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V. R. HEGDE, J. R. MILLER, M. G. PATEL, A. H. KING, M. S. PUAR, A. HOR ...
1993 Volume 46 Issue 2 Pages
207-213
Published: February 25, 1993
Released on J-STAGE: April 19, 2006
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A highly potent inhibitor of calmodulin-sensitive phosphodiesterase (PDE) activity was isolated from the culture broth of an unidentified fungal isolate, SCF-125. A chemically defined medium was developed for production of this compound. The PDE inhibitor was isolated from the fermentation filtrate by adsorption on a macro-reticular resin and further purified by gel filtration chromatography and reverse-phase HPLC. The major PDE inhibitor was identified as cephalochromin, a bis-naphthopyrone, by spectral data analysis. The compound, SCH 45752, inhibited calmodulinsensitive PDE activities with IC
50 values of 40-47nM. It inhibited the activities of calmodulin-independent PDE and various protein kinases with higher IC
50 values (2-40 μM). SCH 45752 does not appear to be a calrnodulin antagonist. Furthermore, SCH 45752 affects smooth muscle contraction at a concentration of 30 μM; it potentiated the relaxing effect of sodium nitroprusside on carotid artery media contracted by histamine. Thus SCH 45752 is one of the most potent inhibitors of calmodulin-sensitive PDE activity known, and it is capable of exerting a pharmacological effect in at least one intact tissue model.
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SUI-MING WONG, RUDOLPH KULLNIG, JONAS DEDINAS, KENNETH C. APPELL, GWEN ...
1993 Volume 46 Issue 2 Pages
214-221
Published: February 25, 1993
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Substance P (SP) is an undecapeptide belonging to a family of chemically related neurotransmitters and neuromodulators known as neurokinins. In our search for SP antagonists, we screened microbial broth extracts for the ability to inhibit radiolabeled SP binding to membranes prepared from rat forebrain. Anthrotainin was isolated from a fungal culture and determined to be a novel tetracyclic compound, with an IC
50 of 3 μM against [
125I]SP. The structure, spectroscopic, chemical, and pharmacological properties of anthrotainin are presented.
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I. PRODUCING STRAIN, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITY
SATOSHI OMURA, DIDIER VAN DER PYL, JUNJI INOKOSHI, YOKO TAKAHASHI, HID ...
1993 Volume 46 Issue 2 Pages
222-228
Published: February 25, 1993
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Pepticinnamins A, B, C, D, E and F, a family of farnesyl-protein transferase (FPT) inhibitors were isolated from the fermentation broth of
Streptomyces sp. OH-4652. These inhibitors were purified from whole broth by extraction with chloroform, followed by silica gel column chromatography, Sephadex LH-20 chromatography and reverse phase HPLC. Among these, pepticinnamin C showed the most potent inhibition (IC
50-100nM).
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II. STRUCTURAL ELUCIDATION OF PEPTJCINNAMIN E
KAZURO SHIOMI, HONG YANG, JUNJI INOKOSHI, DIDIER VAN DER PYL, AKIRA NA ...
1993 Volume 46 Issue 2 Pages
229-234
Published: February 25, 1993
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Structure of novel farnesyl transferase inhibitor, pepticinnamin E, is elucidated by NMR study. Pepticinnamin E is composed of five amino acids and
o-pentenylcinnamic acid, having a molecular weight of 907.
C-terminal glycylserine of the compounds is in the cyclized diketopiperazine form.
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STRUCTURE DETERMINATION
YOUICHI UOSAKI, SHO-ZOU KAWADA, HIROFUMI NAKANO, YUTAKA SAITOH, HIROSH ...
1993 Volume 46 Issue 2 Pages
235-240
Published: February 25, 1993
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The relative stereo structure of UCT4B was determined by means of chemical derivatization and spectral analysis, in relation to known antitumor antibiotics terpentecin, which was simultaneously produced with UCT4B by
Streptomyces sp.
