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YUKI UCHIHATA, NORITAKA ANDO, YOKO IKEDA, SHINICHI KONDO, MASA HAMADA, ...
2002 年 55 巻 1 号 p.
1-5
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
The novel cyclic hexadepsipeptide named pipalamycin was isolated from a culture filtrate of
Streptomyces sp. ML297-90F8 as an apoptosis-inducing agent. The antibiotic was found to be consisting of each one mole of alanine,
N-hydroxyalanine, glycine,
N-acylated 3-hydroxyleucine, and two moles of piperazic acid. Pipalamycin induced apoptosis in apoptosis-resistant human pancreatic adenocarcinoma AsPC-1 cells at 0.3μg/ml in 24-48 hours. It also showed antibacterial activity on Gram-positive bacteria such as
Staphylococcus aureus and
Micrococcus luteus. Fermentation, isolation, structural elucidation and the biological activities of pipalamycin are described.
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SHINICHI SAKEMI, JON BORDNER, DEBRA L. DECOSTA, KOEN A. DEKKER, HIDEO ...
2002 年 55 巻 1 号 p.
6-18
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
CJ-15, 696 and 7 novel furopyridine antibiotics were isolated from the fungus
Cladobotryum varium CL12284. Their structures were determined by X-ray crystallography and spectral analysis. Three biotransformed analogs were also prepared from CJ-15, 696. CJ-15, 696 showed moderate activity against various Gram-positive bacteria including some drug resistant strains such as methicillin resistant
Staphylococcus aureus (MRSA).
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YUTAKA SUGIE, KOEN A. DEKKER, TAISUKE INAGAKI, YOON-JEONG KIM, TATSUO ...
2002 年 55 巻 1 号 p.
19-24
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
A new antibiotic, CJ-17, 572 (
I) was isolated from the fermentation broth of a fungus
Pezicula sp. CL11877. The structure of
I was determined to be a new equisetin derivative by spectroscopic analyses. The compound inhibits the growth of multi-drug resistant
Staphylococcus aureus and
Enterococcus faecalis with IC
50s of 10 and 20μg/ml, respectively.
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YUTAKA SUGIE, SAE INAGAKI, YOSHINAO KATO, HIROYUKI NISHIDA, CHANG-HONG ...
2002 年 55 巻 1 号 p.
25-29
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
A new equisetin derivative, CJ-21, 058 (
I) was isolated from the fermentation broth of an unidentified fungus CL47745. It shows antibacterial activity against Gram-positive multi-drug resistant bacteria by inhibiting ATP-dependent translocation of precursor proteins across a bacterial cell membrane.
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MASATOSHI TANIGUCHI, KOJI NAGAI, MASATO WATANABE, NAMI NIIMURA, KEN-IC ...
2002 年 55 巻 1 号 p.
30-35
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
A novel benz[
a]anthraquinone, YM-181741, was isolated from the culture broth of actinomycete strain Q57219. The strain was identified as
Streptomyces sp. by morphological and chemotaxonomic characterization. YM-181741 was purified from the culture supernatant by serial column chromatography. The structure of YM-181741 was determined by spectroscopic analysis including one- and two-dimensional NMR experiments. YM-181741 showed selective anti-
Helicobacter pylori activity with a MIC value of 0.2μg/ml.
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1. Production, Isolation and Biological Activities
BÄRBEL KÖPCKE, MARTIN JOHANSSON, OLOV STERNER, HEIDRUN ANKE
2002 年 55 巻 1 号 p.
36-40
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Eight secondary metabolites were isolated from submerged cultures of the ascomycete A111-95 during a search for new nematicidal metabolites. (-)-Galiellalactone (
7) and compound
2 are metabolites previously obtained from cultures of
Galiella rufa while the compounds
1, 3, 4, 5, 6 and
8 (
3 and
4 were obtained as an unseparable mixture), were isolated as natural products for the first time. Compound
2, pregaliellalactone (
5) and the mixture of
3 and
4 showed nematicidal activities towards
Caenorhabditis elegans and
Meloidogyne incognita. All compounds showed moderate or weak cytotoxic activities.
