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DISCOVERY, FERMENTATION, BIOLOGICAL AS WELL AS IONOPHORE PROPERTIES AND TAXONOMY OF THE PRODUCING CULTURE
CHAO-MIN LIU, THERON E. HERMANN, MARK LIU, BARBARA LA T. PROSSER, NORB ...
1981 Volume 34 Issue 10 Pages
1241-1247
Published: 1981
Released on J-STAGE: April 12, 2006
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X-14667A and X-14667B are two novel polyether antibiotics produced by
Streptomyces cinnamonensis subsp.
urethanofaciens. The antibiotics are active
in vitro against Gram-positive bacteria and exhibit high affinity for monovalent cations.
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JOHN W. WESTLEY, RALPH H. EVANS, Jr., LILIAN H. SELLO, NELSON TROUPE, ...
1981 Volume 34 Issue 10 Pages
1248-1252
Published: 1981
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Antibiotics X-14667A (
1) and X-14667B (
2) are novel monovalent polyether antibiotics of the spiroketal type isolated from fermented cultures of
Streptomyces cinnamonensis subsp.
urethanofaciens together with monensin (
3), its lower homolog, factor B (
4) and 1, 3-diphenethylurea (
6). By a combination of microanalysis, mass spectrometry and
13C nmr, antibiotics X-14667A and B have been shown to be natural 2-phenethylurethanes of monensin B and A respectively. Both structures have been confirmed by reacting the appropriate monensin with 2-phenethylisocyanate to yield semi-synthetic compounds that are identical to the natural products.
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SATOSHI OMURA, KAZUHIKO OTOGURO, TAKAAKI NISHIKIORI, RUIKO OIWA, YUZUR ...
1981 Volume 34 Issue 10 Pages
1253-1256
Published: 1981
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A new antibiotic, setamycin, was extracted from the mycelia of a rare actinomycete strain KM-6054. The antibiotic, the molecular formula of which was found to be C42H61NO12 (tentative), is a yellow powder showing activity against some fungi, trichomonads and weakly against Gram-positive bacteria.
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R. CRICCHIO, P. ANTONINI, P. FERRARI, A. RIPAMONTI, G. TUAN, E. MARTIN ...
1981 Volume 34 Issue 10 Pages
1257-1260
Published: 1981
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Rifamycin Z is a novel ansamycin produced by a mutant of
Nocardia mediterranea. Physico-chemical data indicate that it possesses a lactone-type structure directly derived from rifamycin W.
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I. PRODUCTION, ISOLATION AND INSECTICIDAL PROPERTIES OF ISARIINS B, C AND D
ROBERT BAUTE, GÉRARD DEFFIEUX, DANIELLE MERLET, MARIE-ANTOINETT ...
1981 Volume 34 Issue 10 Pages
1261-1265
Published: 1981
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Three new cyclodepsipeptides related to the previously described isariin were isolated from a strain of
Isaria felina. They were named isariins B, C and D. Isariin D and, to a lesser extent, isariin C, exhibited insecticidal activity against
Galleria mellonella larvae, whereas isariin B and isariin itself proved inactive.
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II. STRUCTURE ELUCIDATION OF ISARIINS B, C AND D
GÉRARD DEFFIEUX, DANIELLE MERLET, ROBERT BAUTE, GUY BOURGEOIS, ...
1981 Volume 34 Issue 10 Pages
1266-1270
Published: 1981
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Isariins B, C and D, isolated from a strain of
Isaria felina, were shown to be cyclodepsipeptides constituted by a pentapeptide cyclized through a β-hydroxyacid. The nature of the latter and the sequence of the peptide were determined for each compound. Relations between insecticidal activity and structure of the depsipeptides were pointed out.
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THE ALLIACOLS A AND B FROM MARASMIUS ALLIACEUS (JACQ. ex FR.) FR.
T. ANKE, W. H. WATSON, B. M. GIANNETTI, W. STEGLICH
1981 Volume 34 Issue 10 Pages
1271-1277
Published: 1981
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Two antimicrobial and cytotoxic metabolites were isolated from fermentation broth of
Marasmius alliaceus. The structures of the two crystalline antibiotics, alliacols A
(6) and B
(1) were elucidated by spectroscopic methods and chemical correlation with alliacolide
(3). The alliacols show weak antibacterial and antifungal activity. Both antibiotics strongly inhibit DNA synthesis in cells of the ascitic form of Ehrlich carcinoma at concentrations of 2-5μg/ml. Both alliacols A and B react with cysteine to form adducts with strongly reduced biological activities.
