The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 47 , Issue 6
Showing 1-16 articles out of 16 articles from the selected issue
  • TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
    YASUHISA TSURUMI, NOBUTAKA OHHATA, TOSHIRO IWAMOTO, NOBUHARU SHIGEMATS ...
    1994 Volume 47 Issue 6 Pages 619-630
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    WS79089A, B and C, which are novel endothelin converting enzyme (ECE) inhibitors have been isolated from the fermentation broth of Streptosporangium roseum No. 79089. These inhibitors were purified from an acetone extract of whole culture broth followed by Silicar CC-4 column chromatography and HPLC. WS79089A, B and C showed highly selective ECE inhibition activity with IC50 values of 0.73μM 0.14μM and 3.42μM, respectively. On the basis of spectroscopic and chemical evidence, the tentative structures of WS79089A, B and C have been proposed, they have benzo[a]naphtacen chromophores.
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  • KAZUSHIGE TANAKA, SHIGERU MATSUTANI, AKIKO KANDA, TOSHIYUKI KATO, TADA ...
    1994 Volume 47 Issue 6 Pages 631-638
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Evidence accumulated to date suggests that extracellular group II phospholipase A2 (PLA2-II) is involved in the pathogenesis of inflammatory disease. During screening for PLA2 inhibitors, we found a novel PLA2 inhibitor named thielocin B3 in the culture broth of an ascomycetes. Thielocin B3 strongly inhibited human PLA2-II (IC50 = 0.076 μM) in a reversible and noncompetitive manner (Ki=0.098 μM), whereas it inhibited human group IPLA2 only weakly (IC50 = 18 μM). It also quenched the tryptophan fluorescence of Naja mocambique venom PLA2; almost 100% quenching being attained at a thielocin B3/enzyme molar ratio of 1.0. Its inhibitory activity toward human PLA2-II and Naja mocambique PLA2 was markedly decreased by methylation of its two carboxyl groups, while the quenching observed for Naja mocambique PLA2 was not altered. These results suggest that the two carboxyl groups do not participate in the binding of thielocin B3 to the enzyme, but play a crucial role in the PLA2 inhibition. Furthermore, in the rat carrageenan-induced pleurisy model, thielocin B3 significantly reduced both exudate volume and PLA2 activity in the exudate when coinjected with carrageenan.
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  • TAXONOMY, YIELD IMPROVEMENT, FERMENTATION AND BIOLOGICAL ACTIVITY
    SHOICHI OHSHIMA, MIEKO YANAGISAWA, AKIRA KATOH, TOSIHIKO FUJII, TAKASH ...
    1994 Volume 47 Issue 6 Pages 639-647
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Fungal strain NR 6356, Fusarium merismoides Corda, was discovered as the source of the protein kinase C (PKC) inhibitor, azepinostatin. The strain was identified based on its growth on potato sucrose agar, slender conidial shape, characteristic polyphialide and production of abundant chlamydospores. Fusarium aquaeductuum Lagh. IMI 103658 and Fusarium sp. NR 7222 were also found to produce the same inhibitor. After single colony isolation and medium optimization trials, a more than 30-fold increase in the production of azepinostatin over the original culture was achieved.
    Azepinostatin selectively and potently inhibited rat brain PKC with an IC50 value of 70 nM. Other enzymes utilizing ATP, including hexokinase, were not affected. The Ki of azepinostatin for PKC was 0.5 nM. The inhibition of PKC was competitive with ATP and uncompetitive with histone.
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  • I. TAXONOMY, MUTATION, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITIES
    HIDEAKI UCHIDA, YASUKAZU NAKAKITA, NOBUYASU ENOKI, NAOKI ABE, TAKEHIKO ...
