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I. Taxonomy of Producing Strain, Fermentation, Isolation, and Physico-chemical and Biological Properties
TATSUHIRO OGAWA, KATSUHIKO ANDO, TAKEO TANAKA, YOUICHI UOSAKI, YUZURU ...
1996 Volume 49 Issue 1 Pages
1-5
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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RES-1149-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the cultured broth of a fungus,
Aspergillus sp. RE-1149. RES-1149-1 and -2 selectively inhibited the ET-1 binding to endothelin type B receptor (ET
B receptor) with IC
50 values of 1.5μM and 20μM, respectively. Taxonomy of producing strains, fermentation, isolation, and physico-chemical properties of RES-1149-1 and -2 are described.
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II. Structure Determination and Derivatization
YOUICHI UOSAKI, MAYUMI YOSHIDA, TATSUHIRO OGAWA, YUTAKA SAITOH
1996 Volume 49 Issue 1 Pages
6-12
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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The structures of two novel non-peptidic endothelin type B receptor antagonists, RES-1149-1 and -2 were determined by spectroscopic methods. Several derivatives were synthesized from RES-1149-1 for biological assay.
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I. Fermentation, Isolation and Biological Activity
BARBARA E. ROGGO, FRANK PETERSEN, MATTHEW SILLS, JOHANNES L. ROESEL, T ...
1996 Volume 49 Issue 1 Pages
13-19
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Six novel Spirodihydrobenzofuranlactams I-VI (1-6) and a related spirodihydrobenzofuranalcohol, the previously described natural compound L-671, 776 (7), were isolated from cultures of two different
Stachybotrys species. These secondary metabolites showed antagonistic effects in the endothelin receptor binding assay and inhibited HIV-1 protease. Both biological activities are novel for L-671, 776 (7). The pseudosymmetric spirodihydrobenzofuranlactam VI (6) is the most potent representative of this class of compounds exhibiting IC
50 values of 1.5 μm in the ET-A receptor binding assay and 11 μM in the HIV-1 protease inhibition assay.
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I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological Activities
WON-GON KIM, JONG-PYUNG KIM, CHANG-JIN KIM, KE-Ho LEE, ICK-DONG Yoo
1996 Volume 49 Issue 1 Pages
20-25
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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In the course of screening for free radical scavengers, rare metabolites, benzastatins A and B having aminobenzamide skeleton, and benzastatins C and D having tetrahydroquinoline skeleton, were isolated from the culture broth of
Streptomyces nitrosporeus 30643. They showed inhibitory activity against lipid peroxidation in rat liver microsomes. In the cell assay, benzastatins C and D inhibited glutamate toxicity in N18-RE-105 cells with EC
50 values of 2.0 and 5.4μM, respectively.
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II. Structure Determination
WON-GON KIM, JONG-PYUNG KIM, ICK-DONG Yoo
1996 Volume 49 Issue 1 Pages
26-30
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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The structures of benzastatins A, B, C, and D, new free radical scavengers, were determined by spectroscopic studies. Benzastatins A and B incorporate the
para-aminobenzamide unit which is rare in fungal metabolites. Benzastatins C and D are unique alkaloids related to virantmycin; they contain the tetrahydroquinoline unit in the molecules.
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YOUNG-KOOK KIM, HYUN-WOO LEE, KWANG-HEE SON, BYOUNG-MOG KWON, TAE-SOOK ...
1996 Volume 49 Issue 1 Pages
31-36
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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A new inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), designated GERI-BP002-A, was isolated from the culture broth of
Aspergillus fumigatus F93 by acetone extraction, EtOAc extraction, SiO
2 column chromatography and reverse phase HPLC. Spectroscopic analyses of the compound identified bis (2-hydroxy-3-
tert-butyl-5-methylphenyl) methane as the structure and its molecular weight and formula to be 340 and C
23H
32O
2, respectively. GERI-BP002-A inhibited ACAT activity by 50% at the concentration of 50 μM in an enzyme assay system using rat liver microsomes.
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Taxonomy of the Producing Organism, Fermentation, Isolation, Physico-chemical Properties and Biological Activities
KAZUTOSHI SAKAMOTO, EISAKU TSUJII, FUMIE ABE, TOMOKO NAKANISHI, MICHIO ...
1996 Volume 49 Issue 1 Pages
37-44
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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FR901483, a novel immunosuppressant, has been isolated from the fermentation broth of
Cladobotryum sp. No. 11231. The molecular formula of FR901483 has been determined as C
20H
31N
2O
6P. FR901483 exerts a potent immunosuppressive activity
in vitro and significantly prolongs graft survival time in the rat skin allograft model. This compound has an intriguing tricyclic structure possessing a phosphate ester in its molecule. The ester residue may play an important role in exerting immunosuppressive activity because the desphosphoryl compound is devoid of activity. It is thought that the primary target of immunosuppression by this compound is inhibition of purine nucleotide biosynthesis.
