[Successful inhibition of bladder tumor recurrence by oral administration of UFT].
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Administration, Oral↗
Biomedical subjects
T Usui
Publications and source records attributed to T Usui.
Synthesis and aldose reductase inhibitory activity of 2-substituted-6-fluoro-2,3-dihydrospiro [4H-1-benzopyran-4, 4'-imidazolidine]-2',5'-diones.
Optically active and racemic 2-substituted-6-fluoro-2,3-dihydrospiro[4H-1-benzopyran-4, 4'-imidazolidine]-2',5'-diones were synthesized from (+)-, (-)-, and (+-)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid. These compounds were then evaluated for in vitro and in vivo aldose reductase inhibitory activity. The 2S,4S isomers were found to be more potent aldose reductase inhibitors than the other corresponding stereoisomers. Among these compounds, (2S,4S)-6-fluoro-2,3-dihydro-2',5'-dioxospiro[4H-1-benzopyran-4, 4'-imidazolidine]-2-carboxamide ((+)-1b, SNK-860, CAS 105300-43-4) showed the most potent in vitro and in vivo activity.
Aldehyde Reductase↗
Transglycosylation reaction of maltotriose-forming amylase from Streptomyces griseus.
A maltotriose-forming amylase from Streptomyces griseus produced predominantly p-nitrophenyl alpha-maltotetraoside through a transglycosylation reaction from maltotetraose as a donor and p-nitrophenyl alpha-D-glucopyranoside as an acceptor in an organic co-solvent. With p-nitrophenyl beta-D-glucopyranoside acceptor, the enzyme catalyzed the formation of an alpha-(1-->3)-linked tetrasaccharide (p-nitrophenyl 3(1)-O-alpha-maltotriosyl-beta-D-glucopyranoside) in a yield of 16%, based on the acceptor added with its isomer p-nitrophenyl beta-maltotetraoside. This was also the case for the formation of o-chloro-p-nitrophenyl 3(1)-O-alpha-maltotriosyl-beta-D-glucopyranoside with o-chloro-p-nitrophenyl beta-D-glucopyranoside acceptor. The results shows that the anomeric configuration of the aryl group in the glucosyl acceptors had an effect on the position of transglycosylation.
Amylases↗
Immunoreactive corticotropin-releasing hormone levels in discrete hypothalamic nuclei of genetically obese Zucker rats.
The levels of immunoreactive corticotropin-releasing hormone (ir-CRH) were measured in discrete hypothalamic nuclei and the median eminence of obese Zucker rats and their lean littermates. More than 90% of total hypothalamic ir-CRH was detected in the median eminence in both obese and lean rats. Though ir-CRH levels in the paraventricular nucleus of obese rats tended to be lower than those of their lean littermates, no significant difference of ir-CRH levels was observed in any hypothalamic nuclei studied between obese and lean rats. However, ir-CRH levels in the median eminence of obese rats were significantly lower than those of their lean littermates (5263 +/- 438 pg/tissue vs. 7050 +/- 473 pg/tissue, P < 0.05). These results suggest that the hypoactive hypothalamic CRH tonus would play some role in the phenotypic expression of obesity in the genetically obese Zucker rats.
Animals↗
A single chain 19-kDa fragment from bovine thrombospondin binds to type V collagen and heparin.
Location of the type V collagen-binding domain within bovine thrombospondin (TSP) was investigated by using fragments of reduced and alkylated TSP. A fragment of relative molecular mass (19 kDa) was isolated, which inhibited binding of 125I-TSP to type V collagen in a solid-phase binding assay. A direct binding assay using the 125I-labeled fragment confirmed that the fragment actually bound to collagen. The fragment retained specificity for the native structure of type V collagen like the intact TSP molecule. Its binding to the collagen, however, was not inhibited by Ca2+ in contrast to intact TSP. Amino acid sequence analysis of the 19-kDa fragment suggested that this fragment corresponded to Val333-Lys412, a part of the stalklike region in the human TSP primary structure. It was found that the fragment also bound well to heparin in a specific and saturable manner and, furthermore, binding to type V collagen was inhibited by soluble heparin. Removal of the N-linked sugar chain from this fragment resulted in a 14-kDa fragment. The deglycosylated fragment retained the ability to bind to type V collagen as well as heparin. These results suggest that a type V collagen-binding site is present in the 80-residue portion of bovine TSP (Val333-Lys412) and is likely to be identical or lie very close to a heparin-binding site, which exists in the type I repeat structure.