    1994 Volume 47 Issue 6 Pages 648-654
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Three novel antibiotics, named chrymutasins A, B and C, were isolated from the fermentation products of a mutant strain obtained by NTG (N-methyl-N'-nitro-N-nitrosoguanidine) treatment. The mutant strain produced the chrymutasins, which differed in the aglycone moiety from chartreusin, and related compounds. The production of these compounds needed a characteristically long fermentation period. The antitumor activity of chrymutasin A is better in vivo than that of chartreusin, the cytotoxic activity against cell lines in vitro is equivalent, and the antimicrobial spectrum is narrower.
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  • II. CHARACTERIZATION AND STRUCTURAL ELUCIDATION
    HIDEAKI UCHIDA, YASUKAZU NAKAKITA, NOBUYASU ENOKI, NAOKI ABE, TAKEHIKO ...
    1994 Volume 47 Issue 6 Pages 655-667
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Chrymutasins A, B and C are glycosidic antibiotics produced by a mutant of the chartreusin producer-organism Streptomyces chartreusis. We report here the structure elucidation of these compounds. The sugar moieties involved were determined by comparison with the related chartreusins. The structure of the aglycone, the same in all three compounds, was elucidated by NMR, incorporation studies of labeled compounds and synthesis of derivatives. The chrymutasin aglycone differs from that of chartreusin by a single carbon and an amino group.
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  • I. TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES, AND ANTIMICROBIAL ACTIVITY
    KAZUO SHIMANAKA, NAOKO KINOSHITA, HIRONOBU IINUMA, MASA HAMADA, TOMIO ...
    1994 Volume 47 Issue 6 Pages 668-674
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Novel antibacterial antibiotics, amythiamicins A, B, C and D, have been isolated from the fermentation broth of Amycolatopsis sp. MI481-42F4. In this paper, the taxonomy of the producing strain, fermentation, isolation, physico-chemical properties and biological activities of amythiamicins are reported. Amythiamicins inhibit the growth of Gram-positive bacteria including multi-drug resistant strains.
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  • I. TAXONOMY, FERMENTATION AND BIOLOGICAL PROPERTIES
    HUNG-CHI LIN, SHU-CHEN CHANG, NAN-LI WANG, LI-REN CENG
    1994 Volume 47 Issue 6 Pages 675-680
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Six new kinamycin antibiotics, designated as FL-120A-D' (1-6) were isolated from the culture filtrate of Streptomyces sp. strain IY2-13. Based on its cultural, physiological, morphological and chemical characteristics, this strain was identified as a new subspecies of Streptomyces chattanoogensis and named S. chattanoogensis subsp. taitungensis. These kinamycins have demonstrated a potent activity against Gram-positive aerobic and anaerobic bacteria.
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  • II. ISOLATION AND STRUCTURE DETERMINATION
    JENN-JONG YOUNG, SU-NENG HO, WEI-MEI JU, LI-REN CHANG
    1994 Volume 47 Issue 6 Pages 681-687
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Six new kinamycin antibiotics have been isolated from the culture filtrate of Streptomyces chattanoogensis. The structures of six related components were determined employing ID and 2D NMR spectroscopy and mass spectrometry. These structures represent the first reported epoxide kinamycin (2, 3) and propionyl derivative of kinamycin (5), and new isobutyryl derivatives of kinamycin (1, 4, 6).
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  • SHIGENORI KUMAZAWA, YASUKO ASAMI, KAORU AWANE, HIROYUKI OHTANI, CHIZUK ...
    1994 Volume 47 Issue 6 Pages 688-696
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The structures of new antibiotics, shurimycins A and B produced by Streptomyces hygroscopicus A1491, were elucidated from the physico-chemical properties, 2D NMR techniques and chemical degradation experiments to be 36-membered macrolides related to azalomycins, scopafungin and guanidylfungins. Shurimycins were active against fungi and Gram-positive bacteria.
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  • I. TAXONOMY, PRODUCTION, ISOLATION AND PRELIMINARY CHARACTERIZATION
    SHINICHI KOBAYASHI, KOUICHI TSUCHIYA, TAKASHI HARADA, MITUYUKI NISHIDE ...