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TOSHIKI INOUE, KEIJI HASUMI, TOHRU KUNIYASU, AKIRA ENDO
1996 Volume 49 Issue 1 Pages
45-49
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Four novel cyclic pentapeptides, designated plactins A, B, C and D, were isolated by solvent extraction and reverse-phase HPLC from mycelium of a fungal strain F165 that belongs to the order of Agonomycetales. By a combination of chemical and spectroscopic analyses and chemical synthesis, the structures of plactins A, B, C and D were determined to be
cyclo(-D-Val-L-Leu-D-
alloIle-L-Tyr-D-Arg-),
cyclo(-D-Val-L-Leu-D-Leu-L-Tyr-D-Arg-),
cyclo(-D-Val-L-Leu-D-
alloIle-L-Phe-D-Arg-) and
cyclo(-D-Val-L-Leu-D-Leu-L-Phe-D-Arg-), respectively. Plactins stimulated U937 cellmediated degradation of
125I-fibrin plates by 50% at a concentration of 7.5-32 μM.
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YUMI ENOMOTO, KAZURO SHIOMI, MASAHIKO HAYASHI, ROKURO MASUMA, TOMOYA K ...
1996 Volume 49 Issue 1 Pages
50-53
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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A new herquline analog, herquline B was isolated from the culture broth of
Penicillium herquei Fg-372. Herquline B contains one piperazine and two cyclohexenones. The pyrrolidine ring of herquline A was cleaved to yield herquline B. The IC
50 value of herquline B against platelet aggregation induced by ADP and platelet-activating factor were 1.6 and 5.0 μM, respectively.
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I. Taxonomy of Producing Organism, Fermentation, Isolation, and Structure Elucidation
TOSHIO TAKATSU, MASAAKI TAKAHASHI, YUMI KAWASE, RYUZO ENOKITA, TAKAO O ...
1996 Volume 49 Issue 1 Pages
54-60
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Novel heparanase inhibitors, A-72363 A-1, A-2, and C, were isolated from the culture filtrate of
Streptomyces nobilis SANK 60192 by column chromatography on various resinous adsorbents, followed by preparative anion exchange HPLC. Spectroscopic studies revealed that they are diastereomers of siastatin B, a neuraminidase inhibitor.
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II. Biological Activities
YUMI KAWASE, MASAAKI TAKAHASHI, TOSHIO TAKATSU, MASATOSHI ARAI, MOTOWO ...
1996 Volume 49 Issue 1 Pages
61-64
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Inhibitory activities of A-72363 A-1, A-2, and C, the diastereomers of a neuraminidase inhibitor siastain B, against various glycosidases were tested in comparison to siastatin B. Despite these compounds differing only in their configuration, each compound showed strikingly different specificities towards the various glycosidases tested. A-72363 C inhibited bovine liver β-glucuronidase and tumor cell heparanase with IC
50 values of 1.6 μM and 12 μM, respectively.
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II. Isolation, Physico-chemical Properties and Structure Elucidation
MAKOTO UBUKATA, TETSU-ICHIRO MORITA, MASAKAZU URAMOTO, HIROYUKI OSADA
1996 Volume 49 Issue 1 Pages
65-70
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Sparoxomycins Al and A2, isolated from the fermentation broth and mycelium of
Streptomyces sparsogenes SN2325, are new inducers of the flat reversion of NRK cells transformed by temperature sensitive Rous sarcoma virus. Sparoxomycins Al and A2 were isolated by active carbon chromatography, centrifugal partition chromatography (CPC), ODS column chromatography and preparative HPLC. The structure of Sparoxomycins were determined by spectroscopic evidences. Stereochemical assignments of these inducers were executed from the analyses of CD spectra.
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Production, Physico-chemical and Biological Properties of Jerangolid A
KLAUS GERTH, PETER WASHAUSEN, GERHARD HÖFLE, HERBERT IRSCHIK, HAN ...
1996 Volume 49 Issue 1 Pages
71-75
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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An antifungal activity was detected in the culture broth of the myxobacterium,
Sorangium cellulosum strain So ce 307. The activity was excreted into the supernatant during the log and early stationary phase. When the organism was fermented in the presence of the adsorber resin XAD-16, the metabolite was quantitatively bound to the resin. The main component, Jerangolid A, has structural similarities to ambruticin, which is also produced by strains of
Sorangium cellulosum.
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HITOSHI IZUMIDA, NOBUTAKA IMAMURA, HIROSHI SANO
1996 Volume 49 Issue 1 Pages
76-80
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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A new chitinase inhibitor, CI-4, was isolated from the culture broth of a marine bacterium
Pseudomonas sp. IZ208. The structure of CI-4 was determined to be cyclo(L-Arg-D-Pro) by spectral studies and comparison with a synthetic sample. CI-4 showed inhibitory activity against chitinase.
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YUICHI NAGANO, NAOTO TAKEUCHI, RYO MURAMATSU, YOICHI OHBA, SHIN-ICHIRO ...
