The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 42 , Issue 12
Showing 1-23 articles out of 23 articles from the selected issue
  • JUN'ICHI SHOJI, RYUJI SAKAZAKI, TERUO HATTORI, KOICHI MATSUMOTO, NOBUO ...
    1989 Volume 42 Issue 12 Pages 1729-1733
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    New antibiotics, agglomerins A, B, C and D, were isolated from the culture broth of a bacterial strain identified as Enterobacter agglomerans. These antibiotics are acidic in nature and their sodium salts are obtained as colorless crystalline powders, soluble in lower alcohols. All the antibiotics shows characteristic UV maxima at 248 and 298nm. Molecular formulas: A, C15H21O4Na; B, C17H23O4Na; C, C17H25O4Na and D, C19H27O4Na; were indicated by elemental analysis and MS. These antibiotics are active against a wide variety of anaerobic bacteria and weakly against aerobic Gram-positive bacteria in vitro.
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  • TAXONOMY, FERMENTATION, ISOLATION, STRUCTURE ELUCIDATION AND BIOLOGICAL CHARACTERISTICS
    SHINJI FUNAYAMA, MASAMI ISHIBASHI, YUMI ANRAKU, MAYUMI MIYAUCHI, HIROH ...
    1989 Volume 42 Issue 12 Pages 1734-1740
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Two novel antibiotics, glucopiericidinols A1 (1) and A2 (2) were isolated from the cultured broth of Streptomyces sp. OM-5689. The structures of these two compounds were deduced employing spectroscopic analyses. These antibiotics showed potent cytocidal activities against HeLa S3 cells in vitro (MIC 1: 0.39μg/ml, 2: 0.10μg/ml) when the cells were exposed to the antibiotics for 3 days. Although 1 and 2 showed no activity at 1, 000 μg/ml against various Gram-positive and Gram-negative bacteria, yeast or fungi, they did have inhibitory activity against Piricularia oryzae (MIC of 1: 125μg/ml, of 2: 31μg/ml).
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  • MUTSUO NAKAJIMA, TAKAO OKAZAKI, SEIGO IWADO, TAKESHI KINOSHITA, TATSUO ...
    1989 Volume 42 Issue 12 Pages 1741-1748
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    New antibiotics spirocardins A and B were isolated from the culture broth of an actinomycete isolated from a soil sample collected near Lake Hibara, Fukushima Prefecture, Japan. The producing strain was classified as Nocardia sp. SANK 64282.
    The antibiotics were isolated from the culture filtrate by solvent extraction and purified further by silica gel and preparative reverse phase column chromatography. They were primarily active against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus and limited species of Gram-negative bacteria such as Bacteroides fragilis and Klebsiella pneumoniae. They were also moderately active against several species of Mycoplasma. The molecular formulae of spirocardins A and B were C20H30O6 and C20H32O6, respectively.
    From their physico-chemical characteristics they were revealed to be diterpenoid antibiotics with closely related structures and the former was easily converted to the latter by the reduction with NaBH4.
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  • I. PRODUCTION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE
    MASATAKA KONISHI, MAKI NISHIO, KYOICHIRO SAITOH, TAKEO MIYAKI, TOSHIKA ...
    1989 Volume 42 Issue 12 Pages 1749-1755
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A new antibiotic, cispentacin, was isolated from the culture broth of a Bacillus cereus strain, L450-B2. The antibiotic is water-soluble and amphoteric; its structure was determined by spectroscopic analysis and chemical synthesis to be (1R, 2S)-2-aminocyclopentane-l-carboxylic acid. Cispentacin demonstrated only weak in vitro activity against certain fungi but strong protection of mice from lethal infection of Candida albicans A9540.
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  • II. IN VITRO AND IN VIVO ANTIFUNGAL ACTIVITIES
    TOSHIKAZU OKI, MINORU HIRANO, KOZO TOMATSU, KEI-ICHI NUMATA, HIDEO KAM ...
    1989 Volume 42 Issue 12 Pages 1756-1762
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Cispentacin ((-)-(1R, 2S)-2-aminocyclopentane-l-carboxylic acid) is a new antifungal antibiotic possessing potent anti-Candida activity. The 50% inhibitory concentration (IC50) and IC100 values of cispentacin against clinical isolates of Candida albicans were in the ranges 6.3-12.5 and 6.3-50μg/ml, respectively, by turbidimetric measurement in yeast nitrogen base glucose medium. No significant activity was seen against any yeasts and molds when tested by the agar dilution method using three different agar media; KNOPF'S agar, yeast extract - glucose - peptone agar and Sabouraud dextrose agar. This antibiotic demonstrated good therapeutic efficacy against a systemic Candida infection in mice by both parenteral and po administrations. The 50% protection dose (PD50) values after single iv and po administrations were 10 and 30mg/kg, respectively. It was also effective in a systemic infection with Cryptococcus neoformans and in both lung and vaginal infections with C. albicans in mice. Cispentacin did not induce acute lethal toxicity at 1, 000mg/kg by iv injection and 1, 500mg/kg by ip and po administrations in mice.
