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TOSHIKATSU FUJII, HIROSHI MAEDA, FUJIO SUZUKI, NAKAO ISHIDA
1978 Volume 31 Issue 11 Pages
1079-1090
Published: 1978
Released on J-STAGE: April 12, 2006
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A new antitumor and antiviral substance, KS-2, was prepared by ethanol precipitation
of the hot water extract of culture mycelia of
Lentinus edodes KSLE 007. It was further
purified by ECTEOLA-cellulose and Sephadex G-100 column chromatography based on the interferon-inducing activity. Its homogeneity was revealed by CsCl density gradient centrifugation, electrophoresis on cellulose acetate and Sephadex G-100 and ECTEOLA-cellulose column chromatography. KS-2 is mainly composed of α-linked mannose and contains a small amount of peptide which consists of serine, threonine and alanine with residual amounts of the other amino acids. The estimated molecular weight of KS-2 is between 6.0×10
4 and 9.5×10
4. KS-2 suppressed the growth of EHRLICH as well as Sarcoma-180 tumors in mice when given either orally or intraperitoneally. It is also capable of inducing an interferon in mice when dosed orally or intraperitoneally. The acute LD
50 of KS-2 was found to be extremely low, more than 12, 500 mg/kg when administered orally to mice.
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SATOSHI OMURA, HARUO TANAKA, YUZURU IWAI, KAZUE NISHIGAKI, JUICHI AWAY ...
1978 Volume 31 Issue 11 Pages
1091-1098
Published: 1978
Released on J-STAGE: April 12, 2006
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A new antibiotic, setomimycin, was isolated from the culture broth of strain AM-2947, which was identified as
Streptomyces pseudovenezuelae. The compound is a weakly acidic substance, and has UV-absorptions at 228, 268 and 422 nm and a molecular formula of C
34H
28O
9(MW 580). It is active against Gram-positive bacteria including
Mycobacteria, and has antitumor activity against Sarcoma-180 solid tumor in mice.
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I. FERMENTATION, ISOLATION AND ANTIBACTERIAL PROPERTIES
MARIE-ANTOINETTE BAUTE, GERARD DEFFIEUX, ROBERT BAUTE, ARLETTE NEVEU
1978 Volume 31 Issue 11 Pages
1099-1101
Published: 1978
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An atmosphere isolate of the fungus
Epicoccum nigrum was found to exhibit an activity against
Staphylococcus aureus. A more active, non-sporulating variant of this strain was selected. From its fermentation broth, two novel compounds, epicorazines A and B, were isolated by preparative TLC and tested against a series of bacteria.
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II. EPICORAZINE A: STRUCTURE ELUCIDATION AND ABSOLUTE CONFIGURATION
GÉRARD DEFFIEUX, MARIE-ANTOINETTE BAUTE, ROBERT BAUTE, MARIE-JO ...
1978 Volume 31 Issue 11 Pages
1102-1105
Published: 1978
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An antibiotic, epicorazine A, isolated from a particular strain of the fungus
Epicoccum nigrum, was shown to be a new epidithiodiketopiperazine from its UV, IR, mass, NMR and CD spectra. X-Ray diffraction measures confirmed this structure and its absolute configuration.
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III. EPICORAZINE B: STRUCTURE ELUCIDATION AND ABSOLUTE CONFIGURATION
GÉRARD DEFFIEUX, MARIE-JOSÉ FILLEAU, ROBERT BAUTE
1978 Volume 31 Issue 11 Pages
1106-1109
Published: 1978
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Comparison of UV, IR, PMR and CD spectra of epicorazine B with those of epicorazine A, a previously isolated metabolite of
Epicoccum nigrum, showed that they were isomers with the same epidithiodiketopiperazine skeleton. X-Ray determination of epicorazine B indicated that the difference is related to a
cis-trans configuration.
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A. J. MIDDLETON, D. S. COLE, K. D. MACDONALD
1978 Volume 31 Issue 11 Pages
1110-1115
Published: 1978
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An iron-complexing antibiotic with a narrow spectrum of biological activity was produced by several strains of
Aspergillus nidulans when grown in a low-iron, chemically defined medium. Its chemical and biological properties closely resembled those of desferritriacetylfusigen, a metabolite of several other
Aspergilli and
Penicillia.
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HIROIE OHNO, TSUNEO SAHEKI, JUICHI AWAYA, AKIRA NAKAGAWA, SATOSHOI OMU ...
