The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 49 , Issue 12
Showing 1-16 articles out of 16 articles from the selected issue
  • GERHARD ERKEL, UTA BECKER, TIMM ANKE, OLOV STERNER
    1996 Volume 49 Issue 12 Pages 1189-1195
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Nidulal (1), a novel inducer of differentiation of human HL-60 promyelocytic leukemia cells, was isolated from fermentations of the basidiomycete Nidula Candida together with low amounts of niduloic acid (2). Both compounds are bisabolane sesquiterpenes. Their structures were elucidated by spectroscopic methods. In reporter gene assays nidulal (1) preferentially activated the transcription factor complex AP-1 - mediated expression of secreted alkaline phosphatase in COS-7 cells. In addition nidulal (1) and niduloic acid (2) exhibited weak cytotoxic and antibiotic activities.
    Download PDF (670K)
  • I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological Activities
    HIDENORI NAKAJIMA, BUNJI SATO, TAKASHI FUJITA, SHIGEHIRO TAKASE, HIROS ...
    1996 Volume 49 Issue 12 Pages 1196-1203
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    New antitumor substances, FR901463, FR901464 and FR901465 were isolated from the culture broth of a bacterium of Pseudomonas sp. No.2663.
    FR901463, FR901464 and FR901465 remarkably enhanced the transcriptional activity of the promoter of SV40 DNA virus. Further, these compounds exhibited potent anti tumor activities against murine and human tumor cell lines in vitro.
    Download PDF (645K)
  • II. Activities against Experimental Tumors in Mice and Mechanism of Action
    HIDENORI NAKAJIMA, YASUHIRO HORI, HIROSHI TERANO, MASAKUNI OKUHARA, TO ...
    1996 Volume 49 Issue 12 Pages 1204-1211
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    FR901463, FR901464 and FR901465, novel antitumor substances, were isolated from the fermentation broth of Pseudomonas sp. No. 2663. Their antitumor activities were examined in three mouse tumor systems and one human tumor system. The three FR compounds prolonged the life of mice bearing murine ascitic tumor P388 leukemia (T/C values were 160%, 145% and 127% for FR901463, FR901464 and FR901465, respectively), and inhibited the growth of a human solid tumor, A549 lung adenocarcinoma, with different effective dose ranges. FR901464 exhibited most prominent effects on these tumor systems among the three FR compounds. FR901464 also inhibited the growth of murine solid tumors, Colon 38 carcinoma and Meth A fibrosarcoma. To address the involvement of transcriptional activation ability of the three FR compounds in the antitumor effect, we selected FR901464 as a candidate compound and investigated cell cycle transition, chromatin status and endogenous gene expression in FR901464-treated tumor cells having elevated transcriptional activity. FR901464 induced characteristic G1 and G2/M phase arrest in the cell cycle and internucleosomal degradation of genomic DNA with the same kinetics as activation of SV40 promoter-dependent cellular transcription in M-8 tumor cells. In contrast to the potent activation of the viral promoter, FR901464 suppressed the transcription of some inducible endogenous genes but not house keeping genes in M-8 cells. These results suggest that FR901464 may induce a dynamic change of chromatin structure, giving rise to strong antitumor activity, and therefore may represent a new type of drug for cancer chemotherapy.
    Download PDF (672K)
  • Taxonomy, Production, Isolation, Physico-chemical Properties, Structure Elucidation and Biological Properties
    JUN KOHNO, MAKI NISHIO, KIMIO KAWANO, NORIYUKI NAKANISHI, SHIN-ICHI SU ...
    1996 Volume 49 Issue 12 Pages 1212-1220
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Four new antitumor antibiotics, TMC-1 A, B, C and D were isolated from a fermentation broth of Streptomyces sp. A-230. Spectroscopic studies have shown that TMC-1 A to D were new members of the manumycin class of antibiotics. These antibiotics showed cytotoxic activities against various tumor cell lines in vitro.
    Download PDF (593K)
  • HIROOMI WATABE, TAKESHI MIKUNIYA, SHIGEHARU INOUYE, SHIGERU ABE, HIDEY ...
    1996 Volume 49 Issue 12 Pages 1221-1225
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Benanomicin A is an antifungal antibiotic produced by Actinomadura spadix. In the present study, we investigated the effect of benanomicin A on the phagocytosis of Candida albicans by murine peritoneal macrophages and on the cell-surface hydrophobicity (CSH) of C. albicans. Although pretreatment of macrophages with benanomicin A had no effect on the phagocytosis, addition of benanomicin A to the culture of macrophages and Candida cells increased the susceptibility of Candida cells to the phagocytosis by the macrophages. Pretreatment of Candida cells with benanomicin A also increased the susceptibility of Candida cells to the phagocytosis. When Candida cells were mixed with benanomicin A, the antibiotic bound irreversibly to Candida cells. These data suggest the possibility that the increased susceptibility of Candida cells to the phagocytosis is mediated by the binding of benanomicin A to Candida cells. Examination of physicochemical property of Candida cell surface showed that the CSH of Candida cells significantly decreased by the treatment with benanomicin A. Thus, binding of benanomicin A to Candida cells may induce biochemical/physicochemical alternation of the surfaces, so that they become more susceptible to phagocytosis by murine macrophages. These properties of benanomicin A, along with its antifungal activity, seem to be beneficial in the treatment of fungal infections.