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  • PRODUCTION, ISOLATION, CHARACTERIZATION AND BIOLOGICAL PROPERTIES
    JAMES A. MATSON, JAMES A. BUSH
    1989 Volume 42 Issue 12 Pages 1763-1767
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A new antitumor antibiotic, sandramycin, was isolated from cultured broth of a Nocardioides sp. (ATCC 39419) and purified by solvent partition and column chromatography. Sandramycin, a new depsipeptide, was moderately active in vitro against Gram-positive organisms and in vivo against leukemia P388 in mice.
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  • MITSUNOBU KARA, KOZO ASANO, ISAO KAWAMOTO, TOSHIMITSU TAKIOUCHI, SHIGE ...
    1989 Volume 42 Issue 12 Pages 1768-1774
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Leinamycin (DC 107) is newly discovered antitumor antibiotic with an unusual 1, 3-dioxo-1, 2-dithiolane structure. Five different producing strains were isolated from soils collected in Japan during 1985 - 1988 and were taxonomically assigned as Streptomyces. Fermentation studies indicate: Leinamycin was unstable in culture broth. A chemically defined medium could be designed for a preferable production. Streptomyces sp. S-140 grew on medium supplemented with Zn2+ and high porus polymer resin and accumulated 32μg/ml of leinamycin. Improved isolation methods are described along with identification of mikamycin A co-produced with leinamycin by the strain S-140.
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  • SATOSHI NAKANISHI, KATSUHIKO ANDO, ISAO KAWAMOTO, TORU YASUZAWA, HIROS ...
    1989 Volume 42 Issue 12 Pages 1775-1783
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Novel inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase were isolated from the culture broth of a fungus, Mollisia ventosa KAC-1148. They were designated as KS-504a, KS-504b and KS-504d. A degradative product of KS-504a, called KS-504e, was also isolated and found to inhibit the enzyme. The 50% inhibitory concentration (IC50) values of KS-504a, KS-504b, KS-504d and KS-504e for bovine brain enzyme were 122, 109, >500 and 139μM, respectively.
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  • II. STRUCTURE DETERMINATION
    JERZY GOLIK, TERRENCE W. DOYLE, BALA KRISHNAN, GEORGE DUBAY, JAMES A. ...
    1989 Volume 42 Issue 12 Pages 1784-1789
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The chemical structures of AT2433-A1 (2), AT2433-A2 (3), AT2433-B1 (4) and AT2433-B2 (5) were elucidated by degradation and spectroscopic studies. Compounds 2-5 are disaccharides closely related to rebeccamycin. The aglycone in 2 and 3 was determined to be 6-N-methyl-11-chloro-5H-indolo[2, 3-a]pyrolo[3, 4-c]carbazole and in 4 and 5 it was determined to be 6-N-methyl-5H-indolo[2, 3-a]pyrolo[3, 4-c]carbazole. Compounds 2 and 4 are 4-N"-methyl analogs of 3 and 5.
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  • GEORGE F. GAUSE, MARIYA G. BRAZHNIKOVA, NINA N. LOMAKINA, TATIANA F. B ...
    1989 Volume 42 Issue 12 Pages 1790-1799
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    By a combination of chemical and spectroscopic (1H and 13C NMR) studies the structure of a glycopeptide antibiotic eremomycin has been elucidated. It is closely related to vancomycin, but differs in sugar and chlorine content. The eremomycin aglycone contains monodechlorovancomycinic acid; the only chlorine atom is situated in the second amino acid after the N-terminal amino acid residue of the peptide. The sugar part is composed of glucose and two residues of an amino sugar shown to be 2, 3, 6-trideoxy-3-amino-C-3-methyl-L-arabino-hexopyranose (4-epi-vancosamine). One of the amino sugar residues is a component of the disaccharide 2-O-(α-L-4-epi-vancosaminyl)-β-Dglucopyranose, attached to a triphenyl ether moiety; the position of another one is at the serine oxygen in the C-terminal region of the aglycone.
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  • ADRIANO MALABARBA, PIETRO FERRARI, GIUSEPPE CIETTO, ROSA PALLANZA, MAR ...
    1989 Volume 42 Issue 12 Pages 1800-1816
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A series of peptide derivatives of teicoplanin A2 (CTA) and deglucoteicoplanin (TD) was prepared by condensation of the 63-carboxyl function with the α-amino group of selected amino acids and their derivatives.