1978 Volume 31 Issue 11 Pages
1116-1123
Published: 1978
Released on J-STAGE: April 12, 2006
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αElasnin, a new human granulocyte elastase inhibitor, produced by the strain of KM-2753 designated as
Streptomyces noboritoensis KM-2753 has been isolated from the fermentation broth by column chromatography on silica gel and neutral alumina. Elasnin is a neutral, colorless, and viscous oil (n
17D=1.4983, [α]
18D -0.9°, λ
EtOHmax291 nm (ε, 7, 760)) having a molecular formula of C
24H
40O
4 (MW 392) as shown by its elemental analysis and mass spectrum. Elasnin markedly inhibits human granulocyte elastase, but it is almost inactive against pancreatic elastase, chymotrypsin, and trypsin. At 1.3 μg/ml (3.3×10
-6 M), elasnin is 50%,
inhibitory to human elastase, but it causes 50% inhibition of pancreatic elastase at 30.1μg/ml (76.8×10-
-6 M)
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I. ISOLATION AND IDENTIFICATION OF PROTORIFAMYCIN I
ORESTE GHISALBA, PETER TRAXLER, JAKOB NUESCH
1978 Volume 31 Issue 11 Pages
1124-1131
Published: 1978
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A mutant strain derived from
Nocardia mediterranei N813 was found to accumulate a number of novel ansamycins structurally related to the protostreptovaricins and to rifamycin W. One of the main components of this ansamycin complex, protorifamycin I (8-deoxyrifamycin W), was purified and identified by means of chemical and spectroscopic methods.
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II. DIRECT BIOLOGICAL CORRELATION OF COMPONENTS IN THE FERMENTATION BROTH
ROGER D. MILLER, NORBERT NEUSS
1978 Volume 31 Issue 11 Pages
1132-1136
Published: 1978
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A portion of the eluent, during liquid chromatography of a fermentation broth, is applied directly to a paper strip at the same rate as the recording of the U. V. absorption. The paper is then placed on the agar inoculated with an appropriate test organism. This procedure permits direct correlation of biological activity with corresponding peaks in the U. V.
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I. HAUPT, R. HÜBENER, H. THRUM
1978 Volume 31 Issue 11 Pages
1137-1142
Published: 1978
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The effect of streptothricin F on macromolecular syntheses in intact cells and cell-free protein synthesis of
E. coli was studied. The results indicate that protein synthesis is the primary site of inhibition by streptothricin F in growing
E. coli cells. Cell-free polypeptide synthesis from
E. coli directed by poly (U) was inhibited, while poly (A) and poly (C) directed polypeptide syntheses were both stimulated by the drug. Furthermore, streptothricin F caused misreading of translation of poly (U), poly (A) and poly (C) directed protein syntheses in
E. coli systems. The extent of misreading by streptothricin F increases with increasing drug concentrations. The results are compared with those of other miscoding antibiotics. In rat liver extracts protein synthesis directed by poly (U) or endogenous mRNA was not inhibited.
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KOZO OCHI, EDWARD KATZ
1978 Volume 31 Issue 11 Pages
1143-1148
Published: 1978
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The treatment of
Streptomyces parvulus and Streptomyces antibioticus with acriflavine or novobiocin resulted in the loss of ability to produce actinomycin. The concomitant loss of ability to form aerial mycelium and the incidence of auxotrophic progeny (S. parvulus) were both low relative to the loss of the antibiotic-producing property. Protoplast fusion induced by polyethylene glycol 4000, using suitable auxotrophic strains of S. parvulus, resulted in high recombination frequencies to prototrophy (9.6-15%). When fusion was carried out between auxotrophic act+ and act- strains, respectively, there was a high frequency (84-95%) of the actinomycin synthesizing character among the prototrophic recombinants examined. No actinomycin-producing recombinant was detected in similar experiments between auxotrophic non-producing strains.
