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I. Producing Organism, Fermentation, Isolation and Biological Properties
KAICHIRO KOMINATO, YOSHIO WATANABE, SHIN-ICHI HIRANO, TOMOYUKI KIOKA, ...
1995 Volume 48 Issue 2 Pages
99-102
Published: February 25, 1995
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A strain of
Streptomyces was found to produce new piericidins. The compounds were purified and separated into two substances named Mer-A2026A and B.
These new piericidins exhibited vasodilating and depressor activities.
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II. Physico-Chemical Properties and Chemical Structures
KAICHIRO KOMINATO, YOSHIO WATANABE, SHIN-ICHI HIRANO, TOMOYUKI KIOKA, ...
1995 Volume 48 Issue 2 Pages
103-105
Published: February 25, 1995
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The structure of vasodilating acitive substances, Mer-A2026A and B, produced by
Streptomyces pactum Me2108 were determined on the basis of their spectral and chemical properties.
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KOICHI MATSUMOTO, KAZUSHIGE TANAKA, SHIGERU MATSUTANI, RYUJI SAKAZAKI, ...
1995 Volume 48 Issue 2 Pages
106-112
Published: February 25, 1995
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Thielocins A2α, A2β, A3, B1, B2 and B3 were isolated as a novel family of phospholipase A
2 inhibitors from the fermentation broth of
Thielavia terricola RF-143 together with thielavins and thielocins A1α and A1β. The most potent inhibitory activity (IC
50 = 0.0033μM) against rat group II phospholipase A
2 was shown by thielocin A1β. Against human group II phospholipase A
2, thielocin B3 (IC
50 = 0.076μM) was the most potent.
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Taxonomy, Isolation and Characterization
OSAMU NOZAWA, TADAYASU OKAZAKI, NORIYOSHI SAKAI, TOSHI KOMURASAKI, KAZ ...
1995 Volume 48 Issue 2 Pages
113-118
Published: February 25, 1995
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During our screening program for natural product drugs effective against multidrug-resistant mammalian cells, we have discovered a new δ lactone FD-211 from the fermantation broth of
Myceliophthora lutea TF-0409. FD-211 had a broad spectrum activity against cultured tumor cell lines, including adriamycin-resistant HL-60 cells.
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Production, Isolation, Structure Elucidation, and Biological Activity
U. GRÄFE, R. SCHLEGEL, M. RITZAU, W. IHN, K. DORNBERGER, C. STENG ...
1995 Volume 48 Issue 2 Pages
119-125
Published: February 25, 1995
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Aurantimycins A (
1), B (
2) and C (
3) were isolated from the mycelium of
Streptomyces aurantiacus JA 4570 as new representatives of the azinothricin group of hexadepsipeptide antibiotics. Their structures were settled by X-ray diffraction analysis of crystalline aurantimycin A (
1), high field homo- and heteronuclear 2D NMR experiments, high-resolution mass spectrometry and amino acid analysis. Aurantimycins are characterized by a new side chain containing fourteen carbon atoms. They display strong activity against Gram-positive bacteria and cytotoxic effects against L-929 mouse fibroblast cells.
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U. GRÄFE, W. IHN, M. RITZAU, W. SCHADE, C. STENGEL, B. SCHLEGEL, ...
1995 Volume 48 Issue 2 Pages
126-133
Published: February 25, 1995
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Helioferins A and B were detected as novel aminolipopeptides in cultures of
Mycogone rosea DSM 8822 in the course of a screening for mediators of helianthate anion transfer from aqueous to toluene phases. Their structures as novel antibiotics and cytotoxic agents were elucidated by mass spectrometry and NMR spectroscopic methods. Antimicrobial activity was estimated against
Candida albicans and Gram-positive bacteria including
Mycobacterium spp.
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Fermentation, Isolation, Structural Elucidation and Biological Activities
SHINICHI SAKEMI, TAISUKE INAGAKI, KEIJI KANEDA, HIDEO HIRAI, ETSUKO IW ...