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NOBUTAKA IMAMURA, MIYUKI NISHIJIMA, KYOUKO ADACHI, HIROSHI SANO
1993 Volume 46 Issue 2 Pages
241-246
Published: February 25, 1993
Released on J-STAGE: April 19, 2006
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Two novel antimycin antibiotics, urauchimycins A and B, were isolated from a fermentation broth of a
Streptomyces sp. Ni-80. The strain was isolated from an unidentified sponge. Their chemical structures were determined by 2D NMR analysis. They are the first antimycin antibiotics which possess a branched side chain moiety. They exhibited inhibitory activity against morphological differentiation of
Candida albicans.
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I. FERMENTATION, ISOLATION AND CHARACTERIZATION
REI KANETO, HIROYUKI CHIBA, HITOSI AGEMATU, NORIO SHIBAMOTO, TAKEO YOS ...
1993 Volume 46 Issue 2 Pages
247-250
Published: February 25, 1993
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Mer-WF3010, a new member of the papulacandin family, was isolated from the mycelia of
Phialophora cyclaminis Mer-WF3010 (PERM P-11475). The molecular formula of Mer-WF3010 was determined as C
45H
60O
16.
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I. TAXONOMY OF THE PRODUCING ORGANISM, FERMENTATION AND ANTIFUNGAL ACTIVITY
DANTE CIDARIA, GIORGIO BORGONOVI, GIORGIO PIRALI
1993 Volume 46 Issue 2 Pages
251-254
Published: February 25, 1993
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AB023 is a complex of polyene antibiotics produced by an actinomycete, SD581, which was isolated from a Kenyan soil sample. The two main components, pentaene antibiotics AB023a and AB023b, have antifungal activity against some phytopathogenic fungi, particularly against
Botrytis cinerea (MIC of 5μg/ml).
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II. ISOLATION AND STRUCTURE DETERMINATION
ROSSELLA BORTOLO, SILVIA SPERA, GIANFRANCO GUGLIELMETTI, GIORGIO CASSA ...
1993 Volume 46 Issue 2 Pages
255-264
Published: February 25, 1993
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AB023, a complex of new polyene antibiotics, was isolated from a soil
Streptomyces strain.
The two main components, pentaene antibiotics AB023a and AB023b, were separated and purified by preparative chromatographic methods and their structures were determined by extensive NMR and mass spectrometric studies.
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SCREENING, TAXONOMY, DIRECTED BIOSYNTHESIS, ISOLATION AND CHARACTERIZATION
TAMOTSU FURUMAI, KYOICHIRO SAITOH, MASATOSHI KAKUSHIMA, SATOSHI YAMAMO ...
1993 Volume 46 Issue 2 Pages
265-274
Published: February 25, 1993
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BMS-181184 is a new semisynthetic pradimicin derivative with a broad-spectrum antifungal activity. In a search for actinomycetes producing BMS-181184, 4 strains of
Actinomadura sp. isolated from soil samples were found to produce the antibiotic under conditions of directed biosynthesis. Among them,
Actinomadura sp. AB1236 proved most useful in the production of BMS-181184 when fermented in a medium containing D-serine and D-cycloserine. A minor product isolated from the broth of strain AB1236 was identified as the dexylosyl analog of BMS-181184, which was also obtained by acid hydrolysis of BMS-181184.
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TAXONOMY OF THE PRODUCING OGRANISM, FERMENTATION PRODUCTION AND BIOLOGICAL PROPERTIES OF THE ANTIBIOTICS
CHAO-MIN LIU, JOHN W. WESTLEY, JENNIFER CHU, T. E. HERMANN, MARK LIU, ...
1993 Volume 46 Issue 2 Pages
275-279
Published: February 25, 1993
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Antibiotic X-14889A, C, and D are novel polyether antibiotics related to lysocellin and antibiotic X-14873A. They are produced by a streptomycete isolated from a soil of Wisconsin. The antibiotic X-14889C is active against Gram-positive bacteria and exhibits ionophore property.
