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JAMES L. MERTZ, JAMES S. PELOSO, BILL J. BARKER, GEORGE E. BABBITT, JO ...
1986 Volume 39 Issue 7 Pages
877-887
Published: 1986
Released on J-STAGE: April 19, 2006
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Avilamycin is an antibiotic complex produced by cultures of the organism
Streptomyces viridochromogenes, strain NRRL 2860. These compounds belong to the orthosomycin family of antibiotics. Structural composition of the major avilamycins and several minor avilamycins are known. Nine additional minor avilamycins, designated F through N, have been isolated
via semi-preparative silica gel or reverse-phase high performance liquid chromatography with final purification using a reverse-phase column loading solvent switching technique.
1H NMR and mass spectroscopy, negative ion fast atom bombardment (neg FAB) and electron impact, were used to structurally identify the avilamycins. All of the compounds were microbiologically
active and similar in structure to other known avilamycins.
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NONGNUCH VANITTANAKOM, WOLFGANG LOEFFLER, ULRIKE KOCH, GÜNTHER JU ...
1986 Volume 39 Issue 7 Pages
888-901
Published: 1986
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Fengycin is an antifungal lipopeptide complex produced by
Bacillus subtilis strain F-29-3. It inhibits filamentous fungi but is ineffective against yeast and bacteria. The inhibition is antagonized by sterols, phospholipids and oleic acid, whereas two other unsaturated fatty acids increase the antifungal effect. Fengycin consists of two main components differing by one amino acid exchange. Fengycin A is composed of 1 D-Ala, 1 L-Ile, 1 L-Pro, 1 D-allo-Thr, 3 L-Glx, 1 D-Tyr, 1 L-Tyr, 1 D-Orn, whereas in fengycin B the D-Ala is replaced by D-Val. The lipid moiety of both analogs is more variable, as fatty acids have been identified as
anteiso-pentadecanoic acid (
ai-C
15),
iso-hexadecanoic acid (
i-C
16 ),
n-hexadecanoic acid (
n-C
16), and there is evidence for further saturated and unsaturated residues up to C
18.
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AKIHIRO YOSHIMOTO, SHIZUKA FUJII, OSAMU JOHDO, KATSURO KUBO, TOMOYUKI ...
1986 Volume 39 Issue 7 Pages
902-909
Published: 1986
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A new potent anthracycline antibiotic oxaunomycin was isolated from the culture broth of a blocked mutant derived from a baumycin producer and was identified as 7-
O-(α-L-daunosaminyl)-β-rhodomycinone. It exhibited about 100 times more strongly cytotoxic activity against leukemic L1210 cell culture than doxorubicin.
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GYULA BATTA, FERENC SZTARICSKAI, JÁNOS CSANÁADI, ISTV&Aa ...
1986 Volume 39 Issue 7 Pages
910-913
Published: 1986
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The configuration of the glycosidic linkages and the conformation of the carbohydrate moieties in the molecules of the glycopeptide-type antibiotics actinoidins A and B (1a, 1b) have been determined by means of two-dimensional
13C/
1H correlation NMR technique and with the application of model compounds 2-4.
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A. G. PISABARRO, F. J. CAÑADA, D. VÁZQUEZ, P. ARRIAGA, A ...
1986 Volume 39 Issue 7 Pages
914-921
Published: 1986
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We have studied the modification of
Escherichia coli peptidoglycan induced by bicyclomycin. For this purpose liquid chromatography for peptidoglycan analysis has been used. The main alteration found was an increase of diaminopimelyl-diaminopimelyl bridge containing subunits. Our results show that bicyclomycin impairs the normal breakage of that interpeptidic bond, whose cleavage is needed for the normal remodeling of peptidoglycan
and cell growth. Based on the analysis of the possible structure of diaminopimelyl-diaminopimelyl bond and bicyclomycin, we propose a hypothesis on the mechanism of action of bicyclomycin.
