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Volume 47, Issue 9
Displaying 1-16 of 16 articles from this issue
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TSUTOMU KAMIYAMA, TAKAYUKI UMINO, YUMIKO NAKAMURA, YOSHIKO ITEZONO, SA ...1994 Volume 47 Issue 9 Pages 959-968
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSNovel thrombin inhibitors, bacithrocins A, B and C, have been isolated from the culture broth of Bacillus laterosporus Laubach NR 2988. The structures of these inhibitors have been determined to be N-acyl-L-phenylalanyl-DL-arginal by the 2D-NMR experiments on their oxidation products and by amino acid analysis. Bacithrocin A inhibits thrombin, factor Xa and trypsin with IC50s of 48, 13 and 0.65μM, respectively, which are similar to those of bacithrocins B and C. Bacithrocins prolong the clotting time induced by thrombin and factor Xa.View full abstractDownload PDF (572K) -
II. GENINTHIOCIN, A NOVEL THIOPEPTIDE PRODUCED BY Streptomyces sp. DD84BONG-SIK YUN, TOMOMI HIDAKA, KAZUO FURIHATA, HARUO SETO1994 Volume 47 Issue 9 Pages 969-975
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSGeninthiocin was isolated from the mycelium of Streptomyces sp. DD84 as a tip A promoter inducing substance. Based on various NMR studies, its structure was established as a thiopeptide with oxazole and thiazole moieties, and several unusual amino acids.View full abstractDownload PDF (360K) -
AKIO MAEDA, HIROSHI NAGAI, KATSUKIYO YAZAWA, YASUSHI TANAKA, TAMAE IMA ...1994 Volume 47 Issue 9 Pages 976-981
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThree new metabolites were isolated from a pathogenic bacterium, Nocardia brasiliensis IFM 0075 strain, a producer of a new anthracycline antibiotic (SO-075R1) and its mutant strain (IFM 0075-13-1). The structural studies showed that they are reduced anthracyline related compounds. Some biosynthetic routes of these matabolites were discussed.View full abstractDownload PDF (325K) -
III. FERMENTATION AND CONTROLLED BIOSYNTHESIS OF EURYSTATIN ANALOGS BY Streptomyces eurythermusKIYOSHI SUZUKI, SOICHIRO TODA, TAMOTSU FURUMAI, YASUO FUKAGAWA, TOSHIK ...1994 Volume 47 Issue 9 Pages 982-991
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSAccurate and precise component analysis of eurystatin analogs in fermentation broth was devised by HPLC methods with and without 2, 4-dinitrophenylhydrazonation. Detailed optimization of fermentation conditions and strain improvement by HPLC analysis significantly increased the eurystatin productivity of Streptomyces eurythermus. Chemically denned fermentation media which produced eurystatins A and B at fermentation yields comparable to complex media were elaborated for radio-isotope fermentation studies and controlled biosynthesis. Radio-isotope incorporation study using 14C-labeled amino acids in chemically defined medium demonstrated that L-leucine and L-ornithine were the direct precursors for the L-leucine and L-ornithine moieties of eurystatins A and B, respectively. Based on this finding, L-valine and L-isoleucine were supplemented to the growing culture of S. eurythermus in chemically defined medium, which resulted in the controlled biosynthesis of new eurystatin analogs named eurystatins C, D, E and F.View full abstractDownload PDF (546K) -
TIM BUCHAN, CLAUDIA ROACH, CAROLYN RUBY, DEAN TAYLOR, CAROL PREISIG, C ...1994 Volume 47 Issue 9 Pages 992-1000
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThienamycin non-producing mutants of Streptomydes cattleya were identified that displayed a cross-feeding relationship. A diffusible product from one of these mutants (RK-11) resulted in restoration of thienamycin production when fed to cultures of another mutant (RK-4). In vivo radiolabeling experiments were conducted to test whether the RK-11 mutant produced a late biosynthetic intermediate which contained a carbapenem ring and a cysteaminyl and/or a hydroxyethyl side chain. Both [35S]cystine and [methyl-3H]methionine were used to label the RK-11 product which was then fed to RK-4 cultures. None of the thienamycin subsequently produced by RK-4 converter cells was labeled, implying the lack of either side chain of the thienamycin molecule in the RK-11 product. Further stability studies suggested that the RK-11 product does not contain a carbapenem ring. Additional feeding experiments with RK-4 cells also ruled out the possibility that the RK-11 product is a co-factor necessary for thienamycin production. It is concluded that the RK-11 product may regulate expression of the thienamycin gene cluster.View full abstractDownload PDF (522K) -
CATHY S. TAFT, CAROL S. ENDERLIN, CLAUDE P. SELITRENNIKOFF1994 Volume 47 Issue 9 Pages 1001-1009
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSAn in vitro assay for (1, 3)β-glucan synthase activity from the filamentous ascomycete Neurospora crassa, suitable for use as a high throughput screen for enzyme inhibitors is described. Samples were added to 25μl reaction mixtures in 96-well V-bottom microtiter plates and plates incubated at 22°C. Reactions were terminated by the addition of TCA and the contents transferred to a Milliblot D apparatus containing Inotech 201-A glass fiber filters. Filters were washed to remove unincorporated substrate and the amount of 14C-labeled (1, 3)β-glucan formed by each reaction was quantitated using a Phosphorlmager. As little as 50 ng of an inhibitor with a Ki of 4μM was detected by this assay. This assay is rapid and cost effective, permitting its use as a screen to detect compounds that inhibit (1, 3)β-glucan synthase activity.View full abstractDownload PDF (686K) -