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MASAKI SUGIURA, MASAHIKO KISUMI, ICHIRO CHIBATA
1981 Volume 34 Issue 10 Pages
1278-1282
Published: 1981
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An amino acid was formed by α-aminobutyrate-resistant mutants of
Serratia marcescens grown in a medium containing norvaline. This amino acid was identified as
erythro β-methyl-L-norleucine [(2
S, 3
S)-2-amino-3-methylhexanoic acid] by instrumental analyses. β-Methylnorleucineinhibited the growth of several bacteria in synthetic medium.
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MASAKI SUGIURA, MASAHIKO KISUMI, ICHIRO CHIBATA
1981 Volume 34 Issue 10 Pages
1283-1289
Published: 1981
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β-Methylnorleucine biosynthesis was examined in
Serratia marcescens using regulatory mutants of branched-chain amino acid biosynthesis. The accumulation of β-methylnorleucine from norvaline in the wild-type strain was inhibited by the simultaneous additions of isoleucine, valine and leucine, although its accumulation in the derepressed mutant of isoleucine, valine and leucine biosynthesis was markedly increased and was not inhibited by additions of these amino acid. Accumulation of this compound was not observed in an isoleucine-valine auxotroph, although its accumulation was not affected in an isoleucine or leucine auxotroph. Transaminase B catalyzed the conversion of α-keto-β-methylcaproate to β-methylnorleucine. These results suggest that β-methylnorleucine is formed from α-ketovalerate, α-ketoacid corresponding to norvaline, by enzymes of the isoleucine-valine biosynthetic pathway.
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SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF α-HYDROXYIMINOARYLACETYL CEPHALOSPORINS
TAKAO TAKAYA, HISASHI TAKASUGI, TAKASHI MASUGI, HIROMU KOCHI, HIROSHI ...
1981 Volume 34 Issue 10 Pages
1290-1299
Published: 1981
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The synthesis and antibacterial activity
in vitro of the 2-aryl-2-hydroxyiminoacetyl cephalosporins
(2) are described. Within this cephalosporin series, analogs
(9f-13f) with 2-hydroxyimino -2-(3-hydroxyphenyl)acetyl group at the 7-position of a cephem nucleus were found to have the highest antibacterial activity against a wide-range of microorganisms, including β-lactamaseproducing bacteria. Structure-activity relationships of
2 are discussed.
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SYNTHESIS AND ENZYMATIC STABILITY OF 3-ACYLOXYMETHYL-7β-[(Z)-2-(2-AMINO-4-THIAZOLYL)-2-(METHOXYIMINO)ACETAMIDO]-3-CEPHEM-4-CARBOXYLIC ACIDS
TAKAO TAKAYA, HISASHI TAKASUGI, TAKEO MURAKAWA, HIROSHI NAKANO
1981 Volume 34 Issue 10 Pages
1300-1310
Published: 1981
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3-Acyloxymethyl-7β-[
(Z) -2-(2-amino-4-thiazolyl)-2-(methoxyimino) acetamido]-3-cephem-4-carboxylic acids
(7) were synthesized. The stability of
7 to enzymatic hydrolysis and their antimicrobial activity were evaluated.
7 showed good antimicrobial activity gainst a wide range of microorganisms. Cephems (
7b and
7c) with sterically more hindered acyl groups such as
t-butyl and cyclohexyl were most resistant to enzymatic hydrolysis.
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SYNTHESIS AND STRUCTURE ACTIVITY RELATIONSHIPS OF PARENTERALLY ACTIVE 7-[4-(SUBSTITUTED METHYL)PHENYL]- ACETAMIDO-3-CEPHEM-4-CARBOXYLIC ACIDS
ABRAHAM NUDELMAN, FORTUNA HAVIV, ABRAHAM PATCHORNICK, EVA KAROLY-HAFEL ...
1981 Volume 34 Issue 10 Pages
1311-1317
Published: 1981
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A group of novel 4-substituted phenylacetic acids were prepared and coupled with several 7-amino-Δ-3-cephems to afford a family of parenterally active cephalosporins. A compound designated
131 had the broadest spectrum of activity and the highest potency of the group against both Gram-positive and Gram-negative bacteria. The activity of
131 included high potency against penicillinase-producing staphylococci and activity against anaerobes, including
Bacteroides fiagilis.
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TETSUO SAWAI, TAKASHI YOSHIDA, KIKUO TSUKAMOTO, SABURO YAMAGISHI
1981 Volume 34 Issue 10 Pages
1318-1326
Published: 1981
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A set of bacterial strains composed of nine bacterial groups, with each made up of three or four strains, was used to estimate the stability of β-lactam antibiotics to nine types of β-lactamases from Gram-negative bacteria. The strains in the same group produced the same kind of enzyme constitutively, but the enzyme activity achieved in the bacterial cell differed with different strains. The difference in antibacterial activity of each antibiotic on the strains of each group, easily measured by a simple plate technique, permits an estimation of its relative stability to each β-lactamase. This method was applied to thirteen β-lactam antibiotics including seven new ones.
