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I. DISCOVERY, PRODUCTION AND BIOLOGICAL ACTIVITIES
LOUIS J. NISBET, RAJ J. MEHTA, YONG OH, CHARLES H. PAN, CLAIRE G. PHEL ...
1985 年 38 巻 2 号 p.
133-138
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
Chlorocardicin is a new monocyclic β-lactam produced by a
Streptomyces sp. It is structurally related to nocardicin A but differs in having a
m-chloro substituent on the
p-hydroxyphenylglycine unit. The biological activity of chlorocardicin was similar to nocardicin A but the former showed less antagonism in complex media. Moderate
in vitro activity was Observed against Enterobacteriaceae and
Pseudomonas aeruginosa. Chlorocardicin showed low activity against
Staphylococcus aureus whereas nocardicin A was inactive. Both compounds Were shown to be strongly potentiated by antibiotics that inhibit peptidoglycan biosynthesis and Were antagonized by selected L-and D-amino acids.
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II. ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE DETERMINATION
JAMES A. CHAN, ELVA A. SHULTIS, JOHN J. DINGERDISSEN, CHARLES W. DEBRO ...
1985 年 38 巻 2 号 p.
139-144
発行日: 1985年
公開日: 2006/04/19
ジャーナル
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Chlorocardicin, a novel monocyclic β-lactam, was isolated from the fermentation broth of a
Streptomyces sp. by the use of non-ionic porous resin and reverse phase chromatography. This chlorine-containing antibiotic is structurally related to nocardicin A. Its physico-chemical characteristics and detailed NMR analysis are described.
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H. IRSCHIK, R. JANSEN, G. HÖFLE, K. GERTH, H. REICHENBACH
1985 年 38 巻 2 号 p.
145-152
発行日: 1985年
公開日: 2006/04/19
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From the culture broth of the myxobacterium,
Corallococcus (Myxococcus) coralloides, three new antibiotics have been isolated: corallopyronin A, B and C. The compounds, which are chemically related to the recently discovered myxopyronins, act mainly on Gram-positive bacteria, with MIC values between 0.1 and 10 μg/ml, and only exceptionally or at much higher concentrations (MIC values; 100 and more μg/ml) on Gram-negatives. They do not inhibit eukaryotic organisms and show no toxicity for mice (sc). The corallopyronins appear to block specifically eubacterial RNA polymerase.
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I. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES
HIROSHI OGAWARA, KEIJIRO UCHINO, TETSU AKIYAMA, SHUN-ICHI WATANABE
1985 年 38 巻 2 号 p.
153-156
発行日: 1985年
公開日: 2006/04/19
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A new 5'-nucleotidase inhibitor named nucleoticidin was produced by
Pseudomonas sp. YM-3229G. It was isolated from a fermentation broth by trichloroacetic acid extraction, ethanol precipitation and Dowex 1 and DEAE-52 column chromatography. It inhibited 5'-nucleotidase activity of snake venom and rat liver membrane. It also showed antitumor activity against solid type Sarcoma 180.
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II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE ELUCIDATION
KEIJIRO UCHINO, HIROSHI OGAWARA, TETSU AKIYAMA, AKIRA FUKUCHI, SHOJI S ...
1985 年 38 巻 2 号 p.
157-160
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
A novel 5'-nucleotidase inhibitor, named nucleoticidin, was isolated from a fermentation broth of
Pseudomonas sp. The molecular weight was estimated by gel filtration to be over 1, 000, 000. Nucleoticidin is composed of D-glucose and n-mannose at a molar ratio of 1.7 to 1.0. Combined analyses using chemical and physico-chemical methods, such as gas liquid chromatography and mass fragmentography, revealed that nucleoticidin has a structural unit with mannosyl residues at the terminal of a (1→4) linked D-glucosyl main chain with β-configuration.
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MICHAEL A. GOETZ, PAMELA A. MCCORMICK, RICHARD L. MONAGHAN, DAN A. OST ...
1985 年 38 巻 2 号 p.
161-168
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
A new antiparasitic macrolide, L-155, 175, produced by a strain of
Streptomyces hygroscopicus, has been isolated ; its structure was determined by physico-chemical means. It is active against the tapeworm
Hymenolepis diminuta in rats.
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I. MASS SPECTROMETRIC ANALYSIS OF DODECAHYDROAMPHOTERICIN A
PAWEL SOWINSKI, PAWEL KOLODZIEJCZYK, EDWARD BOROWSKI
1985 年 38 巻 2 号 p.
169-174
発行日: 1985年
公開日: 2006/04/19
ジャーナル
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Amphotericin A had been transformed into dodecahydroamphotericin A by hydrogenation. Subsequently, the product obtained was reduced with metal borohydrides or borodeuterides and derivatized to volatile compounds which were analyzed by mass spectrometry.
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II. THE COMPLETE STRUCTURE OF THE ANTIBIOTIC
PAWEL SOWINSKI, JAN K. PAWLAK, EDWARD BOROWSKI, TAKASHI IWASHITA
1985 年 38 巻 2 号 p.
