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Volume 46, Issue 5
Displaying 1-24 of 24 articles from this issue
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HIROAKI OHKUMA, KOJI TOMITA, YUTAKA HOSHINO, KIYOSHI SUZUKI, MASAMI HA ...1993 Volume 46 Issue 5 Pages 705-711
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThree new 5-lipoxygenase inhibitors, designated as BU-4601 A, B and C, were found in the fermentation broth of Streptomyces sp. strain No. AA2807. Their structures were identified as isodecyl, isoundecyl and isolauryl esters of 5-hydroxyanthranilic acid, respectively. Based on their structures, five related esters were synthesized and evaluated for biological activity as inhibitors of 5-lipoxygenase. Both naturally-occurring and chemically-synthesized compounds exhibited almost equal levels of 5-lipoxygenase inhibibory activities in vitro.View full abstractDownload PDF (389K) -
PRODUCTION, ISOLATION, STRUCTURE DETERMINATION AND BIOLOGICAL ACTIVITIESTAKAYUKI AOYAMA, FUKIKO KOJIMA, TADAO YAMAZAK, TOCHIRO TATEE, FUMINORI ...1993 Volume 46 Issue 5 Pages 712-718
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSBenastatin C, a new member of the benastatins, has been isolated from the culture broth of Streptomyces sp. MI384-DF12. The structure of benastatin C was elucidated as 2-decarboxybenastatin A by NMR studies. Benastatin D, 2-decarboxybenastatin B, was derived from benastatin B. Benastatins C and D showed inhibitory activities against human pi class glutathione S-transferase (GST π) and excellent stimulatory activities on the murine lymphocyte blastogenesis in vitro.View full abstractDownload PDF (353K) -
I. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITYMITSUHIRO UENO, MASAHIDE AMEMIYA, MASATOMI IIJIMA, MICHIYO OSONO, TORU ...1993 Volume 46 Issue 5 Pages 719-727
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSIn order to develop a new class of immunomodulator we have searched for a low molecular weight inhibitors of cell adhesion to components of extracellular matrix (ECM), fibronectin (FN), laminin (LM) and collagen type IV (CL), and succeeded to find a group of novel antibiotics, named delaminomycins. Delaminomycins were isolated from the mycelium and cultured broth of Streptomyces albulus MJ202-72F3. It was purified by use of centrifugal partition chromatography (CPC), preparative reverse phase HPLC and Sephadex LH-20 and was obtained as a white powder. Delaminomycins with inhibitory activity for cell adhesion to ECM components suppressed immune responses in vitro and in vivo and exhibited antimicrobial activity on Gram-positive bacteria.View full abstractDownload PDF (504K) -
I. SCREENING, TAXONOMY, PURIFICATION AND BIOLOGICAL ACTIVITIESKEIICHI ABE, MINORU YOSHIDA, SUEHARU HORINOUCHI, TERUHIKO BEPPU1993 Volume 46 Issue 5 Pages 728-734
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSLeptolstatin, a new inhibitor of the progression of Gl and G2 phases of the mammalian cell cycle, was discovered through a unique screening system, in which effects of microbial metabolites on the cell cycle progression of the cultured rat fibroblasts were monitored by flow cytometry. The new inhibitor was extracted from the fermentation broth of Streptomyces sp. SAM 1595 with ethyl acetate, and purified by silica gel column chromatography and HPLC. Leptolstatin showed a strong cytostatic effect on rat normal fibroblasts 3Y1 with an IC50 value of 0.4ng/ml, but its antimicrobial activity was very weak. A 24-hour treatment of the fibroblast cells with lOng/ml of leptolstatin caused an arrest at Gl or G2 phase, as determined by flow cytometry. When the G2-arrested cells were freed from leptolstatin, those containing 4C DNA entered a new S phase without intervening M phase, resulting in the formation of proliferative tetraploid cells.View full abstractDownload PDF (437K) -
II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTUREKEIICHI ABE, MINORU YOSHIDA, HIDEO NAOK, SUEHARU HORINOUCHI, TERUHIKO ...1993 Volume 46 Issue 5 Pages 735-740
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSLeptolstatin, a product from Streptomyces sp. SAM 1595, is a gap phase-specific inhibitor of the mammalian cell cycle. Physico-chemical properties and spectrometric analyses showed that the structure of leptolstatin is (2Z, 6E, 8Z, 12E, 14E, 22E)-19, 24-dihydroxy-8, 10, 14, 16, 18, 20, 22-heptamethyl-17-oxo-2, 6, 8, 12, 14, 22-tetracosahexaen-5-olide.View full abstractDownload PDF (237K) -
PRODUCTION, ISOLATION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIESFLORENZ SASSE, HEINRICH STEINMETZ, GERHARD HÖFLE, HANS REICHENBAC ...1993 Volume 46 Issue 5 Pages 741-748