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MASAHIRO KONDO, KANJI TSUCHIYA
1981 Volume 34 Issue 10 Pages
1327-1333
Published: 1981
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The effect of cefsulodin in combination with various β-lactam antibiotics was examined against
Serratia marcescens.
In vitro, the optimum ratio for all combinations tested was almost the same (cefsulodin-other antibiotic=1:1-1:4). The combinations of cefsulodin-cefazolin and cefsulodin-cefotiam were found to have a synergistic effect and other combinations, such as cefsulodin-cefmenoxime, -ampicillin and -sulbenicillin, an additive effect with the checkerboard dilution and the fixed combination methods. The synergistic effect of cefsulodincefotiam was more potent than that of cefsulodin-cefazolin and the effect of both combinations was clearer with heavy than with light inoculum size. With the killing kinetic method, all combinations tested showed a synergistic effect.
In vivo, the optimum combination ratios of cefsulodin-cefazolin and cefsulodin-cefotiam were 1: 2 and 1: 1, respectively, the protective effect of the latter combination being much stronger than that of the former. With the fixed combination method (cefsulodin - other antibiotic= 1: 1 - 1: 4), the effect of the combination of cefsulodin with all antibiotics except cefazolin and cefotiam was additive.
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THOMAS A. HOFFMAN, TIMOTHY J. CLEARY, DON H. BERCUSON
1981 Volume 34 Issue 10 Pages
1334-1340
Published: 1981
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The activity of carbenicillin, ticarcillin, piperacillin, cefotaxime, moxalactam, and N-formimidoyl thienamycin was evaluated against 262 clinical isolates of
Pseudoanams aeruginosa. There were 242 (92%) of the isolates that were susceptible to carbenicillin or ticarcillin by an agar dilution method. Against this population of susceptible isolates, the median MICs were 1.56 μg/ml of N-formimidoyl thienamycin, 3.13 μg/ml of piperacillin, 25 μg/ml of ticarcillin, 25 μg/ml of cefotaxime, 50 μg/ml of carbenicillin and 50 μg/ml of moxalactam.
N-Formimidoyl thienamycin was the only beta-lactam antibiotic not affected by an inducible betalactamase detected in 24 randomly selected susceptible isolates by a disk approximation assay, while cefotaxime was inactivated to a greater extent than any of the other beta-lactam antibiotics. Resistance to carbenicillin and ticarcillin was noted in 20 isolates (8%); these were susceptible to
N-forn-iimidoyl thienamycin, but cross-resistance with piperacillin, cefotaxime, and moxalactam was frequent. Only four of these resistant isolates were found to have a constitutive beta-lactamase. Gentamicin resistance occurred in 51 isolates (19) and was an independent variable of resistance to the beta-lactam drugs.
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I. CLAVULANIC ACID AND PS-5
HIROSHI OGAWARA, ATSUSHI MANTOKU
1981 Volume 34 Issue 10 Pages
1341-1346
Published: 1981
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Inactivation of a β-lactamase of
Streptonzyces cacaoi by clavulanic acid and PS-5 was investigated and compared with that of a β-lactamase of
Bacillus cereus. Inhibition of the enzymes induced by clavulanic acid and the β-lactam antibiotic PS-5 was found to be progressive with time. However, the degree of inhibition of the β-lactamase from
S. cacaoi increased more progressively with time than that of the enzyme from
B. cereus. Conformative response constants were determined. As compared with clavulanic acid, over ten times higher concentrations of PS-5 were necessary to give a similar degree of inhibition. At lower concentrations, both clavulanic acid and PS-5 behaved as competitive inhibitors. Ki values calculated from the integrated form of the LINEWEAVER-BURKty pe were 1.1×10-7 M and 7.6×10-6 M for clavulanic acid and PS-5, respectively.
