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VINOD R. HEGDE, PING DAI, MIN CHU, MAHESH PATEL, ROBERT BRYANT, JOSEPH ...
1997 Volume 50 Issue 12 Pages
983-991
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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Seven neurokinin (NK) receptor inhibitors SCH 60059 (
1), SCH 60065 (
2), SCH 64879 (
3), SCH 60061 (
4), SCH 60063 (
5), SCH 60057 (
7), and SCH 64878 (
9) and two uncharacterized components
6 and
8, were isolated from the fermentation broth of a fungus taxonomically classified as an
Acremonium sp. These compounds were isolated from the fermentation broth by ethyl acetate extraction. Purification and separation of the individual compounds were achieved by NK
1 and NK
2 assay-guided fractionation using gel filtration, reverse phase chromatography and HPLC. The NK active compounds were identified to be a family of polyhydroxy isoprenoid derivatives, including glycosylated members, by spectroscopic and degradation studies. Compounds
1-
5 and
7 contain nine isoprene units connected in head to tail fashion and compound
9 contains fifteen isoprene units connected in a similar manner. All these compounds showed dual inhibition in NK
1 and NK
2 assays with IC
50 values ranging from 2.5-11 μM in the NK
1 assay and 6.8-16 μM in the NK
2 assay.
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I. Characterization of Producing Strain and Production, Isolation and Biological Activities
HIROSHI YANO, SATOSHI NAKANISHI, YOU IKUINA, KATSUHIKO ANDO, MAYUMI YO ...
1997 Volume 50 Issue 12 Pages
992-997
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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Novel compounds MS-681a, b, c and d were isolated from the culture broth of a fungal strain KY6568. The strain was identified as
Myrothecium sp. from its morphological characteristics. MS-681a, b, c and d inhibited the activity of purified smooth muscle myosin light chain kinase with IC
50 values of 0.11, 0.29, 0.095 and 0.26 μM, respectively. Cyclic AMP-dependent protein kinase, cyclic GMP-dependent protein kinase and protein kinase C were not inhibited at 100 μM by MS-681 compounds.
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II. Physico-chemical Properties and Structure Elucidation
YOJI IKUINA, CHIEKO BANDO, MAYUMI YOSHIDA, HIROSHI YANO, YUTAKA SAITOH
1997 Volume 50 Issue 12 Pages
998-1006
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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MS-681a, b, c and d are new inhibitors of myosin light chain kinase produced by
Myrothecium sp. They are novel octapeptides containing α-alkyl-α-amino acids and a polyamine moiety. The structures were determined by NMR and FAB-MS/MS spectral analyses of the intact peptides. Their absolute configurations were elucidated by GC analysis on a chiral column of the constituent amino acids and by chemical synthesis of the polyamine moieties.
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AKINOBU TSUNOO, MASAYUKI KAMIJO, NAOKI TAKETOMO, YOSHIO SATO, KATSUMI ...
1997 Volume 50 Issue 12 Pages
1007-1013
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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A new Cyclodepsipeptide, designated roseocardin, was isolated from the culture broth of
Trichothecium roseum TT103. Roseotoxin B and destruxins A and B were also isolated during the same procedure. The structure of roseocardin was determined by EI-MS, NMR and X-ray crystallographic analysis. Roseocardin as well as the other cyclodepsipeptides were shown to produce positive inotropic effects on rat heart muscles.
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P. R. GRAUPNER, S. THORNBURGH, J. T. MATHIESON, E. L. CHAPIN, G. M. KE ...
1997 Volume 50 Issue 12 Pages
1014-1019
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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A new tetramic acid containing metabolite, A90931a has been isolated from
Streptomyces sp., along with a second factor (A90931b) recently described and known as maltophilin. The structures were determined from spectroscopic data of the isolates and their acetylated products. A90931a was spectroscopically identical to the previously described antibiotic TAN-883b whose structure was not reported. A90931a and A90931b exhibit fungicidal activity against the grape pathogen
Plasmopara viticola. Due to its similarity to maltophilin, A90931a has been called dihydromaltophilin.
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I. Taxonomy, Production, Isolation and Biological Properties
MASAYUKI IGARASHI, NAOKO KINOSHITA, TAKAKO IKEDA, MAY KAMEDA, MASA HAM ...
1997 Volume 50 Issue 12 Pages
1020-1025
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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Resormycin, a novel herbicidal and antifungal antibiotic, was isolated from the cultured broth of streptomycete strain. The strain was isolated from a soil collected at Yokohama-shi, Kanagawa Prefecture, Japan, and identified as
Streptomyces platensis MJ953-SF5.
Resormycin was purified by active charcol, Amberlite IRC-50, Amberlite CG-50 and Sephadex LH-20 column chromatographies. Resormycin markedly inhibited the growth of monocotyledonous and dicotyledonous weed. The antibiotic showed antimicrobial activity against phytopathogenic fungi.
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II. Structure Elucidation of Resormycin
MASAYUKI IGARASHI, HIKARU NAKAMURA, HIROSHI NAGANAWA, TOMIO TAKEUCHI
1997 Volume 50 Issue 12 Pages
1026-1031
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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A novel herbicidal antibiotic, resormycin, was isolated from the culture broth of
Streptomyces platensis MJ953-SF5.
The structure of resormycin is determined to be (2
Z)-2-
N-[2
N-[(3
S)-3, 6-diaminoheptanoyl](2
S)-3-hydroxyvalyl]amino-3-(4-chloro-3, 5-dihydroxy)phenylpropenoic acid by spectroscopic analyses, degradation studies and X-ray crystallography.