    1994 Volume 47 Issue 6 Pages 697-702
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A novel plant growth regulator, pironetin, was isolated from the culture broth of Streptomyces sp. NK10958. It was extracted from the culture broth with ethyl acetate and purified by column chromatographies. Pironetin showed 23% inhibition on the growth of rice plants without any loss of crop yield at lOg/a on 9 days before heading.
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  • II. STRUCTURAL ELUCIDATION
    SHINICHI KOBAYASHI, KOUICHI TSUCHIYA, TAKASHI KUROKAWA, TAIZO NAKAGAWA ...
    1994 Volume 47 Issue 6 Pages 703-707
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A novel plant growth regulator, pironetin was isolated from the culture broth of Streptomyces sp. NK10958. The structure of pironetin was determined to be (5R, 6R)-5-ethyl-5, 6-dihydro-6-[(E)-(2R, 3S, 4R, 5S)-2-hydroxy-4-methoxy-3, 5-dimethyl-7-nonenyl]-2H-pyran-2-one by FAB-MS, 1H and 13C NMR, COSY, COLOC, DEPT, IR, X-ray crystallographic analyses and adapted MOSHER'S method.
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  • YASUKI SAKAMOTO, TETSURD MATSUMOTO, JOICH KUMAZAWA
    1994 Volume 47 Issue 6 Pages 708-714
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    We have investigated the immunosuppressive effect of cyclosporin A (CsA) on delayed-type hypersensitivity (DTH) to syngeneic testicular cells (TC). DTH to syngeneic TC was induced by subcutaneous (sc) immunization with viable syngeneic TC and was augmented by a high dose of cyclophosphamide (CY)-pretreatment. DTH was suppressed by administration of CsA in a dose-dependent manner. When the mice were immunized alone or with 100 mg/kg of CY-pretreatment, 30mg/kg or more of CsA suppressed DTH to TC. In mice immunized with 200mg/kg of CY-pretreatment, 50 mg/kg of CsA was needed to suppress DTH.
    DTH is thought to play a key role in the induction and/or maintenance of experimental autoimmune orchitis (EAO). Our data show that DTH to syngeneic TC induced by immunization is suppressed by administration of CsA. Pretreatment of mice with immunization and administration of CsA suppressed DTH significantly when the mice were challenged with immunization with CY-pretreatment. However, DTH was rather enhanced significantly in mice pretreated with administration of CsA alone without preimmunization. Therefore, even though administration of CsA with immunization suppresses DTH, administration of CsA alone might rather eliminate suppressive mechanism resulting in augmentation of DTH.
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  • RYSZARD ANDRUSZKIEWICZ, TERESA ZIENIAWA, HENRYK CHMARA, LESZEK KASPRZA ...
    1994 Volume 47 Issue 6 Pages 715-723
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Peptide analogues of Sch 37137 the antifungal antibiotic have been synthesized and evaluated in vitro against Candida sp. Di- and tripeptides containing methionine, leucine, norvaline, lysine, glutamic acid and N3-(trans-epoxysuccmamoyl)-L-2, 3-diaminopropanoic acid, (EADP) were obtained. Peptides containing (d)-, and (L)-trans-epoxysuccinamic acid were also prepared. All of the analogues examined displayed in general higher anticandidal activity than a mixture of diastereomers of Sch 37137.
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  • Y. K. T. LAM, P. DAI, R. BORRIS, A. DOMBROWSKI, R. RANSOM, G. YOUNG, M ...
    1994 Volume 47 Issue 6 Pages 724-726
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • REI KANETO, KAZUYUKI DOBASHI, IKUO KOJIMA, KAZUYA SAKAI, NORIO SHIBAMO ...
    1994 Volume 47 Issue 6 Pages 727-730
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • RYUICHI SAWA, YUMI MORI, HIRONOBU IINUMA, HIROSHI NAGANAWA, MASA HAMAD ...
    1994 Volume 47 Issue 6 Pages 731-732
    Published: June 25, 1994
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Download PDF (131K)
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