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I. PRODUCTION, ISOLATION, CHARACTERIZATION AND ANTITUMOR ACTIVITY
HIROAKI OHKUMA, FUMIHIDE SAKAI, YUJI NISHIYAMA, MASARU OHBAYASHI, HIDE ...
1980 Volume 33 Issue 10 Pages
1087-1097
Published: 1980
Released on J-STAGE: April 12, 2006
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A complex of the antitumor antibiotic BBM-928 was produced by an actinomycete strain No. G455-101. Four components, BBM-928 A, B, C and D, were isolated in crystalline form and characterized. They were shown to be cyclic depsipeptide antibiotics containing a quinoline nucleus as the chromophore. BBM-928 A is a monoacetyl derivative of BBM-928 B and a diacetyl derivative of BBM-928 C. BBM-928 components exhibit antimicrobial activity against Gram-positive and acid-fast bacteria. BBM-928 A is highly active in mice against various experimental tumors including leukemia P388, leukemia L1210, melanoma B16, LEWIS lung carcinoma and sarcoma 180. BBM-928 B is less active than BBM-928A, and BBM-928 C has no antitumor activity.
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II. TAXONOMIC STUDIES ON THE PRODUCING ORGANISM
KOJI TOMITA, YUTAKA HOSHINO, TAKASHI SASAHIRA, HIROSHI KAWAGUCHI
1980 Volume 33 Issue 10 Pages
1098-1102
Published: 1980
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An actinomycete strain No. G455-101 isolated from a soil sample collected in Luzon Island, Philippines produced a new antitumor antibiotic complex BBM-928. The organism was determined to be a new species of the genus
Actinomadura and designated Actinomadura luzonensis nov. sp. The type strain, No. G455-101, has been deposited under the number ATCC 31491.
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HIROICHI IKUSHIMA, EIKO IGUCHI, MASANOBU KOHSAKA, HATSUO AOKI, HIROSHI ...
1980 Volume 33 Issue 10 Pages
1103-1106
Published: 1980
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A new species of
Streptomyces is described and designated
Streptomyces auranticolor (FERM-P No. 5365) which produces new anticoccidial antibiotics, designated as WS-5995 A and WS-5995 B
1). The organism is characterized by gray spore mass color, spiral spore chain with smooth spores, non-chromogenic reaction, soluble pigment, and carbon utilization characteristics. It differs from previously described streptomycetes on the basis of carbon utilization, and pigment production.
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I. ISOLATION AND CHARACTERIZATION
HIROICHI IKUSHIMA, MASANORI OKAMOTO, HIROKAZU TANAKA, OSAMU OHE, MASAN ...
1980 Volume 33 Issue 10 Pages
1107-1113
Published: 1980
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WS-5995 A, B and C are produced by a new strain of
Streptomyces designated
Streptomyces auranticolor. These antibiotics were purified by solvent extraction followed by chromatography on silica gel and then crystallized. WS-5995 A (C
19H
12O
6, m.p., 289-291°C) and WS-5995 B (C
19H
14O
6, sublimation at 300°C) protect chickens from infection with
Eimeria
tenella, a species of coccidia, which produces morbidity or mortality in chickens. WS-5995 C (C
19H
14O
7, m.p., 288-290°C), a biologically inactive component, was found to be converted to WS-5995 A on treatment with trifluoroacetic anhydride.
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YUZURU IWAI, AKIRA NAKAGAWA, NORIAKI SADAKANE, SATOSHI OMURA, HITOSHI ...
1980 Volume 33 Issue 10 Pages
1114-1119
Published: 1980
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A new benzoquinonoid ansamycin, herbimycin B was isolated from the culture broth of
Streptomyces hygroscopicus No. AM-3672, a herbimycin A-producing strain. Herbimycin B showed potent anti-TMV activity. Herbicidal effect of herbimycin B was less than that of herbimycin A.
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YO TAKIGUCHI, HIROSHI MISHIMA, MICHIHISA OKUDA, MICHIYA TERAO, ATSUSHI ...
1980 Volume 33 Issue 10 Pages
1120-1127
Published: 1980
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A search for novel insecticides has yielded the milbemycins, a new family of macrolide antibiotics with insecticidal and acaricidal activity. They are produced in submerged cultures of
Streptomyces hygroscopicus subsp.
aureolacrimosus. Fermentation studies on the strain were conducted in shaken flasks and 30-liter jar fermentors. From the culture broth 13 milbemycins were purified to homogeneity by column and thin-layer chromatography on silica gel and alumina. Physico-chemical data, such as mass spectra, UV and IR absorption spectra, optical rotations and melting points of the milbemycins are described.
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NORIO SHIBAMOTO, AKIHIKO KOKI, MASAYOSHI NISHINO, KOSUMI NAKAMURA, KOH ...
