO WAT ...
2000 Volume 53 Issue 3 Pages
269-275
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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23-(
O-ADP-Ribosyl)rifampicin [RIP-TAs (
3, Na
+ form), RIP-TAf (
4, H
+ form)] was obtained as an intermediate in the conversion process of rifampicin (
1) to RIP-Mb (
2) that is mediated by cell homogenates of
Mycobacterium smegmatis DSM43756 or of
Escherichia coli carrying a mycobacterial mono(ADP-ribosyl) transferase gene, in the presence of NADH. 23-[
O-(5'-Phosphoribosyl)]rifampicin (
5, RIP-TAp) was also obtained by the reaction of rifampicin with NADH in the presence of a homogenate of
M. smegmatis. The structures of
3,
4, and
5 were determined by means of MS and NMR analyses.
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MARKUS WOEGERBAUER, HEINZ BURGMANN, JULIAN DAVIES, WOLFGANG GRANINGER
2000 Volume 53 Issue 3 Pages
276-285
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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Preparations of antimicrobials from biotechnological sources containing nucleic acids may serve as vector for the dissemination of resistance genes. An essential prerequisite for the acquisition of a new resistance phenotype in a transformational scenario is the availability of physically intact DNA molecules capable of transforming competent microorganisms. DNA is thought to be an easy target for catabolic processes when present in the natural habitat of bacteria (
e.g. gastrointestinal tract, soil) due to the overall presence of nucleolytic enzymes. Aminoglycoside antibiotics are known to display a strong affinity to nucleic acids rendering these compounds to be primary candidates for exerting DNA protective functions in the gastrointestinal tract when applied orally during antibiotic chemotherapy. Using a DNase I protection assay it could be demonstrated that neomycin B at a concentration of 2mM completely inhibited degradation of plasmid DNA
in vitro. No inhibition of degradation was observed with streptomycin and kanamycin and the non-aminoglycoside antibiotics oxytetracycline and ampicillin under identical assay conditions. Thus, neomycin preparations may be able to promote structural integrity of contaminating DNA-fragments in DNase-rich environments.
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OLGA V MIROSHNIKOVA, SVETLANA S. PRINTSEVSKAYA, EUGENIA N. OLSUFYEVA, ...
2000 Volume 53 Issue 3 Pages
286-293
Published: March 25, 2000
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A series of new carboxamides of the glycopeptide antibiotic eremomycin was synthesized and investigated
in vitro. The goal of the study was the comparison of the influence of the substituents introduced onto the eremomycin skeleton on the activity of these compounds against vancomycin susceptible and resistant bacterial strains. Eremomycin amides derived from amines with small substituents (C
0-C
4) demonstrated antibacterial activity against vancomycin susceptible strains similar to that of the parent antibiotic and were inactive against vancomycin resistant strains. The derivatives of alkylamines with linear lipophilic substituents (like C
10H
21) were active against
VanA. and
VanB enterococci strains with the scope of activity similar to that of
N'-decyl or 7d-CH
2NH-decyl eremomycins described earlier. Eremomycin amides of 5-methoxy- and 5-benzyloxytryptamine were active both against vancomycin susceptible and resistant strains. The introduction of a spacer (lysine or piperazine) between the decyl and antibiotic moieties did not seriously influence antibacterial properties of the compounds in comparison with the corresponding derivatives without a spacer. The most active carboxamides are of interest for secondary modifications of the antibiotic.
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RYUICHIRO NAKAI, HARUMI OGAWA, AKIRA ASAI, KATSUHIKO ANDO, TSUTOMU AGA ...
2000 Volume 53 Issue 3 Pages
294-296
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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NOBUO HOSOKAWA, ISAO MOMOSE, RYUICHI SEKIZAWA, HIROSHI NAGANAWA, HIRON ...
2000 Volume 53 Issue 3 Pages
297-300
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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MICHAEL S. PACEY, CHRISTOPHER J. DUTTON, ROBERT A. MONDAY, JOHN C. RUD ...
2000 Volume 53 Issue 3 Pages
301-305
Published: March 25, 2000
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NOBUO HOSOKAWA, HIRONOBU IINUMA, TOMIO TAKEUCHI, SHIGEO SATO, TAKAO YA ...
2000 Volume 53 Issue 3 Pages
306-308
Published: March 25, 2000
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YOSHIO SAITO, MARIKO NAKAMURA, TSUNEYA OHNO, CHANYA CHAICHAROENPONG, E ...
2000 Volume 53 Issue 3 Pages
309-313
Published: March 25, 2000
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HIDEAKI IMAMURA, AYA SHIMIZU, HIROKI SATO, YUICHI SUGIMOTO, SHUNJI SAK ...
2000 Volume 53 Issue 3 Pages
314-316
Published: March 25, 2000
Released on J-STAGE: September 19, 2008
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