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I. PRODUCING STRAIN, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITY
HIROMASA OKADA, HAJIME SUZUKI, TOMOKO YOSHINARI, HIROHARU ARAKAWA, AKI ...
1994 年 47 巻 2 号 p.
129-135
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
A new topoisomerase II inhibitor, designated BE-22179, was isolated from the culture broth of
Streptomyces sp. A22179, which resembles "
Streptomyces gangtokensis". The inhibitor was extracted from the mycelial cake of the culture broth with organic solvent and successively purified by silica gel chromatography. BE-22179 inhibited topoisomerase II strongly but not topoisomerase I and showed potent antitumor activity against various tumor cell lines both
in vitro and
in vivo.
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I. FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITY
BARBARA E. ROGGO, FRANK PETERSEN, RON DELMENDO, HANS-BEAT JENNY, HEINR ...
1994 年 47 巻 2 号 p.
136-142
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
In the course of a screening program for HIV-1 protease inhibiting activity, six new homologues of 3-alkanoyl-5-hydroxymethyl tetronic acids (
1-
6) and the known natural product resistomycin (
7) were isolated from cultures of the
Actinomycete strain DSM 7357. The substituted tetronic acids belong to a recently described structural class of secondary metabolites. The HIV-1 activity of resistomycin (
7) has not been reported before.
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II.STRUCTURE DETERMINATION
BARBARA E. ROGGO, PAUL HUG, SERGE MOSS, FRITZ RASCHDORF, HEINRICH H. P ...
1994 年 47 巻 2 号 p.
143-147
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
The structures of six new homologues of 3-alkanoyl-5-hydroxymethyl tetronic acid (
1 -
6) were determined by spectroscopic methods.
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I. PRODUCTION, ISOLATION, AND BIOLOGICAL PROPERTIES
HIROSHI TOMODA, YOUNG KOOK KIM, HIROYUKI NISHIDA, ROKURO MASUMA, SATOS ...
1994 年 47 巻 2 号 p.
148-153
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
Aspergillus fumigatus FO-1289, a soil isolate, was found to produce a series of novel inhibitors of acyl-CoA: cholesterol acyltansferase (ACAT). Four active compounds, named pyripyropenes A, B, C and D, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography, ODS column chromatography and preparative HPLC. Pyripyropenes A, B, C and D show very potent ACAT inhibitory activity in an enzyme assay system using rat liver microsomes with IC
50 values of 58, 117, 53 and 268 nM, respectively.
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II. STRUCTURE ELUCIDATION OF PYRIPYROPENES A, B, C AND D
YOUNG KOOK KIM, HIROSHI TOMODA, HIROYUKI NISHIDA, TOSHIAKI SUNAZUKA, R ...
1994 年 47 巻 2 号 p.
154-162
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
The structures of pyripyropenes A, B, C and D, novel acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors, were determined mainly by spectroscopic studies including various NMR measurements. Pyripyropenes have a common structure which consists of pyridine, α-pyrone and sesquiterpene moieties. One of the three
O-acetyl residues in the sesquiterpene moiety of pyripyropene A is replaced with an
O-propionyl residue in pyripyropenes B, C and D.
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I. FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITY
CHIKARA SHINOHARA, KEIJI HASUMI, YOSHIO TAKEI, AKIRA ENDO
1994 年 47 巻 2 号 p.
163-167
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
A novel inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), designated gypsetin, was isolated from the cultured broth of
Nannizzia gypsea var.
incurvata IFO 9228 by solvent extraction, silica gel chromatography and crystallization. Gypsetin inhibited rat liver microsomal ACAT activity competitively with respect to the substrate oleoyl-CoA with an apparent
Ki value of 5.5μM. In cultured macrophage J774 cells incubated with oxidized low density lipoprotein, gypsetin inhibited cholesteryl ester formation from [
14C]oleate by 50% at a concentration of 0.65μM without affecting cell surface binding, uptake and degradation of the lipoprotein.
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II. STRUCTURE DETERMINATION
BERNHARD NUBER, FRITZ HANSSKE, CHIKARA SHINOHARA, SHINJI MIURA, KEIJI ...
1994 年 47 巻 2 号 p.
