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TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITY
TOSHIRO IWAMOTO, EISAKU TSUJII, MASAMI EZAKI, AKIHIKO FUJIE, SEIJI HAS ...
1990 Volume 43 Issue 1 Pages
1-7
Published: January 25, 1990
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FR109615, a new antibiotic active against
Candida, was isolated from
Streptomyces setonii No. 7562. Based on the spectroscopic data, the structure of FR109615 was elucidated as
cis-2-aminocyclopentane-1-carboxylic acid (
1). The compound showed the excellent
in vivo efficacy in a generalized infection test of mice.
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I. PRODUCTION, ISOLATION, STRUCTURE AND BIOLOGICAL ACTIVITY
KOKO SUGAWARA, MASAMI HATORI, YUJI NISHIYAMA, KOJI TOMITA, HIDEO KAMEI ...
1990 Volume 43 Issue 1 Pages
8-18
Published: January 25, 1990
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Streptomyces hygroscopicus No. P247-71 (ATCC 53709) produced a novel antibiotic eponemycin which exhibited specific
in vivo antitumor effect against B16 melanoma. Structural studies assigned (4
S)-1, 2-epoxy-2-hydroxymethyl-4-(
N-isooctanoyl-L-serylamino)-6-methylhept-6-ene-3-one to eponemycin which is unrelated to the known antitumor antibiotics.
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GIUSEPPE CASSINELLI, EMANUELE ARLANDINI, MARZIA BALLABIO, TERESA BORDO ...
1990 Volume 43 Issue 1 Pages
19-28
Published: January 25, 1990
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Three new anthracyclines, FCE 21424 (
2), FCE 24366 (
3) and FCE 24367 (
4), were isolated from culture broths of
Streptomyces peucetius and its mutant strains after addition of sodium barbiturates during the fermentation. Structural assignment, achieved through spectroscopic and degradative studies, that the new anthracyclines had a common barminomycin-like structure incorporating different barbiturate moieties.
The new anthracyclines were found to display outstanding cytotoxicity and remarkable potency "
in vivo" against P388 ascitic leukemia.
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I. TAXONOMY, FERMENTATION, ISOLATION AND PHYSICO-CHEMICAL PROPERTIES
SEIJI HASHIMOTO, HIDETSUGU MURAI, MASAMI EZAKI, NORIYUKI MORIKAWA, HIR ...
1990 Volume 43 Issue 1 Pages
29-37
Published: January 25, 1990
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WSl358Al (FR104007) and Bl (FR104008), new potent inhibitors of renal dehydropeptidase, were isolated from the culture broth of strain No. 1358 which was identified as
Streptomyces parvulus subsp.
In vitro inhibitory activities (IC
50 value) of WSl358Al and Bl against porcine renal DHP were 3 and 600 nM, respectively.
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II. STRUCTURAL ELUCIDATION AND SYNTHESIS OF WSl358A1 AND B1
SHIGEHIRO TAKASE, ITSUO UCHIDA, SEIJI HASHIMOTO, HIROKAZU TANAKA, MASA ...
1990 Volume 43 Issue 1 Pages
38-42
Published: January 25, 1990
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The structures of WSl358A1 and Bl, new dehydropeptidase inhibitors isolated from
Streptomyces parvulus subsp.
tochigiensis No. 1358, have been established to be 2-hydroxy-2-hydroxyaminocarbonyl-3-methylglutaric acid (
1) and 2-hydroxy-2-hydroxyaminocarbonylglutaric acid (
2), respectively, on the basis of spectroscopic evidence and synthesis of the racemates.
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NIKKOMYCINS Wz AND Wx, NEW CHITIN SYNTHETASE INHIBITORS FROM STREPTOMYCES TENDAE
HEINRICH DECKER, FRANZ WALZ, CHRISTIANE BORMANN, HANS ZÄHNER, HAN ...
