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WEN-CHIN LIU, DOROTHY SMITH SLUSARCHYK, GAIL ASTLE, WILLIAM H. TREJO, ...
1978 Volume 31 Issue 9 Pages
815-819
Published: 1978
Released on J-STAGE: April 12, 2006
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Ionomycin, a new polyether antibiotic with a high affinity for calcium ions, is obtained in pure form from fermentation broths of
Streptomyces conglobatus sp. nov. TREJO by solvent extraction. It is unique amongst known polyether antibiotics in that it has a UV absorption maximum at 300 nm, thereby distinguishing it from other antibiotics of its class. The Ca salt has the molecular formula C
41H
70O
9Ca. Ionomycin is a narrow spectrum antibiotic being active against Gram-positive bacteria.
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CAMILLA KELLER-JUSLÉN, HAMILTON D. KING, MAX KUHN, HANS-RUDOLF ...
1978 Volume 31 Issue 9 Pages
820-828
Published: 1978
Released on J-STAGE: April 12, 2006
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Noboritomycins A and B, two new polycyclic ionophoric polyethers were isolated from a strain of
Streptomyces noboritoensis. The crystal structure and absolute configuration of noboritomycin A were established by X-ray analysis of its silver salt C
43H
63O
14Ag. Noboritomycin A is the first metabolic polyether possessing two carboxylic acid functions on the carbon backbone (C-31), namely a free acid and an additional carboxylic acid ethylester group. An unusual spiroketal system as well as a salicylic acid chromophore represent further remarkable elements. Noboritomycin A shows in this respect a structural relationship to salinomycin and lasalocid respectively. Comparison of physico-chemical data, in particular the interpretation of the
1H- and
13C-NMR spectra, revealed that noboritomycins A and B are structurally closely related, noboritomycin B carrying an ethyl substituent on the aromatic ring in the place of a methyl group present in noboritomycin A. Both metabolites exhibit activity against Gram-positive bacteria and against
Eimeria tenella (chicken coccidiosis).
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I. PRODUCING ORGANISM, FERMENTATION AND ISOLATION
MAMORU ARAI, YASUHIRO ITOH, RYUZO ENOKITA, YASUYUKI TAKAMATSU, TAICHI ...
1978 Volume 31 Issue 9 Pages
829-833
Published: 1978
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New antibiotics, enaminomycins A, B and C, were found in the culture broth of streptomycete strain No. 13120, which was identified as
Streptomyces baarnensis and designated as
S. baarnensis No. 13120. Fermentation of enaminomycins were performed by conventional submerged culture in a 30-liter jar fermentor. Isolation of the antibiotics was performed by centrifugation of the culture broth and adsorption of the antibiotics from the supernatant on a column of activated carbon, followed by elution with aqueous acetone. Enaminomycins A, B and C were separated from each other on a column of Sephadex LH-20.
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II. PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
YASUHIRO ITOH, TOMOKO MIURA, TOSHIAKI KATAYAMA, TATSUO HANEISHI, MAMOR ...
1978 Volume 31 Issue 9 Pages
834-837
Published: 1978
Released on J-STAGE: April 12, 2006
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Physico-chemical characterization of enaminomycins revealed that these antibiotics are new members of the epoxy quinone family. From elementary analysis and mass spectroscopic measurements the molecular formulae of enaminomycins A, B and C appear to be C
7H
5NO
5, C
10H
11NO
6 and C
7H
7NO
5, respectively. They are very unique in their chemical properties, possessing various functions, such as epoxy, primary amine and carboxylic acid, in their small structural units.
Enaminomycin A, the most potent component, has activity against Gram-positive and Gram-negative bacteria and shows cytostatic effect on L1210 mouse leukemia cells
in vitro, but enaminomycins B and C are only weakly active against Gram-positive and Gram-negative bacteria.
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III. THE STRUCTURES OF ENAMINOMYCINS A, B AND C
YASUHIRO ITOH, TATSUO HANEISHI, MAMORU ARAI, TADASHI HATA, KIMIE AIBA, ...