168-172
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
The elucidation of the structure of gypsetin, a new inhibitor of acyl-CoA: cholesterol acyltransferase, is described in this paper. By spectroscopic and X-ray crystallographic analyses, the structure of gypsetin has been determined to be 8a, 16a-dihydroxy-5a, 13a-bis[1, 1-dimethylallyl][l]benzazolidine[3"', 2'":4", 5"]azolidino[1", 2":4', 5'][1, 4]perhydrodiazin[1'2':1, 5]azolidino[2, 3-
b] [1] benzazolidine-7, 15-dione.
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I. FUNGI
FUMIHIRO FUJIMORI, TORU OKUDA
1994 年 47 巻 2 号 p.
173-182
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
For efficient fungal strain selection in microbial screening, we applied the random amplified polymorphic DNA (RAPD) method using the polymerase chain reaction (PCR). In order to evaluate this system, the genus
Trichoderma was employed, because its species are difficult to distinguish from each other. We selected an appropriate oligonucleotide decamer, R28 (5'-ATGGATCCGC), determined the optimal cycles of PCR as 30 cycles, simplified the template preparation method, and determined optimal concentrations of the template and
Taq DNA polymerase. We then examined 74 closely related strains of
Trichoderma. The electrophoretic band patterns of the PCR products were compared. According to the statistical analysis with the phylogenetic analysis using parsimony (PAUP), the results were consistent with the morphological, physiological and ecological data on these strains. Therefore, we conclude that RAPD is a simple, efficient and reliable method for the selection of fungal strains employed in screening.
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II. ACTINOMYCETES
YOJIRO ANZAI, TORU OKUDA, JUNKO WATANABE
1994 年 47 巻 2 号 p.
183-193
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
We evaluated the random amplified polymorphic DNA (RAPD) method using
Streptomyces lavendulae and
Streptomyces virginiae strains to eliminate duplicate actinomycete strains in our microbial screening program. The RAPD data were compared with phenotypic characteristics, DNA relatedness, HPLC analysis of metabolites and low-frequency restriction fragment analysis by pulsed-field gel electrophoresis. These results were consistent with each other. Therefore, we conclude that RAPD is a simple, efficient, and reliable method for the selection of actinomycete strains.
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III. BACTERIA
HITOMI TANAKA, SAYOKO SAWAIRI, TORU OKUDA
1994 年 47 巻 2 号 p.
194-200
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
Random amplified polymorphic DNA (RAPD) analysis was evaluated for the selection and elimination of bacterial strains used in microbial screening. For this pilot study we used eight bacterial strains producing fragin and two
Pseudomonas fragi strains, which are often isolated during the screening. A dendrogram constructed by the statistical analysis using parsimony, PAUP, based on the band patterns of RAPD with primer R28 was in good correlation with the results of DNA-DNA hybridization, HPLC analysis of metabolites, and conventional morphological and physiological characterization. RAPD was also applicable to a wide range of bacteria. This rapid selection system by RAPD was a very useful tool for excluding similar bacterial isolates encountered during screening.
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P. AMADE, M. MALLEA, N. BOUAÏCHA
1994 年 47 巻 2 号 p.
201-208
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
From the culture broth of a fungus, two metabolites have been isolated: bis(2-ethylhexyl) phthalate (DEHP) precedently isolated from
Streptomyces sp. and 2-(4-hydroxyphenyl)-2-oxoacetaldehyde oxime (PHBA) here reported as a natural compound in the (
E)-
s-
cis configuration. The producing organism was identified as a strain of
Penicillium olsonii. Culture growth and chemical identification are discussed in the present work.
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TETSURO FUJITA, KENICHIRO INOUE, SATOSHI YAMAMOTO, TAKESHI IKUMOTO, SH ...
1994 年 47 巻 2 号 p.
208-215
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
A potent immunosuppressive activity was found in the culture broth of the fungus
Isaria sinclairii (ATCC 24400). The metabolite, ISP-I ((2
S, 3
R, 4
R)-(
E)-2-amino-3, 4-dihydroxy-2-hydroxymethyl-14-oxoeicos-6-enoic acid, myriocin = thermozymocidin) suppressed the proliferation of lymphocytes in mouse allogeneic mixed lymphocyte reaction, but had no effect on the growth of human tumor cell lines. It also suppressed the appearance of plaque-forming cells in response to sheep red blood cells and the generation of allo-reactive cytotoxic T lymphocytes in mice after intraperitoneal or oral administration. The metabolite was 10- to 100-fold more potent than cyclosporin A as an immunosuppressive agent of the immune response
in vivo, and
in vivo, and appears to be a candidate for clinical application as a powerful immunosuppressant.