175-180
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
The structure of amphotericin A without the configuration of asymmetric carbon atoms has been elucidated. The stereochemistry of the sugar moiety has been determined. On the basis of homoscalar correlated 2D
1H spectra of amphotericin A the position of the hemiketal moiety has been located, and the chemical shifts of all the protons in the antibiotic molecule have been determined.
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ALINE COLLINE, JACQUES BOLARD, LAURENT CHINSKY, JIN-RUI FANG, KENNETH ...
1985 年 38 巻 2 号 p.
181-185
発行日: 1985年
公開日: 2006/04/19
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The Raman spectra of the polyene antibiotic nystatin have been investigated between 1500 and 1650cm
-1. Only one band is observed in the resonance Raman spectra obtained with a 3045 Å excitation radiation. Two major bands are observed in the preresonance spectra of pure nystatin obtained with a 4545 Å excitation. A supplementary band at 1557cm
-1 observed in the preresonance spectra of samples of commercial origin is ascribed to the presence of heptaene impurities, the Raman spectra of which are preferentially enhanced by resonance, owing to the closer proximity of their absorption to the excitation radiation.
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V. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 3'-OR 4'''-DE-N-METHYLSPIRAMYCIN I AND THEIR N-SUBSTITUTED DERIVATIVES
HIROSHI SANO, HARUO TANAKA, KINYA YAMASHITA, RYO OKACHI, SATOSHI OMURA
1985 年 38 巻 2 号 p.
186-196
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
The 3'- and 4'''-de-
N-methylspiramycins were synthesized selectively, and then were converted to various
N-substituted derivatives. 4'''-De-
N-methyl derivatives were more active than 3'-de-
N-methyl ones. Among the derivatives, 4'''-
N-Fmoc-glycyl and 4'''-
N-benzyl-4'''-de-N-methylspiramycin I were the most active
in vitro, and were comparable to spiramycin I. 4'''-De-
N-methylspiramycin I was about half as active as spiramycin I
in vivo.
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II. SPECTINOMYCIN C-3'-MODIFICATION VIA DIAZOKETONE INTERMEDIATES
RICHARD C. THOMAS, EDWARD L. FRITZEN
1985 年 38 巻 2 号 p.
197-207
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
The C-3'-carbonyl group of
N-protected spectinomycin is efficiently converted into a diazo group
via base treatment of the corresponding tosylhydrazone. The diazo group imparts a new synthetically useful reactivity pattern on the sugar ring of the molecule. The synthesis of C-3'-deoxo-, monohalo- and dihalospectinomycins
via the intermediacy of these diazo compounds is described. The reduced bioactivity of these analogs as compared to the parent and the C-3'-dihydro and aminospectinomycins established the need for hydrogen bonding groups in this region of the molecule for good activity, further refining the structure activity relationships in the spectinomycin series.
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III. SPECTINOMYCIN ANALOGS WITH C-3'-BRANCHED CHAIN SUGARS
RICHARD C. THOMAS, EDWARD L. FRITZEN
1985 年 38 巻 2 号 p.
208-219
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
A variety of C-3'-branched chain analogs of spectinomycin has been synthesized
via the intermediacy of spectinomycin derived diazoketones.
In vitro antibacterial assay of these compounds has underscored the importance of hydrogen bonding functional groups in this region of the molecule. The most potent of these analogs had activity greater than or equal to the parent.
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KANKI KOMIYAMA, KENJI OKADA, HIROFUMI OKA, SHIGERU TOMISAKA, TETSUJI M ...
1985 年 38 巻 2 号 p.
220-223
発行日: 1985年
公開日: 2006/04/19
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The structure of a new antitumor antibiotic, kazusamycin produced by
Streptomyces sp. No. 81-484, was determined on the basis of its spectral and chemical properties. Kazusamycin has a structure characteristic of an unsaturated, branched-chain fatty acid with a terminal δ-lactone ring.
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KANKI KOMIYAMA, KENJI OKADA, YUMIKO HIROKAWA, KAZUAKI MASUDA, SHIGERU ...
1985 年 38 巻 2 号 p.
224-229
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
The antitumor activity of a new antibiotic, kazusamycin, against various murine tumors was studied by various treatment schedules. Single, intermittent, and successive injections of the antibiotic were almost equally effective against Ehrlich carcinoma, IMC carcinoma and sarcoma 180 tumor, but successive injections showed more efficacy than the other schedules against Meth A fibrosarcoma and Lewis lung carcinoma. Interestingly, there was no clear dose response for the efficacy of kazusamycin on murine tumors. When HeLa cells were exposed to kazusamycin for 72 hours
in vitro, the IC
50 value was about 1ng/ml, however the cytotoxicity of the antibiotic depended on the incubation time.
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TAKAYOSHI OKABE, BAO DING YUAN, FUJIO ISONO, ISAO SATO, HIDESUKE FUKAZ ...
1985 年 38 巻 2 号 p.