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSA new cytostatic compound, rhizopodin, was isolated from the culture broth of the myxobacterium, Myxococcus stipitatus. The compound inhibited growth of various animal cell cultures without killing the cells. The ID50, measured by an MTT assay, was 12 - 30 ng/ml, depending on the cell line. Especially cells growing fibroblast-like showed typical morphological changes. They became larger and within hours formed long branching and reticular runners. These morphological changes were irreversible. Rhizopodin suppresses bleb formation in K-562 cells, and therefore could act by interacting with protein phosporylation.View full abstractDownload PDF (522K) -
PRODUCTION, ISOLATION AND PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIESNORIKO TABATA, YASUKO SUZUMURA, HIROSHI TOMODA, ROKURO MASUMA, KATSUJI ...1993 Volume 46 Issue 5 Pages 749-755
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSHumicola sp. FO-888, a soil isolate, was found to produce a series of new anticoccidial compounds. Five active compounds, designated xanthoquinodins Al, A2, A3, Bl and B2 were isolated from the fermentation broth of the producing strain by solvent extraction and HPLC. Xanthoquinodins inhibited the growth of Eimeria tenella in an in vitro assay system using BHK-21 cells as a host. No schizont in the cells was observed at concentrations of 0.02-0.2μg/ml for xanthoquinodins Al, A3, Bl and B2 and at 0.02μg/ml for xanthoquinodin A2.View full abstractDownload PDF (464K) -
I. PRI. PRODUCTION, ISOLATION AND PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIESNORIKO TABATA, HIROSHI TOMODA, YOKO TAKAHASHI, KATSUJI HANEDA, YUZURU ...1993 Volume 46 Issue 5 Pages 756-761
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSStreptomyces sp. WK-2955, a soil isolate, was found to produce a series of new anticoccidial compounds. Four active compounds, designated diolmycins A1, A2, B1 and B2, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography, gel filtration on Sephadex LH-20, and preparative HPLC. Diolmycins inhibited the growth of Eimeria tenella in an in vitro assay system using BHK-21 cells as a host. No schizont in the cells was observed at concentrations of 0.02-2.0μg/ml for diolmycin Al, at 0.2-2.0μg/ml for diolmycin A2, and at 20μg/ml for diolmycins Bl and B2.View full abstractDownload PDF (325K) -
II. STRUCTURE ELUCIDATION OF DIOLMYCINS A1, A2, B1 AND B2, AND SYNTHESIS OF DIOLMYCIN A1NORIKO TABATA, TOSHIAKI SUNAZUKA, HIROSHI TOMODA, TOHRU NAGAMITSU, YUZ ...1993 Volume 46 Issue 5 Pages 762-769
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThe structures of diolmycins Al, A2, Bl and B2, novel anticoccidial agents, were determined by spectroscopic analyses. Diolmycins Al and A2 are stereoisomers with the structure of 1 -(3-indolyl)-4-(p-hydroxyphenyl)-2, 3-butanediol. From the chemical synthesis of the erythro-isomer, the relative configurations of diolmycins A1 and A2 were determined to be the erythro- and threo-isomers, respectively. The stereoisomers, diolmycins B1 and B2, were also deduced to be erythro- and threo-1, 4-di-(p-hydroxyphenyl)-2, 3-butanediol, respectively.View full abstractDownload PDF (377K) -
I. TAXONOMY, FERMENTATION AND PURIFICATIONGILLES ETIENNE, BERNARD FABRE, ELISE ARMAU, FRÉDÉRIC LEG ...1993 Volume 46 Issue 5 Pages 770-776
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSCL307-24, a complex of new antibiotics has been isolated from the fermentation broth of Saccharopolyspora aurantiaca sp. nov. The complex was purified by cation-exchange and hydrophobic interaction chromatographies. It was then resolved as one major and three minor components by silica gel chromatography and HPLC.View full abstractDownload PDF (390K) -
TETSUYA MATSUMOTO, MITSUO KAKU, NOBUHIKO FURUYA, TOSHIAKI USUI, SHIGER ...1993 Volume 46 Issue 5 Pages 777-784
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSWe evaluated the effects of amphotericin B (AmB) against Pseudomonas aeruginosa (P. aeruginosa) infection in mice. Pretreatment with 2mg/kg of AmB 24 hours before infection significantly increased the survival rates of mice intraperitoneally infected with either P. aeruginosa or Escherichia coli. To evaluate the mechanism of this AmB-induced resistance to infection, we conducted a number of experiments. Peritoneal macrophages exposed in vitro to AmB showed superior bactericidal activity compared to that of control macrophages. Interleukin-1 production by peritoneal macrophages from mice pretreated with 2 mg/kg of AmB was significantly higher than that in control mice. Serum tumor necrosis factor level after intravenous injection of P. aeruginosa was also higher in mice pretreated with 2 mg/kg of AmB than in control mice. These data indicate that AmB induces resistance to P. aeruginosa in mice. Furthermore AmB-induced activation of peritoneal macrophages and their production of interleukin-1 and tumor necrosis factor appeared to play important roles in this phenomenon.View full abstractDownload PDF (515K) -