1995 Volume 48 Issue 2 Pages
134-142
Published: February 25, 1995
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A fermentation broth of an unidentified fungus (N983-46) was found to produce DNA gyrase inhibitors, CJ-12, 371 (
1) and CJ-12, 372 (
2). Following isolation by solvent extraction and silica gel and ODS (reverse phase) chromatographies, the structures were determined to be novel spiro-ketal compounds with S-configuration at position C-1. CJ-12, 371 and CJ-12, 372 inhibit both DNA supercoiling and relaxation mediated by
Escherichia coli DNA gyrase. The interaction of these compounds with DNA gyrase appears to be novel in that the compounds inhibit supercoiling and relaxation without blocking religation; thus, no cleavage intermediate of double strand DNA is observed. Both compounds have antibacterial activity against several species of pathogenic Grampositive bacteria, with MICs between 25 and 100μg/ml. These results suggest that the antibacterial potency of CJ-12, 371 and CJ-12, 372 is attributed to the inhibition of DNA gyrase. However, the compounds did not inhibit DNA gyrase selectively, as they also inhibited eukaryotic topoisomerase II-mediated relaxation. Semi-synthetic modifications to the dihydroxy motif in CJ-12, 371 altered both gyrase- and topoisomerase Il-inhibitory activities, but did not enhance selectivity.
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YANG CAI, ANDREAS FREDENHAGEN, PAUL HUG, HEINRICH H. PETER
1995 Volume 48 Issue 2 Pages
143-148
Published: February 25, 1995
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From the staurosporine-producing strain
Streptomyces longisporoflavus R-19 various minor metabolites were isolated: They include a new compound with a nitro function in C-4' and other metabolites related to Staurosporine. The new structures were elucidated by spectroscopic methods, mainly
1H NMR and
13C NMR and by comparison with TAN-1030A. The new compounds inhibited protein kinase C with IC
50 values in the nanomolar range.
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V. Production, Isolation and Biological Activities of Bromine-containing Mycorrhizin and Lachnumon Derivatives and Four Additional New Bioactive Metabolites
MARC STADLER, HEIDRUN ANKE, OLOV STERNER
1995 Volume 48 Issue 2 Pages
149-153
Published: February 25, 1995
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Eight novel bioactive metabolites were isolated from submerged cultures of the ascomycete
Lachnum papyraceum (Karst.) Karst, when CaBr
2 was added to the cultures after the onset of secondary metabolism. Four of these metabolites (
16-
19) are bromo analogues of mycorrhizin A and lachnumon, while (1'
Z)-dechloromycorrhizin A (
12) and the papyracons A (13), B (
14), and C (
15) are non-halogenated compounds structurally related to the mycorrhizins. All compounds exhibited antimicrobial, cytotoxic, nematicidal and phy to toxic activities. The brominated mycorrhizins and lachnumons were found to be slightly less active than the chlorine-containing compounds. All mycorrhizin derivatives were mutagenic in the Ames test, suggesting DNA-alkylating properties.
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VI. Structure Determination of Non-halogenated Metabolites Structurally Related to Mycorrhizin A
MARC STADLER, HEIDRUN ANKE, RUDONG SHAN, OLOV STERNER
1995 Volume 48 Issue 2 Pages
154-157
Published: February 25, 1995
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The structure determination of four new biologically active non-halogenated metabolites isolated from submerged cultures of the ascomycete
Lachnum papyraceum is described. The compounds are structurally related to the antibiotic mycorrhizin A: (1'
Z)-Dechloromycorrhizin A (
12), a stereoisomer of dechloromycorrhizin A (
5) previously isolated from the same fungus, as well as papyracon A (
13), papyracon B (
14) and papyracon C (
15) containing an exocyclic double bond. The amounts of the latter three increased significantly when CaBr
2 was added to the culture medium. The structures were determined by spectroscopic methods.
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VII. Structure Determination of Brominated Lachnumon and Mycorrhizin A Derivatives
MARC STABLER, HEIDRUN ANKE, OLOV STERNER
1995 Volume 48 Issue 2 Pages
158-161
Published: February 25, 1995
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The structure determination of lachnumon B1 (
16) and lachnumon B2 (
17), brominated derivatives of lachnumon (
1), as well as mycorrhizin B1 (
18) and mycorrhizin B2 (
19), brominated derivatives of mycorrhizin A (
3), is described. The compounds, which exhibit similar antimicrobial and nematicidal activity as their chlorinated analogues, were isolated from extracts of cultures of the ascomycete
Lachnum papyraceum to which CaBr
2 had been added. The structures were elucidated by spectroscopic methods.
