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I. TAXONOMY, FERMENTATION AND ISOLATION
J. B. TUNAC, L. E. MCDANIEL, C. P. SCHAFFNER
1979 Volume 32 Issue 12 Pages
1223-1229
Published: 1979
Released on J-STAGE: April 12, 2006
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A soil isolate of
Streptomyces, which has been deposited in the culture collection of the
Waksman Institute of Microbiology, Rutgers University as IMRU 3962, produces a new
heptaene macrolide antifungal antibiotic, hydroheptin. The producing microorganism, which
co-produces the antibiotic, chartreusin, has been identified as a strain of
Streptomyces chartreuris.
Fermentation and bioassay procedures were developed for the production and analysis
of hydroheptin and chartreusin. Isolation and purification procedures based on solvent
extraction and precipitation of an organic acid yielded a relatively pure product of hydroheptin.
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II. CHEMICAL AND BIOLOGICAL PROPERTIES
J. B. TUNAC, L. E. MCDANIEL, M. PATEL, C. P. SCHAFFNER
1979 Volume 32 Issue 12 Pages
1230-1238
Published: 1979
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Hydroheptin, a new polyene macrolide antifungal antibiotic, is co-produced with the
antibiotic, chartreusin, by a strain of
Streptomyces chartreusis designated as IMRU 3962
isolated in our laboratory. The unique water-solubility of this antibiotic at neutrality, revealing
in aqueous solution molecular dispersion and an ultraviolet-visible absorption spectrum
characteristic of an all-
trans heptaene chromophore, clearly distinguishes it from all previouslydescribed
and naturally-occurring heptaene macrolides. The isolation and identification of
the amino sugar, mycosamine (3-amino-3, 6-dideoxy-D-mannose), in acid hydrolysates of
hydroheptin and the absence of an aromatic amine upon retrograde alkaline dealdolization
of the molecule certainly characterize the antibiotic as a member of the non-aromatic heptaene
macrolide group. Chromatographic and countercurrent distribution studies likewise support
its novelty. With little or no demonstrable activity against bacteria, hydroheptin as compared
to other non-aromatic heptaene macrolides exhibits excellent but somewhat less activity
against a wide variety of yeasts and fungi. Likewise, its parenteral toxicity appears to be less
than that of other heptaene macrolides.
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S. J. BOX, J. D. HOOD, S. R. SPEAR
1979 Volume 32 Issue 12 Pages
1239-1247
Published: 1979
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Four β-lactam antibiotics with β-lactamase inhibitory activity MM 22380, MM 22381,
MM 22382 and MM 22383 containing the carbapenem nucleus have been isolated from a
culture of
Streptomyces olivaceus ATCC 31365. Fermentation conditions for their production
and methods for their isolation are described. Evidence for a biosynthetic link between these
compounds and the previously described olivanic acid derivatives MM 4550, MM 13902 and
MM 17880 is presented.
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IBRAHIM R. SHIMI, SAFWAT SHOUKRY, FAHMY T. ALI
1979 Volume 32 Issue 12 Pages
1248-1255
Published: 1979
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Staphcoccomycin (SCM) is a new member of the basic macrolide family of antibiotics which was isolated from the fermentation broth of
Streptomyces sp. AS-NG-16. The production, purification and determination of physical and chemical properties of this novel metabolite have been completed. Comparison of the mass fragmentation patterns of SCM and its peracetate with those of angolamycin peracetate suggested a des-mycarosyl derivative of angolamycin. Moreover, the molecular ion peak (
m/e 771) corresponded to C
39H
65NO
14and the
1H-NMR of SCM was also consistent with the proposed structure.
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ISOLATION OF EMODIN, ENDOCROCIN AND SECALONIC ACIDS FROM PYRENOCHAETA TERRESTRIS AND ASPERGILLUS ACULEATUS
ITSUO KUROBANE, LEO C. VINING, A. GAVIN MCINNES
1979 Volume 32 Issue 12 Pages
1256-1266
Published: 1979
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Cynodontin, emodin, endocrocin and secalonic acids A, E and G have been isolated from five strains of
Pyrenochaeta terrestris.