1978 Volume 31 Issue 9 Pages
838-846
Published: 1978
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The structures of enaminomycins A and B were determined by their physico-chemical properties and X-ray crystallographic analyses to be 4-amino-2, 5-dioxo-7-oxa-bicyclo[4, 1, 0]-hept-3-ene-3-carboxylic acid and 2-oxo-4-amino-5-hydroxy-5-acetonyl-7-oxa-bicyclo[4, 1, 0]-hept-3-ene-3-carboxylic acid, respectively. The structure of enaminomycin C was also determined by the analysis of NMR spectrum and other physico-chemical properties to be 2-oxo-4-amino-5-hydroxy-7-oxa-bicyclo[4, 1, 0]hept-3-ene-3-carboxylic acid.
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HIROSHI FUKUMI, FUMIO MARUYAMA, KAYOKO YOSHIDA, MAMORU ARAI, AKINORI K ...
1978 Volume 31 Issue 9 Pages
847-849
Published: 1978
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A procedure is described for the large-scale production of mimosamycin, a satellite antibiotic found in the culture filtrate of
Streptomyces lavendulae No. 314. The
1H and
13C NMR, and mass spectroscopic data, are explained in terms of the structure of mimosamycin.
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M. PODOJIL, Z. VANEK, V. PRIKRYLOVÁ, M. BLUMAUEROVÁ
1978 Volume 31 Issue 9 Pages
850-854
Published: 1978
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From a mixture of substances formed by producing strains of
Streptomyces aureofaciens under conditions of submerged fermentation a new metabolite, ekatetrone, was isolated. Its isolation and basic physical and chemical data are described. Ekatetrone is a quinone derivative with a carboxamide group. In tests
in vitro with cells of EHRLICH's ascites tumour evidence was provided that ekatetrone inhibits proteo- and nucleosynthesis.
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VERA PRIKRYLOVÁ, MILOSLAV PODOJIL, PETR SEDMERA, JINDRICH VOKOU ...
1978 Volume 31 Issue 9 Pages
855-862
Published: 1978
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The structure of ekatetrone has been determined from physico-chemical data obtained using the natural compound, its derivatives and products of degradation reactions. Ekatetrone was found to be the lactone of 1, 8-dihydroxy-2-(1'-hydroxy-2'-carbamoyl)ethyl-9, 10-anthraquinone-3-acetic acid (
I). It is proposed that ekatetrone is related, biogenetically, to protetrone.
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ISAMU WATANABE, TSUTOMU TSUCHIYA, FUJIO NAKAMURA, MASA HAMADA, SUMIO U ...
1978 Volume 31 Issue 9 Pages
863-867
Published: 1978
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The titled compound was prepared by condensation of 3'-deoxyparomamine derivative (
5) with 2, 3-
O-bis(
p-nitrobenzoyl)-5-
O-tosyl-D-xylofuranosyl bromide followed by 1-
N-acylation with the active ester of (
S)-4-benzyloxycarbonylamino-2-hydroxybutyric acid.
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D. J. FLOURNOY
1978 Volume 31 Issue 9 Pages
868-871
Published: 1978
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Ten clinical isolates of
Serratia marcescens were tested on MUELLER-HINTON agar containing gentamicin or netilmicin with carbenicillin. The isolates grew on plates where inactivation occurred, at higher antibiotic concentrations, but failed at lower concentrations. This growth response was individualistic and not closely related to the minimum inhibitory concentrations.
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SUMIO UMEZAWA, SHIGEAKI SATO, TAKASHI SUGIMURA
1978 Volume 31 Issue 9 Pages
872-874
Published: 1978
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Pepstatin, an acid protease inhibitor purified from the culture medium of
Actinomycetes, had a strong diuretic effect in C3H/He mice. A single subcutaneous injection of pepstatin at 80 mg/kg body weight caused 3- to 4-fold increase in the urine volume over that of control mice during the first 24 hours after the injection and 6- to 7-fold increase during the second and third 24-hour periods. The effect was maximal after 72-96 hours, and gradually disappeared within 168 hours after the injection. The serum potassium concentration increased to 7.6 mEq/liter at 24 hours after the injection but the serum sodium concentration did not change significantly. This change in electrolytes disappeared within 168 hours after the injection. The soluble derivative of pepstatin, lactyl-pepstatin, which has a higher ID50 than pepstatin for renin, had no significant diuretic effect at the same molar dose. From these findings the strong diuretic effect of pepstatin is concluded to be due to inhibition of rennin-mediated conversion of angiotensinogen to angiotensin I, which in turn is normally converted to angiotensin II, resulting in release of aldosterone.
