巻号一覧
54 巻, 4 号
選択された号の論文の9件中1～9を表示しています
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TOMOKAZU NAGAO, KYOKO ADACHI, MIHO SAKAI, MIYUKI NISHIJIMA, HIROSHI SA ...2001 年 54 巻 4 号 p. 333-339
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーSeven new macrolactins (named G-M) and known macrolactins A and F were isolated from a culture broth of Bacillus sp. PP19-H3. The strain had been isolated from the macroalga, Schizymenia dubyi. Macrolactin A, which was 24-membered lactone, had previously been reported to show antibacterial, cytotoxic and antiviral activities. The new macrolactins include 22-membered ring or dicyclic lactone in addition to geometric isomers of known macrolactins A and F. The antibacterial activities of all the macrolactins examined in this study were relatively weak.抄録全体を表示PDF形式でダウンロード (495K) -
YIDING HU, HEINZ G. FLOSS2001 年 54 巻 4 号 p. 340-348
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーFive new type II manumycins, containing the hydroxyquinol mC7N unit, asukamycins A-II, B-II, C-II, D-II, E-II, were discovered in cultures of Streptomyces nodosus ssp. asukaensis. The biosynthetic origin of the type II manumycins from the type I compounds, containing an epoxyquinol mC7N unit, was deduced from the time course of production and proven by preparing [7'-13C] asukamycin A and demonstrating its incorporation into asukamycin A-II.抄録全体を表示PDF形式でダウンロード (585K) -
MASAFUMI HAMADA, SHIGERU YAMAMOTO, SATORU MORIOUCHI, YASUO KISHINO2001 年 54 巻 4 号 p. 349-353
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーPhagocytic functions of rat alveolar macrophages (AM) following intraperitoneal injection of conagenin (CNG) and of AM sub-populations fractionated by Percoll discontinuous gradient centrifugation were investigated. Phagocytosis of opsonized-sheep red blood cells (SRBC) following in vitro incubation with CNG showed a significant increase in a higher density of AM (fraction IV). In addition, phagocytosis was also increased in lower density ones (fractions I and II) by macrophage-activating factor (MAP) co-cultivation. CNG-injected rats for 5 consecutive days showed a dose-dependent increase in phagocytosis of AM compared to the control rats. Although the distribution of AM sub-population in rats injected CNG was not significantly different compared to the control rats, phagocytosis was significantly increased in AM of a lower density fraction (fraction II). These results suggest that CNG directly increases phagocytosis of AM in a higher density fraction, and indirectly enhances phagocytosis in AM of a lower density fraction via increasing MAF-like material production.抄録全体を表示PDF形式でダウンロード (349K) -
LÁSZLÓ VÉRTESY, MICHAEL KURZ, ERICH F. PAULUS, DI ...2001 年 54 巻 4 号 p. 354-363
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーThe characterization of the structure of mumbaistatin (1), an effective inhibitor of the glucose-6-phosphatase system (EC 3.1.3.9), is reported. Isolation of mumbaistatin from cultures of Streptomyces sp. DSM 11641 was achieved by anion-exchange and reversed-phase chromatography. The acid-labile inhibitor was methylated for the structure determination. Single-crystal X-ray structure analysis of a triply methylated dehydration product, C31H24O11, revealed the structure of an aromatic dispirodiketal (2), a compound containing a previously undescribed ring system. Extensive 2D-NMR experiments with mumbaistatin and with the methylation products showed that mumbaistatin itself possesses the hydroxydiketodicarboxylic acid structure 1, C28H20O12, which, in the presence of acid or upon activation through methyl ester formation, undergoes self-condensation with loss of water to the dispirodiketal form (2). Mumbaistatin is an anthraquinone derivative, whose open-chain diketo form acts as a specific and powerful inhibitor of glucose-6-phosphate translocase: IC50=5nM. The activity towards the same enzyme of the cyclized dispirodiketal derivatives is roughly one thousand times lower.抄録全体を表示PDF形式でダウンロード (653K) -
IV. A Novel Water-soluble N-Phosphono Type Prodrug for Parenteral AdministrationTOMOYASU ISHIKAWA, YUTAKA NAKAYAMA, MITSUMI TOMIMOTO, SHIN-ICHI NIWA, ...2001 年 54 巻 4 号 p. 364-374
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーA systematic approach for improving the water-solubility of anti-MRSA (methicillin-resistant Staphylococcus aureus) cephalosporin derivatives is described. We first tried to improve the water-solubility of 7β-[2-(5-amino-1, 2, 4-thiadiazol-3-yl)-2(Z)-fluoromethoxyimino-acetamido]-3-[(E)-2-(1-methylimidazo[1, 2-b)]pyridazinium-6-yl)thiovinyl]-3-cephem-4-carboxylate (1a) by substitution of the C-3' pharmacophore. Replacement of the C-3' pharmacophore with a 1-methyl-4-pyridinio group improved the water-solubility without decreasing the anti-MRSA activity. Furthermore, we applied the N-modified prodrug strategy to the C-7 acyl group in order to enhance the water-solubility drastically. Among the compounds prepared, the N-phosphono type prodrugs 2a (1-methylimidazo[1, 2-b]pyridazinium derivative) and 2b (1-methyl-4-pyridinio derivative) showed water-solubility appropriate for a product intended for intravenous injection and in vivo anti-MRSA activity comparable to that of vancomycin.抄録全体を表示PDF形式でダウンロード (781K) -
BONG-SIK YUN, TOMOMI HIDAKA, TOMOHISA KUZUYAMA, HARUO SETO2001 年 54 巻 4 号 p. 375-378
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーPDF形式でダウンロード (533K) -
TAIJIRO TOMIKAWA, KAZUO SHIN-YA, TAISEI KINOSHITA, ATSUSHI MIYAJIMA, H ...2001 年 54 巻 4 号 p. 379-381
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーPDF形式でダウンロード (209K) -
MASAKI HANDA, TOSHIAKI SUNAZUKA, KENICHIRO NAGAI, RYOUKO KIMURA, TATSU ...2001 年 54 巻 4 号 p. 382-385
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーPDF形式でダウンロード (223K) -
MASAKI HANDA, TOSHIAKI SUNAZUKA, KENICHIRO NAGAI, RYOUKO KIMURA, KAZUH ...2001 年 54 巻 4 号 p. 386-391
発行日: 2001/04/25
公開日: 2008/09/19
ジャーナル フリーPDF形式でダウンロード (322K)
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