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YULIN PENG, JACOB YASHPHE, ARNOLD L. DEMAIN
1997 Volume 50 Issue 12 Pages
1032-1035
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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Actinomadura sp. strain 2966 can effectively convert compactin to pravastatin. The degree of conversion observed was 65% to 78% of compactin added and 65% to 88% of compactin taken up, depending on the concentration of compactin and duration of the experiment. Increasing the compactin concentration resulted in a higher final pravastatin concentration especially when compactin was added intermittently. Higher glucose concentrations had no effect on the bioconversion although uptake of compactin was inhibited. The conversion was linear over 16 hours. The system requires no induction and thus appears to be different from previously studied hydroxylases from actinomycetes.
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YASUSHI TANAKA, HISAYUKI KOMAKI, KATSUKIYO YAZAWA, YUZURU MIKAMI, AKIR ...
1997 Volume 50 Issue 12 Pages
1036-1041
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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A new 32-membered macrolide antibiotic, brasilinolide A was isolated from the fermentation broth of
Nocardia sp. IFM 0406. The producer was identified as
Nocardia brasiliensis. The antibiotic was only active against
Aspergillus niger, but not active against other fungi including yeasts as well as other filamentous like fungi and bacteria. Brasilinolide A exerted an immunosuppressive activity in the assay system of a mixed lymphocyte reaction (MLR).
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MAKI WATANABE, HIROMI TOHYAMA, TAMIO HIRATANI, HIROOMI WATABE, SHIGEHA ...
1997 Volume 50 Issue 12 Pages
1042-1051
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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The mechanism of fungitoxic action of an antifungal antibiotic benanomicin A was studied with intact cells and protoplasts of
Saccharomyces cerevisiae as well as with its enzymic preparations. The results obtained are summarized as follows: (1) benanomicin A at relatively high concentrations (almost equal to MIC) was fungicidal and disrupted the cell permeability barrier, inducing leakage of intracellular K
+ and ATP in growing cells, while the antibiotic had none of these effects in non-growing cells; (2) no biosynthesis of any of several major cellular constituents in yeast cells was inhibited markedly or selectively enough to explain its fungitoxic activity; (3) whereas benanomicin A induced lysis of metabolically active yeast protoplasts incubated in the presence of glucose, inactive yeast protoplasts incubated without glucose were refractory to the lytic action of the antibiotic; (4) osmotically shocked yeast cells became feasible to the cidal action of benanomicin A; (5) benanomicin A substantially inhibited uptake of 6-deoxy-glucose by yeast cells; (6) liposomes composed of phospholipids and cholesterol were not susceptible to benanomicin A; and (7) benanomicin A inhibited
in vitro activity of H
+-ATPase from yeast cell membranes to a greater extent than that for H
+-ATPase from yeast mitochondria or H
+-ATPase from yeast vacuolar membranes.
Based on these and our previous data that benanomicin A preferentially binds to mannan or mannoproteins constituting the cell wall and cell membrane of yeasts, such binding of the antibiotic is suggested to deteriorate the normal structure and function of those cell membranes of yeasts which are in a growing or metabolically active state, ultimately leading to cell death.
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MASASHI UEKI, MAKOTO TANIGUCHI
1997 Volume 50 Issue 12 Pages
1052-1057
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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UK-2A and UK-3A are structural relatives of antimycins, which were isolated as antifungal antibiotics with little cytotoxicity that demonstrated inhibition of respiratory activity. They halve the cellular respiration of yeast within 4-5 minutes and the intracellular ATP content within 2-5 minutes. Moreover, they inhibited the yeast mitochondrial respiration using β-hydroxybutyrate and succinate as a respiratory substrate, but no inhibition was observed using ascorbate-reduced tetramethyl p-phenylenediamine as the substrate. The site of respiratory inhibition of UK-2A and UK-3A was thought to be the cytochrome bc1 complex in the mitochondrial electron transport chain of yeast cells. They also inhibited the mitochondrial respiration of rat liver. It has been suggested that intact animal cells might have some system to defend themselves from the actions of UK-2A and UK-3A.
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YUHTA MASUOKA, KAZUO SHIN-YA, KAZUO FURIHATA, YOICHI HAYAKAWA, HARUO S ...
1997 Volume 50 Issue 12 Pages
1058-1060
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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M. CHU, I. TRUUMEES, R. MIERZWA, M. PATEL, M. S. PUAR
1997 Volume 50 Issue 12 Pages
1061-1063
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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GEONSEEK RYU, SEUNGJIN HWANG, SI-KWAN KIM
1997 Volume 50 Issue 12 Pages
1064-1066
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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CHRISTOPH PFEFFERLE, JENS BREINHOLT, HANNE GURTLER, HANS-PETER FIEDLER
1997 Volume 50 Issue 12 Pages
1067-1068
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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II. Physico-chemical Properties and Structural Elucidation
SATOSHI TAKAMATSU, YONG-PIL KIM, AKIKO ENOMOTO, MASAHIKO HAYASHI, HARU ...
1997 Volume 50 Issue 12 Pages
1069-1072
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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MICHAEL G. O'SHEA, RODNEY W. RICKARDS, JENNIFER M. ROTHSCHILD, ERNEST ...
1997 Volume 50 Issue 12 Pages
1073-1077
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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HONG-Woo LEE, EUNG-NAM KIM, TAB WON KANG, SOON-KIL AHN, NAM-HEE CHOI, ...
1997 Volume 50 Issue 12 Pages
1078-1082
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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WON KEUN OH, HYUN SUN LEE, Bo YEON KIM, SOON CHEOL AHN, DAE OOK KANG, ...
1997 Volume 50 Issue 12 Pages
1083-1085
Published: December 25, 1997
Released on J-STAGE: November 25, 2006
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