Amino Acid Sequence↗
A convenient synthesis of beta-D-galactosyl disaccharide derivatives using the beta-D-galactosidase from Bacillus circulans.
beta-D-Gal-(1-->4)-beta-D-GlcNAc-OC6H4NO2-p (p-nitrophenyl N-acetyl-beta-lactosaminide) and beta-D-Gal-(1-->6)-beta-D-GlcNAc-OC6H4NO2-p (p-nitrophenyl N-acetyl-beta-isolactosaminide) were regioselectively synthesized from lactose and p-nitrophenyl 2-acetamido-2-deoxy-glucopyranoside, employing transglycosylation by the beta-D-galactosidase from Bacillus circulans and by controlling the concentration of organic solvent in the reaction system. The (1-->4)-linked disaccharide was formed exclusively when the concentration of organic solvent was high, whereas the (1-->6)-linked isomer was produced with a low concentration. Further utilization of the transglycosylation by the enzyme led to the regioselective formation of beta-D-Gal-(1-->4)-D-GalNAc and beta-D-Gal-(1-->4)-beta-D-GalNAc-OC6H4NO2-p. With the enzyme, beta-D-galactosyl transfer occurred preferentially at the O-4 position of GlcNAc and GalNAc, regardless of the configuration of the hydroxyl group.
Bacillus↗
Propolypeptide of von Willebrand factor serves as a substrate for factor XIIIa and is cross-linked to laminin.
The propolypeptide of von Willebrand factor (pp-vWF) was found to serve as a substrate for Factor XIIIa (FXIIIa). FXIIIa catalyzed polymerization of pp-vWF as well as the incorporation of monodansylcadaverine and [14C]putrescine into pp-vWF in a Ca(2+)- and time-dependent manner. The amount of putrescine incorporated into pp-vWF was increased as a function of putrescine concentration and reached a maximum of 3 mol/mol of pp-vWF, indicating that there are at least 3 glutamine residues in the pp-vWF molecule responsible for the reaction. 125I-pp-vWF was incubated with FXIIIa in the presence of various adhesive glycoproteins. Laminin, among the proteins tested, specifically formed a large molecular weight complex with 125I-pp-vWF in a Ca(2+)- and time-dependent manner. It was also found that FXIIIa catalyzed polymerization of laminin as well as the incorporation of monodansylca-daverine into laminin. The high molecular weight complexes of 125I-pp-vWF (or 125I-laminin) formed in the presence of laminin (or pp-vWF) were immunoprecipitated with anti-laminin (or anti-pp-vWF) antibodies. Taking all the data together it can be concluded that both pp-vWF and laminin have glutamine and lysine residues responsive to FXIIIa and make copolymers by virtue of FXIIIa.
Animals↗
Simultaneous determination of a new inhibitor of acyl CoA:cholesterol acyltransferase, YM17E, and five metabolites using high-performance liquid chromatography with electrochemical detection.
We describe a reversed-phase high-performance liquid chromatographic method for the determination in plasma of YM17E (I), an inhibitor of acyl CoA:cholesterol acyltransferase, and its five metabolites using electrochemical detection. This method enables simultaneous quantification of I and five active metabolites. The plasma sample is extracted by a one-step solid-phase extraction using a SepPak C18 cartridge, with high recovery and reproducibility of the analytes. The method is sensitive and the limits of determination are 0.5 ng/ml for I and 1 ng/ml for metabolites M1, M2-a, M2-b, M3 and M4. This method is applicable to rat, dog and human plasma, and is useful for pharmacokinetic studies.
Animals↗
Inguinal lymph node metastasis from contralateral testicular origin.
A twenty-eight-year-old man had a testis tumor eighteen years after orchiopexy and inguinal lymph node metastasis in the contralateral side. It is suggested that scrotal surgery may lead to the formation of new lymph channels and alter the pattern of nodal metastases.
Adult↗
Isolation of Drosophila CREB-B: a novel CRE-binding protein.
CREB is a DNA-binding protein that stimulates gene transcription upon activation of the cAMP signaling pathway. The mammalian CREB protein consists of an amino-terminal transcriptional activation domain and a carboxy-terminal DNA-binding domain comprised of a basic region and a leucine zipper. Recent studies have shown that the mammalian CREB is one of many transcription factors that can bind to the cAMP regulated enhancer (CRE) sequence. Consequently, a complete understanding of regulation through the CRE sequence requires the elucidation of how the various CRE-binding proteins interact with each other. To accomplish this goal, we have begun to characterize the family of CRE-binding proteins in a system that is amenable to genetic manipulations, Drosophila melanogaster. We have previously cloned a protein designated dCREB-A from a Drosophila embryonic cDNA library. Here, we describe an additional member of the Drosophila CREB gene family, isolated by screening a lambda gt11 library of adult Drosophila head cDNAs with a multimerized CRE sequence. This protein, dCREB-B, contains 285 amino acids and is remarkably similar within the basic/zipper region to the corresponding portion of mammalian CREB. In contrast, the dCREB-B and mammalian CREB zipper domains differ considerably from the dCREB-A zipper in both length and composition. However, the putative DNA binding domains for all three proteins are highly conserved. The activator region of dCREB-B is completely different from that of both mammalian CREB and dCREB-A. Northern blot analysis shows that multiple transcripts of the dCREB-B gene are expressed in embryonic and adult tissues and that these transcripts arise from both strands of the DNA.(ABSTRACT TRUNCATED AT 250 WORDS)
Amino Acid Sequence↗
Long-term results of endourologic treatment of urinary calculi: investigation of risk factors for recurrence or regrowth.
