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I. TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION
YOSHIO KURODA, MASAKUNI OKUHARA, TOSHIO GOTO, MICHIO YAMASHITA, EIKO I ...
1980 Volume 33 Issue 3 Pages
259-266
Published: 1980
Released on J-STAGE: April 12, 2006
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A strain of
Streptomyces, isolated from a soil sample and identified as
Streptomyce xanthocidicus, has been found to produce FR-900148, a new antibiotic containing chlorine in its molecule. The antibiotic inhibits both Gram-positive and negative bacteria. However, it is not effective against wild type of Pseudomonas aeruginosa. Its antibacterial action is considered to result from cell wall synthesis inhibition since it causes spheroplast formation from susceptible cells.
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II. STRUCTURE DETERMINATION OF FR-900148
YOSHIO KURODA, MASAKUNI OKUHARA, TOSHIO GOTO, MASANORI OKAMOTO, MICHIO ...
1980 Volume 33 Issue 3 Pages
267-271
Published: 1980
Released on J-STAGE: April 12, 2006
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The structure of FR-900148, a new antibiotic produced by a strain of
Streptomyces Xanthocidicus, has been established as 1-N-valyl-3-chloro-2, 5-dihydro-5-oxo-1H-pyrrole-2-carboxylic acid on the basis of spectroscopic and chemical evidence.
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I. TAXONOMY AND FERMENTATION OF THE ORGANISM, AND ISOLATION AND CHARACTERIZATION OF THE ANTIBIOTIC
YOSHIO KURODA, TOSHIO GOTO, MASANORI OKAMOTO, MICHIO YAMASHITA, EIKO I ...
1980 Volume 33 Issue 3 Pages
272-279
Published: 1980
Released on J-STAGE: April 12, 2006
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A strain of
Streptomyces, isolated from a soil sample and identified as
Streptomyces unzenensis sp. nov. has been found to produce FR-900137, an interesting new antibiotic, containing phosphorus in its molecule. The antibiotic, obtained as white powder, was shown to inhibit a wide variety of Gram-positive and Gram-negative bacteria except
Pseudomonas aeruginosa.
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II. STRUCTURE DETERMINATION OF FR-900137
YOSHIO KURODA, HIROKAZU TANAKA, MASANORI OKAMOTO, TOSHIO GOTO, MASANOB ...
1980 Volume 33 Issue 3 Pages
280-283
Published: 1980
Released on J-STAGE: April 12, 2006
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The structure of FR-900137, a new antibiotic produced by a new strain of
Streptomyces has been established as methyl hydrogen N
1-methyl N
2-(L)-leucyl phosphorohydrazidate on the basis of spectroscopic and chemical evidence.
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I. 4″-O-ACYL ANALOGS OF DELTAMYCINS
YASUTAKA SHIMAUCHI, KOSUMI HORI, MICHIKO SAKAMOTO (nee HASEGAWA), YOSH ...
1980 Volume 33 Issue 3 Pages
284-292
Published: 1980
Released on J-STAGE: April 12, 2006
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Using 4"-O-deacyldeltamycin as a starting material, various 4"-O-acyl derivatives were chemically synthesized by the following scheme: 2'-O-acetylation→4"-O-acylation→2'-O-deacetylation. 4"-O-Deacyldeltamycin is produced during the fermentation of deltamycin producing organisms or can be prepared by the biological deacylation of the deltamycins. 4"-O-Phenylacetyl-4"-O-deacyldeltamycin (PAD) showed good activity against various bacteria and mycoplasma. Among
para-substituted PAD derivatives, NPAD (
p-nitrophenyl-acetyl-) and SPAD (
p-methylsulfonylphenylacetyl-) showed increased potency as compared to PAD against certain bacteria. The PAD was evaluated by
in vivo experiments for plasma levels in mice and dogs and curative activity on the infected mice with
Staphylococcus aureus Smith by subcutaneous or oral administration.
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KAZUHIKO OKAMURA, MICHIKO SAKAMOTO, TOMOYUKI ISHIKURA
1980 Volume 33 Issue 3 Pages
293-302
Published: 1980
Released on J-STAGE: April 12, 2006
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Inhibition of
Proteus vulgaris β-lactamase by a new β-lactam antibiotic, PS-5 was studied kinetically. There were two stages of inhibition. In the early stage, PS-5 inhibited the β-lactamase by formation of a MICHAELIS-complex, and showed a competitive inhibition pattern with
Ki-value of 0.22 μM (substrate, cephaloridine). After the formation of a MICHAELIS-complex between PS-5 and the enzyme, PS-5 showed a characteristic progressive inhibition pattern with time. Maximum inactivation was obtained after several minutes of preincubation of the enzyme with PS-5; as hydrolysis of PS-5 progressed, the enzyme activity was gradually recovered. Reactivation by an excess of substrate (cephaloridine) was not substantially realized in the presence of PS-5. PS-5 was very slowly hydrolyzed by the enzyme, showing a triphasic pattern in its reaction curve.
