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MASAKAZU URAMOTO, CHANG-JIN KIM, KAZUO SHIN-YA, HIROO KUSAKABE, KIYOSH ...
1991 Volume 44 Issue 4 Pages
375-381
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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A new nucleotide antibiotic, phosmidosine was isolated from a culture filtrate of a newly isolated streptomycete identified as
Streptomyces sp. RK-16. HRFAB-MS and elemental analysis established the molecular formula of C
16H
24N
7O
8P.
1H,
13C and
31P NMR indicated the presence of a methyl phosphate group and UV spectra were similar to those of 8-hydroxyadenosine. The antibiotic inhibited spore formation of
Botrytis cinerea at the concentration of 0.25 μg/ml.
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OSAMU ANDO, HITOMI SATAKE, MUTSUO NAKAJIMA, AKIRA SATO, TAKEMICHI NAKA ...
1991 Volume 44 Issue 4 Pages
382-389
Published: April 25, 1991
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Synerazol, a new antifungal antibiotic, was isolated from cultured broth of
Aspergillus fumigatus SANK 10588. The structure was determined based on NMR and mass spectral evidences. Synerazol was found to be a related substance to pseurotin A. Synerazol was active against
Candida albicans and other fungi, and showed marked synergistic activity with azole-type antifungal agents.
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MASAMI ISHIBASHI, SHINJI FUNAYAMA, YUMI ANRAKU, KANKI KOMIYAMA, SATOSH ...
1991 Volume 44 Issue 4 Pages
390-395
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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Furaquinocins C, D, E, F, G and H, congeners of furaquinocins A and B, were isolated from the culture broth of
Streptomyces sp. KO-3988 and their structures have been determined on the basis of their spectroscopical and chemical properties. These antibiotics showed cytocidal activities against HeLa S3 and B16 melanoma cells
in vitro.
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RYUICHI SAWA, NAOKO MATSUDA, TAKESHI UCHIDA, TAKAKO IKEDA, TSUTOMU SAW ...
1991 Volume 44 Issue 4 Pages
396-402
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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A new antibiotic, dioxamycin (
1) was isolated from the culture broth of the strain MH406-SF1, which was closely related to
Streptomyces xantholiticus. This antibiotic was purified by countercurrent chromatography, column chromatography and preparative HPLC. The molecular formula of
1 was determined to be C
38H
40O
15 by HRFAB-MS. The structure was determined by spectral analysis of 2D NMR;
1H-
1H COSY,
13C-
1H COSY, long range
13C-
1H COSY (HMBC) and NOESY. The antibiotic is active
in vitro against Gram-positive bacteria and some tumor cells. Dioxamycin is a benz[α]anthraquinone antibiotic related to capoamycin.
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MINORU HANADA, HIROAKI OHKUMA, TERUO YONEMOTO, KOJI TOMITA, MASARU OHB ...
1991 Volume 44 Issue 4 Pages
403-414
Published: April 25, 1991
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Maduropeptin, a complex of new macromolecular antitumor antibiotics, is a metabolite of
Actinomadura madurae H710-49. The active components maduropeptins A
1, A
2 and B are acidic chromopeptides with MW of around 22, 500 and composed of 14 types of amino acids and an unstable chromophore. The antibiotics are active
in vitro against Gram-positive bacteria and highly cytotoxic to tumor cells. They produced significant prolongation of survival time of mice implanted with P388 leukemia and B16 melanoma.
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II. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF CEPHALOSPORINS WITH SUBSTITUTED 1, 3-DITHIETANE DIRECTLY ATTACHED TO THE C-3 POSITION
NORIAKI NAGANO, KOHJI NAKANO, TADAO SHIBANUMA, RYUICHIRO HARA
1991 Volume 44 Issue 4 Pages
415-421
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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Preparation of cephaloosporins bearing a 1, 3-dithietane ring attached to the C-3 position using intramolecular rearrangement are described. The diastereoisomers (
6a-I and
6a-II) were separated by silica gel column chromatography. These 3-[4-(carbamoyl carboxymethylene)-l, 3-dithietan-2-yl]cephems showed comparable activity against Gram-negative bacteria to that of ceftazidime.
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III. SYNTHESES AND ANTIBACTERIAL ACTIVITIES OF NEW 3-(1, 3-DITHIOLAN-2-YL)CEPHALOSPORINS, YM-22508, YM-16457 AND THEIR PRODRUG-TYPE ESTERS
NORIAKI NAGANO, MASATO SATOH, RYUICHIRO HARA
1991 Volume 44 Issue 4 Pages
422-428
Published: April 25, 1991
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The syntheses and biological activities of new 7-β-[(
Z)-2-(2-amino-4-thiazolyl)-2-hydroxy-iminoacetamido]-3-(l, 3-dithiolan-2-yl)-3-cephem-4-carboxylic acid (YM-22508,
1a), 7-β-[(
Z)-2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-(1, 3-dithiolan-2-yl)-3-cephem-4-carboxylic acid (YM-16457,
1d) and their prodrug-type esters are described. Among them, YM-22561 (
1c), the 1-acetoxyethyl ester of
1a, showed good
in vivo efficacy in mice against infections of
Staphylococcus aureus Smith,
Streptococcus pyogenes S 23 and
Escherichia coll NY-17 and a long plasma T
1/2 in mice.