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TETSURO FUJITA, KENICHIRO INOUE, SATOSHI YAMAMOTO, TAKESHI IKUMOTO, SH ...
1994 年 47 巻 2 号 p.
216-224
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
In order to investigate the structure-activity relationships, fourteen derivatives of myriocin ((2
S', 3
R, 4
R)-(
E)-2-amino-3, 4-dihydroxy-2-hydroxymethyl-14-oxoeicos-6-enoic acid) were prepared and examined for immunosuppressive activity on mouse allogeneic mixed lymphocyte reaction
in vitro. Among them, 14-deoxomyriocin ((2
S, 3
R, 4
R)-(
E)-2-amino-3, 4-dihydroxy-2-hydroxymethyl-eicos-6-enoic acid) was the most potent. It also suppressed the generation of allo-reactive cytotoxic T lymphocytes in mice upon intraperitoneal administration, with a potency 10-fold greater than that of myriocin.
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A. Y. PAVLOV, E. N. OLSUFYEVA, T. F. BERDNIKOVA, I. V. MALKOVA, M. N. ...
1994 年 47 巻 2 号 p.
225-232
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
Alkylation of glycopeptide antibiotic eremomycin by the action of different alkyl halides leads, depending on the structure of alkyl halides used, to eremomycin derivatives of six types; alkylated at the
N-terminus, quaternary compounds at the
N-terminus, eremomycin esters, esters of eremocycin alkylated at the
N-terminus, esters of eremomycin quaternised at the
N-terminus, esters of eremomycin alkylated both at the
N-terminus and at the aminogroup of disaccharide branch. Five compounds demonstrated high antibacterial activity
in vitro,
N-allyleremomycin and methyl ester of
N,
N-dimethyleremomycin being at least as good as the parent eremomycin.
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SATORU NAITO, TOSHIHIKO NANBA, YUKA OWATARI, YASUO NAKADA, SHIGEKI MUR ...
1994 年 47 巻 2 号 p.
233-242
発行日: 1994/04/25
公開日: 2006/04/19
ジャーナル
フリー
Protection of the hydroxyl group at the C-5 position of milbemycin A
4 and D was carried out to investigate the influence of the C-5 hydroxyl group on the anthelmintic potency of these derivatives. Moreover, the hydroxyl group was converted into amide groups as bioisosters. Biological activities of these derivatives were measured against
Nippostrongylus brasiliensis in vitro, and minimal concentrations which induce 100% immotility in worms were determined for each derivative. Biological testing revealed that the hydroxyl group at C-5 is a structural requirement for retaining anthelmintic activity.
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YOSHIYUKI KOBAYASHI, MASAO SHIOZAKI
1994 年 47 巻 2 号 p.
243-246
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
Synthesis of trehazolin β-anomer (
3) from a D-glucose derived azido alcohol (
4), was accomplished. 2-Chloro-l-methylpyridinium iodide was used in place of 2-chloro-3-ethylbenzoxazolium tetrafluoroborate as a means of preventing concomitant anomerization. Evaluation of compound (
3) reveals that the stereochemistry of the anomeric position is significant for generation of inhibitory activities towards trehalases.
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RICHARD J. P. CANNELL, MICHAEL J. DAWSON, RICHARD S. HALE, Richard M. ...
1994 年 47 巻 2 号 p.
247-249
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
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KENICHI YASUMURO, MRTSUYOSHI SHIBAZAKI, TOSHIO SASAKI, HARUMITSU IMAI, ...
1994 年 47 巻 2 号 p.
250-252
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
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JOHN H. BATESON, GEORGE BURTON, STEPHEN C.M. FELL, HAZEL C. SMULDERS
1994 年 47 巻 2 号 p.
253-256
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
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N. IMAMURA, K. ADACHI, H. SANO
1994 年 47 巻 2 号 p.
257-261
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー
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KUNIAKI TATSUTA, MANABU ITOH
1994 年 47 巻 2 号 p.
262-265
発行日: 1994/02/25
公開日: 2006/04/19
ジャーナル
フリー