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I. TAXONOMY, FERMENTATION AND ISOLATION
TOSHIYUKI KATO, HIROSHI HINOO, JUN'ICHI SHOJI, KOICHI MATSUMOTO, TATSU ...
1987 Volume 40 Issue 2 Pages
135-138
Published: February 25, 1987
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New monobactams, PB-5266 A, B and C were isolated from the culture filtrate of
Cytophaga johnsonae PB-5266 by various types of column chromatography and preparative reversephase HPLC. PB-5266 A, B and C exhibited weak antibacterial activity against a sensitive mutant of
Escherichia coli to β-lactam antibiotics.
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II. PHYSICO-CHEMICAL PROPERTIES AND CHEMICAL STRUCTURES
TOSHIYUKI KATO, HIROSHI HINOO, YOSHIHIRO TERUI, JUNKO NISHIKAWA, Yuzo ...
1987 Volume 40 Issue 2 Pages
139-144
Published: February 25, 1987
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The chemical structures of three new monobactams, PB-5266 A, B and C, were elucidated by their physico-chemical properties and spectrometric studies. In contrast to previously described monobactams, they all possess a dehydroasparagine residue.
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JILL E. HOCHLOWSKI, WILLIAM W. ANDRES, ROBERT J. THERIAULT, MARIANNA J ...
1987 Volume 40 Issue 2 Pages
145-148
Published: February 25, 1987
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A new antibiotic, abbeymycin, has been isolated from
Streptomyces sp. AB-999F-52. The structure of abbeymycin was assigned on the basis of NMR, mass spectrometric and UV spectral data. Abbeymycin has weak activity against a limited number of anaerobic bacteria.
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MASARU MATSUMOTO, KIN-ICHI MOGI, KATSUHIKO NAGAOKA, SEIJI ISHIZEKI, RY ...
1987 Volume 40 Issue 2 Pages
149-156
Published: February 25, 1987
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The new piericidin group antibiotics, glucopiericidins A and B were isolated from the culture broth of
Streptomyces pactum S48727 (FERM P-8117) as co-metabolite of piericidin A
1.
The structures of glucopiericidins A and B were determined as piericidin A
1, 10-
O-β-D-glucoside and piericidin A
1 3'-
O-D-glucoside on the basis of their spectral and chemical properties, respectively.
Glucopiericidins were more potent in inhibiting antibody formation than piericidin A
1 in vitro. In addition, these substances showed better antimicrobial activities than piericidin A
1 Acute toxicities of these substances in mice were lower than that of piericidin A
1.
This indicates that D-glucose in glucopiericidin molecules is important in modulating their physiological activities.
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TADJUDDIN NAID, TOSHIHARU KITAHARA, MIYUKI KANEDA, SHOSHIRO NAKAMURA
1987 Volume 40 Issue 2 Pages
157-164
Published: February 25, 1987
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Carbazomycins C (
III), D (
IV), E (
V) and F (
VI), the minor components of the carbazomycin complex, were isolated from the cultured broth of
Streptoverticillium ehimense together with carbazomycins A (
II) and B (
I). Among them,
III and
IV were shown to be new substances and their structures were elucidated as 4-hydroxy-3, 6-dimethoxy-1, 2-dimethylcarbazole and 3, 4, 6-trimethoxy-1, 2-dimethylcarbazole, respectively, by spectroscopic and chemical means. The other components,
V and
VI, were found to contain an aldehyde function and were identified as carbazomycinal and 6-methoxycarbazomycinal, respectively. The antimicrobial activity of
III and
IV are also reported.
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J. J. DINGERDISSEN, R. D. SITRIN, P. A. DEPHILLIPS, A. J. GIOVENELLA, ...
1987 Volume 40 Issue 2 Pages
165-172
Published: February 25, 1987
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An unidentified
Nocardia sp. (SK&F-AAJ-193) was isolated and found to produce actinoidin A and a novel analog which we have named actinoidin A
2. This new glycopeptide antibiotic differs from actinoidin A by the presence of rhamnose instead of acosamine. This analog was isolated using Dianion HP-20 resin followed by a specific glycopeptide affinity column (Affigel-10-D-Ala-D-Ala). The purification was accomplished using preparative ion-pairing chromatography. Actinoidin A
2 is active against
Staphylococcus aureus and coagulase-negative Staphylococci although it is less potent than actinoidin A.