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I. THE EFFECT ON MACROMOLECULAR SYNTHESES
HIROSHI YAMAKI, HIDEO SUZUKI, TOSHIO NISHIMURA, NOBUO TANAKA
1978 Volume 31 Issue 11 Pages
1149-1154
Published: 1978
Released on J-STAGE: April 12, 2006
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The mechanism of action of aclacinomycin A was investigated with mouse tumor cells and
Escherichia coli. The antibiotic inhibited growth of mouse lymphoblastoma L5178Y cells completely at a concentration of 0.0125 μg/ml, and partially at 0.0063-0.0031 μg/ml. A greater inhibition of RNA than DNA synthesis was found in the intact cells of L5178Y:
i.e. , approximately 50% inhibition of the former occurred at an antibiotic concentration of 0.07 μg/ml, and that of the latter at 1.0 μg/ml. The degree of preferential inhibition by aclacinomycin A was more pronounced than that by adriamycin. Protein synthesis was not significantly affected. RNA synthesis by RNA polymerase II, from EHRLICH mouse carcinoma cells, was sensitive to aclacinomycin A. By the method employed, approximately 50% inhibition was observed at an antibiotic concentration of 1 μg/ml, with calf thymus DNA or poly(dAdT) as a template. In contrast, RNA polymerase reaction with poly (dIdC) was resistant to the antibiotic. The inhibition of RNA polymerase reaction with poly(dAdT) as template was apparently competitively reversed by increasing concentrations of the template but not of the enzyme, suggesting a direct interaction of the antibiotic with the template. Growth and macromolecular biosyntheses of
E. coli were rather resistant to aclacinomycin A. RNA and DNA polymerase reactions with toluenized cells of
E. coli P3478 (polA
-) were prevented by the antibiotic. RNA synthesis was inhibited by
ca. 60% and DNA synthesis by
ca. 25% at an antibiotic concentration of 10 μg/ml. RNA polymerase reaction, using
E. coli enzyme and calf thymus DNA as a template, was blocked by aclacinomycin A: approximately 50% inhibition was observed at an antibiotic oncentration of 10 μg/ml; whereas DNA polymerase I reaction was not significantly affected by the antibiotic.
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SHIMPEI NASU, YUZURU SEKINE, KAZUO IZAKI, HAJIME TAKAHASHI
1978 Volume 31 Issue 11 Pages
1155-1161
Published: 1978
Released on J-STAGE: April 12, 2006
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Six strains of chloramphenicol (CM)-resistant endospore-forming bacteria, which can grow in the presence of 100 μg/ml of CM, were isolated and identified as
Bacillus badius. Mechanism of CM-resistance in one of the isolated strains,
Bacillus badius 211, was investigated. No inactivation of CM was demonstrated when the strain was grown in nutrient broth containing 100 μg/ml of CM, as evidenced by paper-disc bioassay of CM in the growth medium. In accordance with this result, no CM acetylation activity was demonstrated either with the intact cells or with the crude extracts of the CM-resistant strain. Poly U- and Poly A-directed polyphenylalanine and polylysine syntheses by S-30 preparations of both CM-resistant and CM-sensitive strains of
Bacillus badius were almost equally inhibited by CM. From these results, the mechanism of CM resistance in
Bacillus badius 211 seems to be due to other unknown mechanism.
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JON P. DURKIN, THAMMIAH VISWANATHA
1978 Volume 31 Issue 11 Pages
1162-1169
Published: 1978
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Inactivation of β-lactamase I by clavulanic acid was investigated. Clavulanic acid induced inhibition of the enzyme was found to be progressive with time. Benzylpenicillin provided protection against the adverse effects of the inhibitor initially, however, the enzyme was irreversibly inhibited in a progressive manner even in the presence of substrate. Reaction of β-lactamase I with clavulanic acid, in the presence of ampicillin, led to a very rapid inactivation of the enzyme.
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PRAMOD M. SHAH, GUDRUN TROCHE, WOLFGANG STILLE
1978 Volume 31 Issue 11 Pages
1170-1174
Published: 1978
Released on J-STAGE: April 12, 2006
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The
in vitro activity of HR 756, a new cephalosporin, has been determined against recent clinical isolates and compared with that of other β-lactam antibiotics. The geometric means of the minimum inhibitory concentrations (MIC) for different isolates of
Escherichia coli (100 isolates),
Klebsiella pneumoniae (84),
Pseudomonas aeruginosa (121),
Proteus mirabilis (52), indole-positive
Proteus species (9),
Salmonella species (19),
Staphylococcus aureus penicillinsensitive (29) and penicillin-resistant (39) were: 0.095, 0.124, 11.1, 0.095, 0.0107, 0.078, 1 and 0.95 mcg/ml, respectively. Its activity was affected by rise in inoculum against
