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FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES
M. A. GOETZ, M. LOPEZ, R. L. MONAGHAN, R. S. L. CHANG, V. J. LOTTI, T. ...
1985 Volume 38 Issue 12 Pages
1633-1637
Published: 1985
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The fermentation and isolation of a new, non-peptide cholecystokinin antagonist, asperlicin, produced by
Aspergillus alliaceus is described. The potent and specific interaction of asperlicin with cholecystokinin receptors was shown using
in vitro biochemical assays.
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STRUCTURE ELUCIDATION
JERROLD M. LIESCH, OTTO D. HENSENS, JAMES P. SPRINGER, RAYMOND S. L. C ...
1985 Volume 38 Issue 12 Pages
1638-1641
Published: 1985
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Asperlicin (1, C
31H
29N
5O
4) is a novel cholecystokinin antagonist produced by
Aspergillus alliaceus. The structure of asperlicin has been determined by NMR and mass spectral analysis, and X-ray crystallography.
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DWARD MEYERS, RAYMOND COOPER, LORETTA DEAN, JANICE H. JOHNSON, DOROTHY ...
1985 Volume 38 Issue 12 Pages
1642-1648
Published: 1985
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Two novel antibiotics, catacandin A and catacandin B, were isolated from the fermentation broth of the bacterium,
Lysobacter gummosus, by extraction and adsorption, reverse-phase and gel filtration chromatography. On the basis of their physico-chemical properties, they are acyltetramic acids that are easily distinguishable from others in this class. Catacandin A and catacandin B possess good anticandidal activity.
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BRIGITTE KUNZE, WERNER KOHL, GERHARD HOFLE, HANS REICHENBACH
1985 Volume 38 Issue 12 Pages
1649-1654
Published: 1985
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Angiolam A, a new lactone-lactam antibiotic, was isolated from the culture broth of the myxobacterium
Angiococcus disciformis strain An d30. It was active against a few Gram-positive bacteria and mutant strains of
Escherichia coli with increased permeability. It appears to interfere with protein synthesis.
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PRODUCTION, STRUCTURAL DETERMINATION AND BIOLOGICAL ACTIVITIES
LUCIEN DAVID, HUMBERTO LEAL AYALA, JEAN-CLAUDE TABET
1985 Volume 38 Issue 12 Pages
1655-1663
Published: 1985
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A new polyether antibiotic, abierixin, was found in the mycelium of a culture broth of nigericin-producing
Streptomyces albus NRRL B-1865. Abierixin was extracted with organic solvents and purified by column chromatography and HPLC. The structure of abierixin was determined by FAB/MS/MS and CI/MS/MS and
1H and
13C NMR spectrometries. Abierixin exhibited weak antimicrobial and ionophorous activities, low toxicity but good anticoccidial activity. Nigericin biosynthesis from abierixin is discussed.
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TSUYOSHI TAMAMURA, TSUTOMU SAWA, KUNIO ISSHIKI, TORU MASUDA, YOSHIKO H ...
1985 Volume 38 Issue 12 Pages
1664-1669
Published: 1985
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A new antitumor antibiotic, terpentecin was isolated from the culture broth of strain MF730-N6. Strain MF730-N6, isolated from soil, was found to belong to the genus
Kitasatosporia. The antibiotic was extracted with chloroform, purified by column chromatography using silica gel and Diaion HP-20 successively, and finally purified by high performance reverse-phase thin layer chromatography. The molecular formula of terpentecin was determined to be C
20H
28O
6 (molecular weight, 364). The antibiotic inhibited the growth of Gram-positive and Gram-negative bacteria, and prolonged the survival period of mice bearing leukemia L-1210, P388 and Ehrlich ascites carcinoma.
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TAXONOMY OF PRODUCING ORGANISM, ISOLATION, CHARACTERIZATION AND BIOLOGICAL ACTIVITIES
YUTAKA KIKUCHI, MITSURU NIWANO, NOBUHIRO YAJIMA, GOTO NAKAMURA, NOBUO ...
1985 Volume 38 Issue 12 Pages
1670-1676
Published: 1985
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A novel macromolecular antibiotic SN-07 was obtained from the cultural supernatant of
Actinomadura roseoviolacea var.
miuraeusis nov. var. The antibiotic was soluble in water, had a molecular weight of 18, 000-22, 000 daltons in 50mM Tris-HCl buffer, pH 7.0, containing 2.0 M KCl as compared with authentic proteins. Its major constituents were nucleic acids. The substance had antibacterial activity against Gram-positive bacteria. It was also effective against lymphocytic leukemia P388
in vivo.
