巻号一覧
57 巻, 2 号
選択された号の論文の11件中1～11を表示しています
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1. Taxonomy, Fermentation, Isolation and Biological PropertiesMASATO TANI, YASUHIRO GYOBU, TORU SASAKI, OSAMI TAKENOUCHI, TAKASHI KA ...2004 年 57 巻 2 号 p. 83-88
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーSix novel chymase inhibitors, SF2809-I, SF2809-II, SF2809-III, SF2809-IV, SF2809-V and SF2809-VI, were isolated from the fermentation broth of an actinomycete strain SF2809. The strain was identified as Dactylosporangium sp. by morphological, chemotaxonomical and phylogenetic studies. These six novel compounds inhibited recombinant human chymase in the range between IC50 of 0.014 and 7.3μM. However, they showed little or no inhibitory activity against chymotrypsin or cathepsin G, even though these two and chymase belong to the chymotryptic serine protease family. This result indicates that these compounds work as specific chymase inhibitors.抄録全体を表示PDF形式でダウンロード (1278K) -
2. Structural ElucidationMASATO TANI, KENZO HARIMAYA, YASUHIRO GYOBU, TORU SASAKI, OSAMI TAKENO ...2004 年 57 巻 2 号 p. 89-96
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーNovel chymase inhibitors, SF2809-I, II, III, IV, V and VI, were isolated from the fermentation broth of Dactylosporangium sp. SF2809, and their structures were determined by spectroscopic analyses. SF2809 compounds commonly contain a substituted indole moiety and a quinolinone moiety. The two moieties are connected to a methylene carbon in SF2809-I and III. The other compounds, SF2809-II, IV, V and VI, have an additional moiety, a p-hydroxyphenyl group or a phenyl group. In these compounds, all of three moieties are connected to a methine carbon. Furthermore, studies concerning the stereochemistry of SF2809-V revealed that the isolated compound was racemic, and the isomer possessing (R)-configuration was about thirty times more potent than another isomer.抄録全体を表示PDF形式でダウンロード (958K) -
I. Taxonomy, Fermentation, Isolation and Biological ActivitiesHIROYUKI KUMAGAI, TETSUYA SOMENO, KAZUYUKI DOBASHI, KUNIO ISSHIKI, MAS ...2004 年 57 巻 2 号 p. 97-103
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーIn the course of screening program for inhibitors of angiogenesis, novel substances designated as ICM0301A-H (1-8) were isolated from the culture broth of Aspergillus sp. F-1491. ICM0301s inhibited the growth of human umbilical vein endothelial cells (HUVECs) induced by basic fibroblast growth factor (bFGF) with IC50 values of 2.2-9.3μg/ml. ICM0301A (1) showed significant anti-angiogenic activity at lower than 10μg/ml in the angiogenesis model using rat aorta cultured in fibrin gel. ICM0301s showed very low cytotoxicity against various tumor cells. Furthermore, ICM0301A did not show any toxic symptom in mice by intraperitoneal injection at 100mg/kg.抄録全体を表示PDF形式でダウンロード (1301K) -
II. Physico-chemical Properties and Structure ElucidationTETSUYA SOMENO, HIROYUKI KUMAGAI, SHUN-ICHI OHBA, MASAHIDE AMEMIYA, HI ...2004 年 57 巻 2 号 p. 104-109
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーICM0301A (1), B (2) and their congeners (3-8) were isolated from a culture broth of Aspergillus sp. F-1491 as new angiogenesis inhibitors. Their structures were elucidated by spectroscopic analyses. ICM0301A and B have a substituted decalin skeleton containing two oxirane rings.抄録全体を表示PDF形式でダウンロード (700K) -
New Beauvericins, Potentiators of Antifungal Miconazole Activity, Produced by Beauveria sp. FKI-1366I. Taxonomy, Fermentation, Isolation and Biological PropertiesTAKASHI FUKUDA, MASAYOSHI ARAI, YUICHI YAMAGUCHI, ROKUROU MASUMA, HIRO ...2004 年 57 巻 2 号 p. 110-116
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーThree new beauvericins, designated beauvericins D, E and F, were isolated along with known beauvericin and beauvericin A, from the culture of Beauveria sp. FKI-1366 by solvent extraction. ODS column chromatography and HPLC. These compounds potentiate miconazole activity against not only wild Candida albicans but also fluconazole resistant C. albicans. Beauvericins D and E decreased the IC50 value of miconazole against fluconazole resistant C. albicans from 1.3μM to 0.25 and 0.31μM, respectively.抄録全体を表示PDF形式でダウンロード (1321K) -