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II. CP-45, 899, IZUMENOLIDE AND CEPHAMYCINS
ATSUSHI MANTOKU, HIROSHI OGAWARA
1981 Volume 34 Issue 10 Pages
1347-1350
Published: 1981
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Inhibition of a β-lactamase of
Streptomyces cacaoi by CP-45, 899, izumenolide and cephamycins was investigated and compared with that of a β-lactamase of
Bacillus cereus. S. cacaoi enzyme could not hydrolyze CP-45, 899. Instead, hydrolysis of benzylpenicillin by the enzyme was inhibited in the presence of CP-45, 899. Although inhibition increased gradually with time, the inhibition line produced by CP-45, 899 with time was less curved than that produced by clavulanic acid and PS-5. Furthermore, preincubation of
S. cacaoi β-lactamase with CP-45, 899 for up to 120 seconds did not obviously affect the degree of inhibition. When the concentration was lowered, it behaved as a competitive inhibitor, a
Ki value being 6.2×10-7 M. Izumenolide, on the other hand, did not inhibit the enzyme activity of
S. cacaoi β-lactamase at 1.28×10-4M, although it inhibited
B. cereus enzyme slightly in a competitive manner. Oganomycins were inert to the both β-lactamases.
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AKIRA ENDO, NOBUAKI KITAHARA
1981 Volume 34 Issue 10 Pages
1351-1354
Published: 1981
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Hydroxybenzoic and phthalic acids and their related compounds were tested for inhibitory activity to brain glutamate decarboxylase. Of mono-, di-, and trihydroxybenzoic acids, gallic acid was the most inhibitory, giving 50% inhibition at a concentration of 0.17 mm. Dihydroxybenzoic acids were less inhibitory than the trihydroxyacids but more than monohydroxybenzoic acids. Of the phthalic acid-related compounds tested, 4, 5-dihydroxyisophthalic acid was the most potent inhibitor, producing 50% inhibition at 0.61 μm. The inhibition of these compounds was competitive with respect to L-glutamate. The Ki values were 0.02, 1.2 and 4.9 pM for 4, 5-dihydroxyisophthalic acid, 5-hydroxyisophthalic acid and gallic acid, respectively. When administered intraventricularly to mice, 4, 5-dihydroxyisophthalic acid produced a significant decrease in the γ-aminobutyric acid content of the brain, resulting in induction of convulsions.
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HISAYOSHI OKAZAKI, KAZUHIKO OHTA, TSUNEO KANAMARU, TAKENORI ISHIMARU, ...
1981 Volume 34 Issue 10 Pages
1355-1356
Published: 1981
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STRUCTURE-ACTIVITY RELATIONSHIPS OF 7β-[(Z)-2-ALKOXYI M INO-2-(2-AMINO-4-TH IAZOLYL)ACETAMIDO]-3-CEPHEM- 4-CARBOXYLIC ACIDS
TAKAO TAKAYA, HISASHI TAKASUGI, TAKASHI MASUGI, HIROMU KOCHI, HIROSHI ...
1981 Volume 34 Issue 10 Pages
1357-1359
Published: 1981
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SHUZO OKUMURA, TAKASHI DEGUCHI, HIROFUTO MARUMO
1981 Volume 34 Issue 10 Pages
1360-1362
Published: 1981
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NORIO EZAKI, TAKASHI SHOMURA, MASAO KOYAMA, TOMIZO NIWA, MICTUO KOJIMA ...
1981 Volume 34 Issue 10 Pages
1363-1365
Published: 1981
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MIYUKI KANEDA, SHOSHIRON AKAMURA, NORIO EZAKI, YOICHI IITAKA
1981 Volume 34 Issue 10 Pages
1366-1368
Published: 1981
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THE STRUCTURES OF TM-531B (4'-O-DEM ETHYLDIANEM YCIN) AND TM-531C(3'-HYDROXYDIANEMYCIN), NEW POLYETHER ANTIBIOTICS CONTAINING SUGARS OTHER THAN 4-O-METHYL AMICETOSE
TAKU MIZUTANI, MICHIO YAMAGISHI, KAZUTOSHI MIZOUE, AKIRA KAWASHIMA, SA ...
1981 Volume 34 Issue 10 Pages
1369-1373
Published: 1981
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AKIHIRO TANAKA, TSUTOMUT SUCHIYA, SUMIO UMEZAWA, HAMAO UMEZAWA
1981 Volume 34 Issue 10 Pages
1374-1376
Published: 1981
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AKIHIRO TANAKA, TSUTOMU TSUCHIYA, SUMIO UMEZAWA, MASA HAMADA, HAMAO UM ...
1981 Volume 34 Issue 10 Pages
1377-1380
Published: 1981
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AKIHIRO TANAKA, AZUMA WATANABE, TSUTOMU TSUCHIYA, SUMIO UMEZAWA, HAMAO ...
1981 Volume 34 Issue 10 Pages
1381-1384
Published: 1981
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U. GRÄFE, I. ERITT, W. F. FLECK
1981 Volume 34 Issue 10 Pages
1385-1387
Published: 1981
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