TSUTOMU OIKAWA, HIROMI ASHING, MARIKO SHIMAMURA, MASAMI HASEGAWA, IKUO ...1993 Volume 46 Issue 5 Pages 785-790
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSHere we describe the inhibitory effect of erbstatin, a specific tyrosine kinase inhibitor, on in vivo angiogenesis. Inhibition of angiogenesis was determined in a bioassay system involving chorioallantoic membranes of growing chick embryos. Erbstatin produced a dose-dependent inhibitory action on embryonic angiogenesis. This inhibition occurred at as small a dose as 10 ng/egg and the ID50 value was 80 ng/egg. To analyze this inhibition, in vitro experiments involving vascular endothelial cells were also performed. Erbstatin affected the proliferation of vascular endothelial cells, one of angiogenic components. This inhibition was dose-dependent, the IC50 value being 3.6 μM. These data indicate that erbstatin-sensitive tyrosine kinase(s) is involved in angiogenic endothelial cell proliferation, and that experiments involving erbstatin will provide an important clue to understand a mechanism of angiogenesis.View full abstractDownload PDF (439K) -
TOSHIO OTANI1993 Volume 46 Issue 5 Pages 791-802
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSCharacterization of the secondary structure of the antitumor antibiotic C-1027 has been made from a comparison of C-1027 and its apoprotein by various analytical means. The results indicated the antibiotic to be abundant in β-structure by measurements of Fourier-transform infrared (FT-IR) spectroscopy and the circular dichroism (CD) spectrum, and by a prediction of the secondary structure based on the amino acid sequence of the peptide. In comparison of the IR spectra of their proteins in D2O, the apoprotein exhibited a faster H-D exchange than C-1027, indicating an increase in the "non-motile parts" of the β-sheets formed through the protein-chromophore interaction in holo-C-1027. The prediction of hydropathic index indicated the hydrophobic residues of the apoprotein to be predominantly located in the β-sheet structures, suggesting hydrophobic interaction in the binding between chromophore and apoprotein. Further, the interaction between chromophore and apoprotein was detected by a fluorescence method. The result showed the dissociation constant (Kd) to be 6.88 × 10-5 M, indicating that the chromophore is tightly bound to the protein moiety.View full abstractDownload PDF (732K) -
TSUNEAKI HIDA, SHIGETOSHI TSUBOTANI, NOZOMI KATAYAMA, YASUNORI FUNABAS ...1993 Volume 46 Issue 5 Pages 803-812
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSModification of sperabillins was carried out. The 2-amidinoethylamino moiety was removed by brief acidic hydrolysis. The 2, 4-hexadienoyl moiety was hydrogenated to the hexanoyl moiety and this was cleaved by an enzymatic reaction using the cells of Pseudomonas acidovorans IFO 13582. The 2-amidinoethylamino and the 2, 4-hexadienoyl moieties were replaced with other groups. The derivative which was prepared by condensation of two molar amounts of dehexadienoylsperabillin A with (E, E)-muconic acid showed better protective effects than sperabillin A against Gram-negative bacteria.View full abstractDownload PDF (613K) -
SYNTHESES AND ANTIMICROBIAL ACTIVITIES OF 3''-EPI-ERYTHROMYCIN A AND (9S)11-DEHYDROXY-9-DEOXO-9-HYDROXY-11-OXOERYTHROMYCIN AMASAYA NAKATA, TETSURO TAMAI, YUKIKO MIURA, MITSUHIRO KINOSHITA, KUNIA ...1993 Volume 46 Issue 5 Pages 813-826
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSTwo new derivatives, 3''-epi-erythromycin A (2) and (9S)-11-dehydroxy-9-deoxo-9-hydroxy-11-oxoerythromycin A (3), have been synthesized by using glycosylation with glycal (Ferrier rearrangement), bromomethoxylation and bis(tributyltin) oxide-bromine oxidation as the key steps. Their antimicrobial activities were compared with those of erythromycin A (1).View full abstractDownload PDF (871K) -
YUTAKA TAKEUCHI, TAKAAKI INOUE, MAKOTO SUNAGAWA1993 Volume 46 Issue 5 Pages 827-832