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III. MODIFICATION OF BENZOXAZOLE RING SUBSTITUENTS, IONOPHOROUS PROPERTIES IN AN ORGANIC PHASE
M. PRUDHOMME, G. DAUPHIN, G. IEMINET
1986 Volume 39 Issue 7 Pages
922-933
Published: 1986
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Ten semi-synthetic analogs of A23187 (calcimycin), with only the benzoxazole ring substituents modified together with the ionophore X14885A were studied with regard to their calcium and magnesium carrier properties through an organic phase (toluene-butanol, 70:30). The results indicate that the carboxylic group and the oxazolic nitrogen, maintained in the
ortho position are essential for the ionophorous properties. Further, the introduction
of a substituent in place of the NHCH
3 group, producing steric hindrance of the carboxylic group leads to a destabilization of the 2:1 associations with cations.
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IV. CATION CARRIER PROPERTIES IN MITOCHONDRIA OF ANALOGS WITH MODIFIED BENZOXAZOLE RINGS. ANTIMICROBIAL ACTIVITY
M. PRUDHOMME, J. GUYOT, G. JEMINET
1986 Volume 39 Issue 7 Pages
934-937
Published: 1986
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The transporting abilities in the mitochondrial membrane for Ca
++ and Mg
++ of ten semi-synthetic analogs A23187 (calcimycin) and X14885A are compared. Analogs classified as efficient divalent cation carrier retained the calcimycin antimicrobial activity against three Gram-positive strains tested.
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M. E. GRACE, F. J. GREGORY, P. P. HUNG, K. P. Fu
1986 Volume 39 Issue 7 Pages
938-942
Published: 1986
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A cephalosporin-hydrolyzing enzyme from strains of
Proteus penneri resistant to β-lactam antibiotics was purified and characterized. The enzyme gave a single protein band on SDS-polyacrylamide gel electrophoresis with a molecular weight of 30, 000. This cephalosporinase has an isoelectric point of 6.8, a pH optimum of 6.5 and a temperature optimum of 45°C. The enzyme hydrolyzed cephaloridine, cephalothin, cefuroxime, and cefotaxime more
rapidly than penicillins. The relative rate, with cephaloridine as 100, were: cephalothin, 50; cefuroxime, 93; cefotaxime, 48; ceftriaxone, 23; cefoperazone, 11; benzylpenicillin, 3; ampicillin, 9; and carbenicillin, <1. Cephamycins had low affinities for the enzyme. However, clavulanic acid and sulbactam, with high affinites for the enzyme, were inhibitors of this enzyme.
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TOMIZO NIWA, TAKASHI YOSHIDA, ATSUSHI TAMURA, YUZO KAZUNO, SHIGEHARU I ...
1986 Volume 39 Issue 7 Pages
943-955
Published: 1986
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SF-2103A, a new carbapenem antibiotic, exhibited a broad antibacterial spectrum and a potent inhibitory activity against a wide range of β-lactamases, in particular, against cephalosporinases, with lower I
50 values than those displayed by sulbactam and clavulanic acid. Using a fixed combination and checkerboard titration,
in vitro synergy against the majority of the β-lactamase-producing strains tested was demonstrated between SF-2103A and various β-lactam antibiotics, especially cefotaxime, ceftizoxime, and cefoperazone. The synergistic effect of SF-2103A was more pronounced than that of sulbactam. The
in vitro synergy was also confirmed by bactericidal and bacteriolytic activities and morphological effects.
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TAKASHI YOSHIDA, YUZO KAZUNO, TOMOKO SHOMURA, SHINJIRO MURATA, SHIGEHA ...
1986 Volume 39 Issue 7 Pages
956-965
Published: 1986
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Combinations of SF-2103A with cefotaxime, cefoperazone or cefazolin showed synergistic efficacy at a wide range of combination ratios against experimental infection in mice due to
Proteus vulgaris GN76/C-1, producing type Ic cephalosporinase,
Escherichia coli No. 29/36 RGN823, producing type IIIa (TEM-2) penicillinase and
E. coli GN206, producing type Ib cephalosporinase. These effects by SF-2103A were greater than those seen with sulbactam. The
in vitro and
in vivo synergistic activities were roughly correlated. Potent
in vivo activity of SF-2103A was related to good pharmacokinetic properties, with blood half-life of 30 minutes and urinary recovery of 55.2% after parenteral administration to rats. Furthermore, SF-2103A was stable to rat kidney homogenate. The high stability of SF-2103A in aqueous and biological media was correlated with the sulfonate group at C-3.