1990 Volume 43 Issue 1 Pages
43-48
Published: January 25, 1990
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Two new dipeptidyl nikkomycins of the Z and X type were isolated from the culture broth of
Streptomyces tendae TÜ 901/395-11/32 and characterized. They show a variation in the amino acid moiety of the molecule. Nikkomycin W
z is composed of L-tyrosine and 5-amino-5-deoxy-D-
allo-furanuronic acid
N-glycosidally bound to uracil, whereas nikkomycin W
x is composed of L-tyrosine and 5-amino-5-deoxy-D-
allo-furanuronic acid
N-glycosidally bound to 4-formyl-4-imidazolin-2-one. The new nikkomycins are good inhibitors of chitin synthetase from
Coprinus cinereus but they did not inhibit growth of fungi and yeasts.
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SONOKO ATSUMI, KAZUO UMEZAWA, HIRONOBU IINUMA, HIROSHI NAGANAWA, HIKAR ...
1990 Volume 43 Issue 1 Pages
49-53
Published: January 25, 1990
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In the course of our screening of β-glucosidase inhibitor, a culture filtrate of a mushroom,
Phellinus sp. strongly inhibited the enzyme activity. The active substance was isolated through charcoal separation, column chromatography and crystallization. Spectroscopic and crystallographic analysis revealed that it had a novel cyclitol structure, (1
S, 2
R, 3
S, 4
R, 5
R, 6
R)-5-hydroxymeihy¥-loxabicyclo[4, l, 0]heptane-2, 3, 4-triol, and we named it cyclophellitol. It inhibited almond-derived β-glucosidase with an IC
50 of 0.8μg/ml.
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YOSHIO NISHIMURA, KIYOTO ISHII, SHINICHI KONDO
1990 Volume 43 Issue 1 Pages
54-61
Published: January 25, 1990
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The absolute structure of decilonitrose, a sugar component of an antitumor antibiotic decilorubicin was decided to be 2, 3, 6-trideoxy-3-
C-methyl-3-nitro-L-
ribo-hexopyranose by synthesis of its methyl β-glycoside starting from L-rhamnose through the 3-ulose. In the synthetic route, any configurational ambiguities do not exist.
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SEIJI SHIBAHARA, TSUNEO OKONOGI, TAKASHI YOSHIDA, YASUSHI MURAI, TOSHI ...
1990 Volume 43 Issue 1 Pages
62-69
Published: January 25, 1990
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Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities. Among these cephalosporins, ME1228 having (
S)-1-carboxyethoxyimino substituent and being combined with an (
N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.
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I. RACEMIC 6-ETHYLIDENEPENEMS
MICHAEL J. BASKER, NEAL F. OSBORNE
1990 Volume 43 Issue 1 Pages
70-75
Published: January 25, 1990
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The dehydration of various 6-(1-hydroxyethyl)penems to give
E- and
Z-6-ethylidenepenems is described. Both isomers have been shown to be potent broad spectrum inhibitors of bacterial β-lactamases capable of reducing the MIC values of β-lactam antibiotics such as amoxycillin and cephaloridine against a wide range of resistant organisms.
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II. RACEMIC FURYL AND THIENYL DERIVATIVES
NIGEL J. P. BROOM, KENNETH COLEMAN, PAMELA A. HUNTER, NEAL F. OSBORNE
1990 Volume 43 Issue 1 Pages
76-82
Published: January 25, 1990
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A series of racemic 6-(substituted methylene)penems have been prepared. These compounds contain a 5-membered monoheteroaromatic ring at C-8. The antibacterial/synergistic and β-lactamase inhibitory activities of both
E- and
Z-isomers and 2-substituted derivatives are compared.
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ROKURO MASUMA, DE-ZHONG ZHEN, YOSHITAKE TANAKA, SATOSHI OMURA
1990 Volume 43 Issue 1 Pages
83-87
Published: January 25, 1990
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The site of regulation of nanaomycin biosynthesis by inorganic phosphate was studied with washed cells previously grown in a chemically defined medium containing a high- or low-phosphate concentration. The former mycelia produced only about one-tenth the amount of nanaomycin A from acetate as did the latter mycelia. On the other hand, the bioconversions of nanaomycin D to A and nanaomycin A to E were only slightly affected. It is suggested that the site of regulation of nanaomycin biosynthesis by inorganic phosphate lies within steps between acetate and nanaomycin D.