To evaluate the risk factors related to the long-term outcome of endourologic treatment of urinary calculi, we examined rates of recurrence and regrowth in 167 renal units. The following risk factors were examined: age; previous stone; location, number, size, and composition of stone; and procedures. In our study sample, the overall recurrence and regrowth rates were 17% and 10%, respectively. The earliest recurrence and regrowth appeared at 3 months after treatment, and 71% occurred within 2 years. In 22% of renal units that were estimated to be stone-free, stones appeared later, and 45% of inadequately fragmented stones enlarged. Stones located in a renal calix and pelvis, multiple stones, large stones (more than 20 mm), stones composed of calcium oxalate or calcium phosphate or both, and struvite stones were likely to be risk factors, but there were no significant differences statistically. Although the possibility of several risk factors was suggested in our study, thorough fragmentation of stones and complete removal of fragments, combined with extracorporeal shock wave lithotripsy or chemolysis if needed, is ultimately responsible for successful treatment of urinary calculi.
Adolescent↗
Accommodative and pupillary responses to sinusoidal target depth movement.
We evaluated the accommodative and pupillary responses to sinusoidal target depth movement in 10 normal subjects and one patient by analysing frequency responses and associated Bode plots. The phase of the pupillary response significantly lagged behind that of accommodative response, which suggests that they are controlled by separate central nervous systems. We measured the baseline shift of each response trace using a regression line and found that they were larger at higher stimulation frequencies. A patient with severe asthenopia showed a considerable baseline shift in accommodative response. These analyses may be useful for the quantitative assessment of dynamic accommodation and pupillary response.
Accommodation, Ocular↗
Ocular medulloepithelioma in a thoroughbred.
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Animals↗
Conjunctival biopsy in adult form galactosialidosis.
Conjunctival biopsy was performed in two siblings with adult-form galactosialidosis. Electron microscopically, several types of intracytoplasmic inclusion were observed in the fibroblasts in conjunctival stroma, lymphatic capillary endothelial cells, Schwann cells, and epithelial cells. Membrane-bound vesicles with fibrillogranular content were frequently observed, and occasional lamellar structures were noted in these inclusions. Dense granular inclusions and oil droplets were also seen. Dense granular inclusions have not been reported in this disease previously.
Adult↗
Myocardial ischemia after treatment with methotrexate, etoposide and cisplatin.
Cisplatin exerts an additional influence on myocardial ischemia induced by the cardiovascular effects of etoposide. Two cases of myocardial ischemia related to combination chemotherapy with methotrexate, etoposide and cisplatin are reported. While the major toxicity associated with systemic chemotherapy is hematologic, it is suggested that, in elderly patients with increased incidence of atherosclerotic disease, special attention be given to vascular complications of antineoplastic agents.
Aged↗
Velocity profile of human horizontal saccades.
To assess saccadic trajectories, we evaluated the velocity profile using the 'skewness ratio' (the proportion of acceleration time to total saccadic duration) as a parameter. Horizontal cross-center saccades against target movements of 10 degrees, 20 degrees and 30 degrees were measured in 6 normal subjects using the magnetic search coil method. As the amplitude increased the period of the deceleration phase became prolonged: 10 degrees saccades were almost symmetrical and 30 degrees saccades were skewed to a ratio of about 0.3. A close relationship between duration and skewness ratio was found, and the skewness ratios of temporal saccades were smaller than nasal ones. This skewness ratio would be a useful parameter for assessing the velocity profile of human saccades.
Adult↗
A new focal pattern stimulator under direct observation of ocular fundus.
A new focal pattern stimulator was developed. Since this system enables direct observation of ocular fundus during examination, it may be useful for the objective assessment of visual function in patients with various kinds of eye diseases.
Electroretinography↗
Temporal modulation transfer function of vision by pattern visual evoked potentials in patients with optic neuritis.
To reveal the impairment of the temporal modulation transfer function of vision in patients with optic neuritis, the pattern visual evoked potentials (P-VEPs) were recorded at reversal frequencies ranging from 4 to 24 per second, and the fast Fourier transform (FFT) of VEPs were investigated. In normal subjects, curves of the square root of the power of the FFTs of P-VEPs versus temporal frequency showed the maximum peak at 6 Hz (12 reversals/s). The specific distribution of the power spectrum could be found at each temporal frequency, and the amplitudes of higher harmonic components decreased while a single power spectrum peak became prominent as the temporal frequency increased. In patients with optic neuritis, an abnormality of the power spectrum of steady-state P-VEPs could by detected by estimating the 1st and 2nd harmonic components. The abnormality of the power spectrum of transient P-VEPs could be detected by estimating the higher harmonic components of the power spectrum.
Adult↗