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KAZUO EBIHARA, FUMINORI ABE, TAKUMI YAMASHITA, KYOICHI SHIBUYA, EMIKO ...
1986 Volume 39 Issue 7 Pages
966-970
Published: 1986
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The effect of ubenimex on the progression of
N-methyl-
N'-nitro-
N-nitrosoguanidine (MNNG)-induced stomach tumor in rats was studied. Tumor induction was performed by giving MNNG
via drinking water for 34 weeks. Ubenimex was ip administered twice a week at 0.5mg/kg for 84 weeks in one group and 49 weeks in another starting from the first and 36th weeks after initiation of MNNG administration, respectively. The stomachs were endoscopically examined 2 times. At the 64th week after initiation of MNNG administration tumorous lesions were observed with about 70% of the rats in both ubenimex administration groups. In the ubenimex non-administration group nearly 90% of the rats had the lesions. After completion of ubenimex administration almost all the rats had the lesions in the three groups but the sizes were much smaller with the two ubenimex administration groups. Almost all of these lesions were histopathologically identified as tumorous. The tumor volume per rat in the two ubenimex administration groups from the 1 and 36th weeks was 21.0 and 19.2% of the volume in the control group, respectively. Tumor number per rat was similar among the three groups.
The natural killer activity of rats was also examined after completion of the above experiment. The activity markedly increased when ubenimex was administered from the 36th week after initiation of MNNG administration. When ubenimex was administered from the first week, the activity did not increase demonstratively. From all the results described above we conclude that ubenimex exerts an inhibitory action against the progression of MNNG-induced stomach tumor in rats. Contribution of the increase of natural killer activity to ubenimex antitumor action may be dependent on schedule of ubenimex administration.
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N. KLESEL, D. ISERT, M. LIMBERT, G. SEIBERT, I. WINKLER, E. SCHRINNER
1986 Volume 39 Issue 7 Pages
971-977
Published: 1986
Released on J-STAGE: April 19, 2006
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The chemotherapeutic efficacy of cefpirome (HR 810), a new polar aminothiazolylcephalosporin and that of ceftazidime, cefotaxime, cefoperazone, latamoxef and cefodizime were examined against experimental pneumonia caused by
Klebsiella pneumoniae DT-S in mice. When compared in terms of MIC values against the infecting organism and the pharmacokinetic pattern, cefpirome showed equal activity and a similar pharmacokinetic behavior to ceftazidime and cefotaxime in mice. Trials to assess the bactericidial activity
in vivo, however, showed that cefpirome displayed a more marked bactericidal effect in pneumonic mice than the other cephalosporins tested. Only cefodizime, a cephalosporin with extremely high and prolonged blood and tissue levels in experimental animals exerted chemotherapeutic effects similar to cefpirome. After cefpirome or cefodizime medication (50mg/kg), the viable counts in the lungs of experimental animals fell steadily to 1/10, 000 of the pretreatment level and, in contrast to the reference compounds, no regrowth of the challenge organisms could be observed with both drugs. Moreover, with ED
50s ranging from 1.1 to 59.1mg/kg in treatment studies, cefpirome as well as cefodizime were two to ten times more effective than ceftazidime and cefotaxime, whereas cefoperazone and latamoxef were considerably less effective.
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JOYCE I. CIALDELLA, JAMES J. VAVRA, VINCENT P. MARSHALL
1986 Volume 39 Issue 7 Pages
978-984
Published: 1986
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The effects of subinhibitory concentrations of antibiotics on polymorphonuclear leukocyte (PML) and serum killing of
Staphylococcus aureus 502A (UC 9116) and
Escherichia coli UC 9451 were studied. Exposure of these bacteria to subinhibitory levels of certain lincosaminides, spectinomycin, or 6'-
n-propylspectinomycin altered their susceptibility to these host defense mechanisms, while exposure to gentamicin had no effect. However, each organism responded differently to treatment with the antibiotics.