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SHINJI FUNAYAMA, KENJI OKADA, KAZUYO IWASAKI, KANKI KOMIYAMA, IWAO UME ...
1985 Volume 38 Issue 12 Pages
1677-1683
Published: 1985
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The structures of novel antibiotics, trienomycins A, B and C produced by
Streptamyces sp. No. 83-16, have been determined on the basis of their spectroscopical and chemical properties. Trienomycins are unique ansamycin antibiotics with a triene and an 1, 3, 5-trisubstituted benzene moieties in the molecule. The antibiotics possess potent cytocidal activity against HeLa S
3 cells at concentrations of 0.005 (trienomycin A), 0.1 (trienomycin C) and 0.2μg/ml (trienomycin B) (IC
50 value), respectively. However, trienomycins showed no antimicrobial activity against the bacteria, fungi and yeasts examined with the exception of weak activity versus
Piricularia oryzae at a concentration of 1, 000μg/ml.
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SPECTROSCOPIC CHARACTERIZATION AND X-RAY ANALYSIS OF A BROMO DERIVATIVE
HERMANN UHR, AXEL ZEECK, WILLIAM CLEGG, ERNST EGERT, HERMANN FUHRER, H ...
1985 Volume 38 Issue 12 Pages
1684-1690
Published: 1985
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Acetomycin (
1a), known since 1958, has been further characterized by NMR and CD spectra. The β-acetyl side chain of
1a is reduced selectively by sodium cyanoborohydride yielding the diastereomeric alcohols
2a and
3a, which were esterified to the crystalline bromoacetates
2c and
3c. The structure and absolute configuration of
3c was determined by X-ray analysis. From these data the absolute configuration of
1a followed as 3
S, 4
S, 5
R.
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RAY S. DEWEY, BYRON H. ARISON, JOHN HANNAH, DAVID H. SHIH, GEORG ALBER ...
1985 Volume 38 Issue 12 Pages
1691-1698
Published: 1985
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The antibiotic efrotomycin (
I), C
59H
88N
2O
20, was isolated from cultures of
Nocardia lactamdurans as an amorphous yellow powder. Mass spectral and NMR analyses show that the compound is a glycoside of the known antibiotic aurodox (
II), C
44H
62N
2O
12. Ozonolysis and hydrolysis of
I produced the disaccharide V, 6-deoxy-4-
O-(6-deoxy-2, 4-di-
O-methyl-α-L-mannopyranosyl)-3-
O-methyl-β-D-allopyranose. This disaccharide is attached to the 4-hydroxyl group of the hexahydropyran substructure of aurodox
via a β-linkage to C-1 of the allose.
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A. ASZALOS, A. BAX, N. BURLINSON, P. ROLLER, C. MCNEAL
1985 Volume 38 Issue 12 Pages
1699-1713
Published: 1985
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Two polyene antibiotics, nystatin and amphotericin A, were compared by physicochemical and microbiological methods. The two antibiotics were found to have the same molecular weight, 926, by plasma desorption and electron-impact MS. However,
13C NMR spectrometry and HPLC studies indicated that the two molecules are different. The 200 MHz NMR studies indicated a chemical environment of 24 carbons of amphotericin A identical with that of the carbons of amphotericin B and nystatin. The structure of amphotericin A is identical with that of amphotericin B, except that there is a single bond between carbons 28 and 29 instead of a double bond, as shown by two-dimensional NMR studies.
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VÊRA PRIKRYLOVÁ, HELENA LIPAVSKÁ, JOSEF V. JIZBA, ...
1985 Volume 38 Issue 12 Pages
1714-1718
Published: 1985
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Synthesis and antibacterial activity of a number of 7-
O-epoxyalkyl derivatives of daunomycinone prepared from 7-
O-alkenyl derivatives of daunomycinone are described along with their inhibitory effect on leukemia P 388 cells.
