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ATSUSHI TAKAHASHI, KUNIMOTO HOTTAN, ORIKO SAITO, MOTO MORIOKA, YOSHIRO ...
1986 年 39 巻 2 号 p.
175-183
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
An actinomycete isolate designated as TS-1980 with multiple resistance to aminoglycoside antibiotics was found to produce novel antibiotics. The strain showed taxonomic features identical to the type strain of
Nocardiopsis mutabilis except for the temperature range for growth and the utilization of mannitol and raffinose. Based on the capability of growing at lower temperature range, the strain was named N. mutabilis subsp. cryophilis subsp. nov. Physico-chemical and biological characterization of a purified antibiotic revealed its novel polyamine-type nature with a broad antimicrobial activity. The antibiotic was named dopsisamine.
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MASAYUKYI AMATO, HIRONOBU IINUMA, HIROSHI NAGANAWA, YUHJI YAMAGISHI, M ...
1986 年 39 巻 2 号 p.
184-191
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
Valanimycin, a new azoxy antibiotic, was isolated from culture broths of a streptomycete. Valanimycin is an unstable oil at room temperature and active against some Gram-positive and Gram-negative bacteria, mouse leukemia L1210 cells in cultures, and prolongs the life span of mice inoculated with Ehrlich carcinoma or L1210.
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DISCOVERY, FERMENTATION, CULTURE CHARACTERIZATION AND BIOLOGICAL ACTIVITY
J. B. TUNAC, S. W. MAMBER, B. D. GRAHAM, W. E. DOBSON
1986 年 39 巻 2 号 p.
192-197
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
A novel phenazine antitumor antibiotic is described, produced by
Streptomyces lomondensis subsp.
galanosa NRRL 15738. The antibiotic is selectively active
versus the bacterium
Streptococcus pneumoniae (MIC <0.46 μg/ml); the antitumor activity
versus murine P388 leukemia is T/C 149.
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I. TAXONOMY, FERMENTATION, ISOLATION, AND PHYSICO-CHEMICAL AND BIOLOGICAL CHARACTERISTICS
MASANORI OKAMOTO, KEIZO YOSHIDA, MOTOAKI NISHIKAWA, TAKESHI ANDO, MORI ...
1986 年 39 巻 2 号 p.
198-204
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
A PAF antagonist, designated as FR-900452, was isolated from fermentation products of
Streptomyces phaeofaciens and the molecular formula was determined as C
22H
25N
3O
3S. The compound inhibited PAF-induced rabbit platelet aggregation with an IC
50 of 3.7×10
-7 M, but was much less active against collagen-, arachidonic acid- or ADP-induced aggregation (IC
50; 6.4×10
-5, >10
-4 or >10
-4 M, respectively).
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ITSUO KUROBANE, NORIHIRO ZAITA, AKIO FUKUDA
1986 年 39 巻 2 号 p.
205-214
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
Six strains of
Fusarium martii produced fusarubin and dihydrofusarubins A and B. Further examination of strains, T-77 and T-127, showed that four additional metabolites were produced. By
1H and
13C NMR spectral analyses, these additional metabolites have been identified as 3-
O-methyl and 3-
O-ethyl ethers of fusarubin and dihydrofusarubin A. The methyl ethers are new compounds and showed moderate cytostatic activity against mouse leukemia L1210 culture cells as well as moderate antibiotic activity against Gram-positive bacteria and fungi. 3-
O-Methyl and 3-
O-ethyl ethers of dihydrofusarubin A were converted non-enzymically to the respective ethers of fusarubin under alkaline conditions. Since in addition, only dihydrofusarubin derivatives were formed when an acidic pH was maintained in the culture, it can be concluded that only these are true metabolites of
Fusarium martii.
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V. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 3-[2-(2- AMINOTHIAZOL-4-YL)-( Z)-2-(O-SUBSTITUTED OXYIMINO)- ACETAMIDO]-1-(1H-TETRAZOL-5-YL)-2-AZETIDINONES HAVING VARIOUS FUNCTIONAL GROUPS AT C-4 POSITION OF β-LACTAM
CHOSAKU YOSHIDA, KIYOSHI TANAKA, RIKIZO HATTORI, YOSHIKAZU FUKUOKA, MI ...
1986 年 39 巻 2 号 p.
215-229
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
The synthesis and antibacterial activity of the 3-[2-(2-aminothiazol-4-yl)-(
Z)-2-(
O-substituted oxyimino)acetamido]-1-(1
H-tetrazol-5-yl)-2-azetidinones having various functional groups at C-4 position of β-lactam are described. These compounds exhibited a strong activity against a variety of Gram-negative bacteria including β-lactamase-producing strains. Among various C-4 substituents explored, the fluoromethyl and carbamoyloxymethyl moiety were found to increase the activity.
