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Volume 50, Issue 4
Displaying 1-17 of 17 articles from this issue
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I. Fermentation, Isolation and Biological PropertiesKEN-ICHI KIMURA, FUMIKO KANOU, HIROYUKI KOSHINO, MASAKAZU URAMOTO, MAK ...1997 Volume 50 Issue 4 Pages 291-296
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSSNA-8073-B, an inhibitor of prolyl endopeptidase isolated from the broth filtrate of Streptomyces sp. SNA-8073, is a new isotetracenone antibiotic. It was purified by ethyl acetate extraction, silica gel column chromatography and high performance liquid chromatography on ODS column. SNA-8073-B has the molecular formula of C20H16O5 and is a stereoisomer of SNA-8073-A (fujianmycin B, rubiginone A2). SNA-8073-B inhibited prolyl endopeptidase of Flavobacterium non-competitively (IC50=8.9μM) when Z-Gly-Pro-pNA was used as a substrate, but SNA-8073-A did not show any inhibition even at 60μM.View full abstractDownload PDF (347K) -
TAKASHI KAWAUCHI, TORU SASAKI, KEN-ICHIRO YOSHIDA, HIROSHI MATSUMOTO, ...1997 Volume 50 Issue 4 Pages 297-303
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSA new antibiotic, IT-62-B was isolated from the culture broth of Streptomyces sp. IT-62 by extraction with acetone and then with ethyl acetate, followed by conventional column chromatography using silica gel, Sephadex LH-20 and silica ODS. Its structure (C39H47NO15, MW 769) was determined by 1H, 13C NMR, MS, IR and UV spectrometric techniques to be a new member of the baumycin-group anthracyclines. It showed moderate activity against Gram-positive bacteria and had antitumor activity against various tumor cell lines. Further, antibiotic IT-62-B converted the morphology of ras-transformed NIH3T3 cells and T-cells back to normal at concentrations inhibiting cell growth by 30% or more.View full abstractDownload PDF (807K) -
I. Taxonomy of Producing Strain, Fermentation, Isolation and Biological ActivitiesYUJI TABATA, NAOKO MIIKE, MASAHIRO HATSU, YASUSHI KURATA, TAKASHI YAGU ...1997 Volume 50 Issue 4 Pages 304-308
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSThree new nonsteroidal progesterone receptor ligands, PF1092A, B and C, have been isolated from Penicillium oblatum. They were purified from the solid cultures of rice media using ethyl acetate extraction, silica gel and Sephadex LH-20 column chromatographies, and crystallization. All three ligands competitively inhibited [3H]-progesterone binding to porcine uteri cytosol preparations with IG50 of 3.0×10 nM (PF1092A), 2.2×102 nM (PF1092B) and 2.2×103nM (PF1092C).View full abstractDownload PDF (445K) -
II. Physico-chemical Properties and Structure ElucidationYUJI TABATA, MASAHIRO HATSU, YASUSHI KURATA, KAORI MIYAJIMA, MASATO TA ...1997 Volume 50 Issue 4 Pages 309-313
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSThe structures of PF1092A (1), B (2) and C (3), new nonsteroidal progesterone receptor ligands produced by Penicillium oblatum, were elucidated by spectroscopic analyses. These compounds possess an eremophilane-type sesquiterpene carbon skeleton and differ only in that 1 and 2 are different monoacetates of 3. The absolute configurations of 1-3 were determined by single crystal X-ray diffraction analysis of the 4-bromobenzoyl ester of PF1092A and by measuring the optical rotations of the acetylation products of these compounds.View full abstractDownload PDF (377K) -
I. Taxonomy, Fermentation, Isolation and Biological ActivitiesKATSUHIRO SUZUKI, ATSUSHI KUWAHARA, HIROSHI YOSHIDA, SHINJI FUJITA, TA ...1997 Volume 50 Issue 4 Pages 314-317