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AKIKO KURAMOCHI-MOTEGI, HIROSHI KURAMOCHI, KATSUTOSHI TAKAHASHI, TOMIO ...
1991 Volume 44 Issue 4 Pages
429-434
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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Liblomycin (NK313) is a novel derivative of bleomycin (BLM) and peplomycin (PEP). The cell kill kinetics of NK313 on rat ascites hepatoma AH66 were compared with those of PEP. NK313 induced intracellular DNA cleavage and arrested cell cycle progression at the G
2 phase similarly to PEP. The cytocidal effect of NK313, however, was found to be different from that of PEP as described below: 1) The dose-survival curve for cells exposed to PEP for 1 hour was upward concave, whereas in case of NK313, the survival curve was linear. PEP was more effective to AH66 than NK313 at lower concentration, but at higher concentration, NK313 was much more effective. 2) The time-survival curve for cells treated with either NK313 or PEP was biphasic. NK313, however, did not induce temporary resistance of AH66 cells to NK313, while PEP induced resistance to PEP. 3) NK313 was effective against the cells which became temporarily resistant to PEP by the treatment of PEP. These differences suggest that NK313 might be of value to treat PEP-insensitive tumor cells.
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MATSUHISA INOUE, TETSUO MAEJIMA, SIGERU SANAI, RYOOICHI OKAMOTO, HAJIM ...
1991 Volume 44 Issue 4 Pages
435-440
Published: April 25, 1991
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A β-lactamase was purified from
Klebsiella oxytoca strain GN10650. The enzyme was chromosomally-mediated and gave a single protein band on polyacrylamide gel electrophoresis. Its pI was 5.34 and its MW was approximately 27, 000. The optimal pH and temperature were about 7.0 and 50°C, respectively. The specific activity of the enzyme was 1, 207 units per mg of protein for hydrolysis of penicillins and cephalosporins, including cefuroxime, cefotaxime, and aztreonam. The enzyme activity was inhibited by
p-chloromercuribenzoate, iodine, ferrous ion, and by clavulanic acid. Rabbit antibodies raised against the purified
K. oxytoca enzyme showed no cross-reactivity in neutralization tests with β-lactamases produced by other species of Gram-negative bacteria.
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IV. EFFECT OF FR-62765, A DERIVATIVE OF WF-3681, ON THE DIABETIC NEUROPATHY IN RATS
MOTOAKI NISHIKAWA, KEIZO YOSHIDA, MASANORI OKAMOTO, YOSHIKUNI ITOH, MA ...
1991 Volume 44 Issue 4 Pages
441-444
Published: April 25, 1991
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Pharmacokinetic properties of WF-3681 and FR-62765 in rats were examined. FR-62765 showed higher peak concentrations in the plasma and higher concentrations in the sciatic nerve than WF-3681 when each compound was administered orally to rats. We therefore evaluated FR-62765 in rats with diabetic neuropathy. As a result, FR-62765 at 32mg/kg/day administered for 3 weeks to streptozotocin-induced diabetic rats significantly prevented the accumulation of sorbitol in the sciatic nerve and the reduction of motor nerve conduction velocity in the tail. From these results it was concluded that the aldose reductase inhibitor FR-62765 might be a useful drug for diabetic neuropathy.
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TOHRU YASUZAWA, YUTAKA SAITOH, MICHIO ICHIMURA, ISAMI TAKAHASHI, HIROS ...
1991 Volume 44 Issue 4 Pages
445-447
Published: April 25, 1991
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CLARENCE J. MARING, LESLIE A. FREIBERG, PAUL A. LARTEY, DAVID J. GRAMP ...
1991 Volume 44 Issue 4 Pages
448-450
Published: April 25, 1991
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HIROAKI IWASAKI, KEI-ICHI KAMISANGO, HITOSHI KUBONIWA, HIROSHI SASAKI, ...
1991 Volume 44 Issue 4 Pages
451-452
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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YOKO IKEDA, SHINICHI KONDO, HIROSHI NAGANAWA, SEIKO HATTORI, MASA HAMA ...
1991 Volume 44 Issue 4 Pages
453-455
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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KUNIAKI TATSUTA, YOSHIHISA NIWATA, KAZUO UMEZAWA, KAZUNOBU TOSHIMA, MA ...
1991 Volume 44 Issue 4 Pages
456-458
Published: April 25, 1991
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MAKOTO SUNAGAWA, HARUKI MATSUMURA, TAKAAKI INOUE, MASATOMO FUKASAWA, M ...
1991 Volume 44 Issue 4 Pages
459-462
Published: April 25, 1991
Released on J-STAGE: April 19, 2006
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