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HIDEO SUZUKI, TOSHIO NISHIMURA, KEIKO MUTO, NOBUO TANAKA
1978 Volume 31 Issue 9 Pages
875-883
Published: 1978
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The effects of macromomycin (MCR), a high molecular weight peptide antibiotic, on cell division, DNA synthesis and DNA fragmentation were examined in cultured mammalian tumor cells. When MCR was added to HeLa cell culture simultaneoussly with [
3H]thymidine, inhibition of DNA synthesis was observed depending on the amount of the drug present, although the inhibition was partial even at a high concentration of the drug. Preincubationof cells with MCR for 2 hours before assay was required for the complete inhibition of DNA synthesis. Cell division of synchronized L5178Y cells, arrested at metaphase, was strongly inhibited by MCR, indicating that the inhibition of cell mitosis by the drug was not dependent on the inhibition of DNA synthesis.
Strand scission of DNA in MCR-treated cells was observed by alkaline sucrose gradient centrifugation. The fragmentation of cellular DNA occurred at low concentration of the drug and within a very short incubation time (37°C, 5 minutes). At high concentrations of the drug, however, the size of the fragmented DNA remained constant. DNA polymerase activity in isolated nuclei from HeLa and L5178Y cells was stimulated by MCR. These data suggest that MCR works directly on cell nuclei and strand scission of DNA is one of the more important actions of the drug.
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KEN TAKEDA, SETSUKO KAWAI, FUMIO KATO, TSUNAO TETSUKA, KUNIO KONNO
1978 Volume 31 Issue 9 Pages
884-887
Published: 1978
Released on J-STAGE: April 12, 2006
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The activity of purified prolyl hydroxylase (proline, 2-oxoglutarate dioxygenase, EC 1. 14. 11. 2) was enhanced 3-8-fold at a low concentration of ferrous ion (1×10
-5 M) by addition of bleomycin, a glycopeptide antibiotic with antineoplastic activity and a side effect of producing pulmonary fibrosis. The maximum stimulation was attained at a concentration of 15 μg/ml bleomycin (about 1×10
-5 M), which was approximately equimolar with the ferrous ion, one of the cofactors of this enzyme. Addition of bleomycin to the assay mixture resulted in a change of the optimal concentration of ferrous ion from 2 ×10
-3 M to 1×10
-5 M. Changing the order of addition of ferrous ion, enzyme and bleomycin in assay medium before
incubation at 37°C, the stimulatory activity was varied. Bleomycin A
2-Cu
++(Cu
++-chelated bleomycin), which scarcely complexed with Fe
++, had no enhancing effects on the enzymatic activity. We discuss the possible reasons as to why the activity of prolyl hydroxylase was enhanced by addition of bleomycin in the assay mixture.
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THE IONOPHORE-MEDIATED CALCIUM TRANSPORT AND CONCOMITANT OSMOTIC SWELLING OF MITOCHONDRIA
MITSUAKI MITANI, NOBORU OTAKE
1978 Volume 31 Issue 9 Pages
888-893
Published: 1978
Released on J-STAGE: April 12, 2006
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The effects of various carboxylic ionophores on divalent metal cation translocation in mitochondria have been investigated. High levels of divalent cation ionophores lysocellin and lasalocid A (10-50 μM) produced mitochondrial osmotic swelling in Ca
2+ or Mg
2+ medium, which was associated with an increase of cation influx. The extent of swelling was a function of both the ionophore and cation concentrations in the medium. This effect was larger in mitochondria de-energized by treatment with antimycin A and oligomycin than in respiring mitochondria. On the other hand, the monovalent cation ionophores carriomycin and etheromycin at concentrations of 50- 100 μM also induced mitochondrial swelling in Ca
2+ medium but were ineffective in Mg
2+ medium. Addition of ruthenium red reversed divalent cation ionophore-induced swelling and released Ca
2+ from preloaded mitochondria. In contrast, ruthenium red increased monovalent cation ionophore-induced swelling. In a divalent cation-free medium, lysocellin and lasalocid A caused depletion of membrane-bound Ca
2+ and released endogenous Ca
2+ and Mg
2+ from mitochondria, while carriomycin and etheromycin exerted only a limited effect. These results indicate that the divalent cation ionophores affect divalent cation distribution in mitochondria by increasing both influx and efflux of the cations through the inner membrane.
