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ROBERT E. SCHWARTZ, CLAUDE DUFRESNE, JAMES E. FLOR, AUGUST J. KEMPF, K ...
1991 Volume 44 Issue 5 Pages
463-471
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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Restricticin (
1) is a naturally-occurring antifungal agent which contains triene, pyran and glycine ester functionalities and is unrelated to any previously known family of natural products. This unstable compound, as well as its corresponding
N,
N-dimethyl derivative (
2), have been produced and isolated from both solid and liquid fermentations of
Penicillium restrictum. The desglycyl hydrolysis product, restrictinol (
3), was produced
via the hydrolysis of pure restricticin and as an artifact of the isolation of restricticin.
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I. TAXONOMY OF PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY
KIN SING LAM, GRACE A. HESLER, DONALD R. GUSTAVSON, ALFRED R. CROSSWEL ...
1991 Volume 44 Issue 5 Pages
472-478
Published: May 25, 1991
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Strain L585-6 (ATCC 53650) is an actinomycete isolated from a soil sample collected in Maharastra State, India. It produces a new chromoprotein antitumor antibiotic, designated kedarcidin. Taxonomic studies demonstrated that strain L585-6 is an unidentified and unknown actinomycete. Kedarcidin shows potent antitumor activity against implanted P388 leukemia (3.3 μg/ml/kg) and B16 melanoma (2 μg/kg) in mice. Kedarcidin also shows potent antimicrobial activity against Gram-positive bacteria but no activity against Gram-negative bacteria.
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TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION
KENICHI SUZUKI, TSUTOMU SATO, MOTO MORIOKA, KOJI NAGAI, KENJI ABE, HIR ...
1991 Volume 44 Issue 5 Pages
479-485
Published: May 25, 1991
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A new antibacterial antibiotic tetrazomine was found from the fermentation broth of an actinomycete strain which was isolated from beach sand collected at Chichijima, Ogasawara Islands, Tokyo, Japan. The strain Y-09194L, was identified as
Saccharothrix mutabilis subsp.
chichijimaensis subsp. nov. The antibiotic exhibited broad antimicrobial activity against Gram-positive and Gram-negative bacteria
in vitro. It also exhibited strong cytotoxic activity against P388 leukemia cells and showed antitumor activity against P388 leukemia. The apparent molecular formula of tetrazomine was determined as C
24H
34N
4O
5. It has a rare structure which consists of six rings including piperidine, piperadine, oxazole, and pyrrolidine.
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I. TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION
HIROFUMI OKA, TOMOKO YOSHINARI, TAKASHI MURAI, KENJI KAWAMURA, FUMIO S ...
1991 Volume 44 Issue 5 Pages
486-491
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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A new topoisomerase inhibitor, BE-10988, was isolated from the culture broth of a strain of actinomycetes. The producing strain had a close resemblance to
Streptomyces fimicarius and
Streptomyces xanthocidicus. The active principle was extracted from the whole broth of strain BA10988 with ethyl acetate and purified by silica gel chromatography and by HPLC. BE-10988 increased DNA-topoisomerase complex formation and inhibited the growth of both doxorubicin-resistant and vincristine-resistant P388 murine leukemia cell lines, as well as sensitive P388 cell lines.
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SIMON E. BLANCHFLOWER, RHONA M. BANKS, JEREMY R. EVERETT, BRIAN R. MAN ...
1991 Volume 44 Issue 5 Pages
492-497
Published: May 25, 1991
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Paraherquamide (
1) an anthelmintic alkaloid, was isolated from a species of
Penicillium along with three novel analogues
2,
3 and
4. Anthelmintic activity at least equal to that of paraherquamide is described for the 14-de-hydroxy compound, VM 54159 (
4).
View full abstract
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III. SYNTHESIS, ANTIBACTERIAL ACTIVITY AND ORAL ABSORPTION OF NEW3-(SUBSTITUTED-ALKYLTHIO)-7β-[(Z)-2-(2-AMINOTHIAZOL-4-YL)-2-(CARBOXYMETHOXYIMINO)ACETAMIDO]CEPHALOSPORINS
CHIHIRO YOKOO, MASAMI GOI, AKIRA ONODERA, MITSUO MURATA, TAKATOSHI NAG ...
1991 Volume 44 Issue 5 Pages
498-506
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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The synthesis, antibacterial activity and oral absorption in rats of new 7β-[(
Z)-2-(2-aminothiazol4-yl)-2-(carboxymethoxyimino)acetamido]cephalosporins (
1) having various substituted-alkylthio groups at the C-3 position of the cephem nucleus are described. Of these, the cephalosporins with a cyanomethylthio group (
1d) and fluoroethylthio group (
1p) at the C-3 position showed a potent
in vitro antibacterial activity against Gram-positive and Gram-negative bacteria as well as good oral absorption in rats. When administered orally to mice infected with
Klebsiella pneumoniae,
1d had stronger protective effect than
1p. The structure-activity relationships of
1 are also presented.
View full abstract
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XIX. STRUCTURE-ACTIVITY RELATIONSHIPS OF CEPHALOSPORINS HAVING A THIADIAZOLYLTHIOMETHYL GROUP AT THE C-3 SIDE CHAIN
YOSHIKO INAMOTO, JIRO GOTO, KAZUO SAKANE, TOSHIAKI KAMIMURA, TAKAO TAK ...
1991 Volume 44 Issue 5 Pages
507-516
Published: May 25, 1991
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The synthesis and antibacterial activity of 7β-[(
Z)-2-(2-amino-4-thiazolyl)-2-(hydroxy or alkoxy)iminoacetamido] cephalosporins with various thiadiazolylthiomethyl moieties at the 3-position are discussed.