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSFive novel cytotoxic antibiotics, NF00659A1 (1), A2(2), A3(3), B1(4) and B2(5) were discovered. They were isolated from a culture mycelium of Aspergillus sp. These compounds were proved to have 4, 5-seco-tricyclic diterpene α-pyrone structure by spectroscopic analyses. They showed potent antitumor activities against human ovarian carcinoma A2780 and human colorectal adenocarcinoma SW480 cells, but did not show any antimicrobial activities at 1, 000μg/ml against Gram-positive and Gram-negative bacteria, yeasts and fungi.View full abstractDownload PDF (380K) -
II. Structural ElucidationKATSUHIRO SUZUKI, ATSUSHI KUWAHARA, TAKAAKI NISHIKIORI, TAIZO NAKAGAWA1997 Volume 50 Issue 4 Pages 318-324
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSNF00659A1, A2, A3, B1 and B12, having insecticidal and antitumor activities, were isolated from a culture mycelium of Aspergillus sp. NF 00659. The novel structure of NF00659s were determined mainly by spectroscopic studies including various NMR measurements. NF00659s have a common structure which consists of acyl, α-pyrone and 4, 5-seco-tricyclic diterpene moieties.View full abstractDownload PDF (406K) -
I. Production, Isolation and Biological ActivitiesMICHAELA ENGLER, TIMM ANKE, OLOV STERNER, ULRICH BRANDT1997 Volume 50 Issue 4 Pages 325-329
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSPterulinic acid (1) and pterulone (2), two novel halogenated antibiotics, were isolated from fermentations of Pterula sp. 82168. Both compounds exhibited significant antifungal and weak or no cytotoxic activities. 1 and 2 are effective inhibitors of eucaryotic respiration. The target of the antibiotics resides within the mitochondrial NADH: ubiquinone oxidoreductase (complex I).View full abstractDownload PDF (324K) -
II. Physico-chemical Properties and Structure ElucidationMICHAELA ENGLER, TIMM ANKE, OLOV STERNER1997 Volume 50 Issue 4 Pages 330-333
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSThe structures of two novel fungal antibiotics, isolated from a Pterula species, that interfere with the NADH: ubiquinone oxidoreductase and inhibit the respiration of eucaryotes, were determined by spectroscopic techniques. Both compounds, pterulinic acid (1a) and pterulone (2), contain a 1-benzoxepin ring system and are chlorinated. Pterulinic acid (1a), which was obtained as a 1:5 inseparable mixture of the two isomers (Z)-1a and (E)-1a, in addition contains a furan. Their structures were determined by mass spectrometry and NMR spectroscopy, and 2D heteronuclear correlation experiments permitted the assignment of all NMR signals.View full abstractDownload PDF (271K) -
J. C. ONISHI, J. A. MILLIGAN, A. BASILIO, J. BERGSTROM, J. CUROTTO, L. ...1997 Volume 50 Issue 4 Pages 334-338
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSA family of-aminoacyl alkyl citrate compounds called viridiofungins, are novel squalene synthase inhibitors. The compounds have broad spectrum fungicidal activity but lack antibacterial activity. Although the compounds inhibit squalene synthase, the first committed step in ergosterol biosynthesis, results presented in this paper show that inhibition of fungal growth is not related to inhibition of ergosterol synthesis.View full abstractDownload PDF (342K) -
SUZANNE M. MANDALA, ROSEMARY A. THORNTON, BETH R. FROMMER, SARAH DREIK ...1997 Volume 50 Issue 4 Pages 339-343
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSViridiofungins are broad spectrum antifungal agents that inhibit the squalene synthase in vitro, but do not specifically inhibit fungal ergosterol synthesis in whole cells, indicating a different mode of action for antifungal activity. In this report, we show that viridiofungins are potent in vitro inhibitors of serine palmitoyltransferase, the first committed enzyme in Sphingolipid biosynthesis, and their antifungal activity is due to inhibition of Sphingolipid synthesis. Additional related components with the same mode of action were isolated from the producing culture, Trichoderma viride, and inhibition of the serine palmitoyltransferase and antifungal activity is presented.View full abstractDownload PDF (402K) -