    The modification of the ionic character of CTA and TD influenced their in vitro and in vivo antimicrobial properties to a different extent, depending on the structure of the amino acidic moiety at C-63. A certain effect on binding strength to Ac2-L-Lys-D-Ala-D-Ala, a synthetic model of the antibiotic's target peptide, was also observed.
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  • EDWARD G. BRAIN, ANDREW K. FORREST, ERIC HUNT, CHRISTINE SHILLINGFORD, ...
    1989 Volume 42 Issue 12 Pages 1817-1822
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Erythromycin A oxime 11, 12-carbonate (5a) and its oxime ethers 5b-5p have been prepared and their antibacterial activities compared with those of erythromycin A (1) and .its 11, 12-carbonate 2. The oxime 5a and many of its oxime ether derivatives showed good activity in vitro against Gram-positive and the more permeable Gram-negative organisms, in some cases being even more active than the carbonate 2.
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  • J. C. FLORENT, A. GENOT, C. MONNERET
    1989 Volume 42 Issue 12 Pages 1823-1830
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    New anthracyclines including 2-deoxy-L-fucose, 2-deoxy-L-rhamnose and 2, 6-dideoxy-2-iodo-α-L-mannose as sugar moieties, respectively 8, 11 and 14, have been obtained by glycosidation of the 4-demethoxy-9-hydroxymethyl-9-deacetyl daunorubicinone (1) with appropriate sugars under Koenigs-Knorr conditions. They were found to display high cytotoxicity on L1210 leukemia, but also an outstanding antileukemic activity in mice in the case of 8 and 14.
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  • KAYOKO SUZUKAKE-TSUCHIYA, YUKARI MORIYA, MAKOTO HORI, YOSHIMASA UEHARA ...
    1989 Volume 42 Issue 12 Pages 1831-1837
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Herbimycin A, an inhibitor of pp60src tyrosin kinase, caused src oncogene-expressed cells to become sensitive to contact inhibition, but did not affect ras oncogene-expressed cells. The cell lines tested were temperature sensitive v-src- and temperature sensitive v-ras-integrated nontransformed rat kidney cell line (NRK) (srctsNRK and rastsNRK, respectively) and a wild-type v-src-integrated NIH3T3 (src3T3). srctsNRK cells in densely populated cultures (plated at 1.25 × 104 cells/cm2), grown at 33°C in the presence of 0.45 μg/ml of herbimycin A, ceased the cell cycle at the G0-G1 stage within 2 days, and the cells showed normal morphology. Upon removal of herbimycin A, the quiescent cells resumed the cell cycle in concert with morphological alteration from 'normal' to 'transformed', and proceeded through the S and M stages successively in a synchronized manner. Cells in the late S stage, compared with those in other stages of the cell cycle, were more sensitive to the killing effect of 5-fluorodeoxyuridine. Such synchronism of the cell cycle was not observed with sparsely populated cultures (2.5 × 103 cells/cm2); the cells resumed their asynchronous growth after removal of herbimycin A, although their morphology returned to 'transformed' as in the experiment with the densely populated cultures. The induction by herbimycin A of contact inhibition in densely populated cultures was also observed with src3T3 (grown at 37°C) but not with rastsNRK (grown at 33°C).
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  • KEN-ICHI KIMURA, TOMONORI MORINAGA, NOBUO MIYATA, GOSEI KAWANISHI
    1989 Volume 42 Issue 12 Pages 1838-1843
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    DNase I footprinting was used to investigate binding sites for SN-07 chromophore on DNA fragments prepared from pBR322. Six sites were protected on about 150 base pair DNA fragments by SN-07 chromophore, but not by related anthracycline antibiotics from DNase I digestion. All the protected sites contained the dinucleotide sequence 5'-GC-3', but no other regularities could be discerned. A drug-induced conformational change of DNA was suggested by enhancement of DNase I sensitivity between the protected sites. These results support covalent interaction of the carbinolamine function of SN-07 chromophore to 2-amino group of guanine residues.
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  • KIYOSHI SATO, RYO OKACHI, IKUO MATSUKUMA, KENICHI MOCHIDA, TADASHI HIR ...