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Hydroxylation of Epo A and B to Epothilones E and F
KLAUS GERTH, HEINRICH STEINMETZ, GERHARD HÖFLE, HANS REICHENBACH
2002 年 55 巻 1 号 p.
41-45
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
When
Sorangium cellulosum So ce90 is grown without XAD adsorber resin there is a steady state of epothilone A and B biosynthesis and hydroxylation of these products to epothilones E and F. This biotransformation at position C-21 of the thiazole ring is not restricted to producers of epothilones. It is carried out by a substrate induced monooxygenase. Epothilones E and F are further degraded by opening of the lactone ring by an esterase. Steps of degradation of different strains of
S. cellulosum are compared.
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I. 13C-Labeling Experiments
HIROSHI HORI, TAKAYUKI KAJIURA, YASUHIRO IGARASHI, TAMOTSU FURUMAI, KA ...
2002 年 55 巻 1 号 p.
46-52
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Biosynthesis of hibarimicin was studied based on the feeding experiments with
13C labeled acetates. All carbons in the aglycon, except for the methoxy carbons, were derived from acetate. The carbon framework of the aglycon was proved to be constructed by dimerization of an intermediate which was biosynthesized
via the decarboxylation and skeltal rearrangement starting from an undecaketide. The rearrangement was confirmed by detecting the long range (three-bond) coupling between two carbons in the difference spectra of selective
13C decoupled INADEQUATE of hibarimicin B labeled with sodium [1, 2-
13C
2] acetate.
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II. Elucidation of Biosynthetic Pathway by Cosynthesis Using Blocked Mutants
TAKAYUKI KAJIURA, TAMOTSU FURUMAI, YASUHIRO IGARASHI, HIROSHI HORI, KA ...
2002 年 55 巻 1 号 p.
53-60
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
The biosynthetic pathway of hibarimicin (HBM) was proposed on the basis of the experimental results obtained by using blocked mutants of
Microbispora rosea subsp.
hibaria TP-A0121, the HBM producer. In its biosynthesis, the oxidative coupling of the aromatic undecaketide unit generates a symmetrical aglycon HMP-Y1 (hibarimicin-mutant product Y1), which is oxidatively modified to hibarimicinone, the HBM aglycon. The following glycosylation of hibarimicinone gives rise to the HBM complex. We identified that HMP-Y1 prepared by methanolysis of HMP-Y6, a glycosylated metabolite from a blocked mutant, was the key intermediate: transformation of
13C-labeled HMP-Y1 to HBM B was confirmed by NMR measurements. Mutant strain produced another type of aglycon HMP-P1 in which the coupled polyketide units were intramolecularly bridged by the ether bond. This metabolite also arose by the spontaneous elimination of methanol molecule from hibarimicinone.
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III. Structures of New Hibarimicin-related Metabolites Produced by Blocked Mutants
YASUHIRO IGARASHI, TAKAYUKI KAJIURA, TAMOTSU FURUMAI, HIROSHI HORI, KA ...
2002 年 55 巻 1 号 p.
61-70
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Structures of metabolites produced by blocked mutants of
Microbispora rosea subsp.
hibaria TP-A0121, hibarimicin-producer, were determined by spectroscopic analysis. HMP-Y6 is the dimer of the west half of hibarimicin B, the aglycon of which is the genuine biosynthetic intermediate. HMP-P1 is the shunt product arising from the release of a methanol molecule from hibarimicinone. HMP-P4, the glycoside of HMP-P1, is glycosylated with two amicetoses and two digitoxoses same as hibarimicin B. HMP-M1, M2, M3 and M4 are shunt products derived from the monomeric undecaketide intermediates.
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III. Immunosuppressive Efficacy
KAZUHIKO KUROSAWA, KOSAKU TAKAHASHI, NOBUAKI FUJISE, YASUSHI YAMASHITA ...
2002 年 55 巻 1 号 p.