Aspergillus aculeatus produces emodin, endocrocin and secalonic acids B, D and F. No cynodontin was detected. Isolation of emodin in small amounts supports previous evidence that it is an intermediate in secalonic acid biosynthesis. Isolation of cynodontin and endocrocin, which are co-produced with secalonic acids in other organisms, suggests that these compounds are formed by a common branching pathway. A natural isolate of
P. terrestris contained variant strains which produced different relative amounts of secalonic acids A, E and G. From the combinations of secalonic acids produced in organisms so far examined it is concluded that precursor tetrahydroxanthone units are formed in pairs differing in stereo-chemistry only at C-5 or at the
trans-invariant C-6 : C-10a positions. A possible biosynthetic pathway is discussed.
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II. ISOLATION AND IDENTIFICATION OF PROANSAMYCIN B-M1 AND PROTORIFAMYCIN I-M1
ORESTE GHISALBA, PETER TRAXLER, HERMANN FUHRER, WILHELM J. RICHTER
1979 Volume 32 Issue 12 Pages
1267-1272
Published: 1979
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Proansamycin B-M1 and protorifamycin I-M1 were isolated as minor compounds from fermentations of the protorifamycin I producing strain
Nocardia mediterranei F 1/24
1), identified by means of chemical and spectroscopic methods and shown to be degradation products of the hypothetical proansamycin B postulated in part I of this series of papers
1) and of protorifamycin I, respectively.
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TAKAO IIDA, MORIYUKI SATO, ISAO MATSUBARA, YASUKI MORI, KUNIKATSU SHIR ...
1979 Volume 32 Issue 12 Pages
1273-1279
Published: 1979
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Fortimicins C, D, and KE are new aminocyclitol antibiotics produced by a mutant of fortimicin-producing organisms. Their structures have been determined by
1H and
13C NMR and mass spectra and chemical degradations. Fortimicin C is 4-N-hydantoylfortimicin B, fortimicin KE is 6'-demethylfortimicin B, and fortimicin D is 4-N-glycylfortimicin KE. The last two antibiotics have purpurosamine C instead of 6-epi-purpurosamine B.
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TERUO HAYASHI, HIROMICHI SAEKI, NORIKO TAKEDA, EIJI OHKI
1979 Volume 32 Issue 12 Pages
1280-1287
Published: 1979
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Butirosin(
Ia), 5''-amino-5''-deoxy-(
Ic). 3', 4'-dideoxy-(
Ie). and 5''-amino-3', 4', 5''-trideoxybutirosin A (
If) were converted into the corresponding 1'''-deoxo derivatives,
Ib, Id, Ig, and
Ih by borane reduction. In addition, xylostasin (
IIIa) was converted into its 1-N-ethyl derivative (
IIIb) by reductive ethylation. Their antibacterial activities were discussed.
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FRANÇOIS LE GOFFIC, FRÉDÉRIC TANGY, BERNARD MOREA ...
1979 Volume 32 Issue 12 Pages
1288-1292
Published: 1979
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A sample of [
3H] tobrarnycin (5, 000 Ci/Mole) has been synthetized and incubated with
the bacterial ribosome and its subunits. The results obtained show that this antibiotic has
two types of binding sites. The primary one is probably responsible for the inhibition of
protein synthesis whereas the secondary one is probably related to the misreading and reading
tiirough of the messenger RNA.
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ROLAND SÜSSNIUTEIR, AINER HAAG, FRANZ LINGENS
1979 Volume 32 Issue 12 Pages
1293-1302
Published: 1979
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The chloramphenicol resistance of some flavobacteria was investigated comparatively.
This resistance can be explained either by acetylation of chloramphenicol to
O-acetylchloramphenicol
via constitutively formed acetyltransferases, followed by cometabolic degradation
(strain CB 60), or by limited uptake and total degradation (strain CB 6) by inducible
enzymes or by other mechanisms (
F. devorans). The mechanisms of resistance, CM-acetylation,
CM-degradation and limited uptake are discussed.