230-235
発行日: 1985年
公開日: 2006/04/19
ジャーナル
フリー
An antibiotic, identical with naphthomycin, was isolated from a soil
Streptomyces. The antibiotic displayed significant therapeutic activity by ip administration against murine tumors : Ehrlich carcinoma and IMC carcinoma implanted ip. The maximum increase of life-span was more than 169% in Ehrlich carcinoma, and 128% in IMC carcinoma. The antibiotic exhibited a potent cytotoxicity against murine leukemic cells : P388, L1210, and L5178Y. IC
50 was 0.4-1.3μg/ml in culture. The activity of naphthomycin was reversed by SH compounds : 2-mercaptoethanol, dithiothreitol, and glutathione. DNA and RNA syntheses were more markedly inhibited by naphthomycin than protein synthesis in L5178Y cells. Approximately 50% inhibition of nucleic acid syntheses was observed at an antibiotic concentration of 2μg/ml. Naphthomycin blocked alkaline phosphodiesterase obtained from L5178Y cells : IC
50 was
ca. 7.6μg/ml. The antibiotic neither caused metaphase arrest nor prevented tubulin polymerization. The results suggest that the mechanism of cytotoxicity of naphthomycin is the inhibition of various SH enzymes, particularly those involved in nucleic acid biosynthesis. The mode of action is unique in the ansamycin group of antibiotics.
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ANDREAS FREDENHAGEN, URS SÉQUIN
1985 年 38 巻 2 号 p.
236-241
発行日: 1985年
公開日: 2006/04/19
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The cytotoxicities of hedamycin and photohedamycin A as well as of kidamycin and isokidamycin were determined using HeLa cell cultures. Photohedamycin A proved to be 15 times less cytotoxic than hedamycin thus explaining the loss of biological activity observed for solutions of hedamycin left in daylight. The fact that photohedamycin A is less active than hedamycin, and isokidamycin less than kidamycin points to the important role the rings E and F play in the biological activity of hedamycin and kidamycin.
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GUY T. CARTER, AMEDEO A. FANTINI, JOHN C. JAMES, DONALD B. BORDERS, RI ...
1985 年 38 巻 2 号 p.
242-248
発行日: 1985年
公開日: 2006/04/19
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The biosynthetic origin of the carbon atoms in the chromophores of chrysomycins A and B was investigated in feeding experiments using
13C labeled acetates and propionate. A biosynthetic scheme is proposed involving the condensation and rearrangement of a decaketide intermediate which contains either propionate (chrysomycin A) or acetate (chrysomycin B) as the chain initiator.
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ISAMU SUZUKI, HISATO SENDA, TAKESHI YOKOTA
1985 年 38 巻 2 号 p.
249-258
発行日: 1985年
公開日: 2006/04/19
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The protective activity of cefbuperazone (T-1982) was compared with those of latamoxef, Cefotaxime, and cefmetazole against intraperitoneal and urinary tract infections in mice. In both tests, cefbuperazone manifested a higher activity than the other cephems against infections with
Escherichia coli and
Klebsiella pneumoniae. Cefbuperazone also showed a comparatively high degree of prophylactic effect; this activity was observed even when given 4 hours before bacterial challenge. The good
in vivo activity of cefbuperazone could not be explained by the differences between the antibiotics on the basis of the serum levels and
in vitro activity. Mice, treated with cefbuperazone, showed a statistically significant prolongation of survival time against intraperitoneal challenge with Candida a lbicans, but not when treated with the other cephems. This finding suggests that the host defense mechanisms stimulated by cefbuperazone may contribute to the good
in vivo activity of this antibiotic.
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2. SYNTHESIS AND ACTIVITY OF 23-EPI-25-DEACETYLRIFAMYCIN S
M. BRUFANI, G. CECCHINI, L. CELLAI, M. FEDERICI, M. GUISO, A. SEGRE
1985 年 38 巻 2 号 p.
259-262
発行日: 1985年
公開日: 2006/04/19
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SUSAN E. JENSEN, DONALD W. S. WESTLAKE, SAUL WOLFE
1985 年 38 巻 2 号 p.
263-265
発行日: 1985年
公開日: 2006/04/19
ジャーナル
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TAKESHI YAMADA
1985 年 38 巻 2 号 p.
266-269
発行日: 1985年
公開日: 2006/04/19
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NAOKI TSUJI, MASAAKI KOBAYASHI, YOSHIHIRO TERUI, KOICHI MATSUMOTO, YAS ...
1985 年 38 巻 2 号 p.
270-274
発行日: 1985年
公開日: 2006/04/19
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RAINER ALBERT, KARL DAX, ARNOLD E. STÜTZ, JOHANNES HILDEBRANDT
1985 年 38 巻 2 号 p.
275-278
発行日: 1985年
公開日: 2006/04/19
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YUJI MATSUHASHI, TAKESHI MURAKAMI, CHUHEI NOJIRI, HIROMI TOYAMA, HIROY ...
1985 年 38 巻 2 号 p.
279-282
発行日: 1985年
公開日: 2006/04/19
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HAMAO UMEZAWA, MASAAKI ISHIZUKA, TOMIO TAKEUCHI, FUMINORI ABE, KYUICHI ...
1985 年 38 巻 2 号 p.
283-284
発行日: 1985年
公開日: 2006/04/19
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