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ALESSANDRO ASSANDRI, TITO CRISTINA, LUIGI MORO
1978 Volume 31 Issue 9 Pages
894-901
Published: 1978
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The disposition of four C
3-substituted piperazinyl rifamycins was studied in the rat following the intravenous administration of 5 mg/kg of the
14C-labelled antibiotics. Considerable quantitative differences in the pharmacokinetics of these antibiotics were shown in blood levels, tissue distributions and body clearances. Feces were largely the major route of elimination for the parent drug and metabolites. The results suggest that the liver compartimentalization, regulating the biliary excretion, is to be the kinetic parameter affecting the pharmacokinetic behaviour of this class of antibiotics.
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A. CIHÁK, L. KORBOVÁ, J. KOHOUT
1978 Volume 31 Issue 9 Pages
902-905
Published: 1978
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Cycloheximide and streptovitacin A administered
in vivo to rats display a similar dual effect on the labelling of soluble liver proteins by valine-
14C, and result in a similar enhancement of liver uridine kinase activity. On the other hand, in pylorus-ligated rats, both antibiotics markedly depress gastric secretion, acid output, and the level of mucoproteins and proteolytic activity in secreted juice. Streptovitacin A on a molar basis was in all cases 5-8 times more effective than cycloheximide.
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NILS MILMAN, JORGEN DAHLAGER
1978 Volume 31 Issue 9 Pages
906-910
Published: 1978
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The
in vitro effects of polymyxin antibiotics on
o-
125I-hippurate (OIH) accumulation in rabbit renal cortical slices were studied using incubation media with pH ranging from 6.9 to 7.9 and containing polymyxin B sulfate, colistin sulfate, sodium colistimethate and antibacterially inactive N-succinyl colistin in concentrations ranging from 1 to 2, 000μg base/ml. Polymyxin B, colistin and colistimethate depressed OIH accumulation significantly in Concentrations≥300μg/ml. The effects on accumulation were clearly pH-dependent and most pronounced at alkaline pH. N-Succinyl colistin had only a marginal influence on accumulation, even in high concentrations. Colistimethate produced a significantly smaller decrease in accumulation at all pH values than both polymyxin B and colistin. The results suggest that the presence of free amino groups is necessary to obtain a decrease in accumulation and correlate with the known
in vivo nephrotoxicity of these antibiotics.
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M. A. HANNAN, LAURENCE H. HURLEY
1978 Volume 31 Issue 9 Pages
911-913
Published: 1978
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VWILLIAM V. CURRAN, JAMES H. BOOTHE
1978 Volume 31 Issue 9 Pages
914-918
Published: 1978
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IWAO KITAMURA, TOSHIKAZU OKI, TAIJI INUI
1978 Volume 31 Issue 9 Pages
919-922
Published: 1978
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HIROSHI OGAWARA, TAKEHITO MINAGAWA, HIROKO NISHIZAKI
1978 Volume 31 Issue 9 Pages
923-925
Published: 1978
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HARUO SETO, MARIKO SHIBAMIYA, HIROSHI YONEHARA
1978 Volume 31 Issue 9 Pages
926-928
Published: 1978
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HARUO SETO, KAZUTOSHI MIZOUE, NOBORU OTAKE, MICHIO YAMAGISHI, TAKU MIZ ...
1978 Volume 31 Issue 9 Pages
929-932
Published: 1978
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TSUTOMU TSUCHIYA, ISAMU WATANABE, FUJIO NAKAMURA, MASA HAMADA, SUMIO U ...
1978 Volume 31 Issue 9 Pages
933-935
Published: 1978
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YUKIHIKO KAMEDA, NAOKI ASANO, TADASHI HASHIMOTO
1978 Volume 31 Issue 9 Pages
936-938
Published: 1978
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