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Y. SAWADA, N. A. HUNT, A. L. DEMAIN
1979 Volume 32 Issue 12 Pages
1303-1310
Published: 1979
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The rate of microbiological ring-expansion of penicillin N to deacetoxycephalosporin C using protoplast lysates of the antibiotic-negative mutant
Cephalosporium acremonium M-0198 has been increased some 70-fold over that of our earlier system. We confirmed the stimulatory effects of FeSO
4 and ascorbate described by HOOK
et al. (Biochem. Biophys. Res. Commun. 87: 258, 1979); the optimum concentrations found were 0.04 mM FeSO
4 and 0.67 mM ascorbate. Adenosine triphosphate concentration was lowered to 0.83 mM; phosphoenolpyruvate and pyruvate kinase were eliminated. The optimum pH and temperature for the reaction were 7.2 and 25°C, respectively. α-Ketoglutarate and MnCl
2 showed no marked effect on the reaction, MgSO
4 and KCl were mildly stimulatory, and CUSO
4 and ZnSO
4 were very inhibitory. Penicillin N was optimal at a concentration of 0.07 mM. Specific ring-expansion activity reached its peak 13 hours after growth ceased and then disappeared rapidly.
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CEPHALOSPORIN DERIVATIVES IN THE NAPHTHALENE SERIES CHEMICAL AND MICROBIOLOGICAL PROPERTIES
E. QUARESIMA, M. O. TINTI, P. FORESTA, P. DE WITT, M. T. RAMACCI
1979 Volume 32 Issue 12 Pages
1311-1318
Published: 1979
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A series of new 7-acylamidocephalosporins, containing a substituted naphthalene moiety
in the side chain, has been prepared and tested for their
in vitro antibacterial activity. Some
observations are made on the structure-activity relationships.
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MINORU NISHIDA, TOSHIAKI KAMIMURA, NAOHIKO OKADA, YOSHIMI MATSUMOTO, Y ...
1979 Volume 32 Issue 12 Pages
1319-1327
Published: 1979
Released on J-STAGE: April 12, 2006
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FK 749 is a distinctive new parenteral cephalosporin antibiotic with a broad antibacterial spectrum which is more potently active against a wide variety of Gram-negative bacilli, including the opportunistic pathogens such as
Citrobacter and
Enterobacter species and
Serratia marcescens, than SCE 963, T 1551 and cefmetazole. The activity of FK 749 against Escherichia coli, Klebsiella pneumoniae, indole-positive and -negative Proteus species, Haemophilus influenzae and Streptococcus pyogenes was by far superior to that of the three other antibiotics. These test organisms were not resistant to FK 749. The antibacterial activity of FK 749 against Pseudomonas aeruginosa was almost the same as that of ticarcillin but was inferior to that of gentamicin and T 1551. The bactericidal activity of FK 749 against E. coli, K. pneumoniae and Proteus mirabilis was more potent than that of the three other antibiotics. FK 749, like cefmetazole, was extremely stable to &-lactaniases. In studies in mice, the therapeutic effect of subcutaneous injection of FK 749 against various infections due to Gram-negative bacilli was by far superior to that of SCE 963, T 1551 and cefmetazole, was almost the same as that of SCE 963 and cefmetazole against Staphylococcus aureus infection and that of ticarcillin against P. aeruginosa infection.