S. aureus pretreated during log phase growth with subinhibitory concentrations of clindamycin, lincomycin, or pirlimycin was more susceptible to killing by PMLs than untreated bacteria. No effect on phagocytic killing was found when
S. aureus was pretreated with spectinomycin, 6'-
n-propylspectinomycin, or gentamicin. The
S. aureus remained resistant to serum lysis despite antibiotic treatment. In contrast, spectinomycin and 6'-
n-propylspectinomycin as well as clindamycin dramatically increased the susceptibility of
E. coli to serum lysis (>99% destroyed). Moderate killing of
E. coli by PMLs was also found.
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AKIO IWASAKI, HIROSHI KISHIDA, MASANORI OKANISHI
1986 Volume 39 Issue 7 Pages
985-993
Published: 1986
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The gene for an extracellular xylanase from
Streptomyces sp. No. 36a was cloned into
Streptomyces lividans TK21 using pIJ702 as a vector plasmid. The smallest DNA fragment encoding the xylanase gene and its possible promotor was determined to be a 1.04kb Sph I-Sac I fragment by sub-cloning studies. This xylanase gene fragment was transferred into the pSK2 series of plasmids and introduced into
Streptomyces kasugaensis G3 protoplasts. The cloned xylanase gene was expressed in both
S. lividans TK21 and
S. kasugaensis G3, and these clones produced and secreted high yields of xylanase into the culture medium. The xylanase production was not detected when a foreign DNA fragment was inserted into the
BclI site locating in the xylanase gene fragment.
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KEI-ICHI NUMATA, HARUAKI YAMAMOTO, MASAMI HATORI, TAKEO MIYAKI, HIROSH ...
1986 Volume 39 Issue 7 Pages
994-1000
Published: 1986
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An aminoglycoside hypersensitive mutant, Kp-126, was isolated from the aminoglycoside-resistant strain, Kp-8, of
Klebsiella pneumoniae through selection using sorbistin, a nonaminocyclitol-aminoglycoside antibiotic. The mutant Kp-126 was approximately 100-fold more sensitive to sorbistin than the parent strain Kp-8. The mutant also showed hypersensitivityto various aminocyclitol-aminoglycoside antibiotics.
K. pneumoniae Kp-126 was used in screening and a new aminoglycoside antibiotic, 3, 3'-neotrehalosadiamine (BMY-28251), was discovered in the fermentation broths of soil isolate strain of
Bacillus pumilus.
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TAKASHI TSUNO, CHIHARU IKEDA, KEI-ICHI NUMATA, KOJI TOMITA, MASATAKA K ...
1986 Volume 39 Issue 7 Pages
1001-1003
Published: 1986
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LEONE DALL'ASTA, ANDREA COMINI, EUGENIO GAREGNANI, DARIO ALBERTI, GERM ...
1986 Volume 39 Issue 7 Pages
1004-1006
Published: 1986
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A. L. DEMAIN, Y.-Q. SHEN, S. E. JENSEN, D. W. S. WESTLAKE, S. WOLFE
1986 Volume 39 Issue 7 Pages
1007-1010
Published: 1986
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JUN'ICHI SHOJI, TOSHIYUKI KATO, HIROSHI HINOO, TERUO HATTORI, KEIICHIR ...
1986 Volume 39 Issue 7 Pages
1011-1012
Published: 1986
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KUNIO ISSHIKI, TSUTOMU SAWA, KEIKO MIURA, BINGSHENG LI, HIROSHI NAGANA ...
1986 Volume 39 Issue 7 Pages
1013-1015
Published: 1986
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HIROSHI NAKAYAMA, TOSHIAKI HANAMURA, YUICHI ABE, AKIRA SHIMAZU, KEIKO ...
1986 Volume 39 Issue 7 Pages
1016-1020
Published: 1986
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TSUTOMU TSUCHIYA, SHUICHI SAKAMOTO, NORIO KAJIKAWA, SUMIO UMEZAWA, MAS ...
1986 Volume 39 Issue 7 Pages
1021-1024
Published: 1986
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ANDRZEJ CZERWINSKI, JOLANTA GRZYBOWSKA, EDWARD BOROWSKI
1986 Volume 39 Issue 7 Pages
1025-1027
Published: 1986
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F. SÁNCHEZ, G. JIMÉNEZ, A. AGUILAR, F. BAQUERO, V. RUBIO
1986 Volume 39 Issue 7 Pages
1028-1030
Published: 1986
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J. DAVIES
1986 Volume 39 Issue 7 Pages
1031-1032
Published: 1986
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