S. aureus and
P. aeruginosa but not against
K. pneumoniae and
E. coli. Bactericidal activity was determined by membrane filtration method. HR 756 was found to be bactericidal to
E. coli, K. pneumoniae, P. aeruginosa and
Proteus species. Although the MICs of the tested
S. aureus strains were 1 mcg/ml, 5 mcg/ml of HR 756 failed to kill 99% of the inoculum within 24 hours.
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N. A. KUCK, G. S. REDIN
1978 Volume 31 Issue 11 Pages
1175-1182
Published: 1978
Released on J-STAGE: April 12, 2006
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Piperacillin sodium is a novel semisynthetic penicillin with broad spectrum activity against Gram-negative and -positive bacteria including anaerobes. In agar dilution tests with 522 clinical isolates, it inhibited at least 70-90% of each group of organisms at 16 mcg/ml with the exception of the
Serratia group which required 64 mcg/ml to inhibit 70% of the isolates. Piperacillin was more potent than carbenicillin, ticarcillin and ampicillin against
Klebsiella, Pseudomonas, Enterobacter and
Serratia. Against Gram-positive cocci it was generally comparable to carbenicillin and ticarcillin except in the case of enterococci where it was significantly more potent. Piperacillin exhibited a broader spectrum than the cephalosporins which lacked antipseudomonal activity. It was more potent than cephalothin, cefamandole and cefoxitin against indole-positive
Proteus, Acinetobacter and enterococci. Piperacillin is bactericidal; minimal bactericidal concentrations were within four-fold of the minimal inhibitory concentrations. Its activity was not significantly altered by pH, media or serum, but was reduced when inoculum size was increased from 10
5 to 10
7 CFU/ml. Synergistic effects were observed when piperacillin was combined with gentamicin or amikacin. Piperacillin was effective against both acute lethal infections and chronic kidney infections in mice. Our results indicate that piperacillin has a spectrum of activity that spans those of other semisynthetic penicillins and cephalosporins.
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NILS MILMAN, JORGEN DAHLAGER
1978 Volume 31 Issue 11 Pages
1183-1187
Published: 1978
Released on J-STAGE: April 12, 2006
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The effects of aminoglycoside antibiotics on
125I-hippurate (OIH) accumulation in rabbit renal cortical slices were assessed
in vitro using incubation media with pH-values ranging from 6.4 to 8.4 and containing streptomycin, kanamycin, amikacin, gentamicin and tobramycin in concentrations ranging from 100 to 2, 000 μg base/ml. The aminoglycoside-induced inhibition of OIH accumulation was clearly pH-dependent and most pronounced at alkaline pH-values. At pH 6.4 and 7.4 the aminoglycosides had either no or only moderate effects on OIH accumulation, while all drugs produced a distinct depression in accumulation at pH 7.9 and 8.4. The microbiologically inert
N-acetyl gentamicin had no influence on accumulation. The influence of aminoglycosides on OIH accumulation is probably related to the pKa-values of these drugs and implies the presence of free amino groups.
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A. P. INTOCCIA, S. S. WALKENSTEIN, G. JOSEPH, R. WITTENDORF, C. GIRMAN ...
1978 Volume 31 Issue 11 Pages
1188-1194
Published: 1978
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SK&F 75073 is a new cephalosporin with broad spectrum antibacterial activity. SK&F 75073-
14C and cefazolin-
35S were administered separately to groups of rats as a single intramuscular dose of 20 mg/kg. Tissues with highest drug levels 15 minutes following dose were as follows: (SK&F 75073/cefazolin levels), kidney - 86/70 μμg/g, liver - 33/22 μg/g, lung - 29/17μg/g, heart - 23/10 μg/g, adrenal - 13/7 μg/g. Plasma levels at peak were 134 μg SK&F 75073/ml (half-life, 1.9 hours) and 72 μg cefazolin/ml (half-life, 0.75 hours). Dose excreted in 24 hours was: SK&F 75073, urine 66% and feces 27% ; cefazolin, urine 96% and feces 2%. Both antibiotics were also administered, at 20 mg/kg, to rats with the carrageenan-induced inflammatory pouches. Exudate from these pouches contained from 2 to 10 times more SK&F 75073 than cefazolin. Radioassay and bioassay of these substances in the exudate gave similar results. Serum protein binding ranged from 96-98% for SK&F 75073 and 34-69% for cefazolin. Data indicated that highly protein bound SK&F 75073 enters tissues and tissue fluid to a greater extent than the lesser bound but therapeutically proven antibiotic agent cefazolin.
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L. STANZANI, A. P. VENTURINI, V. MANTOVANI
1978 Volume 31 Issue 11 Pages
1195-1200
Published: 1978
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GEORGE M. STRUNZ, RONALD E. WALL, DOUGLAS J. KELLY
1978 Volume 31 Issue 11 Pages
1201-1202
Published: 1978
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MASATOSHI INUKAI, MICHIKO TAKEUCHI, KEIKO SHIMIZU, MAMORU ARAI
1978 Volume 31 Issue 11 Pages
1203-1205
Published: 1978
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YUKIO SUGIURA
1978 Volume 31 Issue 11 Pages
1206-1208
Published: 1978
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U. TAUBENECK
1978 Volume 31 Issue 11 Pages
1209
Published: 1978
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