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HIROSHI OGAWARA, SUSUMU HORIKAWA
1979 Volume 32 Issue 12 Pages
1328-1335
Published: 1979
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A β-lactamase from culture supernatant of
Streptomyces celluldosae was purified about 1, 450-fold to apparent homogeneity in polyacrylamide gel electrophoresis and isoelectric focusing on polyacrylamide gel sheet. The methods used were ammonium sulfate precipitation, CM-52 cellulose ion-exchange chromatography and affinity chromatography on Blue Sepharose CL-6B. The molecular weight was determined to be approximately 27, 000 by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. This value was in good agreement with the previous value determined by gel filtration on Sephadex G-75. The isoelectric point was pH 9.5. The enzyme behaved primarily as penicillinase and apparent Km value for benzylpenicillin was 500 μM. The β-lactamase of S. cellulosae interacted strongly with blue dextran
and NADP+-agarose but not with Sepharose. In addition, the presence of NADP+ but not
NAD+ and ATP diminished sharply the intrinsic fluorescence intensity of the enzyme and the apparent association constant was calculated to be 1.4×103M-1. The β-lactamase decrease, its enzymatic activity against benzylpenicillin in the presence of NADP+. From these results, it is suggested that this β-lactamase has a dinucleotide binding fold.
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FUJIO SUZUKI, CHIEKO SUZUKI, EMIKO SHIMOMURA, HIROSHI MAEDA, TOSHIKATS ...
1979 Volume 32 Issue 12 Pages
1336-1345
Published: 1979
Released on J-STAGE: April 12, 2006
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Oral (PO) administration of KS-2 to adult DDI mice resulted in a peak serum interferon (IF) titer of 800 units (U)/ml 20 hours after administration with detectable levels persisting until 30 hours. After intraperitoneal (IP) injection, a peak serum IF titer of 1, 600 U/ml was
detected and it followed the same time course as that of oral administration. The IF induced
by KS-2 shared certain physico-chemical properties with the standard preparation of immune IF and was not neutralized by an antiserum against type I IF. In mice infected intranasally (IN) with influenza A
2 (H
2N
2) virus, KS-2 was found to possess significant protective activities.
Efficacy of the agent was evidenced by an increase in survivor number, a prolongation of mean survival time, an inhibition of the development of lung consolidation induced by the viral infection and a decrease in virus titer in lung tissues. Both PO and IP administrations of KS-2 protected mice against infection and significant antiviral activities were achieved not only by prophylactic but also chemotherapeutic administration. No virocidal or virostatic activities of KS-2 to the influenza virus were found
in vitro. The protective activities of KS-2 against influenza virus infection in mice are discussed in view of the immunopotentiation of the host animals.
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L. DOLAK
1979 Volume 32 Issue 12 Pages
1346-1347
Published: 1979
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TAKAKI HAYAKAWA, NOBORU OTAKE, HIROSHI YONEHARA, TERUO TANAKA, KENJI S ...
1979 Volume 32 Issue 12 Pages
1348-1350
Published: 1979
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TSUTOMU TSUCHIYA, TOMO JIKIHARA, TOSHIAKI MIYAKE, SUMIO UMEZAWA, MASA ...
1979 Volume 32 Issue 12 Pages
1351-1353
Published: 1979
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SHIGEHARU INOUYE, KAZUNORI OHBA, TAKASHI SHOMURA, MICHIO KOJIMA, TAKAS ...
1979 Volume 32 Issue 12 Pages
1354-1356
Published: 1979
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DAISHIRO IKEDA, TSUYOSHI MIYASAKA, KENZABURO YOSHIDA, KATSUHARU IINUMA ...
1979 Volume 32 Issue 12 Pages
1357-1359
Published: 1979
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HAMAO UMEZAWA, DAISHIRO IKEDA, TSUYOSHI MIYASAKA, SHINICHI KONDO
1979 Volume 32 Issue 12 Pages
1360-1364
Published: 1979
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DAISHIRO IKEDA, TSUYOSHI MIYASAKA, MAKOTO YOSHIDA, YUKIO HORIUCHI, SHI ...
1979 Volume 32 Issue 12 Pages
1365-1366
Published: 1979
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KYOKO MATSUYAMA, YOKO TAKAHASHI, MARIKO YAMASHITA, ATSUSHI HIRANO, SAT ...
1979 Volume 32 Issue 12 Pages
1367-1369
Published: 1979
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SUMIO UMEZAWA, KUNIAKI TATSUTA
1979 Volume 32 Issue 12 Pages
1371-1372
Published: 1979
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