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JOHN W. WESTLEY, CHAO-MIN LIU, JOHN F. BLOUNT, LOUIS TODARO, LILLIAN H ...
1993 Volume 46 Issue 2 Pages
280-286
Published: February 25, 1993
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Streptomyces sp. X-14889 (NRRL 15517) has been found to produce a number of novel polyether antibiotics and an orange pigment. One of the antibiotics, X-14889B (
3) was identified as ferensimycin A, which in turn is an isomer of the well-studied polyether antibiotic, lysocellin (
1). Of the three other antibiotics, X-14889C (
4) is a lower homolog of ferensimycin A and antibiotics X-14889A (
2) and D (
5) which are respectively the descarboxy and anhydro-descarboxy forms of this same molecule. The latter compound, X-14889D is of interest as it contains an ether bridge across the terminal tetrahydrofuranyl ring in an analogous relationship to that reported earlier for antibiotics X-14873A (
6) and G.
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ISOLATION, CHARACTERIZATION AND STRUCTURE ELUCIDATION
SHIGETOSHI TSUBOTANI, NOZOMI KATAYAMA, YASUNORI FUNABASHI, HIDEO ONO, ...
1993 Volume 46 Issue 2 Pages
287-293
Published: February 25, 1993
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Novel iron-containing peptide antibiotics, ferrocins A, B, C and D, have been isolated from the culture nitrate of
Pseudomonas fluorescens YK-310. These antibiotics were purified by butanol extraction, followed by column chromatography using adsorption resin, silica gel and preparative reverse-phase HPLC. The structures of ferrocins were elucidated using spectroscopic and degradative methods. Ferrocins contain three hydroxamate moieties per ferric ion which forms an octahedral iron complex.
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BARBARA E. ROGGO, HEINRICH H. PETER
1993 Volume 46 Issue 2 Pages
294-299
Published: February 25, 1993
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N-Hydroxy-desferrioxamine B (
5), a postulated metabolite of the microbial product desferrioxamine B (
1), has been prepared by reduction of the intermediate oxime
6 with sodium cyanoborohydride. The oxime was obtained by selective oxidation of desferrioxamine B with hydrogen peroxide and a catalytic amount of sodium tungstate dihydrate. The iron complex derived from
5 enabled definite proof of the structure of one of four metabolites of desferrioxamine B found in urine samples of patients treated with this drug.
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TOSHIAKI KUDO, YOSHIO NISHIMURA, SHINICHI KONDO, TOMIO TAKEUCHI
1993 Volume 46 Issue 2 Pages
300-309
Published: February 25, 1993
Released on J-STAGE: April 19, 2006
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Potent inhibitors of neuraminidase, 3, 4-didehydro-4-deoxysiastatin B, 4-deoxysiastatin B and
N-[(
S and
R)-1, 2-dmydroxypropyl] derivatives of siastatin B, 3, 4-didehydro-4-deoxysiastatin B and 4-deoxysiastatin B have been synthesized by the chemical modifications of siastatin B.
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SHINICHI KONDO, ATSUSHI TAMURA, SHUICHI GOMI, YOKO IKEDA, TOMIO TAKEUC ...
1993 Volume 46 Issue 2 Pages
310-315
Published: February 25, 1993
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Only a limited number of strains of methicillin-resistant
Staphylococcus aureus (MRSA) moderately resistant to arbekacin (ABK) have been isolated clinically. Three inactivated products of ABK have been obtained by reaction with excess amounts of a crude enzyme preparation extracted from an ABK-resistant MRSA strain (MIC, 25μg/ml). The 2''-
O-phosphate was the major product together with small amounts of the 6'-
N-acetate and the double modification product. The structures of these modification products were determined by MS and NMR spectral analyses.
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III. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF NEW 3-HETEROCYCLICTHIOMETHYLTHIO-7β-[(Z)-2-(2-AMINOTHIAZOL-4-YL)-2-HYDROXYIMINOACETAMIDO]-3-CEPHEM-4-CARBOXYLIC ACIDS
MASAHARU KUME, TADATOSHI KUBOTA, YASUO KIMURA, HIROMU NAKASHIMIZU, KIY ...