New Beauvericins, Potentiators of Antifungal Miconazole Activity, Produced by Beauveria sp. FKI-1366II. Structure ElucidationTAKASHI FUKUDA, MASAYOSHI ARAI, HIROSHI TOMODA, SATOSHI OMURA2004 年 57 巻 2 号 p. 117-124
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーThe structures of beauvericins D, E and F, novel potentiators of miconazole activity against Candida albicans produced by Beauveria sp. FKI 1366, were elucidated by various spectroscopic analyses including UV, NMR, and MS and degradation experiments. They have the common skeleton of the 18-membered cyclodepsipeptides.抄録全体を表示PDF形式でダウンロード (782K) -
KEN-ICHI HARADA, KOJI TOMITA, KIYONAGA FUJII, KATSUYOSHI MASUDA, YUZUR ...2004 年 57 巻 2 号 p. 125-135
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーMadurastatins A1 (1), A2 (2) and A3 (3), novel pentapeptides that were acylated with salicylic acid at the N-terminus, were isolated from the culture broth of a pathogenic Actinomadura madurae IFM 0745 strain. These structures were mainly determined by 2D NMR and MS/MS spectral techniques. The strain produced simultaneously madurastatins B1 (4) and B2 (5) consisting of Ser and salicylic acid moieties. Compounds 1 and 4 had an antibacterial activity against Micrococcus luteus, indicating that the presence of the aziridine ring is essential for such activity. Because 1 has a strong affinity with ferric ion due to the presence of two hydroxamic acids and a salicylic acid, it is considered to be a siderophore that is a low molecular weight iron chelater. The production of siderophores may be one of the characteristics of pathogenic microorganisms.抄録全体を表示PDF形式でダウンロード (1223K) -
KEISUKE ISHIDA, TAKAYUKI TERUYA, SIRO SIMIZU, HIROYUKI OSADA2004 年 57 巻 2 号 p. 136-142
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーIn this paper we describe the establishment of an efficient visual method for screening heparanase inhibitors, and we present the results of screening 10, 000 microbial culture broths. Heparanase-overexpressing stable clones of the human hepatocellular carcinoma HepG2 cells were established and used as an enzyme source. Digestion of heparan sulfate (HS) was detected using novel HS-containing tablets or SDS-polyacrylamide gel electrophoresis. This method was able to find suramin, a known heparanase inhibitor, from a library of typical enzyme inhibitors. By screening 10, 000 culture broths of microorganisms (actinomycetes, fungi, and bacteria) an actinomycete strain, RK99-A234, was found to have heparanase inhibitory activity. RK-682 was identified in the fermentation broth as a heparanase inhibitor, IC50=17μM.抄録全体を表示PDF形式でダウンロード (2122K) -
ANNA N. TEVYASHOVA, ALEXANDER A. SHTIL, EUGENIA N. OLSUFYEVA, VALERIA ...2004 年 57 巻 2 号 p. 143-150
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーThe new hydrophilic derivatives of 14-hydroxycarminomycin were obtained using 13-dimethyl ketal of 14-bromocarminomycin (6) as the starting compound. The reductive alkylation of 6 with melibiose or D-galactose followed by hydrolysis of the corresponding intermediate bromoketals 9 and 11 produced 3'-N-[-α-D-(galactopyranosyl-(1→6)-O-D-1-desoxyglucit-1-yl]-14-hydroxycarminomycin (10) and 3'-N-(1-desoxy-D-galactit-1-yl)-14-hydroxycarminomycin (12), respectively. These novel derivatives 10 and 12 were less toxic than carminomycin or 14-hydroxycarminomycin for leukemia (K562) and breast carcinoma (MCF-7) cells. Importantly, carminomycin, 14-hydroxycarminomycin and compounds 10 and 12 were similarly active for wild type cells and their multidrug resistant (MDR) sublines, K562i/S9 and MCF-7Dox.抄録全体を表示PDF形式でダウンロード (1105K) -
Production, Antimicrobial Activity and Mechanism of ActionBRIGITTE KUNZE, ROLF JANSEN, GERHARD HÖFLE, HANS REICHENBACH2004 年 57 巻 2 号 p. 151-155
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーPDF形式でダウンロード (586K) -
TADASHI EGUCHI, KEITA YAMAMOTO, KAZUTOSHI MIZOUE, KATSUMI KAKINUMA2004 年 57 巻 2 号 p. 156-157
発行日: 2004/02/25
公開日: 2009/01/27
ジャーナル フリーPDF形式でダウンロード (205K)
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