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61.
Nakazawa J Yajima J Usui T Ueki M Takatsuki A Imoto M Toyoshima YY Osada H 《Chemistry & biology》2003,10(2):131-137
To reveal the mechanism of mitosis, the development of M phase-specific inhibitors is an important strategy. We have been screening microbial products to find specific M phase inhibitors that do not directly target tubulins, and rediscovered terpendole E (TerE) as a novel Eg5 inhibitor. TerE did not affect microtubule integrity in interphase, but induced formation of a monoastral spindle in M phase. TerE inhibited both motor and microtubule-stimulated ATPase activities of human Eg5, but did not affect conventional kinesin from either Drosophila or bovine brain. Although terpendoles have been reported as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT), the Eg5 inhibitory activity of TerE was independent of ACAT inhibition. Taken together, we demonstrate that TerE is a novel Eg5 inhibitor isolated from a fungal strain. 相似文献
62.
Hasegawa Y Fukuda T Hagimori K Tomoda H Omura S 《Chemical & pharmaceutical bulletin》2007,55(9):1338-1341
Six new alkylitaconic acids, designated tensyuic acids A to F, were isolated from the culture broth of Aspergillus niger FKI-2342 by solvent extraction, silica gel column chromatography and HPLC. Their structures were elucidated by spectroscopic analysis including UV, NMR, and MS. They are all alkylitaconic acid derivatives. Only tesyuic acid C showed moderate antimicrobial activity against Bacillus subtilis. 相似文献
63.
Anti-allergic effect of the flavonoid myricitrin from Myrica rubra leaf extracts in vitro and in vivo 总被引:1,自引:0,他引:1
Flavonoids are ingested by the general population as anti-oxidant and anti-inflammatory agents. In this study, we investigated the effects of myricitrin, a flavonoid rich in Myrica rubra leaf, upon anti-inflammatory action. Myrica rubra leaf extracts inhibited pro-inflammatory TNFα production in a macrophage cell line, Raw264.7 cells. We observed that the serum IgE levels in the leaf extract-treated DO11.10, a mouse allergy model, were down-regulated. HPLC was performed to demonstrate that M. rubra leaf extracts contain a large amount of myricitrin. We observed an inhibitory effect of HPLC-purified myricitrin on TNFα production in Raw264.7 cells. Thus, myricitrin may be of potential interest in the management of inflammatory conditions. 相似文献
64.
65.
Toshiyuki Chikuma Yoko ShimabukuroTakeya Iguchi Akira TanakaKyoji Taguchi Takeshi KatoMitsune Yamaguchi Hiroshi Hojo 《Analytica chimica acta》2002,457(2):157-164
A rapid and sensitive assay for the determination of Dns-His-Lys-Arg-His-Lys cleaving enzyme activity is reported. This assay is based on fluorimetric detection of a dansylated dipeptide, 5-dimethylaminonaphthalene-1-sulfonyl-His-Lys, enzymatically formed from the substrate 5-dimethylaminonaphthalene-1-sulfonyl-His-Lys-Arg-His-d-Lys, after separation by high-performance liquid chromatography (HPLC) using a C-18 reversed-phase column by isocratic elution. This assay is sensitive enough to measure 5-dimethylaminonaphthalene-1-sulfonyl-His-Lys at concentrations as low as 7 pmol, and yields highly reproducible results and requires less than 9.0 min per sample for separation and quantitation. The optimum pH for Dns-His-Lys-Arg-His-Lys cleaving enzyme activity was 7.5-8.0. The Michaelis constant (Km) and the maximum velocity (Vmax) values were 33.3 μM and 47.07 pmol/(μg h), respectively with the use of enzyme extract obtained from bovine pituitary. By using this assay, axonal transport of this enzyme activity was observed 48 h after double ligations of rat sciatic nerves. The high sensitivity and selectivity of this assay would be useful for clarification of the physiological role of this enzyme. 相似文献
66.