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GÜNTER RÖMMELE, GABRIELA WIRZ, RENATE SOLF, KLAUS VOSBECK, J ...
1990 Volume 43 Issue 1 Pages
88-91
Published: January 25, 1990
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Sorangicin A, a macrolide polyether antibiotic and the ansamycin antibiotic rifampicin inhibit DNA-dependent RNA polymerase to a similar extent. Resistance to sorangicin A is due to a mutation in the RNA polymerase which renders the enzyme less sensitive. Parallel investigations with rifampicin revealed partial cross-resistance, which was more marked in sorangicin A-resistant mutants than in rifampicin-resistant mutants.
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N. E. ALLEN, J. N. HOBBS, D. A. PRESTON, J. R. TURNER, C. Y. E. WU
1990 Volume 43 Issue 1 Pages
92-99
Published: January 25, 1990
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LY173013 and LY186826 are bicyclic pyrazolidinones containing a novel aza-γ-lactam ring structure. The antibacterial properties of these compounds appear to be related to those of β-lactam antibiotics in that both classes of compounds share certain common binding molecules such as β-lactamases and penicillin-binding proteins.
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N. KLESEL, D. ISERT, M. LIMBERT, A. MARKUS, G. SEIBERT, E. SCHRINNER
1990 Volume 43 Issue 1 Pages
100-106
Published: January 25, 1990
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In systemic and local infections, the therapeutic efficacy of cefpirome was compared to that of imipenem and cefotaxime.
Murine septicemia induced with methicillin-sensitive and methicillin-resistant
Staphylococcus aureus strains responded well to cefpirome and imipenem therapy, the ED
50 values ranged from 0.8 to 28.40 mg/kg and 0.5 to 15.58mg/kg, respectively. The carbapenem also displayed high efficacy against Enterococci and was more potent than cefpirome. Cefotaxime, however, exhibited lower activity or proved to be inactive against these strains.
With ED
50 values of 0.03 to 31.33 mg/kg, cefpirome was the most active of the three antibiotics in protecting mice challenged with Enterobacteriaceae. The corresponding ED
50 values of imipenem and cefotaxime ranged from 0.72 to 70.95 mg/kg and 0.06 to 66.30 mg/kg, respectively.
Despite distinctly lower
in vitro activity against the infecting organism, cefpirome showed efficacy similar to imipenem in the treatment of subcutaneous
S. aureus abscesses in mice. It was more effective than imipenem and cefotaxime against experimental
Klebsiella pneumonia in mice and the
Escherichia coli infected granuloma pouch in rats.
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JOHN A. BEUTLER, GWENDOLYN N. CHMURNY, PATRICK CLARK, CLIMACO J. METRA ...
1990 Volume 43 Issue 1 Pages
107-109
Published: January 25, 1990
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TSUYOSHI KAWANO, TOMOMI HIDAKA, KAZOO FURIHATA, JUNICHIRO MOCHIZUKI, H ...
1990 Volume 43 Issue 1 Pages
110-113
Published: January 25, 1990
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SHINTARO NISHIMURA, NOBUYOSHI YASUDA, HIROSHI SASAKI, YOSHIMI MATSUMOT ...
1990 Volume 43 Issue 1 Pages
114-117
Published: January 25, 1990
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TETSUJI TOMIYA, MASAKAZU URAMOTO, KIYOSHI ISONO
1990 Volume 43 Issue 1 Pages
118-121
Published: January 25, 1990
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TAKUSHI KANEKO, HENRY WONG, WILLIAM C. ROSE, WILLIAM T. BRADNER, TERRE ...
1990 Volume 43 Issue 1 Pages
122-124
Published: January 25, 1990
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TAKUSHI KANEKO, HENRY WONG, JACOB UTZIG, JOHN SCHURIG, TERRENCE W. DOY ...
1990 Volume 43 Issue 1 Pages
125-127
Published: January 25, 1990
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