71-77
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Novel immunosuppressants, SNF4435C and D produced by a strain of
Streptomyces spectabilis, were examined for their pharmacodynamical profiles. SNF4435C and D suppressed the responses of both murine splenocytes and human peripheral blood lymphocytes in the mixed lymphocyte reaction (MLR) with IC
50 values of 0.5μM and 0.2μM, respectively. In the mouse MLR experiments, SNF4435C and D did not block the production of interleukin-2 (IL-2) and the compounds-induced suppression was not restored by the addition of exogeneous IL-2. In addition, the significant inhibitory action was still retained even when SNF4435C or D was added after 48 hours from the start of the culture. These results were distinct from the behaviors observed with FK-506. SNF4435C, the major component, suppressed mouse delayed type hypersensitivity (DTH) and prolonged rat skin allograft survival.
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YUKIO KOIZUMI, KEIJI HASUMI
2002 年 55 巻 1 号 p.
78-82
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
We have found that malformin A
1, a cyclopentapeptide metabolite of
Aspergillus niger, enhanced 2.0-to 3.2-fold the
125I-fibrin clot lysis when incubated at 1-10μM with both U937 cells and blood plasma, both of which were essential to the malformin A
1 action. The effect was inhibited by ε-aminocaproic acid and anti-urokinase serum, but not by anti-tissue-type plasminogen activator IgG, showing that the enhancement was mediated by urokinase-catalyzed plasminogen activation. However, malformin A
1 affected neither cellular urokinase activity nor cell-free reactions involved in the fibrinolytic pathway. Malformin-treated, washed cell had an increased capacity to degrade fibrin in the presence of plasma. These results suggest that malformin A
1 enhances fibrinolytic activity by affecting cell-mediated response to initiate and/or propagate fibrinolytic activity.
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SHIGEKI OHYAMA, YASUKO WADA, KEIJI HASUMI
2002 年 55 巻 1 号 p.
83-91
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Three thiopeptide metabolites that enhance fibrin binding of plasminogen were isolated from a culture of
Streptomyces sp. R1401. A combination of spectroscopic analyses revealed that these compounds were identical with the antibiotic A10255B, E and G. These agents enhanced fibrin binding of plasminogen and plasminogen/urokinase-mediated fibirinolysis at concentrations of 5-20μM. A10255B reversibily increased urokinase-catalyzed activation of plasminogen by lowering
Km, while the agent did not enhance urokinase activity when substrates other than plasminogen were used, indicating that the agent affects plasminogen to increase its affinity to urokinase. A smaller but significant increase in activation was also observed when conformationally relaxed plasminogen derivatives such as Lys-plasminogen and mini-plasminogen were used. Two related thiopeptide antibiotics with a
C-terminal amide had no effect on plasminogen activation, suggesting a role of the terminal carboxyl of the A10255 molecule in activity.
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HAYAMITSU ADACHI, YOSHIO NISHIMURA, TOMIO TAKEUCHI
2002 年 55 巻 1 号 p.
92-98
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
Some derivatives of bactobolin were prepared from bactobolin (1) by transformation of the dichloromethyl group at C-3 to the hydroxymethyl, carboxylic acid, methanesulfonyloxymethyl and aldehydeoxime groups. The derivatives proved to be less active than the parent antibiotic 1 against bacteria as well as cytotoxicity, indicating that the functionality at C-3 considerably influences the biological activity.
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KEITA KONO, MASAKO SUGIURA, TAKAFUMI KOHAMA
2002 年 55 巻 1 号 p.
99-103
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
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2. Structure Elucidation
MARTIN JOHANSSON, BÄRBEL KÖPCKE, HEIDRUN ANKE, OLOV STERNER
2002 年 55 巻 1 号 p.
104-106
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
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SAYRA KHATUN, ALASTAIR C. W. WAUGH, MARIA B. REDPATH, PAUL F. LONG
2002 年 55 巻 1 号 p.
107-108
発行日: 2002/01/25
公開日: 2009/01/27
ジャーナル
フリー
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2002 年 55 巻 1 号 p.
C1
発行日: 2002年
公開日: 2009/01/27
ジャーナル
フリー