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I. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW UREIDOPENICILLIN DERIVATIVES HAVING CATECHOL MOIETIES
NOBUHIRO OHI, BUNYA AOKI, TEIZO SHINOZAKI, KANZI MORO, TAKAO NOTO, TOS ...
1986 年 39 巻 2 号 p.
230-241
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
The synthesis and antibacterial activity of new ureidopenicillin derivatives having catechol moieties in the 6-acyl side chain are described. These compounds showed remarkably strong activities against
Pseudomonas aeruginosa. Especially, 6-[(
R)-2-[3-(3, 4-dihydroxybenzoyl)-3-
methyl-1-ureido]-2-phenylacetamido]penicillanic acid (
7a) had the most potent activity
in vitro against Gram-negative bacteria, its activity being 30-60-fold greater than that of piperacillin against most strains of
P. aeruginosa.
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II. EFFECT ON ANTIBACTERIAL ACTIVITY OF UREIDO NSUBSTITUENTS IN THE 6-[(R)-2-[3-(3, 4- DIHYDROXYBENZOYL)-1-UREIDO]-2- PHENYLACETAMIDO]PENICILLANIC ACIDS
NOBUHIRO OHI, BUNYA AOKI, KANZI MORO, TOSHIHIKO KUROKI, NAOYUKI SUGIMU ...
1986 年 39 巻 2 号 p.
242-250
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
The synthesis and the relationship between
in vitro and
in vivo activities of 6-[(
R)-2-[3-(3, 4-dihydroxybenzoyl)-3-R
1-1-ureido]-2-phenylacetamido]penicillanic acids having C
2-8 alkyl or substituted alkyl groups as the substituents (R
1) are described. In this series, 6-[(
R)-2-[3-(3, 4-dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido]penicillanic acid (1b, AO-1100) showed the most potent protective effect on mice in experimental
Pseudomonas aeruginosa infections, although it did not have the strongest
in vitro activity among the penicillins we synthesized.
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7. DIHYDROSTREPTOMYCIN ANALOGUES
DANA L. DELAWARE, MAHENDRA S. SHARMA, BHASHYAM S. IYENGAR, WILLIAM A. ...
1986 年 39 巻 2 号 p.
251-258
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
Dihydrostreptomycin analogues with structural variations in their guanidino groups were prepared. The analogue with a methyl group on the guanidine at C-1 was nearly as active as dihydrostreptomycin against bacteria. However, the 2-imidazolin-2-ylamino substituent at C-1 eliminated activity. No analogue with a substituent on the C-3 guanidino group was active.
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ACID BY THE THIENAMYCIN PRODUCER, STREPTOMYCES CATTLEYA
MINORU SANADA, TETSUJI MIYANO, SHUICHI IWADARE, JOANNE M. WILLIAMSON, ...
1986 年 39 巻 2 号 p.
259-265
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
An antimetabolite, THX, was isolated from fermentation broths of the thienamycin producer,
Streptomyces cattleya, when the organism was grown in the presence of a fluorine-containing substrate. THX was subsequently identified as one of the four possible stereoisomers of 4-fluorothreonine. Inorganic fluoride or any one of a number of organofluorine compounds can be used as precursors of 4-fluorothreonine. In addition,
19F NMR has provided evidence that the organism synthesizes fluoroacetate under the same fermentation conditions. The in vitro antibacterial spectrum of 4-fluorothreonine is also presented.
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KARL-HEINZ MAURER, DIETER MECKE
1986 年 39 巻 2 号 p.
266-271
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
The production of the sesquiterpenoid antibiotic pentalenolactone in the producer strain
Streptomyces arenae TÜ 469 is controlled by the activity of the enzyme farnesylpyrophosphate cyclase. In contrast to the activity of this enzyme, the specific activities of all other enzymes of the mevalonoid pathway tested so far, proved to be not rate-limiting. Several metabolites of the pentalenolactone pathway were tested for inhibitory effects on the activity of the HMG-CoA reductase and farnesylpyrophosphate cyclase. The activity of the cyclase was inhibited by low concentrations of pentalenolactone and its derivatives, thus suggesting an end product inhibition of the starting enzyme of the pentalenolactone pathway. The activity of HMG-CoA reductase was not inhibited by pentalenene or any pentalenolactone- derivatives. According to these results, an end-product inhibition of the first enzyme which is specific for pentalenolactone synthesis seems to be a mechanism involved in the regulation of pentalenolactone biosynthesis.
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HIROSHI TAKESHIMA, AKIRA ENDO, KENJI WADA, TADASHI TANABE
1986 年 39 巻 2 号 p.