1980 Volume 33 Issue 10 Pages
1128-1137
Published: 1980
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Antibiotics PS-6 and PS-7 which are shown to be 5
R, 6
R-3-(2-acetamido)ethylthio-6-isopropyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid and 5
R, 6
R-3-(
E)-(2-acetamido) vinylthio-6-ethyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid respectively, are new β-lactam compounds isolated from fermentation broths of
Streptomyces cremeus subsp.
auratilis A271,
S. fulvoviridis A933,
S. olivaceus ATCC 31126 and
S. flavogriseus NRRL 8139. Fermentation, isolation, physicochemical properties and structures of antibiotics PS-6 and PS-7 are described.
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MICHIKO SAKAMOTO, NORIO SHIBAMOTO, HIROSHI IGUCHI, KAZUHIKO OKAMURA, S ...
1980 Volume 33 Issue 10 Pages
1138-1145
Published: 1980
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Biological properties of two new β-lactam antibiotics, PS-6 and PS-7, containing the carbapenem nucleus were studied. The
in vitro activities of PS-6 and PS-7 were tested against Bclinical isolates of Gram-positive and Gram-negative bacteria in comparison with those of cefazolin, ampicillin and PS-5. In general, the antibacterial spectra of PS-6 and PS-7 were similar to that of PS-5. PS-7 was slightly less active than PS-5 and ABPC against
Staphylococcus aureus. Clinical isolates of Gram-negative bacteria were found to be 2- to 8-fold more resistant to PS-6 than to PS-5, while PS-7 was 2-fold more active than PS-5 against
Enterobacter, Klebsiella, Proteus, Serratia and
Escherichia coli. The therapeutic effect of PS-6 seemed slightly less than that of PS-5 in an experimental infection with
Staph. aureus Smith in mice.
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FRANCOISE PEYPOUX, FRANCOISE BESSON, GEORGES MICHEL, CHARLES LENZEN, L ...
1980 Volume 33 Issue 10 Pages
1146-1149
Published: 1980
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The characterization of an antibiotic isolated from a strain of
Bacillus subtilis revealed that this compound is a new antifungal antibiotic of the iturin group. It contains a lipid moiety which is a mixture of 3-amino 12-methyl tridecanoic acid (40%) and 3-amino 12-methyl tetradecanoic acid (60%) and a peptide moiety: L-Asp
1, D-Asp
1, L-Glu
1, L-Pro
1, D-Ser
1, L-Thr
1 and D-Tyr
1. These two moieties are joined by a threonyl-β-aminoacid linkage.
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AKIHIRO YOSHIMOTO, YASUE MATSUZAWA, TOSHIKAZU OKI, HIROSHI NAGANAWA, T ...
1980 Volume 33 Issue 10 Pages
1150-1157
Published: 1980
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New anthracycline antibiotics, 1-hydroxy-13-dihydrodaunomycin and N-formyl-1-hydroxy-13-dihydrodaunomycin were biosynthesized by a blocked mutant of
Streptomyces coeruleorubidus MEt30-A4 from ε-pyrromycinone or ε-isorhodomycinone.
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AKIHIRO YOSHIMOTO, TOSHIKAZU OKI, TOMIO TAKEUCHI, HAMAO UMEZAWA
1980 Volume 33 Issue 10 Pages
1158-1166
Published: 1980
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Baumycin-negative mutants of
Streptomyces coeruleorubidus ME130-A4 do not convert daunomycinone to daunomycin and baumycins. They biosynthesize daunomycin from aklavinone and ε-rhodomycinone, indicating the glycosidation of the aglycone before the synthesis of daunomycinone. The biosynthetic pathway from ε-rhodomycinone to daunomycin was further confirmed by studying the bioconversion of anthracyclinones and anthracyclines, which are presumed to be intermediates.
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JOHN M. OSTRANDER, LAURENCE H. HURLEY, A. GAVIN MCINNES, DONALD G. SMI ...
1980 Volume 33 Issue 10 Pages
1167-1171
Published: 1980
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Using
13C-NMR and mass spectral analysis we have demonstrated that the N-10 nitrogen of anthramycin is biosynthetically derived from the indole-nitrogen of tryptophan. Our experimental approach was to bring a
15N atom, which is derived from L-[indole-
15N]tryptophan, and a
13C atom which is derived from DL-[1-
13C]tyrosine, into adjacent positions of anthramycin. From resonance intensities and
13C-
15N spin-spin coupling in the
13C-NMR spectrum of didehydroanhydroanthramycin, a derivative of anthramycin, we could then determine the
13C enrichment at C-11 and the proportion of
13C bonded to
15N at N-10. These results when combined with mass spectral analysis and isotopic dilution measurements proved that the indole nitrogen of tryptophan was completely retained at N-10 of anthramycin.