    Download PDF (428K)
  • II. Structural Elucidation
    MUHAMMAD HANAFI, KOZO SHIBATA, MASASHI UEKI, MAKOTO TANIGUCHI
    1996 Volume 49 Issue 12 Pages 1226-1231
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    UK-2A, B, C and D, novel antibiotics produced by Streptomyces sp. 517-02, exhibit strong antifungal activity. The structures were elucidated based on spectral and chemical evidence that these compounds are the derivatives of the nine-membered dilactone formed from serine and 4-hydroxypentanoic acid moiety.
    Download PDF (437K)
  • PAWEL SOWINSKI, TADEUSZ BIESZCZAD, JAN PAWLAK, EDWARD BOROWSKI
    1996 Volume 49 Issue 12 Pages 1232-1235
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    The Stereostructure of amphotericin A was established on the basis of NMR studies which contained DQF COSY, ROESY, ID TOCSY, HSQC and HMBC experiments.
    Download PDF (289K)
  • ROLF HERMANN, FRANCA RIPAMONTI, GABRIELLA ROMANÒ, ERMENEGILDO R ...
    1996 Volume 49 Issue 12 Pages 1236-1248
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Starting from the antibiotic A-40926 and the aglycone of A-40926 a series of compounds were prepared by modifying the free functionalities. Their antimicrobial activity was determined, particularly against Neisseria gonorrhoeae, against which A-40926, unlike other natural glycopeptides, is active. Improved in vivo activity was displayed by the monomethyl ester of A-40926 esterified at the carboxyl group of the N-acylamino-glucuronyl moiety.
    Download PDF (1042K)
  • P. TAVECCHIA, A. MARAZZI, C. DALLANOCE, A. TRANI, I. CICILIATO, P. FER ...
    1996 Volume 49 Issue 12 Pages 1249-1257
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    New N-acyl derivatives of 1-N-desmethyl goldinamine were obtained from degradation of kirromycin. Periodate-oxidation of these derivatives provided new aldehydic fragments that were further elaborated. Both N-phenyl ureido and N-phthalimido derivatives of 1-N-desmethyl goldinamine are able to inhibit bacterial protein synthesis in cell-free assay and are active against whole microorganisms, although with lower potency than kirromycin. The derivatives from the aldehydic fragments are totally inactive.
    Download PDF (748K)
  • Part I. Synthesis and Biological Activity of Non-aromatic Heterocyclic Derivatives
    GEORGE BURTON, NICOLA J. C. CLEAR, A. JOHN EGLINGTON, ANGELA W. GUEST, ...
    1996 Volume 49 Issue 12 Pages 1258-1265
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    A new series of carbapenems, having a saturated or partially unsaturated heterocycle at C-2, has been synthesised. The in vitro antibacterial activity of these compounds and their stability to human dehydropeptidase-1 (DHP-1) are described. The stereochemistry of the C-2 side-chain and the presence of a double bond in the heterocycle were shown to have significant effects on the stabilities of the compounds to DHP-1.
    Download PDF (731K)
  • Part II. Synthesis and Structure-activity Relationships of Isoxazolin-2-yl, Isoxazolidin-2-yl and 2-Pyrazolin-2-yl Carbapenems Generated Using 1, 3-Dipolar Cycloaddition Chemistry
    GEORGE BURTON, GRAHAM J. CLARKE, JAMES D. DOUGLAS, A. JOHN EGLINGTON, ...
    1996 Volume 49 Issue 12 Pages 1266-1274
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    A series of carbapenems containing novel C-2 semisaturated heterocyclic substituents were synthesised by 1, 3 dipolar cycloaddition reactions of nitrile oxides, nitrile imines and a nitrone to 2-vinylcarbapenem. The isoxazoline and isoxazolidine compounds showed potent antibacterial activity but moderate stability to human dehydropeptidase 1 (DHP-1). Stability to DHP-1 was improved by methyl substitution in the isoxazoline ring, but at the expense of antibacterial activity. The pyrazolines exhibited excellent stability to DHP-1, but reduced potency against Gram-negative organisms.
    Download PDF (726K)
  • HANG SUB KIM, SANG BAE HAN, HWAN MOOK KIM, YOUNG HO KIM, JUNG JOON LEE
    1996 Volume 49 Issue 12 Pages 1275-1277
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Download PDF (210K)
  • RYUJI UCHIDA, KAZURO SHIOMI, JUNJI INOKOSHI, HARUO TANAKA, YUZURU IWAI ...
    1996 Volume 49 Issue 12 Pages 1278-1280
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Download PDF (246K)
  • KOUICHI TSUCHIYA, CFFIKAKO KIMURA, KIYOHIRO NISHIKAWA, TAKASHI HARADA, ...
    1996 Volume 49 Issue 12 Pages 1281-1283
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Download PDF (184K)
  • KEIKO SUZUKI, KOHEI SFFIMADA, SHIGEO NOZOE, KAZUHIKO TANZAWA, TAKESHI ...
    1996 Volume 49 Issue 12 Pages 1284-1285
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Download PDF (177K)
  • JAE YEOL LEE, YONG SUP LEE, DAE WHAN SUK, EUN-RHAN WOO, BONG YOUNG CHU ...
    1996 Volume 49 Issue 12 Pages 1286-1289
    Published: December 25, 1996
    Released: November 21, 2006
    JOURNALS FREE ACCESS
    Download PDF (236K)
feedback
Top