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N-FUNCTIONALIZED ACYLKANAMYCIN A DERIVATIVES">III. SYNTHESIS AND IN VITRO ANTIVIRAL ACTIVITY OF 1-N-HIGHER-ACYL-3"-N-FUNCTIONALIZED ACYLKANAMYCIN A DERIVATIVES
KEIJI MATSUDA, NOBUYOSHI YASUDA, HIDEO TSUTSUMI, TAKAO TAKAYA
1985 Volume 38 Issue 12 Pages
1719-1737
Published: 1985
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The synthesis and antiviral activity of 1-
N-palmitoyl- or 1-
N-(3-hydroxytetradecanoyl)-kanamycin A derivatives (
7, 8) having various type of acyl substituents at the
N-3" position were investigated. The structure-activity relationships between the antiviral activity and the substituent at the
N-3" position is described. In this series, 3"-
N-acetyl-1-
N-palmitoylkanamycin A (
7c) showed the excellent antiviral activity against HSV-I and influenza virus. Further, we examined the synthesis and the antiviral activity of 3"-
N-glycylkanamycin A derivatives (
9) having a higher-acyl group at the
N-1 position. The 3"-
N-glycyl-1-
N-pentadecanoylkanamycin A (
9a) also exhibited excellent antiviral activity.
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IX. SYNTHESIS AND BIOLOGICAL ACTIVITY OF A NEW ORALLY ACTIVE CEPHALOSPORIN, CEFIXIME (FK027)
HIDEAKI YAMANAKA, TOSHIYUKI CHIBA, KOHJI KAWABATA, HISASHI TAKASUGI, T ...
1985 Volume 38 Issue 12 Pages
1738-1751
Published: 1985
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The synthesis and some biological properties of 7β-[(
Z)-2-(2-amino-4-thiazolyl)-2-(carboxymethoxyimino) acetamido]-3-vinyl-3-cephem-4-carboxylic acid (3, FK027)** are described. Diphenylmethyl 7-amino-3-vinyl-3-cephem-4-carboxylate hydrochloride (8), the cephem precursor to FK027 was prepared from 7-aminocephalosporanic acid (7-ACA) by two parallel routes differing primarily in the protection of the 7-amino group. Compound 8 was alternatively prepared from deacetylcephalosporin C sodium salt (DCCNa) with improved yields. Two pathways for the conversion of 8 to FK027 are provided. The new orally active cephalosporin, FK027, possesses a widely expanded antimicrobial activity and high stability to β-lactamases.
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BRUNO CAVALLERI, MARCO TURCONI, ROSETTA PALLANZA
1985 Volume 38 Issue 12 Pages
1752-1760
Published: 1985
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A series of derivatives has been prepared from the antibiotic thermorubin, some of which show a substantial modification of the original structure. The antibacterial activities are reported.
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SOON-YOUNG PAIK, MASANORI SUGIYAMA, RYOSAKU NOMI
1985 Volume 38 Issue 12 Pages
1761-1766
Published: 1985
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Puromycin 2"-
N-acetyltransferase was isolated from cell extracts of puromycin-producing
Streptomyces alboniger KCC S-0309 by ammonium sulfate fractionation, heat treatment to eliminate contaminant proteins and chromatography on DEAE-Toyopearl 650S. After PAGE (polyacrylamide gel electrophoresis) of the final fraction, a single protein band corresponding to puromycin 2"-
N-acetyltransferase was detected. The molecular weight of the enzyme determined by SDS-PAGE and Sephadex G-150 chromatography was about 21, 000 and 85, 000, respectively, suggesting that the enzyme consisted of four subunits. The isoelectric point and the optimum pH for reaction were 6.2 and 7.7, respectively. The
Km values for puromycin and acetyl coenzyme A were 40 μM and 67 μM, respectively. The enzyme was thermostable up to 70°C for 12 minutes. It was shown, by using an
in vitro protein synthesizing system from a puromycin-susceptible organism
S. flavotricini subsp.
pseudochromogenes V-13-1, that the isolated puromycin 2"-
N-acetyltransferase could protect polyphenylalanine synthesis from inhibition by puromycin.
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SHIN-ICHIRO TAKAHASHI, HISANORI KATO, TAI-ICHIRO SEKI, TADASHI NOGUCHI ...
1985 Volume 38 Issue 12 Pages
1767-1773
Published: 1985
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Bestatin, a microbial aminopeptidase inhibitor, inhibited insulin- or epidermal growth factor-induced DNA synthesis and cell proliferation in primary cultured hepatocytes of rats. The aminopeptidase inhibitor also affected the growth of FM3A or LOBN cells of mice, when it is included in the culture media at the concentration of 0.5 mg/ml. These results suggest the important role of the bestatin-sensitive aminopeptidase(s) in the process of DNA synthesis and proliferation of animal cells.
