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I. Taxonomy, Fermentation, Isolation and Biological Activity
FRANK PETERSEN, ANDREAS FREDENHAGEN, HELMUT METT, NICHOLAS B. LYDON, R ...
1995 年 48 巻 3 号 p.
191-198
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
Paeciloquinones A to F as well as versiconol have been isolated as inhibitors of protein tyrosine kinase from the culture broth of the fungus
Paecilomyces carneus P-177. The novel anthraquinones inhibit epidermal growth factor receptor protein tyrosine kinase in the micromolar range. Two compounds, paeciloquinones A and C, are potent and selective inhibitors of the v-abl protein tyrosine kinase with an IC
50 of 0.4μM. Dependent on the fermentation conditions, partially different sets of paeciloquinones may be produced. An HPLC method allows separation of all major active components.
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II. Characterization and Structure Determination
ANDREAS FREDENHAGEN, PAUL HUG, HANSPETER SAUTER, HEINRICH H. PETER
1995 年 48 巻 3 号 p.
199-204
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
Paeciloquinones A to F and versiconol have been isolated as inhibitors of protein tyrosine kinases from the culture broth of the fungus
Paecilomyces carneus P-177. The structures of the new anthraquinones were determined by spectroscopic methods, mainly
1H NMR and
13C NMR. The substitution pattern was established by investigation of the respective methylated derivatives.
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HARUKI YAMADA, KAZURO SHIOMI, QI XU, TAKAYUKI NAGAI, MAKI SHIBATA, IZU ...
1995 年 48 巻 3 号 p.
205-210
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
New panosialin analog, panosialins D and wD have been isolated from the culture broth of
Streptomyces sp. OH-5186. Their structures were elucidated as 5-(13-methylpentadecyl)-1, 3-benzenediol bis(sodium sulfate) and 5-(13-methylpentadecyl)-1, 3-benzenediol 1-(sodium sulfate), respectively. They showed strong inhibitory activity against α-mannosidase, α-glucosidase, and β-glucosidase. Panosialins wA-wD mixture also showed weak mitogenic activity but suppressed the mitogen induced activity.
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SHO-ZOU KAWADA, YOSHINORI YAMASHITA, KEIKO OCHIAI, KATSUHIKO ANDO, TOS ...
1995 年 48 巻 3 号 p.
211-216
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
Terpentecin and UCT4B are new family of antitumor antibiotics with topoisomerase II mediated DNA cleavage activity. Based on the taxonomic studies, the producing strain S-464 was identified as
Streptomyces sp. This strain is different from
Kitasatosporia griseola which had been identified as the terpentecin-producing strain in 1988. Fermentation studies showed that natural nitrogen sources supported higher titer of terpentecin, and the synthetic medium with inorganic nitrogen sources supported selective production of UCT4B. An improved isolation method was developed for the large scale purification of terpentecin.
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I. Taxonomy, Fermentation, Isolation, Characterization and Biological Activities
TOSHIO TSUCHIDA, HIRONOBU IINUMA, NAOKO KINOSHITA, TAKAKO IKEDA, TSUTO ...
1995 年 48 巻 3 号 p.
217-221
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
A new structural class of the antibiotic, azicemicins A (
1) and B (
2) were isolated from the culture broth of the strain MJ126-NF4, which was closely related to
Amycolatopsis sulphurea. They were purified by adsorption on Diaion HP-20, silica gel column chromatography and preparative TLC. The molecular formulas of
1 and
2 were determined to be C
23H
25O
9N and C
22H
23O
9N by HRFAB-MS, respectively. Azicemicins A and B have moderate growth inhibiting activity against Gram-positive bacteria and mycobacteria.
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MASAJI KAWATSU, TAKASHI YAMASHITA, MASAAKI ISHIZUKA, TOMIO TAKEUCHI
1995 年 48 巻 3 号 p.
222-225
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
The antitumor efficacy of antitumor agents at sublethal doses was investigated in combination with conagenin (CNG) against murine leukemias. Mice were inoculated with 1×10
3 L1210 cells iv and given 300mg/kg of cyclophosphamide (CY) ip on days 1 and 2 or on days 1, 5 and 9 after the tumor inoculation, and 5 mg/kg of CNG daily for 10 days. The administration of CNG was effective in increasing the number of cured mice and in prolonging the survival period of mice significantly, on both schedules of CY treatment. Moreover, the antitumor effect of CY against EL-4 was enhanced by CNG in increasing the number of cured mice, in CY treatment on days 1 and 2, and on days 1, 5 and 9.