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I. SYNTHESIS AND IN VITRO ANTI-PSEUDOMONAL ACTIVITY OF 3-ISOTHIAZOLE-CEPHALOSPORIN DERIVATIVES
NORIAKI NAGANO, Komi NAKANO, TADAO SHIBANUMA, YUKIYASU MURAKAMI, RYUIC ...
1987 Volume 40 Issue 2 Pages
173-181
Published: February 25, 1987
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The synthesis and
in vitro activity of 7β-[(
Z)-2-(2-amino-4-thiazolyl)-2-(2-carboxy-2-alkoxyimino)acetamido]cephalosporins with a (4-carboxy-3-hydroxy-5-isothiazolyl)thiomethyl group at the 3-position are described. These cephalosporins (
9a-9i) showed excellent activity against Gram-negative bacteria including β-lactamase producing strains. The most interesting compound of the series was 7β-[(
Z)-2-(2-amino-4-thiazolyl)-2-(2-carboxy-2-propoxyimino)acetamido]-3-cephem-4-carboxylic acid (9g, YM-13115) because of its outstanding inhibitory potency against
Pseudomonas aeruginosa and highly prolonged plasma half-life in rats.
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II. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NOVEL AMINOTHIAZOLYL CEPHEM COMPOUNDS WITH HYDROXYPYRIDONE MOIETY
KENICHI MOCHIDA, YASUYUKI ONO, MOTOO YAMASAKI, CHIHIRO SHIRAKI, TADASH ...
1987 Volume 40 Issue 2 Pages
182-189
Published: February 25, 1987
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The synthesis and antimicrobial activity of novel carbacephem antibiotics which have amido moiety of (
S)-aminothiazolylglycyl side chain are described. Among them, the compound having 5-hydroxy-4-pyridon-2-carboxyl group (KT-4697) showed exceptionally strong activity against
Pseudomonas aeruginosa as well as Gram-negative bacteria. A cephalosporin with this acyl group namely KT-4788 with methylpyridiniumthiomethyl group at C-3 was found to be the most active against Gram-positive and Gram-negative strains including
P. aeruginosa.
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E. E. OSE
1987 Volume 40 Issue 2 Pages
190-194
Published: February 25, 1987
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A new macrolide antibiotic, EL-870, 20-deoxo-20-(3, 5-dimethylpiperidin-l-yl)desmycosin, has been prepared by chemical modification of desmycosin.
In vitro, against selected animal bacterial pathogens, it inhibited growth of
Pasteurella multocida,
Pasteurella haemolytica,
Mycoplasma hyopneumoniae,
Actinobacillus pleuropneumoniae,
Streptococcus suis,
Actinomyces pyogenes and certain other bacteria at levels of 6.25 μg/ml or less. In general, the MICs for Gram-negative enteric bacteria have been >50 μg/ml. Concentrations equivalent to 4 × the MIC value were bactericidal for
Pasteurella sp. EL-870 had other antibacterial properties which were characteristic of macrolide antibiotics.
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PAUL F. WILEY, LUBOMIR BACZYNSKYJ, LESTER A. DOLAK, JOYCE I. CIALDELLA ...
1987 Volume 40 Issue 2 Pages
195-201
Published: February 25, 1987
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Five macrolide antibiotics (erythromycin
A,
1; oleandomycin,
3a; tylosin,
4a; spiramycins,
5a; leucomycin A
3,
6a) have been phosphorylated enzymatically using cell-free extracts derived from
Streptomyces coelicolor UC 5240. The necessary cofactors and the rates of the conversion have been determined.
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JUNJI MAGAE, KAZUO NAGAI, SEIKICHI SUZUKI, MAKARI YAMASAKI, KUNIO ANDO ...