1993 Volume 46 Issue 2 Pages
316-330
Published: February 25, 1993
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3-Heterocyclicthiomethylthio-7β-[(
Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-cephem-4-carboxylic acids (
2) were synthesized. Their antibacterial activity and oral absorbability were much influenced by the structure of heteroaromatic moiety in the side chain at the 3-position of a cephem nucleus. In this cephalosporin series, 3-thiadiazolylthiomethylthiocephalosporins (
2k,
2l and
2m) exhibited potent antibacterial activity against both Gram-positive and Gram-negative bacteria, whereas 3-(2-methyl-1, 2, 3-triazol-4-yl)thiomethylthiocephalosporin (
2b) and 3-(pyridin-2-yl)thiomethylthiocephalosporin (
2n) showed better oral absorption in mice than the other cephalosporins prepared. The structure-activity relationships of
2 are presented.
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RICHARD K. ANDERSON, PAULINE C. CHAPMAN, SUZANNE C. COSHAM, J. SYDNEY ...
1993 Volume 46 Issue 2 Pages
331-342
Published: February 25, 1993
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Syntheses are described for penicillins (
4b-
4i,
5a and
5b) which possess a 6β-(2-heteroaryl-3-substituted)-propenamido side-chain of fixed geometry.
In vitro results for these compounds against a range of Gram-positive and Gram-negative bacteria showed in most cases good stability against both penicillinase and TEM-1 β-lactamase; analogues (
4b-
4i) bearing a 2-(2-aminothiazol-4-yl) unit showed the best intrinsic activity, the cyclohexyl compound (
4b) being the most promising. The 1-acetoxyethyl ester (
6) of
4b was also prepared; in experimental animal studies the
in vivo properties of this compound compared favourably with cefuroxime axetil and are reported together with selected
in vivo data for the other compounds.
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CLONOSTACHYDIOL, A NOVEL ANTHELMINTIC MACRODIOLIDE FROM THE FUNGUS Clonostachys cylindrospora (STRAIN FH-A 6607)
SUSANNE GRABLEY, PETER HAMMANN, RALF THIERICKE, JOACHIM WINK, SIEGRID ...
1993 Volume 46 Issue 2 Pages
343-345
Published: February 25, 1993
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EXFOLIAMYCIN AND RELATED METABOLITES, NEW NAPHTHOQUINONE ANTIBIOTICS FROM Streptomyces exfoliatus
OLIVIER POTTERAT, HANS ZÄHNER, CORINNA VOLKMANN, AXEL ZEECK
1993 Volume 46 Issue 2 Pages
346-349
Published: February 25, 1993
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CHAO-MIN LIU, L. JENSEN, J. W. WESTLEY, D. SIEGEL
1993 Volume 46 Issue 2 Pages
350-352
Published: February 25, 1993
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SHINYA WAKUSAWA, KOHSEI INOKO, KEN-ICHI MIYAMOTO, SHINJI KAJITA, TAKAA ...
1993 Volume 46 Issue 2 Pages
353-355
Published: February 25, 1993
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II. STRUCTURE DETERMINATION
HIROYUKI CHIBA, REI KANETO, HITOSI AGEMATU, NORIO SHIBAMOTO, TAKEO YOS ...
1993 Volume 46 Issue 2 Pages
356-358
Published: February 25, 1993
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HIDENORI OHKI, KOHJI KAWABATA, SHINYA OKUDA, TOSHIAKI KAMIMURA, KAZUO ...
1993 Volume 46 Issue 2 Pages
359-361
Published: February 25, 1993
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RICHARD J. ATKINS, ROGER J. PONSFORD, ANDREW V. SXACHULSKI
1993 Volume 46 Issue 2 Pages
362-365
Published: February 25, 1993
Released on J-STAGE: April 19, 2006
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