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThe structure and solution conformation of meropenem was examined by using 1H and 13C NMR spectroscopy and nuclear Overhauser enhancement experiments. Similar to the X-ray crystal structure, the close spacing of 1β-methyl substituent to the β-lactam ring and the accessible conformation of C-2 side chain in relation to the carbapenem skeleton was confirmed. The structure of the primary metabolite of meropenem by dehydropeptidase-I was shown to be the β-lactam ring-opened product by comparing the spectrpscopic data with those of meropenem, and confirmed by the preparation and structural analysis of its crystalline derivative. This metabolite existed as a mixture of 1-pyrroline and 2-pyrroline isomers, and the coexistence of two isomers at equilibrium in aqueous solution was observed by NMR.View full abstractDownload PDF (396K) -
TAKAAKI OKITA, KIYOTO IMAE, TOSHIFUMI HASEGAWA, SEIJI IIMURA, SHINJI M ...1993 Volume 46 Issue 5 Pages 833-839
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSCephalosporins having a catechol through a variety of linkages to the C3 position and a different C7 side chain were prepared. Among them, 3-(catechol-4-ylcarbonyloxy)methylcephalosporin (14) and 3-[(E)-3-(catechol-4-ylcarbonyloxy)-l-propen-l-yl]cephalosporin (10) showed excellent activity against Gram-negative activity including ceftazidime-resistant Escherichia coli, Pseudomonas aeruginosa, Xanthomonas maltophilia and Pseudomonas cepacia.View full abstractDownload PDF (433K) -
I. ENHANCEMENT OF EFFICACY AGAINST GRAM-NEGATIVE BACTERIAKIYOTO IMAE, SEIJI IIMURA, TOSHIFUMI HASEGAWA, TAKAAKI OKITA, MINORU H ...1993 Volume 46 Issue 5 Pages 840-849
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSTwo groups of cephalosporins substituted with a variety of heterocyclic catechols in the C3 side chain were synthesized. One is a group of 3-(heterocyclic catechol-substituted methyl)cephalosporins and another is 3-[(E)-3-heterocyclic catechol-substituted l-propen-l-yl]cephalosporins. Cephalosporins in the latter group showed higher in vivo efficacies than those in the former group having the same heterocyclic catechol, especially against Pseudomonas aeruginosa A9843A, although there was no significant difference between their in vitro activity. Among the latter group, the 5, 6-dihydroxybenzimidazole derivative (6e) and the 2, 6-dihydro-7-hydroxy-6-oxo-isoquinoline derivative (6b) showed much higher activity than ceftazidime (CAZ) and imipenem (IPM) against P. aeruginosa A9843A both in in vitro and in vivo studies.View full abstractDownload PDF (561K) -
II. IMPROVEMENT OF PHARMACOKINETIC PROFILESEIJI IIMURA, KIYOTO IMAE, TOSHIFUMI HASEGAWA, TAKAAKI OKITA, MASAMI T ...1993 Volume 46 Issue 5 Pages 850-857
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESS7-[(Z)-2-(2-Aminothiazol-4-yl)-2-methoxy-(or hydroxy)-iminoacetamido]-3-[propen-l-yl]-cephalosporins having a variety of heterocyclic catechol in 3-position of the propenyl group were synthesized. Among them, 6, 7-dihydroxyisoquinoline derivatives, 2a and 2b, showed very high and prolonged blood levels after intramuscular administration to mice and higher in vivo antibacterial activity than expected from their in vitro activity. The former cephalosporin (2a) gave wellbalanced in vitro and in vivo antibacterial spectra including anti-methicillin-resistant Staphylococcus aureus (MRSA) activity. The latter cephalosporin (2b) also showed good in vitro and in vivo activities against Gram-positive bacteria, especially against S. aureus A15036, a strain of MRSA, the in vivo activity being comparable to vancomycin but was lacking in anti-pseudomonal activity.View full abstractDownload PDF (435K) -
FERMENTATION, ISOLATION AND PHYSICO-CHEMICAL PROPERTIESMIHO TANAKA, YASUHIRO HORI, HIROTSUGU UEDA, MASAMI EZAKI, TOSHIO GOTO, ...1993 Volume 46 Issue 5 Pages 858-860
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (228K) -
M. CHU, R. YARBOROUGH, J. SCHWARTZ, M. G. PATEL, A. C. HORAN, V. P. GU ...1993 Volume 46 Issue 5 Pages 861-865
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (266K) -
MASAMI OGASAWARA, NOBUAKI NARUSE, ATSUKO YOSHIMURA, YASUTARO HAMAGISHI ...1993 Volume 46 Issue 5 Pages 866-868
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (308K) -
JANICE L. DOULL, STEPHEN W. AYER, AMRIT K. SINGH, PIERRE THIBAULT1993 Volume 46 Issue 5 Pages 869-871
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (225K) -
HIROSHI TOMODA, HIDETOSHI KUMAGAI, HARUO TANAKA, SATOSHI OMURA1993 Volume 46 Issue 5 Pages 872-874
Published: May 25, 1993
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (256K)
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