1987 Volume 40 Issue 2 Pages
202-208
Published: February 25, 1987
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Ascofuranone (AF) enhanced glucose consumption of splenocytes and macrophages, while it enhanced incorporation of [
14C]acetate into macrophages but not into splenocytes. When using tumor cell lines, it inhibited the incorporation of [
14C]acetate into lymphoma cell lines, YAC-1 and P388, and a thymoma, L5178Y, while it stimulated that into P388D1, which is derived from P388 and has macrophage-like characteristics. Incorporation of [
14C]acetate into a mammary carcinoma FM3A was also stimulated by AF. In contrast, AF stimulated uptake of methylglucose in all cell lines tested. The effect of AF was further studied using mouse myeloid leukemia, M1 cells. AF slightly stimulated the incorporation of [
14C]acetate into undifferentiated M1 cells, and strongly stimulated that of hydrocortisone-differentiated M1 cells. In contrast, AF suppressed the incorporation of [
14C]acetate into retinoic acid-differentiated M1 cells. Glucose consumption of these three types of M1 cells was all stimulated. From these results, we conclude that AF specifically stimulates the incorporation of [
14C]acetate into macrophages while it generally stimulates glucose uptake of the cells.
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PASQUALE P. VICARIO, BARBARA G. GREEN, HOWARD M. KATZEN
1987 Volume 40 Issue 2 Pages
209-216
Published: February 25, 1987
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The biosynthesis from L-alanine of D-alanyl-D-alanine, required for the peptidoglycan layer of the cell wall of many bacterial species, is catalyzed by two enzymes in series, alanine racemase and D-alanine: D-alanine ligase. A simple
in vitro method, called the combined assay, for simultaneously testing for effectors of either or both enzymes in a single assay by coupling these enzymes to each other is described here. The experiments used to derive the optimum conditions for the assay are also described. Each enzyme is included in the assay in rate-limiting amounts, wherein the product of the initial racemase reaction, D-alanine, becomes the substrate for the subsequent ligase. The product of the overall reaction, [
14C]-D-alanyl-D-alanine, is separated chromatographically from the L-[1-
14C]alanine substrate, and from any D-[1-
14C]alanine intermediate, at the end of the incubation, is counted and the percent conversion of substrate to product calculated. The inhibitory effects of 3-fluoro-Dalanine-2
d, a known inhibitor of the racemase, and D-cycloserine and DL-1-aminoethylphosphonic acid, inhibitors of both enzymes, were readily detectable. The sensitivity of the combined assay to these inhibitors appears similar to that of earlier assays. This assay has the advantage over previous ones of being able to detect inhibitors of either enzyme in a single assay, thereby avoiding the need to screen each compound in a separate assay of each enzyme.
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MARC LANG, PETER SCHNEIDER, RLCCARDO SCARTAZZINI, WERNER TOSCH, EDWARD ...
1987 Volume 40 Issue 2 Pages
217-220
Published: February 25, 1987
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F. BESSON, M. L. HOURDOU
1987 Volume 40 Issue 2 Pages
221-223
Published: February 25, 1987
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KEIJI HASUMI, MASAOMI ARAHIRA, KAORU SAKAI, AKIRA ENDO
1987 Volume 40 Issue 2 Pages
224-226
Published: February 25, 1987
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YAMAJI NAKANO, SHIGEO MURAKAWA, AKIRA ENDO
1987 Volume 40 Issue 2 Pages
227-229
Published: February 25, 1987
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HIROMASA OKADA, YOSHIO INOUYE, SHOSHIRO NAKAMURA
1987 Volume 40 Issue 2 Pages
230-232
Published: February 25, 1987
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G. T. CARTER, J. A. NIETSCHE, J. J. GOODMAN, M. J. TORREY, T. S. DUNNE ...
1987 Volume 40 Issue 2 Pages
233-236
Published: February 25, 1987
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YOKO KUSAKABE, NOBUKO TAKAHASHI, YASUO IWAGAYA, AKIO SEINO
1987 Volume 40 Issue 2 Pages
237-238
Published: February 25, 1987
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SATOSHI YAGINUMA, MASASHI AWATA, NAOKI MUTO, KENJI KINOSHITA, KIMIO MI ...
1987 Volume 40 Issue 2 Pages
239-241
Published: February 25, 1987
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YOSHITAKE TANAKA, KAZUKO HIRATA, YOKO TAKAHASHI, YUZURU IWAI, SATOSHI ...
1987 Volume 40 Issue 2 Pages
242-244
Published: February 25, 1987
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JILL BARBER, ANNE C. CHAPMAN, TINA D. HOWARD
1987 Volume 40 Issue 2 Pages
245-248
Published: February 25, 1987
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TAKENORI OCHIAI, SEIJI HORI, KAZUAKI NAKAJIMA, MATSUO NAGATA, TAKEHIDE ...
1987 Volume 40 Issue 2 Pages
249-250
Published: February 25, 1987
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