Mochizuki T Kondo Y Abe H Taylor CW Potter BV Matsuda A Shuto S 《Organic letters》2006,8(7):1455-1458
[structure: see text] 5'-Deoxy-5'-phenyladenophostin A (5), designed as a useful IP(3) receptor ligand based on the previous structure-activity relationship studies, was successfully synthesized via two key stereoselective glycosidation steps. This compound proved to be a highly potent IP(3) receptor agonist. 相似文献
67.
Dimethylarsinic acid (DMA) is the most effective inducer of cell‐cycle disruption among the arsenic compounds and their metabolites. The present study was conducted to gain further insight into cell‐cycle disruption induced by DMA. The inhibition of cell proliferation and the mitotic arrest induced by DMA were significant and dose‐dependent in Chinese hamster V79 cells and the two seemed to be closely related. At less than 140 µM the DMA did not inhibit the proliferation of cells, but it significantly induced mitotic arrest. An indirect immunofluorescence assay using anti‐α‐tubulin antibodies revealed that DMA induced the formation of abnormal spindles in the metaphase cells even at 350 µM with 5 h of treatment. At 1.4 mM DMA no metaphase cells could form a definite spindle structure. The spindle figures were similar to those induced by colchicine (125 nM ) or vinblastine (110 nM ), major antimitotic agents. In DMA‐treated interphase cells, the microtubule networks were indistinguishable from those of normal cells. With the tubulin‐assembly assay estimated by turbidity, DMA at less than 200 µM suppressed tubulin assembly in a dose‐dependent manner, whereas at more than 700 µM it enhanced tubulin polymerization remarkably with or without addition of excess guanosine‐5′‐triphosphate. According to the above findings, we discussed the possibility that DMA, a primary metabolite of inorganic arsenic in mammals, is related to arsenic carcinogenicity. Copyright © 2001 John Wiley & Sons, Ltd. 相似文献
68.
Yoko Masuda Kozue Hirabayashi Keiko Sakuma Tadashi Nakanishi 《Colloid and polymer science》2002,280(5):490-494
The swelling behavior of poly(ethylene oxide) (PEO) gels in aqueous solutions of sodium dodecyl sulfate (SDS) with and without
NaCl was investigated. In the absence of NaCl, PEO gels with different degrees of cross-linking began to swell from a concentration
lower than the critical micelle concentration (cmc) of SDS, then showed sigmoidal enhancements of swelling in a higher SDS
concentration region until the degrees of swelling reached maximum values. The SDS concentration at which the swelling began
to appear was in reasonable agreement with the critical aggregation concentration (cac) value reported for the aqueous PEO
system. For the cases where NaCl was present, the swelling behavior of PEO gel was different from that when NaCl was absent
in the following way. The concentrations where the swelling begins to appear, and hence those where the degree of swelling
rises steeply, decreased with an increase in NaCl concentration. The ultimate degrees of swelling at higher concentration
regions also decreased with an increase in the NaCl concentration. The lowering of the SDS concentrations at which the PEO
gel began to swell is in line with the decreases in the cmc of SDS solutions containing NaCl and also with the decreases in
the cac of PEO solution.
Electronic Publication 相似文献
69.
Kazunori Ishikawa Yoko Nambu Takeshi Endo 《Journal of polymer science. Part A, Polymer chemistry》1989,27(5):1625-1629
Polypeptide membranes with several lengths of spacers [? (CH2)n? ; n = 3, 6, 12] between the polymer matrix and viologen moiety as a functional group were prepared. Reduction of K3Fe(CN)6 with Na2S2O4 across the obtained membrane in aqueous media were carried out and reduction rate of K3Fe(CN)6 across the membrane of n = 6 was faster than that of n = 3. However, the reduction of the membrane (n = 12) did not proceed chemically and electrochemically at all. 相似文献
70.
We investigated the effects of added oxide to FeSi2 on thermoelectric properties in order to improve the figure of merit. The oxide was not suggested to chemically react with
the mother material (FeSi2), where the oxide materials existed in the grain boundaries. The oxide addition played a role to reduce thermal conductivity
and possessed electrical resistivity as well as non oxide-added FeSi2. Hereafter, the appropriate added amount of Yb2O3 showed the largest effect on the figure of merit among other oxides. 相似文献