The effect of CNG was examined with mitomycin C (MMC) and adriamycin (ADM) at sublethal doses against leukemias. The antitumor effects of MMC at 10 mg/kg against L1210, and ADM at 15 mg/kg against P388 administered on days 1 and 5 were enhanced by CNG. Although mice treated with ADM at 15 mg/kg died earlier than non-treated controls on days 1 and 2 against L1210, P388 and EL-4, CNG with ADM was effective in prolonging the survival period.
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JONG KOO PARK, KEIJI HASUMI, AKIRA ENDO
1995 年 48 巻 3 号 p.
226-232
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
Binding of modified lipoproteins including oxidized low density lipoprotein (oxidized LDL) to cell surface receptors is an initial step of conversion of monocyte-derived macrophages into lipid-laden foam cells, a key cellular component in the early lesions of atherosclerosis. We have searched for microbial metabolites that inhibit oxidized LDL-induced lipid accumulation in macrophages and isolated three compounds from a strain of
Bacillus sp. as inhibitors of oxidized LDL binding. By chemical and spectroscopic analyses, these metabolites were shown to be related to the cyclic lipopeptide iturin C. Two of these compounds were novel metabolites having long chain β-amino acid moieties of different length. These agents, at concentrations ranging from 5 to 20 μM, inhibited cell surface binding of oxidized
125I-LDL, resulting in reduced intracellular accumulation and degradation of the lipoprotein as well as in reduced cholesteryl ester formation from [
14C]oleate in macrophages J774.
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YOSHITOMO IKAI, HISAO OKA, JUNKO HAYAKAWA, MASAKADO MATSUMOTO, MAKOTO ...
1995 年 48 巻 3 号 p.
233-242
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
Total structures of 13 minor components of bacitracin (BC) were proposed, and their antimicrobial activities were investigated. The components of BC including bacitracins A (BC-A) and F (BC-F) were isolated by preparative HPLC and were hydrolyzed under acidic conditions. The resulting amino acids were derivatized with l-fluoro-2, 4-dinitrophenyl-5-L-alanineamide and were separated by HPLC to determine their absolute configurations. It was found that the
N-terminal amino acids of BC-A and its related components were epimerized during the hydrolysis to yield their enantiomers. The formation of these artifactual amino acids suggests that our previously proposed structures of the BC minor components are incorrect; therefore, the structures were corrected based on these results. The structures of the BC minor components were the same as that of BCs-A and -F except that one to three of the L-isoleucines, including the
N-terminal one, were replaced by L-valines. These structures were confirmed by tandem mass spectrometry under fast atom bombardment (FAB) conditions and Frit-FAB liquid chromatography/mass spectrometry. Based on the UV spectra of the BC components determined by photodiode array detection-HPLC analysis, a new systematic nomenclature was proposed for the minor components. The isolated components were also used for the determination of their minimal inhibition concentrations and it was found that BC-A is 2 - 8 times more potent than the other minor components against strains of
Micrococcus luteus and
Staphylococcus aureus.
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CHIYUKI KAWASAKI, SEIICHI OKAMURA, KAZUYA SHIMODA, KYUICHI NEMOTO, YOS ...
1995 年 48 巻 3 号 p.
243-247
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
15-Deoxy-11-
O-methylspergualin (MeDSG) is an analogue of 15-deoxyspergualin, which has potent immunosuppressive activity. The present study was designed to evaluate the
in vitro effects of MeDSG on the functions of peripheral blood mononuclear cells (PBMC) and bone marrow cells derived from healthy volunteers. MeDSG failed to suppress the proliferation of PBMC stimulated with mitogens. In the allogeneic mixed lymphocyte reaction, MeDSG strongly suppressed both the proliferation of lymphocytes and the generation of alloreactive cytotoxic T lymphocytes, but did not affect the cytolytic activity of the established cytotoxic T lymphocytes. MeDSG had no effect on the cytolytic activity of natural killer cells. Concerning positive hematopoietic regulators, MeDSG had a slight enhancing effect on the release of granulocyte-macrophage colony-stimulating factor and a slight inhibitory effect on the release of interleukin-6 and granulocyte colony-stimulating factor from PBMC stimulated with mitogens. Significantly, MeDSG completely suppressed the colony formation of bone marrow cells in the presence of granulocyte colony-stimulating factor.