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IKUMI TAMAI, TETSUYTA TERASAKI, AKIRA TSUJI
1985 Volume 38 Issue 12 Pages
1774-1780
Published: 1985
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The inhibition effect of several β-lactam antibiotics on the uptake of [
14C] to ibenzylpenicillin (PCG) insolated rat hepatocytes was studied. Monobasic, β-lactam antibiotics such as apalcillin, cloxacillin, nafcillin, piperacillin, cefmetazole, cefoperazone, cefpiramide and cephalothin significantly inhibited the uptake of PCG, while amphoteric β-lactam antibiotics such as amoxicillin, ciclacillin, cephradine, cephalexin and cephaloridine had a slight inhibitory effect on the uptake of PCG. Five monobasic compounds of these antibiotics used (apalcillin, nafcillin, piperacillin, cefmetazole and cefoperazone) which have a tendency to be excreted into bile to a large extent, inhibited the initial uptake rate of PCG in a fully competitive fashion according to the Line-weaver-Burk plots and the corresponding modified Inui-Christensen plots. Thus, it was concluded that almost all β-lactam antibiotics have a common carrier system responsible for their uptake into isolated rat hepatocytes, but it is still uncertain whether or not amphoteric; β-lactam antibiotics have another specific transport system.
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IV. ACTIVATION OF MOUSE MACROPHAGES
YUJI WATANABE, SHUICHI TAWARA, YASUHIRO MINE, HIROYUKI KIKUCHI, SACHIK ...
1985 Volume 38 Issue 12 Pages
1781-1787
Published: 1985
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We investigated the effects of the immunoactive peptides, FK 156 and FK 565, on functions of mouse macrophages. FK 156 and FK 565 given parenterally or orally to mice enhanced spreading of peritoneal macrophages, phagocytosis of latex particles and intracellular killing of bacteria by peritoneal macrophages. FK 156 and FK 565 also enhanced the production of superoxide anion and lysosomal enzyme activities of macrophages. The peptides also activated mouse spleen macrophages, and the kinetics of this activation differed from that of the peritoneal macrophages. In addition, both drugs directly enhanced the production of superoxide anion by mouse peritoneal macrophages treated
in vitro and enhanced the functions of peritoneal macrophages of athymic nude mice. Both these phenomena suggest that direct activation might be one of the mechanisms of macrophage activation by the peptides.
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S. K. ARORA
1985 Volume 38 Issue 12 Pages
1788-1791
Published: 1985
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C. LÜBBE, S. WOLFE, J. E. SHIELDS, S. W. QUEENER, N. NEUSS, A. L. ...
1985 Volume 38 Issue 12 Pages
1792-1794
Published: 1985
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KIYOSHI HIRASAWA, MASARU ICHIHARA, MASANORI OKANISHI
1985 Volume 38 Issue 12 Pages
1795-1798
Published: 1985
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A. VIGEVANI, M. BALLABIO, B. GIOIA, L. MARSILI, S. VIOGLIO, G. FRANCES ...
1985 Volume 38 Issue 12 Pages
1799-1802
Published: 1985
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YOKO IKEDA, SHUICHI GOMI, KAZUTERU YOKOSE, HIROSHI NAGANAWA, TAKAKO IK ...
1985 Volume 38 Issue 12 Pages
1803-1805
Published: 1985
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TOSHIO TAKATSU, HIROSHI NAKAYAMA, AKIRA SHIMAZU, KEIKO FURIHATA, KEIJI ...
1985 Volume 38 Issue 12 Pages
1806-1809
Published: 1985
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YUICHI ABE, HIROSHI NAKAYAMA, AKIRA SHIMAZU, KEIKO FURIHATA, KEIJI IKE ...
1985 Volume 38 Issue 12 Pages
1810-1812
Published: 1985
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HAMAO UMEZAWA, TAKAAKI AOYAGI, KEIJI OGAWA, TAMAMI OBATA, HIRONOBU IIN ...
1985 Volume 38 Issue 12 Pages
1813-1815
Published: 1985
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YUKIHIKO KAMEDA, NAOKI ASANO, MASAYOSHI TAKEUCHI, TAKUJI YAMAGUCHI, KA ...
1985 Volume 38 Issue 12 Pages
1816-1818
Published: 1985
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KUNIO ISSHIKI, TSUYOSHI TAMAMURA, YOSHIKAZU TAKAHASHI, TSUTOMU SAWA, H ...
1985 Volume 38 Issue 12 Pages
1819-1821
Published: 1985
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MARIA VIKMON, ÁGNES STADLER-SZÖKE, JÓZSEF SZEJTLI
1985 Volume 38 Issue 12 Pages
1822-1824
Published: 1985
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