SERGIO LOCIURO, PAOLO TAVECCHIA, ETTORE MARZORATI, PAOLO LANDINI, BETH ...1997 Volume 50 Issue 4 Pages 344-349
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSMDL 62, 879 (GE2270A) 1 is a new inhibitor of elongation factor-Tu (EF-Tu) and belongs to the class of thiazolyl pep tide antibiotics. Controlled acid hydrolysis of 1 followed by treatment with base resulted in the lost of the two terminal amino acids and in the formation of water-soluble MDL 62, 935 2. Although less active in vitro than its parent compound, 2 was able to inhibit by 50% an Escherichia coli cell-free protein synthesis system at roughly the same concentration of 1. MDL 62, 935 2 was subjected to further modification at the β-phenylserine residue. Derivatives obtained from 2 were less active in both antimicrobial (MIC) and enzymatic (IC50) assays. This suggests that β-phenylserine plays an important role for the inhibition of EF-Tu by 1 and 2.View full abstractDownload PDF (441K) -
OLUDOTUN A. PHILLIPS, DAVID P. CZAJKOWSKI, PAUL SPEVAK, MAYA P. SINGH, ...1997 Volume 50 Issue 4 Pages 350-356
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSA new β-lactamase inhibitor, SYN-1012, with a penem skeleton was synthesized and its biological activity compared with clavulanic acid, sulbactam, tazobactam and BRL-42715. The β-lactamase inhibitory activity of SYN-1012 was comparable to BRL-42715. Clavulanate and penam sulphones (sulbactam and tazobactam) were more active against TEM-1 and OXA-1, but were less active against TEM-3 and cephalosporinase (Case) than SYN-1012. In combination with piperacillin, SYN-1012 exhibited comparable or slightly lower synergistic effects than BRL-42715 against all the Gram-positive and Gram-negative isolates tested with only exception of Pseudomonas aeruginosa. The separate combinations of SYN-1012 and BRL-42715 with ceftazidime and cefotaxime provided comparable results against Gram-negatives, but not against Gram-positive isolates. Tazobactam was inferior to SYN-1012 in all cases. In comparison to tazobactam, SYN-1012 and BRL-42715 were relatively unstable in human and mouse plasma, and in mouse liver and kidney homogenates. Serum level of SYN-1012 and BRL-42715 after an intravenous administration of 20mg/kg in rabbit was undetectable after 1 hour.View full abstractDownload PDF (503K) -
HO-JAE LEE, MYUNG-CHUL CHUNG, CHOONG-HWAN LEE, BONG-SIK YUN, HYO-KON C ...1997 Volume 50 Issue 4 Pages 357-359
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSDownload PDF (204K) -
KEN-ICHI KURIHARA, KIYOSHI TANABE, RIE SHINEI, TSUNEO OKONOGI, YASUO O ...1997 Volume 50 Issue 4 Pages 360-362
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSDownload PDF (168K) -
SHINICHI KONDO, HIKARU NAKAMURA, YOKO IKEDA, HIROSHI NAGANAWA, KENJI M ...1997 Volume 50 Issue 4 Pages 363-365
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSDownload PDF (158K) -
V. Preparation of Unsubstituted L-Cladinose Analogues: Effect of Methylation of a 3"-Hydroxyl Group on the BioactivityKEIICHI AJITO, AKIRA SHIMIZU, SEIJI SHIBAHARA, OSAMU HARA, KEN-ICHI KU ...1997 Volume 50 Issue 4 Pages 366-369
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSDownload PDF (278K) -
HIDEAKI KAKEYA, HUI-PING ZHANG, KIMIE KOBINATA, RIE ONOSE, CHIZUKO ONO ...1997 Volume 50 Issue 4 Pages 370-372
Published: April 25, 1997
Released on J-STAGE: November 25, 2006
JOURNAL FREE ACCESSDownload PDF (205K)
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