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IS PROTEIN TURNOVER IN LEUPEPTIN PRODUCER CELLS AFFECTED BY LEUPEPTIN¿
KAYOKO SUZUKAKE, MASAHIKO TAKADA, MAKOTO HORI, HAMAO UMEZAWA
1980 Volume 33 Issue 10 Pages
1172-1176
Published: 1980
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There was no significant difference between the rates of protein degradation in cells of a
leupeptin-producing strain and that of a leupeptin-nonproducing strain, the latter being
derived from the former by mutation. Protein autodigestion in a cell homogenate of the
leupeptin producer was sensitive to EDTA and chymotrypsin and less sensitive to leupeptin.
On the contrary, protein degradation caused by exogenous trypsin in a similar homogenate
was highly sensitive to leupeptin. A labeling experiment with [
14C]-arginine of a culture of
the leupeptin producer strain revealed that leupeptin was accumulated mostly in the medium
and only slightly in the cells; the ratio between the amount in the medium and that in the
cells was about 250: 1. In contrast, leupeptin acid, the proximal intermediate having no
antiplasmin activity, showed a ratio of 5: 1.
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CEPHALOSPORIN DERIVATIVES IN THE FURYL SERIES CHEMICAL AND MICROBIOLOGICAL PROPERTIES
M. O. TINTI, P. FORESTA, E. QUARESIMA, P. DE WITT, M. T. RAMACCI
1980 Volume 33 Issue 10 Pages
1177-1182
Published: 1980
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The synthesis of a series of 7-acylamido cephalosporins having a substituted furyl moiety
in the side chain is described. These new cephalosporins were examined
in vitro for antibacterial
activity and evaluated for resistance to inactivation by β-lactamases.
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B. BALTZER, E. BINDERUP, W. VON DAEHNE, W. O. GODTFREDSEN, K. HANSEN, ...
1980 Volume 33 Issue 10 Pages
1183-1192
Published: 1980
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The principle of combining a β-lactam antibiotic with a β-lactamase inhibitor in a single
molecule functioning as pro-drug for the two active components is illustrated by the linked
esters
3and
4in which ampicillin and mecillinam, respectively, are combined with the β-lactamase
inhibitor penicillanic acid sulfone. It is shown that in man these esters are excellently
absorbed from the gastro-intestinal tract and after absorption hydrolyzed with simultaneous
liberation of the active components. As a result high blood and tissue levels of antibiotic
and β-lactamase inhibitor in a balanced ratio are attained. The advantages of "mutual
pro-drugs" over simple combinations are discussed.
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A. SANFILIPPO, C. DELLA BRUNA, L. MARSILI, E. MORVILLO, C. R. PASQUALU ...
1980 Volume 33 Issue 10 Pages
1193-1198
Published: 1980
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The biological properties of spiro-piperidyl-rifamycins, a new class of rifamycin antibiotics, are described. In these derivatives the positions 3 and 4 have been incorporated into an imidazolyl ring bearing a spiro-piperidyl group N substituted with linear and branched aliphatic chains. The
in vitro antibacterial activity against
Staphylococcus aureus and
Mycobacterium tuberculosis increases with the number of the carbon atoms in the linear side chain, whereas the inhibitory effect on
Escherichia coli is lowered. The antibacterial activity is only marginally
affected by branching of the side chain.
In vivo (experimental infections of mice) the optimal therapeutic activity againt
M. tuberculosis is shown by compounds bearing 3-5 carbon atoms as a linear or branched side chain; in comparison with rifampicin, the potency of these derivatives is 2-3 times higher. The finding is in a good agreement with the exceptional tissue tropism, which seems to be a favourable property of this group of derivatives.
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AKIHIRO YOSHIMOTO, TOSHIKAZU OKI, HAMAO UMEZAWA
1980 Volume 33 Issue 10 Pages
1199-1201
Published: 1980
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DAVID J. NEWMAN, RAJANIKANT J. MEHTA, BETTY ANNE BOWIE, CLAUDE H. NASH ...
1980 Volume 33 Issue 10 Pages
1202-1203
Published: 1980
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RODERICH BRANDSCH, ELENA HEFCO, CSöNGE BRANDSCH, PINCU ROTINBERG, ...
1980 Volume 33 Issue 10 Pages
1204-1205
Published: 1980
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TOMOYOSHI YANAGIDA, HIROSHI OGAWARA
1980 Volume 33 Issue 10 Pages
1206-1207
Published: 1980
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HANS-JÜRGEN PLATTNER, BARBARA STENS, HANS DIEKMANN, IBRAHIM R. SH ...
1980 Volume 33 Issue 10 Pages
1208-1209
Published: 1980
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HIROSHI KASE, TAKAO IIDA, YOSHIHIRO ODAKURA, KUNIKATSU SHIRAHATA, KIYO ...
1980 Volume 33 Issue 10 Pages
1210-1212
Published: 1980
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