    1989 Volume 42 Issue 12 Pages 1844-1853
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    KT3777 is a novel carbacephem antibiotic structurally identical to cefaclor (CCL), except that the sulfur atom of position 1 of the cephem nucleus has been replaced by carbon. KT3777 was investigated for in vitro and in vivo antibacterial activities in comparison with CCL, cephalexin (CEX) and amoxicillin. The MIC50 of KT3777 ranged from 0.2 to 3.13μg/ml for clinical isolates of Staphylococcus aureus, Streptococci, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae, and Neisseria gonorrhoeae. KT3777 possessed an antibacterial spectrum and potency similar to that of CCL. However, against E. coli and K. pneumoniae, KT3777 was about twice as active as CCL. KT3777 was more active than CEX against all strains tested. Killing-curve studies demonstrated bactericidal activity of KT3777 at concentrations above the MIC. KT3777 showed good affinity for penicillin-binding proteins 1A, 1Bs, 3 and 4 of E. coli NIHJ JC-2. The protective effect of KT3777 against systemic infections in mice was comparable to that of CCL with a few exceptions and about 3 to 7 times greater than that of CEX. KT3777 also proved effective against localized infections such as acute pneumonia and ascending urinary tract infections in mice.
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  • YUKIHIRO NISHIYAMA, NAOHIKO YAMAMOTO, YOSHINARI YAMADA, TOHRU DAIKOKU, ...
    1989 Volume 42 Issue 12 Pages 1854-1859
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A series of new compounds, carbocyclic oxetanocins, have been synthesized and their anti-herpesvirus activity determined. Carbocyclic oxetanocin G (OXT-G) was most active against herpes simplex virus (HSV) and human cytomegalovirus (HCMV) among carbocyclic oxetanocins tested; the median effective concentrations (EC50) for HSV-1, -2, and HCMV were 0.23, 0.04 and 0.40 μg/ml, respectively. The EC50 value of carbocyclic OXT-G against HSV-2 was significantly lower than those of acyclovir, ganciclovir (DHPG) and OXT-G, while the value for HCMV was comparable to those of DHPG and OXT-G. Carbocyclic OXT-G showed much higher activity against TK+ HSV-2 than against a TK- mutant, suggesting that this compound is a good substrate for HSV-2-induced TK. The antiviral activity of the compound was only partially reversed even by the addition of 100-fold excess deoxyguanosine. The results suggest that the mode of action of carbocyclic OXT-G is different from that of OXT-G.
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  • QI-CHAO PAN, HUI-YAN GUO
    1989 Volume 42 Issue 12 Pages 1860-1868
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Our previous studies have demonstrated that 3-aminobenzamide (3AB), an inhibitor of adenosine diphosphate-ribosyl transferase (ADPRT) could enhance the cytotoxicity (in vitro) and antitumor activty (in vivo) of bleomycin (BLM) A5 and peplomycin (PEP) against S-180, hepatoma and Ehrlich ascites carcinoma (EAC). In this study, it was shown that the inhibition rates (INR's) of S-180 in two experiments were increased from 42.5 and 46.1% to 66.2 and 75.9% when BLM 2.5mg/kg/day × 8 was combined with SAB 385.4mg/kg/day × 8, while the decrease of body weight could not be enhanced. BLM at a dose of 5mg/kg/day × 8 gave INR's of 64.8 and 75%, similar to the combined group but decreased the body weight more significantly. However, the addition of 3AB 385.4mg/kg/day to BLM did not increase the acute toxicity of BLM alone. There was no significant difference of change of the body weight and subacute toxicity between the BLM and BLM + 3 AB group. There was no difference of peripheral blood white cell count and the pathomorphological and ultrastructural change, wet weight and hydroxyproline content (to reflect the collagen content) of the lung of the mice between BLM alone and BLM + 3AB group. Therefore, the study provided experimental evidences for the reasonable use of nontoxic ADPRT inhibitors in adjunct to the chemotherapy of BLM in cancers.
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  • XI. ISOLATION AND STRUCTURE ELUCIDATION OF A KEY INTERMEDIATE IN THE BIOSYNTHESIS OF THE MYCINAMICINS, MYCINAMICIN VIII
    KENJI KINOSHITA, YUKIMASA IMURA, SATOSHI TAKENAKA, MITSUO HAYASHI
    1989 Volume 42 Issue 12 Pages 1869-1872
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • KOICHI KONDO, YUTAKA HIGUCHI, SHOHEI SAKUDA, TAKUYA NIHIRA, YASUHIRO Y ...
    1989 Volume 42 Issue 12 Pages 1873-1876
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • SHIGETAKA ISHII, MIEKO NAGASAWA, YUKO KARIYA, HARUO YAMAMOTO
    1989 Volume 42 Issue 12 Pages 1877-1878
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • I. CARAZOSTATIN, A NEW FREE RADICAL SCAVENGER PRODUCED BY STREPTOMYCES CHROMOFUSCUS DC 118
    SHINICHIRO KATO, HIROYUKI KAWAI, TOMIKO KAWASAKI, YOICHIRO TODA, TETSU ...
    1989 Volume 42 Issue 12 Pages 1879-1881
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • FRANCESCO PARENTI, BRUNO CAVALLERI
    1989 Volume 42 Issue 12 Pages 1882-1883
    Published: December 25, 1989
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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