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III. Application of the Frit-FAB LC/MS Technique to the Elucidation of the Pradimicin S Biosynthetic Pathway
KYOICHIRO SAITOH, TAMOTSU FURUMAI, TOSHIKAZU OKI, FUMIKO NISHIDA, KEN- ...
1995 Volume 48 Issue 2 Pages
162-168
Published: February 25, 1995
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The biosynthetic pathway of pradimicin S (PRM-S) was investigated by using sinefungin and bioconversion experiments with aglycones of pradimicin A (PRM-A) and
Actinomadura spinosa AA0851, a PRM-S producer. Addition of sinefungin to the strain inhibited the formation of 11-
O-demethyl-7-
O-methylpradinone II (11dM-7M-PNII) as also determined to occur with its addition to the PRM-A producer. In feeding PRM-A aglycone and its analogs to the strain early in PRM-S biosynthesis, good identifications of bioconverted products were obtained by frit-FAB LC/MS as follows: 11-
O-demethylpradinone II (11dM-PNII), 11dM-7M-PNII, 11-
O-demethylpradinone I (11dM-PNI), 11-
O-demethylpradimicinone I (11dM-PMNI) and pradimicinone I (PMNI) were converted to PRM-S. Pradimicin B (PRM-B) and pradimicin L (PRM-L) were converted to PRMs-L and -S and PRM-S, respectively. A biosynthetic pathway for PRM-S is proposed.
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YASUHISA TSURUMI, KEIKO FUJIE, MOTOAKI NISHIKAWA, SUMIO KIYOTO, MASAKU ...
1995 Volume 48 Issue 2 Pages
169-174
Published: February 25, 1995
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WS79089B a highly specific endothelin converting enzyme (ECE) inhibitor has been isolated from the fermentation broth of
Streptosporangium roseum No. 79089. WS79089B showed highly selective ECE inhibition activity with IC
50 value of 0.14μM and behaved as a competitive inhibitor of ECE, with
Ki values of 8.9 × 10
-8M. The sodium salt of WS79089B (FR901533) inhibited big endothelin-1 (big ET-1) induced pressor effect in a dose dependent manner when administered to male Sprague-Dawley rats intravenously dosed 2 minutes prior to big ET-1 challenge.
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HIROYUKI KUMAGAI, TORU MASUDA, MASAAKI ISHIZUKA, TOMIO TAKEUCHI
1995 Volume 48 Issue 2 Pages
175-178
Published: February 25, 1995
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Antitumor effect of cytogenin against IMC carcinoma in mice was investigated. Since cytogenin did not show cytotoxicity against tumor cells
in vitro at 50μg/ml and toxicity at more than 2, 000 mg/kg i.p., it was considered that the antitumor effect is due to host mediated events. Cytogenin showed antitumor activity against a syngeneic murine transplantable tumor, IMC carcinoma by oral administration depending upon schedule of administration. The optimum effect was observed by the administration starting day 8 after transplantation of tumor cells, every other day for 10 times or every 2nd day for 7 times. The antitumor effect was reduced in immunosuppressed mice given anti-asialo GM 1 serum and in athymic mice, but not in mice irradiated with X ray. The antitumor effector cells activated by cytogenin were determined to be macrophages and T cells.
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MOTOMICHI KONO, YUTAKA SAITOH, MASAJI KASAI, KUNIKATSU SHIRAHATA
1995 Volume 48 Issue 2 Pages
179-181
Published: February 25, 1995
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IV. A Mutation in the Elongation Factor Tu Gene in a Resistant Mutant of B. subtilis
KAZUO SHIMANAKA, HIRONOBU IINUMA, MASA HAMADA, SOUICHI IKENO, KAYOKO S ...
1995 Volume 48 Issue 2 Pages
182-184
Published: February 25, 1995
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SATOMI KOSHINO, HIROYUKI KOSHINO, NOBUYASU MATSUURA, KIMIE KOBINATA, R ...
1995 Volume 48 Issue 2 Pages
185-187
Published: February 25, 1995
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YOSHIHIRO SUMITA, HIROSHI NOUDA, HISATOSHI SHINAGAWA, HIROSHI YAMAGA, ...
1995 Volume 48 Issue 2 Pages
188-190
Published: February 25, 1995
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