1996 Volume 49 Issue 1 Pages
81-85
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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We established an improved production of an antitumor polypeptide antibiotic, phenomycin (PHM), by using a genetically engineered
Escherichia coli. Phenomycin consists of 89 natural amino acids without intramolecular disulfide bridge. PHM gene was synthesized as a fusion gene in which PHM at the C-terminus and the residues 1-20 of Hirudin variant 1 (HV1) at the N-terminus connected by the factor Xa recognition sequence (Ile-Glu-Gly-Arg).
E. coli JM 109 transformed with a plasmid containing the synthesized gene expressed a fusion protein and the trypsinization of the fusion protein purified by ultrafiltration and ion-exchange chromatography gave efficiently recombinant PHM at a final yield of 50 mg/liter of culture. This PHM yield was six times higher than that obtained by a natural PHM producing strain of
Streptoverticillium baldacci. Recombinant PHM was not distinguishable from natural PHM in all aspects observed.
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JUNJI MAGAE, MATTHEW W. MILLER, KAZUO NAGAI, GENE M. SHEARER
1996 Volume 49 Issue 1 Pages
86-90
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Metacycloprodigiosin is an antibiotic that has been shown to suppress T-cell proliferation induced by concanavalin A
in vitro. We examined the effect of metacycloprodigiosin on murine allogeneic skin and heart transplantation models, and compared graft rejection with donor-specific cytotoxic T-cells and antibody activity. The antibiotic slightly prolonged the survival of C57B1/6 heart and skin grafts in BALB/c mice, although the effect was less than that of cyclosporin A. The effect was more evident in Bml (H-2D mutant) skin grafts on G57B1/6 hosts or in a minor histocompatibility antigen-mismatched model. In contrast, metacycloprodigiosin suppressed anti-graft cytotoxic T-cell activity of BALB/c spleen grafted with C57B1/6 skin as comparable to cyclosporin A, but had only partial effect on antibody production. Thus, metacycloprodigiosin is more effective in reducing splenic cytotoxic T-cell activity than in prolonging murine skin or cardiac allografts.
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TAKAFUMI KOHAMA, HIROAKI MAEDA, JUNKO IMADA SAKAI, AKIO SHIRAISHI, KAZ ...
1996 Volume 49 Issue 1 Pages
91-94
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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Leustroducsin B (LSN-B), a novel colony-stimulating factor (CSF) inducer produced by an actinomycetes, has previously been shown to induce CSF production in bone marrow stromal cells. To determine the biological activity of LSN-B on hematopoiesis
in vivo, LSN-B was administered intraperitoneally to mice every day for three to six days. Peripheral platelet counts were markedly elevated on days 4 through to 6 compared with the control mice injected with vehicle. Serum IL-6 levels were low (0.8 ng/ml) or virtually undetectable in the drug treated groups. This cytokine profile suggests that LSN-B induction of thrombocytosis is mechanistically distinct from other cytokine inducers such as IL-1 or FK-565.
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II. Physicochemical Properties and Structural Elucidation
SATOSHI TAKAMATSU, YONG-PIL KIM, MASAHIKO HAYASHI, HIDEMI HIRAOKA, MAS ...
1996 Volume 49 Issue 1 Pages
95-98
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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New anticell-adherence compounds, macrosphelides A and B, were isolated from the fermentation broth of
Microsphaeropsis sp. FO-5050, and their structures were elucidated by spectroscopic methods and by chemical transformations. Macrosphelides A (M.W. 342, C
16H
22O
8) and B (M.W. 340, C
16H
20O
8) with three esters in their molecules were classified as 16-membered macrocyclic compounds. Macrosphelide B was found to be a corresponding oxidative product of macrosphelide A at the C-14 position.
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MYUNG-CHUL CHUNG, HYO-KON CHUN, KYOU-HOON HAN, HO-JAE LEE, CHOONG-HWAN ...
1996 Volume 49 Issue 1 Pages
99-102
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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HIROMASA OKADA, MASAO NAGASHIMA, HAJIME SUZUKI, SHIGERU NAKAJIMA, KATS ...
1996 Volume 49 Issue 1 Pages
103-106
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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YUNZHENG LE, KEVIN C. SMITH, LEO C. VINING, ROBERT L. WHITE
1996 Volume 49 Issue 1 Pages
107-109
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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KENICHI HAYASHI, MOTOAKI NISHIKAWA, ICHIRO ARAMORI, SUMIO KIYOTO, MASA ...
1996 Volume 49 Issue 1 Pages
110-112
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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SHINICHI KONDO, YOKO IKEDA, TOMIO TAKEUCHI, RIE SHINEI, SHUICHI GOMI, ...
1996 Volume 49 Issue 1 Pages
113-114
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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LÁSZLÓ VÉRTESY, HANS-WOLFRAM FEHLHABER, HERBERT K ...
1996 Volume 49 Issue 1 Pages
115-118
Published: January 25, 1996
Released on J-STAGE: November 21, 2006
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