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II. Synthesis, Antibacterial Activity and Tissue Distribution of 4'-Deoxy-10, 11, 12, 13-tetrahydrodesmycosin
AMALIA NARANDJA, ZELJKO KELNERIC, LIDIJA KOLACNY-BABIC, SLOBODAN DJOKI ...
1995 年 48 巻 3 号 p.
248-253
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
4'-Deoxy-10, 11, 12, 13-tetrahydrodesmycosin was prepared in six-step reactions. Antibacterial screening shows retained antibacterial spectrum of tylosin with some improvement against tylosin-sensitive
Staphylococci and
Haemophilus influenze. However, pharmacokinetic data demonstrated rapid distribution from blood in tissues and prolonged maintenance in all tissues, especially in the lungs, in comparison with tylosin.
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G. VERTUANI, M. BOGGIAN, A. SCATTURIN, M. RICCI, B. MELI BALBOCCHINO, ...
1995 年 48 巻 3 号 p.
254-260
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
The synthesis and a conformational study of a number of homologues of the well known antibiotic, phytotoxic leucinostatin A are reported. The circular dichroism of all the compounds are discussed. Some conclusions on the SAR of these compounds are drawn. The influence of the α-helical conformation and/or the increased lipophile character on their interesting biological activities is emphasized.
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III. Production of Novel Isocoumarin Derivatives, Isolation, and Biological Activities
MARC STABLER, HEIDRUN ANKE, OLOV STERNER
1995 年 48 巻 3 号 p.
261-266
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
During investigations on the influence of CaBr
2 on the secondary metabolism of
Lachnum papyraceum, the production of mycorrhizins and lachnumon type antibiotics was strongly inhibited in bromide-containing culture media. Instead, six isocoumarin derivatives, 6-hydroxymellein (
6), 4-chloro-6-hydroxymellein (
7), 4-bromo-6-hydroxymellein (
9), 6-methoxymellein (
10), 4-chloro-6-methoxymellein (
11), and 4-chloro-6, 7-dihydroxymellein (
12) were isolated. Compounds
7,
9,
11, and
12 have never been isolated from natural sources. 6-Hydroxymellein has been isolated previously from many sources including
Gilmaniella humicola and proposed to be a precursor of mycorrhizin A (see reference 6). In comparison to the mycorrhizins, the isocoumarin derivatives exhibited only weak antimicrobial, cytotoxic, phytotoxic, and nematicidal activities.
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IV. Structural Elucidation of Novel Isocoumarin Derivatives
MARC STABLER, HEIDRUN ANKE, OLOV STERNER
1995 年 48 巻 3 号 p.
267-270
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
The structures of four new biologically active halogenated dihydroiso coumarins isolated from submerged cultures of the ascomycete
Lachnum papyraceum have been elucidated by spectroscopic methods. The compounds are structurally related to lachnumon and mycorrhizin A, which are also produced by the fungus.
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SUGATA CHATTERJEE, E. K. S. VIJAYAKUMAR, SUKUMAR CHATTERJEE, J. BLUMBA ...
1995 年 48 巻 3 号 p.
271-273
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
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KIKOH OBI, TATSUHIRO SAITO, HIDEYUKI FUKUDA, KEIJI HIRAI, SEIGO SUZUE
1995 年 48 巻 3 号 p.
274-277
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
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KIKOH OBI, TATSUHIRO SAITO, AKIHIKO KOJIMA, HIDEYUKI FUKUDA, KEIJI HIR ...
1995 年 48 巻 3 号 p.
278-281
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
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TAIKWANG M. LEE, MARSHALL M. SIEGEL, GEORGE O. MORTON, JOSEPH J. GOODM ...
1995 年 48 巻 3 号 p.
282-285
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー
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KUNIAKI TATSUTA, SHOZO MIURA, SHIGERU OHTA, HIROKI GUNJI
1995 年 48 巻 3 号 p.
286-288
発行日: 1995/03/25
公開日: 2006/04/19
ジャーナル
フリー