275-280
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
In a previous study (A. ENDO,
et al., J. Antibiotics 38: 599-604, 1985), 2-alkyl glutarate and its derivatives isolated from cultures of
Gongronella butleri were shown to inhibit animal acetyl-CoA carboxylase. In the present communication, the inhibition of liver acetyl-CoA carboxylase was investigated with several 2-alkyl glutarate and 2-alkyl succinate analogs. Their inhibitory potency increased with the chain length of the alkyl moiety, and 2-tetradecanylglutarate was most potent among the inhibitors tested. Kinetic analysis indicated that inhibition by 2-tetradecanylglutarate was non-competitive with respect to the substrates, ATP, HCO
3-and acetyl-CoA, and competitive with respect to the allosteric regulator citrate, giving a
Ki value of 40 μM. Sucrose density gradient centrifugation analysis showed that the citrate-induced polymerization of the enzyme was inhibited by 2-tetradecanylglutarate.
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DONALD B. BOYD, JOHN L. OTT
1986 年 39 巻 2 号 p.
281-285
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
Recent work has shown that the activity of cephalosporins in inhibiting exocellular DD-peptidases from
Streptomyces R61 and
Actinomadura R39 are, at best, only poorly related to minimum inhibitory concentrations against pathogenic isolates. Taking into account the rate at which cephalosporins diffuse through porin channels, such as exist in certain Gram-negative organisms, does not help in establishing a relationship between MIC data and the kinetic data on the model enzymes. Most published cell wall permeability studies, the porin ones being a principal exception, have not examined long enough series of structurally related compounds to establish property-activity relationships.
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HIROYUKI OSADA, KIYOSHI ISONO
1986 年 39 巻 2 号 p.
286-293
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
An ascamycin dealanylating enzyme (Xc-aminopeptidase) has been isolated from
Xanthomonas citri and characterized as a proline iminopeptidase of molecular weight of 38, 000 (H. OSADA & K. ISONO, Biochem. J. 233: 459-463, 1986). Immunological studies have shown that all the mammalian cells tested possess a closely-related enzyme(s) on their cell membranes. This enzyme is more active in transformed cells than in nontransformed cells. A decreased
ratio of ID
50 (ascamycin/dealanylascamycin based on [
35S]methionine uptake) in transformed cells compared with the nontransformed cell can be explained on the basis of the conversion of ascamycin to dealanylascamycin by the enzyme. It is suggested that ascamycin cannot be transported through mammalian cell membranes but dealanylascamycin can permeate; a similar situation exists in prokaryotic cells.
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YUJI WATANABE, SHUICHI TAWARA, YASUHIRO MINE, HIROYUKI KIKUCHI, SACHIK ...
1986 年 39 巻 2 号 p.
294-303
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
The interactions between subinhibitory concentrations of cephalosporins and polymorphonuclear leukocytes in the killing of a strain of
Escherichia coli are described and an attempt is made to define the responsible mechanism. Ceftizoxime was the most potent agent tested. Pretreatment of the
E. coli strain with subinhibitory concentrations of ceftizoxime increased the susceptibility to both; phagocytic killing activity of the polymorphonuclear leukocytes and bactericidal activities of the oxygen metabolites and the granule extracts. A most interesting result was the increased susceptibility of the ceftizoxime-treated
E. coli to killing by β-glucuronidase which normally is not bactericidal. It is suggested that the augmented killing could be due to bacteriolysis by β-glucuronidase.
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MINORU SANADA, TETSUJI MIYANO, SHUICHI IWADARE
1986 年 39 巻 2 号 p.
304-305
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
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II. INHIBITION OF REVERSE TRANSCRIPTASE ACTIVITY
HIROMASA OKADA, HIROYUKI MUKAI, YOSHIO INOUYE, SHOSHIRO NAKAMURA
1986 年 39 巻 2 号 p.
306-308
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
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SATOSHI OMURA, HARUO TANAKA, HIROSHI KUGA, NOBUTAKA IMAMURA
1986 年 39 巻 2 号 p.
309-310
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
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MITSUYUKI HOTTA, YOICHI HAYAKAWA, KAZUO FURIHATA, AKIRA SHIMAZU, HARUO ...
1986 年 39 巻 2 号 p.
311-313
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
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HIKARU NAKAMURA, YOICHI IITAKA, MASAYA IMOTO, KUNIO ISSHIKI, HIROSHI N ...
1986 年 39 巻 2 号 p.
314-315
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー
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TAKAYOSHI OKABE, KOKICHI SUZUKI, HIDEO SUZUKI, YOSHIO INOUYE, SHOSHIRO ...
1986 年 39 巻 2 号 p.
316-317
発行日: 1986年
公開日: 2006/04/19
ジャーナル
フリー