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TAKAYOSHI HIDAKA, KAZUHIKO KATAYAMA, KATSUJI YAMASHITA, TOSHIAKI YAMAS ...
1980 Volume 33 Issue 3 Pages
303-309
Published: 1980
Released on J-STAGE: April 12, 2006
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Single intraperitoneal and intravenous injections of isocoformycin at 1, 200 mg/kg did not cause the death of mice. Isocoformycin which inhibited adenosine deaminase enhanced significantly the toxicity of formycin A and ara-A at various combination ratios. Isocoformycin potentiated antitumor activity of formycin A and ara-A against L1210 leukemia. Formycin A and ara-A disappeared rapidly from the blood and tissues and could not be found in any tissues even 0.5 hour after a single intraperitoneal injection. However, when used in combination with isocoformycin both were detected in the blood and tissues, especially at high concentration in liver and kidney. These indicate that the deamination of formycin
A and ara-A is blocked by isocoformycin
in vivo.
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HITOSHI KOJO, YASUTAKA SHIGI, MINORU NISHIDA
1980 Volume 33 Issue 3 Pages
310-316
Published: 1980
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A novel method is described which allows estimation of the outer membrane permeability to β-lactamase-stable β-lactams by determining antibiotic concentrations in the periplasm. The method is based on measurement of the inhibiting activity of β-lactamase-stable β-lactams on the hydrolysis of a substrate by periplasmic β-lactamase. Application of the method to carbenicillin revealed that the high level of resistance to carbenicillin of an
Escherichia coli strain acquiring the plasmid encoding ampicillin resistance resulted from the poor ability of carbenicillin to penetrate the outer membrane of
E. coli.
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CEPHALOSPORIN DERIVATIVES
HITOSHI KOJO, YASUTAKA SHIGI, MINORU NISHIDA
1980 Volume 33 Issue 3 Pages
317-321
Published: 1980
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The ability of ceftizoxime to penetrate the outer membrane was compared with those of five other new cephalosporins: cefotiam, cefuroxime, cefotaxime, cefmetazole and cefoxitin, using a clinical isolate of
Enterobacter cloacae as a test strain. Estimation of permeability was performed by a method utilizing the inhibitory activities of the cephalosporins against β-lactamase located in the periplasm . Of the cephalosporins tested, both ceftizoxime and cefmetazole gave remarkably high concentrations in the periplasm, several times higher than those of cefotaxime and cefoxitin and ten or more times higher than those of cefuroxime
and cefotiam. The approximate permeability coefficient of ceftizoxime was also several times higher than those of cefotiam and cefmetazole and over ten times higher than those of cefoxitin, cefuroxime and cefotaxime.
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J. A. CAMPILLO, A. A. DOMINGUEZ-GIL, M. CEPEDA, A. DOMINGUEZ-GIL
1980 Volume 33 Issue 3 Pages
322-327
Published: 1980
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The pharmacokinetics of cefamandole have been studied in rabbits with normal renal function and varying degrees of renal impairment caused experimentally, by uranyl nitrate, after i.v. administration of a single dose of 30 mg/kg of the antibiotic. The plasma concentrations of cefamandole 80 minutes after administration were 3 μg/ml in normal rabbits reaching 90 μg/ml at 9 hours in the case of terminal renal impairment. With respect to the pharmacokinetic parameters established in rabbits with normal renal function, the following modifications may be observed in the case of rabbits with renal impairment: α, β, K
12, K
21, K
13, V
c and V
p are decreased, while there is an increase in t
1/2α, t
1/2β and (AUC)
∞0. inear relationships have been established between log α and log β, respectively, and serum creatinine. Biliary excretion of cefamandole is increased parallel to the increase in the degree of renal impairment, there being a linear relationship between the percentage excreted of the antibiotic and serum creatinine. The values of K
B fall from 0.57 h-
1 in rabbits with normal renal function, to 0.26 h-
1 in rabbits with severe renal impairment.
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T. K. MANDAL, S. N. CHATTERJEE
1980 Volume 33 Issue 3 Pages
328-333
Published: 1980
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AKIRA ENDO
1980 Volume 33 Issue 3 Pages
334-336
Published: 1980
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SATOSHI YAGINUMA, MATSUHISA INOUE, SUSUMU MITSUHASHI
1980 Volume 33 Issue 3 Pages
337-341
Published: 1980
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YOSHIO KOIDE, Fumio ISHII, KATSUMI HASUDA, YASUO KOYAMA, KIYOTO EDO, S ...
1980 Volume 33 Issue 3 Pages
342-346
Published: 1980
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KIYOTO EDO, SHIGERU KATAMINE, FUMIO KITAME, NAKAO ISHIDA, YOSHIO KOIDE ...
1980 Volume 33 Issue 3 Pages
347-351
Published: 1980
Released on J-STAGE: April 12, 2006
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