Of the compounds (
1a-
1e,
7a-
7d), 7β-[(
Z)-2-(2-amino-4-thiazolyl)-2-hydroxyiminoacetamido]-3-[(1, 2, 4-thiadiazol-5-yl)thiomethyl]cephalosporin (
1d: FK312) exhibited the highest activity against Gram-positive and Gram-negative bacteria, especially, against methicillin-resistant
Staphylococcus aureus.
Furthermore, the pharmacokinetic profiles of the compound
1d showed longer serum levels than that of ceftriaxone in rats.
View full abstract
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PETRI VILJANEN, HISAMI MATSUNAGA, YUKIO KIMURA, MARTTI VAARA
1991 Volume 44 Issue 5 Pages
517-523
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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The outer membrane permeability-increasing action of deacylpolymyxins was compared to the well-known potent action of polymyxin B nonapeptide (PMBN). Deacylpolymyxin B (DAPB), prepared by treating polymyxin B with polymyxin acylase, was found to be a slightly more effective permeabilizer than PMBN. As low a DAPB concentration as 1μg/ml sensitized
Escherichia coli to the probe antibiotics (rifampin, fusidic acid, erythromycin, clindamycin, novobiocin) by factors 30-100 and
Salmonella typhimurium by factors 10-100. A higher concentration (3μg/ml) of DAPB elicited further sensitization. Also deacylcolistin (DAC) was found to be an effective permeabilizer.
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AKIKO ISHIDA-OKAWARA, YUKIO KIMOTO, KAZUO WATANABE, KOICHI TOKUDA, MIC ...
1991 Volume 44 Issue 5 Pages
524-532
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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We found inhibitors, designated aseanostatins PI and P5, against myeloperoxidase (MPO) release from human polymorphonuclear leukocytes (PMN). Aseanostatins were extracted from an actinomycete isolated in Thailand and purified by a series of column chromatography of charcoal and silica gel, and HPLC. Physico-chemical characterization by gas liquid chromatography and GC-MS indicated that aseanostatins were fatty acids. The active forms of aseanostatins were recovered by hydrolyzing their methyl esters after HPLC. Two components PI and P5 with the IC
50 of 0.96 and 0.54μg/ml to the MPO release were obtained as pure forms, indicating aseanostatin P5 was higher activity than aseanostatin PI. The component PI was identical with 12-methyltridecanoic acid and P5 was indistinguishable to 12-methyltetradecanoic acid (ante-i-15:0). Aseanostatin P5 (1μg/ml) did not inhibit β-glucuronidase release, but O
2- production a little. It has no effect on chemotaxis of PMN to fMet-Leu-Phe (10
-8M), PMN adhesion or phosphorylation of a 64-kD protein in the PMN cell-lysate system.
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KAORI MASUDA, KAZUO SUZUKI, AKIKO ISHIDA-OKAWARA, SATOSHI MIZUNO, KUNI ...
1991 Volume 44 Issue 5 Pages
533-540
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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In order to search for microbial modulators of the activity of neuropeptide, we established a screen based on substance P (SP)-induced myeloperoxidase (MPO) release from human polymorphonuclear leukocytes (PMN). SP induced MPO release in a dose-dependent manner at concentrations ranging from 1-10 × 10
-4M. In comparison at 1 × 10
-4M, induction was also observed with SP derivatives but not with other neuropeptides such as neurokinin and enkephalin. Based on this, we searched for microbial inhibitors against SP-induced MPO release. An actinomycete metabolite designated HS3, which turned out to be identical with dioxapyrrolomycin or A1-R2081, and structurally related pyrrolomycins were found to inhibit SP-induced MPO release. In addition, these compounds inhibited the f-Met-Leu-Phe (FMLP)-induced MPO release from PMlfl. Pyrrolomycin derivatives with an
N-methylated pyrrole ring showed, however, a selective inhibition of the SP-induced MPO release. This was in contrast to results with aseanostatin P5 which selectively inhibited FMLP-induced MPO release.
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III. STRUCTURE OF GLYKENIN IV
FUMIKO NISHIDA, YUJI MORI, CHIHARU SONOBE, MAKOTO SUZUKI, VITHAYA MEEV ...
1991 Volume 44 Issue 5 Pages
541-545
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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HIDENORI OHKI, YOSHIKO INAMOTO, KOHJI KAWABATA, TOSHIAKI KAMIMURA, KAZ ...
1991 Volume 44 Issue 5 Pages
546-549
Published: May 25, 1991
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KIMIYASU SHIRAKI, MICHIO ISHIBASHI, TOSHIOMI OKUNO, KYOKO HAYASHI, KOI ...
1991 Volume 44 Issue 5 Pages
550-552
Published: May 25, 1991
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YOON JEONG KIM, KAZUO FURIHATA, SHIGERU YAMANAKA, RYOSUKE FUDO, HARUO ...
1991 Volume 44 Issue 5 Pages
553-556
Published: May 25, 1991
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TAKASHI YAMASHITA, MASATOMI IIJIMA, HIKARU NAKAMURA, KUNIO ISSHIKI, HI ...
1991 Volume 44 Issue 5 Pages
557-559
Published: May 25, 1991
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SATOSHI OMURA, HARUO IKEDA, HARUO TANAKA
1991 Volume 44 Issue 5 Pages
560-563
Published: May 25, 1991
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TOSHIO OTANI, YOSHINORI MINAMI, KUMIKO SAKAWA, KEN-ICHIRO YOSHIDA
1991 Volume 44 Issue 5 Pages
564-568
Published: May 25, 1991
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MARIKO NAKAMURA, TSUNEYA OHNO, SETSUKO KUNIMOTO, HIROSHI NAGANAWA, TOM ...
1991 Volume 44 Issue 5 Pages
569-571
Published: May 25, 1991
Released on J-STAGE: April 19, 2006
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