CHRISTIE BOROS, SEAN M. HAMILTON, BARRY KATZ, PALANIAPPAN KULANTHAIVEL1994 Volume 47 Issue 9 Pages 1010-1016
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSRecently, we reported the isolation of the potent protein kinase C inhibitor balanol (1) from the fungus Verticillium balanoides. In an earlier study, KÖNIG et al reported the isolation of ophiocordin (3), a structural isomer of 1, from the fungus Cordyceps ophioglossoides. The present study was designed to clarify whether or not balanol and ophiocordin are different compounds. The results indicated that the two fungi produced the same compound, the structure being that assigned to balanol. In addition, a thirty-fold increase in the production of balanol from V. balanoides was observed when the culture medium was changed from cornmeal/tomato paste to soy meal/glycerol.View full abstractDownload PDF (443K) -
THE MNIOPETALS, NEW INHIBITORS OF REVERSE TRANSCRIPTASES FROM A Mniopetalum SPECIES (BASIDIOMYCETES)II. STRUCTURE ELUCIDATIONROBERT VELTEN, DÖRTE KLOSTERMEYER, BERT STEFFAN, WOLFGANG STEGLIC ...1994 Volume 47 Issue 9 Pages 1017-1024
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThe structures of six new drimance sesquiterpenoids, mniopetals A-F, were elucidated by a combination of chemical and spectroscopic methods. The mniopetals are inhibitors of RNA-directed DNA-polymerases.View full abstractDownload PDF (496K) -
HIROSHI TANAKA, KAICHIRO KOMINATO, REIKO YAMAMOTO, TAKEO YOSHIOKA, HIR ...1994 Volume 47 Issue 9 Pages 1025-1029
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDoxorubicin-γ-cyclodextrin conjugates have been synthesized by the coupling of 14-bromodaunomycin with mono half-ester compounds linked to a 6-hydroxyl group of γ-cyclodextrin. Release of drug from the conjugates in saline phosphate buffer solution and in vitro antitumor activity against L1210 leukemia cells were also investigated.View full abstractDownload PDF (292K) -
CHAEUK IM, SAMARENDRA N. MAITI, RONALD G. MICETICH, MOHSEN DANESHXALAB ...1994 Volume 47 Issue 9 Pages 1030-1040
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThe synthesis of β-lactamase inhibitory activity of a series of sodium 6-[(1-heteroarylthioethyl-1, 2, 3-triazol-4-yl)methylene]pemcillanate 1, 1-dioxides are described. Their activity was compared with tazobactam and sulbactam. The Z-isomers were more active than the E-isomers. The in vitro activity of the Z-isomers of the phenylthiadiazole derivatives (13a and 15a) was better than sulbactam against the tested β-lactamases and comparable to tazobactam especially against TEM-2 and cephalosporinase. But their synergistic activity with five antibiotics was inferior to tazobactam.View full abstractDownload PDF (668K) -
SOPHIE VANWETSWINKEL, JACOQUES FASTREZ, JACQUELINE MARCHAND-BRYNAERT1994 Volume 47 Issue 9 Pages 1041-1051
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThree new sulfonylamido-penicillanic acid sulfones have been prepared by reaction of 6-aminopenicillanic esters with the monoester or monoamide derivatives obtained in nucleophilic substitution reactions by alcohol or aniline on the carboxyl chloride function of sulfoacetic dichloride followed by oxidation. These penicillin sulfones are converted to βMactamases suicide inhibitors by removal of the C3 ester protecting group. This synthetic strategy can give access to sulfonamido-penam sulfones bearing a variety of 6-amino side chain. These inhibitors inactivate the RTEM βMactamase rapidly. The kinetics of inactivation are consistent with the partitioning of an acyl-enzyme intermediate between two main pathways: regeneration of free enzyme and irreversible inactivation, little transient inactivation is observed. A slow inhibition by the product of enzymatic hydrolysis of the sulfones is also observed.View full abstractDownload PDF (715K) -
WILLIAM J. HORNBACK, JOHN E. MUNROE, FRED T. COUNTER1994 Volume 47 Issue 9 Pages 1052-1064
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSThe synthesis and microbiological evaluation of a new series of 3-thiazol-4-yl-carba-1-dethiacephalosporins is described. Structure activity relationship was achieved by changing substitution at the 2-position of the thiazole moiety. The result was a marked variance of microbiological activity in the C7 side-chain derivatives. ATMO derivatives possess potent activity against both Gram-positive and Gram-negative bacteria. For example, MICs (μg/ml) of LY215226 against representative organisms are as follows: S. aureus 0.25, S. pneumoniae 0.008, H. influenzae 0.008, E. coli 0.25, K. pneumoniae 0.008, E. cloacae 0.5, S. typhi 0.25, and M. morganii 0.25.View full abstractDownload PDF (840K) -
ATSUKI MORISHITA, SATORU ISHIKAWA, YASUNOBU ITO, KIYOSHI OGAWA, MASAKI ...1994 Volume 47 Issue 9 Pages 1065-1068
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (227K) -
TOMOO KOHYAMA, KEIJI HASUMI, SHIGEO MURAKAWA, AKIRA ENDO1994 Volume 47 Issue 9 Pages 1069-1071
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (175K) -
KAZUTOSHI SHINDO, YUJI YAMAGISHI, YUKIKO OKADA, HIROYUKI KAWAI1994 Volume 47 Issue 9 Pages 1072-1074
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (152K) -
EDWARD KATZ1994 Volume 47 Issue 9 Pages 1075-1076
Published: September 25, 1994
Released on J-STAGE: April 19, 2006
JOURNAL FREE ACCESSDownload PDF (232K)
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